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| Product | Description | |
|---|---|---|
| Checkpoint Kinase 2, Active Human, Recombinant | CHEK2 is the official symbol for the human gene Checkpoint kinase 2. CHEK2 is located on the the long (q) arm of chromosome 22. CHEK2 is tumor suppressor gene that encodes the protein CHK2, a serine threonine kinase. CHK2 operates in an intricate network of proteins to elicit DNA repair, cell cycle arrest or apoptosis in response to DNA damage. Mutations to the CHEK2 gene have been linked to a wide range of cancers including breast cancer. Buffered aqueous glycerol solution, recombinant, expressed in e. coli, > 85% (sds-page). Applications: Kinase activity is measured as the molar amount of phosphate incorporated into the chktide per minute per mg protein at 30°c using a final concentration of 50 μm [32p] atp. Group: Enzymes. Synonyms: Checkpoint Kinase 2; CHEK2; CDS1; CHK2; HuCds1; LFS2; PP1425; RAD53; hCds1; Chek2; Chk2. Purity: > 85% (SDS-PAGE). CHEK2. Mole weight: protein apparent mol wt ~88 kDa. Stability: -70°C. Form: buffered aqueous glycerol solution. Source: E. coli. Species: Human. Checkpoint Kinase 2; CHEK2; CDS1; CHK2; HuCds1; LFS2; PP1425; RAD53; hCds1; Chek2; Chk2. Cat No: NATE-0122. |  |
| Checkpoint Protein Hus1 (213-232) (human) | HDAC1 plays an important role in regulating eukaryotic chromatin structure and specifically interacts with human Hus1 gene products in yeast, mammalian cells, and in vitro. S. Pombe's Hus1 protein is associated with G2/M checkpoint control and is a member of the cell cycle checkpoint Rad protein, which is involved in the mitotic checkpoint induced by DNA damage or DNA replication arrest. Synonyms: H-Leu-Ala-Ser-Glu-Ser-Thr-His-Glu-Asp-Arg-Asn-Val-Glu-His-Met-Ala-Glu-Val-His-Ile-OH. Grades: ≥95%. Molecular formula: C95H150N30O35S. Mole weight: 2304.48. |  |
| 10Z-Hymenialdisine | Insecticidal and cytotoxic. Potent NF-kappaB inhibitor. Inhibits various pro-inflammatory cytokines such as IL-1, IL-2, IL-6, IL-8, TNF-alpha and nitric oxide (NO) in a variety of cell lines. ATP-competitive kinase inhibitor. Inhibits DNA damage checkpoint at G2, cyclin-dependent kinases CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E, CDK4/cyclin D1, CDK5/p25, GSK-3beta and casein kinase 1 (CK1). Potent mitogen-activated protein kinase kinase-1 (MEK-1) inhibitor. MARK (microtubule affinity-regulating kinase) inhibitor. Group: Biochemicals. Grades: Highly Purified. CAS No. 82005-12-7. Pack Sizes: 500ug, 1mg. Molecular Formula: C??H??BrN?O?, Method for Determining. US Biological Life Sciences. |  Worldwide |
| 10Z-Hymenialdisine (Hymenialdisine, 4-(2-Amino-4-oxo-2-imidazolidin-5-ylidene)-2-bromo-4,5,6,7-tetrahydropyrrolo[2,3-c]azepin-8-one) | Isolated from sponge Axinella carteri. A potent inhibitor of mitogen-activated protein kinase kinase-1 (MEK-1) (IC50=6nm). Blocks the in vivo phosphorylation of the microtubule-binding protein tau at sites that are hyperphosphorylated by glycogen synthase kinase-b (GSK-3b) and CDK5/p35 in Alzheimers disease. Inhibitor of DNA damage checkpoint at G2 phase (IC50=6uM), cyclin-dependent kinases CDK1/cyclin B (IC50=22nm), CDK2/cyclin A (IC50=70 nm), CDK2/cyclin E (IC50=40nm), CDK4/cyclin D1 (IC50 = 600nm), CDK5/p25 (IC50=28nm), GSK-3b (IC50=10nm), and casein kinase 1 (CK1) (IC50=35nm). Group: Biochemicals. Grades: Highly Purified. CAS No. 82005-12-7. Pack Sizes: 250ug, 1mg. US Biological Life Sciences. | Worldwide |
| 2-Bromothiazole-5-carboxaldehyde | 2-Bromothiazole-5-carboxaldehyde is a reactant in the preparation of thienopyridines as potent checkpoint 1 kinase (CHK1) inhibitors. Group: Biochemicals. Grades: Highly Purified. CAS No. 464192-28-7. Pack Sizes: 250mg, 500mg. Molecular Formula: C4H2BrNOS, Molecular Weight: 192.03. US Biological Life Sciences. | Worldwide |
| 2OH-BNPP1 | 2OH-BNPP1 is a novel inhibitor of checkpoint kinase BUB1. Group: Biochemicals. Grades: Highly Purified. CAS No. 833481-73-5. Pack Sizes: 1mg, 2.5mg. Molecular Formula: C16H19N5O, Molecular Weight: 297.35. US Biological Life Sciences. | Worldwide |
| 2-Oxa-7-azaspiro[3.5]nonane | 2-Oxa-7-azaspiro[3.5]nonane is an intermediate used to prepare benzothienoazepine derivatives as potent respiratory syncytial virus RNA polymerase inhibitors. It is also used to prepare 1,7-Diazacarbazole derivatives as inhibitors of checkpoint kinase 1. Group: Biochemicals. Grades: Highly Purified. CAS No. 241820-91-7. Pack Sizes: 10mg, 50mg. Molecular Formula: C7H13NO, Molecular Weight: 127.18. US Biological Life Sciences. | Worldwide |
| (2S,3S,4S,5S)-5-(4-benzamido-2-oxopyrimidin-1(2H)-yl)-2-((benzoyloxy)methyl)-4-fluoro-4-methyltetrahydrofuran-3-yl benzoate | (2S,3S,4S,5S)-5-(4-benzamido-2-oxopyrimidin-1(2H)-yl)-2-((benzoyloxy)methyl)-4-fluoro-4-methyltetrahydrofuran-3-yl benzoate is a potential drug candidate used in biomedicine for treating cancer. It is a small molecule inhibitor of WEE1, a protein kinase that regulates the G2/M checkpoint of the cell cycle. Inhibition of WEE1 leads to the activation of CDK1 and CDK2, causing DNA damage and cell death in cancer cells. Synonyms: (2S,3S,4S,5S)-5-(4-benzoylamino-2-oxopyrimidine-1(2H)-yl)-2-((benzoyloxy)methyl)-4-Fluoro-4-methyltetrahydrofuran-3-yl benzoate. Grades: 97%. Molecular formula: C31H26FN3O7. Mole weight: 571.55. | |
| 3,3'-Diindolylmethane | 3,3'-Diindolylmethane is an activator of checkpoint kinase 2 (Chk2) that induces G2/M cell cycle arrest in various cancer cell lines. It is used as an antineoplastic agent. Nutritional supplement in health care products. Synonyms: 1H-Indole, 3,3'-methylenebis-; 3,3'-Methylenebis[1H-indole]; Indole, 3,3'-methylenedi-; 3,3'-Bisindolylmethane; 3,3'-Methanediyldi(1H-indole); Arundine; Bis(1H-indol-3-yl)methane; Bis(3-indolyl)methane; Cervicon-DIM; Di(1H-indol-3-yl)methane; Diindolylmethane; DIM; DIM (AhR agonist); DIM (diindolylmethane); HB 236; Infemin. Grades: ≥99% by HPLC. CAS No. 1968-5-4. Molecular formula: C17H14N2. Mole weight: 246.31. | |
| 8-[(6-Amino)hexyl]-amino-adenosine-2',5'-bisphosphate - DYQ-661 | DYQ-661, a strikingly potent and exclusive inhibitor of CD73, a critical enzyme implicated in the biosynthesis of immunosuppressive adenosine in the tumor microenvironment, presents a hopeful alternative for patients with different types of cancer. The preclinical investigations depict handsome outcomes, enhancing the effectiveness of immune checkpoint inhibitors. DYQ-661 is an exceedingly promising therapeutic approach that demands significant attention in the realm of cancer treatment. Synonyms: 8-[(6-Amino)hexyl]-amino-adenosine-2',5'-bisphosphate, labeled with DYQ 661, Triethylammonium salt. Grades: ≥ 95% by HPLC. Molecular formula: C55H70N9O18P2S2 (Anion). Mole weight: 1271.27 (Anion). | |
| AHR Antagonist 5 | AHR Antagonist 5, an effective and orally active aromatic hydrocarbon receptor (AHR) antagonist with IC50 of less than 0.5 μM. It can significantly inhibit tumor growth in combination with the checkpoint inhibitor anti-PD-1. Synonyms: BCP33104; HY-136220; CS-0120848; (R)-N-(2-(5-Fluoropyridin-3-Yl)-8-Isopropylpyrazolo[1,5-A][1,3,5]Triazin-4-Yl)-2,3,4,9-Tetrahydro-1H-Carbazol-3-Amine Trihydrochloride. Grades: ≥98% by HPLC. CAS No. 2247953-39-3. Molecular formula: C25H27Cl3FN7. Mole weight: 550.9. | |
| Alsevalimab | Alsevalimab is a human monoclonal antibody that targets B7-H4 with potential antineoplastic and immune checkpoint inhibitory activities. CAS No. 2254029-91-7. | |
| AMG510 racemate | AMG510 is a potent KRAS G12C covalent inhibitor with potential antineoplastic activity. At the 2019 World Conference on Lung Cancer (WCLC), Amgen declared the efficacy of AMG510 for treating non-small cell lung cancer (NSCLC) with KRAS G12 C-mutated solid tumors. Amgen also announced prospective directions for AMG510 through academic scholars and reports the few limitations on official drug release as evidence for potential investors to consider the value of AMG510. Uses: Immune checkpoint inhibitors. Synonyms: AMG-510 racemate; AMG 510 racemate; Sotorasib racemate. CAS No. 2296729-00-3. Molecular formula: C30H30F2N6O3. Mole weight: 560.59. | |
| ARRY-520 R enantiomer | ARRY-520 R enantiomer is the R form of ARRY-520, which is a synthetic, small molecule kinesin spindle protein (KSP) inhibitor. ARRY-520 had low nanomolar antiproliferative activity in tumor cell lines and specifically inhibits KSP (kinesin-5 or Eg5), resulting in activation of the spindle assembly checkpoint, induction of cell cycle arrest during the mitotic phase, and consequently cell death in tumor cells that are actively dividing. Synonyms: ARRY-520 R enantiomer; ARRY 520 R enantiomer; ARRY520 R enantiomer; 1,3,4-Thiadiazole-3(2H)-carboxamide, 2-(3-aminopropyl)-5-(2,5-difluorophenyl)-N-methoxy-N-methyl-2-phenyl-, (2R)-. Grades: >98%. CAS No. 885060-08-2. Molecular formula: C20H22F2N4O2S. Mole weight: 420.48. | |
| AZD0156 | AZD0156 is an orally active, potent and selective ataxia telangiectasia mutated (ATM) kinase inhibitor, used for cancer treatment. AZD0156 prevents DNA damage checkpoint activation, and disrupts DNA damage repair, inducing tumor cell apoptosis, and leading to cell death in ATM-overexpressing tumor cells. Uses: Protein kinase inhibitors. Synonyms: 8-[6-[3-(dimethylamino)propoxy]-3-pyridyl]-3-methyl-1-tetrahydropyran-4-yl-imidazo[4,5-c]quinolin-2-one; AZD0156; AZD-0156; AZD 0156. CAS No. 1821428-35-6. Molecular formula: C26H31N5O3. Mole weight: 461.56. | |
| AZD0156 | AZD0156 is a potent, selective and orally active ATM inhibitor with an IC 50 of 0.58 nM. AZD0156 inhibits the ATM -mediated signaling, prevents DNA damage checkpoint activation, disrupts DNA damage repair, and induces tumor cell apoptosis [1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 1821428-35-6. Pack Sizes: 5 mg; 10 mg; 50 mg; 100 mg. Product ID: HY-100016. |  |
| AZD-7762 | AZD-7762 is a synthetic small molecule inhibitor of checkpoint kinases (Chks) with potential chemosensitizing activity. AZD7762 binds to and inhibits Chks, which may prevent cell cycle arrest and subsequent nucleotide excision repair in DNA-damaged tumor cells, resulting in tumor cell apoptosis. Synonyms: AZD 7762; AZD7762. Grades: 0.98. CAS No. 860352-01-8. Molecular formula: C17H19FN4O2S. Mole weight: 362.423. | |
| Besifloxacin Impurity G | Besifloxacin Impurity G is an intermediate used to prepare ureido thiophene carboxamides as checkpoint kinase inhibitors. It is also an impurity of Besifloxacin. Synonyms: (R)-3-Amino-hexahydroazepine; (R)-Azepan-3-amine; (R)-Hexahydro-1H-azepin-3-amine; (R)-3-Amino-Hexahydro-1H-Azepin; 1H-Azepin-3-amine, hexahydro-, (3R)-. Grades: > 95%. CAS No. 124932-43-0. Molecular formula: C6H14N2. Mole weight: 114.19. | |
| BO-264 | BO-264 is a highly potent and orally active transforming acidic coiled-coil 3 (TACC3) inhibitor with an IC50 of 188 nM and a Kd of 1.5 nM. BO-264 demonstrated superior anti-proliferative activity to the two currently reported TACC3 inhibitors, especially in aggressive breast cancer subtypes, basal and HER2+, via spindle assembly checkpoint (SAC)-dependent mitotic arrest, DNA damage and apoptosis, while the cytotoxicity against normal breast cells was negligible. Uses: Designed for use in research and industrial production. Additional or Alternative Names: BO-264; BO 264; BO264. Product Category: Inhibitors. Appearance: Solid powder. CAS No. 2408648-20-2. Molecular formula: C18H19N5O3. Mole weight: 353.38. Purity: >98%. IUPACName: 3-(4-methoxyphenyl)-N-(2-morpholinopyrimidin-4-yl)isoxazol-5-amine. Canonical SMILES: COC1=CC=C(C2=NOC(NC3=NC(N4CCOCC4)=NC=C3)=C2)C=C1. Product ID: ACM2408648202. Alfa Chemistry ISO 9001:2015 Certified. Categories: BF 2649. |  |
| Camrelizumab | Camrelizumab is an anti-PD-1 immune checkpoint inhibitor that is being investigated for hepatocellular carcinoma and Hodgkin lymphoma. Camrelizumab is a humanized anti-PD-1 IgG4 antibody that blocks the binding of PD-L1 and PD-L2 to PD-1 with immune checkpoint inhibitory and antineoplastic activities. Synonyms: SHR-1210. Grades: ≥98%. | |
| CBP501 | CBP501 is a peptide with G2 checkpoint-abrogating activity. G2 checkpoint inhibitor CBP501 inhibits multiple serine/threonine kinases, including MAPKAP-K2, C-Tak1, and CHK1, that phosphorylate serine 216 of the dual-specific phosphatase Cdc25C (cell division checkpoint 25 C); disruption of Cdc25C activity results in the inhibition of Cdc25C dephosphorylation of the mitotic cyclin-dependent kinase complex Cdc2/cyclin B, preventing entry into the mitotic phase of the cell cycle. Check for active clinical trials or closed clinical trials using this agent. Synonyms: CBP-501; CBP 501; H-D-Bpa-D-Ser-D-Trp-D-Ser-D-Phe(F5)-D-Cha-D-Arg-D-Arg-D-Arg-D-Gln-D-Arg-D-Arg-OH. CAS No. 565434-85-7. Molecular formula: C86H122F5N29O17. Mole weight: 1929.06. | |
| CBP-93872 | CBP-93872 is a G2 checkpoint inhibitor. CBP-93872 specifically abrogates the DNA double-stranded break (DSB)-induced G2 checkpoint through inhibiting maintenance. CBP-93872 is an inhibitor of maintenance of the DSB-specific G2 checkpoint and thus might be a strong candidate as the basis for a drug that specifically sensitizes p53-mutated cancer cells to DSB-inducing DNA damage therapy. Synonyms: CBP 93872; CBP93872; 1-amino-3-((2-bromo-4-methylphenyl)amino)propan-2-ol. Grades: 98%. CAS No. 67427-51-4. Molecular formula: C10H15BrN2O. Mole weight: 259.14. | |
| Chk2 Inhibitor | Chk2 inhibitor is an inhibitor of checkpoint kinase 2 (Chk2; IC50 = 13.5 nM). Chk2 inhibitor enhances survival of 184B5, but not MDA-MB-231, cells following ionizing radiation and inhibits cell cycle arrest at the G2 stage induced by ionizing radiation in 184B5 cells. It also inhibits the production of IL-2 in Jurkat cells, the production of TNF-α in LPS-stimulated THP-1 cells and the growth of CEM leukemia T cells. Synonyms: SC-203885; (5Z)-5-(2-amino-1,5-dihydro-5-oxo-4H-imidazol-4-ylidene)-3,4,5,10-tetrahydro-azepino[3,4-b]indol-1(2H)-one; Hymenialdisine Analogue 1. CAS No. 724708-21-8. Molecular formula: C15H13N5O2. Mole weight: 295.3. | |
| CTLA-4 inhibitor | CTLA-4 inhibitor is an inhibitor of CTLA-4, an immune checkpoint negatively regulating T cell function. CTLA-4 is thought to regulate T-cell proliferation early in an immune response, primarily in lymph nodes. Synonyms: MDK24720; MDK 24720; MDK-24720; CTLA-4 inhibitor. 2-(4-Fluorophenyl)-6-methyl-4-(3-(trifluoromethyl)phenyl)-1,2-dihydrodipyrazolo[3,4-b:3',4'-d]pyridin-3(6H)-one; EX-A913. CAS No. 635324-72-0. Molecular formula: C21H13F4N5O. Mole weight: 427.363. | |
| Debromohymenialdisine | Protein kinase C (PKC) inhibitor. Inhibits the ATP binding site. Cytotoxic and insecticidal. G2 DNA damage checkpoint inhibitor. Check point kinases 1 (Chk1) and 2 (Chk2) inhibitor. Does not inhibit ataxia-telangiectasia mutated (ATM) or ATM-Rad3-related proteins. MAP kinase kinase 1 (MEK-1) inhibitor. Interleukin-1 (IL-1) inhibitor. Anti-osteoarthritic. Potential anti-Alzheimer agent. Group: Biochemicals. Grades: Highly Purified. CAS No. 75593-17-8, 125118-55-0. Pack Sizes: 100ug. Molecular Formula: C11H11N5O2. US Biological Life Sciences. | Worldwide |
| Etoposide, 95.0-105.0% (HPLC) USP | Potent anti-cancer compound. Induces apoptosis in normal and tumor cell lines. DNA Topoisomerase II activity inhibitor. Increases Topo II-mediated DNA breakage primarily by inhibiting the ability of the enzyme to religate cleaved nucleic acid molecules. Does not lead to immediate block of DNS synthesis, induces a progressive inhibition of DNA replication. p53 activator. Blocks the cell cycle between the end of the S phase and the early G2 phase. Oncoprotein Mdm2 synthesis inhibitor. Apoptosis inducer through the cytochrome c/Apaf-1/caspase-9 pathway and the Fas-mediated death signaling pathway. Cell cycle checkpoint activator. Affects gene expression at different levels (chromatin remodeling, transcrip- tion and alternative splicing). Chemotherapeutic compound used in cancers. Used in conditioning regimen prior to a bone marrow or blood stem cell transplantation. Highly effective in mobilizing stem cells. Group: Biochemicals. Alternative Names: 4-Des methyl epipodophyllotoxin; VP-16-213, NSC 141540. Grades: USP. CAS No. 33419-42-0. Pack Sizes: 250mg, 1g, 5g, 25g. US Biological Life Sciences. | Worldwide |
| Fianlimab | Fianlimab (REGN3767) is a human monoclonal antibody that targets the immune checkpoint receptor LAG-3 on T cells and has anti-tumour activity [1]. Uses: Scientific research. Group: Inhibitory antibodies. Alternative Names: REGN3767. CAS No. 2126132-98-5. Pack Sizes: 1 mg; 5 mg; 10 mg. Product ID: HY-P99617. | |
| Filanesib | Filanesib, also known as ARRY-520, is a synthetic, small molecule targeting the kinesin spindle protein (KSP) with potential antineoplastic activity. KSP inhibitor ARRY-520 specifically inhibits KSP (kinesin-5 or Eg5), resulting in activation of the spindle assembly checkpoint, induction of cell cycle arrest during the mitotic phase, and consequently cell death in tumor cells that are actively dividing. Synonyms: ARRY-520; ARRY 520; ARRY520. Grades: 0.98. CAS No. 885060-09-3. Molecular formula: C20H22F2N4O2S. Mole weight: 420.479. | |
| Floxuridine | Floxuridine (5-Fluorouracil 2'-deoxyriboside) is a pyrimidine analog and known as an oncology antimetabolite. Floxuridine inhibits Poly(ADP-Ribose) polymerase and induces DNA damage by activating the ATM and ATR checkpoint signaling pathways in vitro. Floxuridine is a extreamly potent inhibitor for S. aureus infection and induces cell apoptosis [1] [2]. Floxuridine has antiviral effects against HSV and CMV [3]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: 5-Fluorouracil 2'-deoxyriboside. CAS No. 50-91-9. Pack Sizes: 10 mM * 1 mL; 100 mg; 200 mg; 500 mg. Product ID: HY-B0097. | |
| Floxuridine | Floxuridine (5-Fluorouracil 2'-deoxyriboside) is a pyrimidine analog and known as an oncology antimetabolite. Floxuridine inhibits Poly(ADP-Ribose) polymerase and induces DNA damage by activating the ATM and ATR checkpoint signaling pathways in vitro. Floxuridine is a extreamly potent inhibitor for S. aureus infection and induces cell apoptosis. Floxuridine has antiviral effects against HSV and CMV. Uses: Designed for use in research and industrial production. Additional or Alternative Names: 1-beta-d-2'-deoxyribofuranosyl-5-flurouracil;1beta-D-2-Deoxyribofuranosyl-5-fluorouracil;2'-deoxy-5-fluoro-uridin;5-fluor-1-(beta-2'-deoxyribofuranosyl)pyrimidin-2,4(1h,3h)-dion;5-Fluor-1-(beta-2-deoxyribofuranosyl)pyrimidin-2,4(1H,3H)-dion;5-Fluoro-2-deoxyiridine;5-Fluorouracil 2-deoxyriboside;5-Fluorouracil deoxyriboside. Product Category: Inhibitors. CAS No. 50-91-9. Molecular formula: C9H11FN2O5. Mole weight: 246.19. Purity: 0.9995. Product ID: ACM50919. Alfa Chemistry ISO 9001:2015 Certified. | |
| Ganciclovir | Ganciclovir (GCV) is a pro-drug nucleoside analog that is activated by phosphorylation. It is useful in the study of gene therapy in cancer research. Upon expression of a viral suicide gene encoding thymidine kinase, the non-toxic pro-drug is converted to a phosphorylated active analog and is incorporated into the DNA of replicating eukaryotic cells, causing death of the malignant dividing cell. The cell cycle is irreversibly arrested at the G2-M checkpoint. Gap junction involvement in the ganciclovir bystander effect has been studied. Ganciclovir has been used to study loss of telomeres and to evaluate sensitivity of viruses to antiviral treatments. Ganciclovir is used in molecular biology for selection against random recombination events when homologous recombination of a gene of interest is required. Group: Biochemicals. Alternative Names: 2-Amino-1, 9-dihydro-9-[[2-hydroxy-1- (hydroxymethyl) ethoxy]methyl]-6H-purin-6-one; 2-NDG; 2-Nor-2-deoxyguanosine; 9-(1,3-Dihydroxy-2-propoxymethyl)guanine; BW 759; BW 759U; BW-B 759U; Biolf 62; DHPG; Denosine; Gancyclovir; Ganguard; Ganquard; HHEMG; Hydroxyacyclovir; Natclovir; RS 21592; Vitrasert. Grades: Highly Purified. CAS No. 82410-32-0. Pack Sizes: 100mg, 500mg, 1g, 5g. Molecular Formula: C?H??N?O?, Molecular Weight: 255.23. US Biological Life Sciences. | Worldwide |
| GDC-0425 | This active molecular is an selective Checkpoint kinase 1 (Chk1) inhibitors and it enhances gemcitabine efficacy in tumor xenograft models. GDC-0425 was safe and yielded responses in patients with a variety of cancers. In Oct 2013, GDC 0425 was in phase I trials for Solid tumours and Lymphoma (late-stage disease) in USA and France. In May 2014, Genentech completed a phase I trial in Lymphoma and Solid tumours (late-stage disease) in USA and France. Uses: Solid tumours and lymphoma. Synonyms: GDC-0425; GDC 0425; GDC0425; 5-((1-ethylpiperidin-4-yl)oxy)-9H-pyrrolo[2,3-b:5,4-c']dipyridine-6-carbonitrile;RG-7602; RG 7602; RG7602. Grades: 98%. CAS No. 1200129-48-1. Molecular formula: C18H19N5O. Mole weight: 321.38. | |
| GDC-0575 freebase | GDC-0575, also known as ARRY-575 and RG7741, is a potent and selective inhibitor of cell cycle checkpoint kinase 1 (Chk1) with an IC50 of 1.2?nM. Chk1 inhibitor GDC-0575 specifically binds to and inhibits Chk1; this may result in tumor cells bypassing Chk1-dependent cell cycle arrest in the S and G2/M phases, which permits the cells to undergo DNA repair prior to entry into mitosis. Uses: Designed for use in research and industrial production. Additional or Alternative Names: GDC-0575; GDC 0575; GDC0575; ARRY-575; ARRY-575; ARRY575; RG7741; RG-7741; RG 7741; AK 687476; AK-687476; AK687476; GDC-0575 HCl; GDC-0575 hydrochloride. Product Category: Inhibitors. Appearance: Solid powder. CAS No. 1196541-47-5. Molecular formula: C16H20BrN5O. Mole weight: 378.27. Purity: >98%. IUPACName: (R)-N-(4-(3-aminopiperidin-1-yl)-5-bromo-1H-pyrrolo[2,3-b]pyridin-3-yl)cyclopropanecarboxamide. Canonical SMILES: O=C(C1CC1)NC2=CNC3=NC=C(Br)C(N4C[C@H](N)CCC4)=C32. Product ID: ACM1196541475. Alfa Chemistry ISO 9001:2015 Certified. | |
| GSK-1070916A | GSK-1070916A is an ATP-competitive inhibitor of the serine/threonine kinases Aurora B and C with potential antineoplastic activity. Aurora B/C kinase inhibitor GSK1070916A binds to and inhibits the activity of Aurora kinases B and C, which may result in inhibition of cellular division and a decrease in the proliferation of tumor cells that overexpress the Aurora kinases B and C. Aurora kinases play essential roles in mitotic checkpoint control during mitosis, and are overexpressed by a wide variety of cancer cell types. Synonyms: GSK 1070916; GSK-1070916; GSK 1070916; GSK1070916A; GSK-1070916A; GSK 1070916A; NMI-900; NMI 900; NMI900. CAS No. 942918-07-2. Molecular formula: C30H33N7O. Mole weight: 507.63. | |
| Hymenialdisine | A potent inhibitor of a variety of kinases including MEK-1, GSK-3B, and CKI. It also exhibits inhibition of the G2 cell cycle checkpoint at the micromolar concentrations. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 1mg. US Biological Life Sciences. | Worldwide |
| Indibulin | Indibulin (ZIO 301), an orally applicable inhibitor of tubulin assembly, shows potent anticancer activity with a minimal neurotoxicity. Indibulin reduces inter-kinetochoric tension, produces aberrant spindles, activates mitotic checkpoint proteins Mad2 and BubR1, and induces mitotic arrest and apoptosis [1]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: ZIO 301; D 24851. CAS No. 204205-90-3. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-13649. | |
| Indoximod | A methylated tryptophan with immune checkpoint inhibitory activity. Indoximod inhibits the enzyme indoleamine 2,3-dioxygenase (IDO), which degrades the essential amino acid tryptophan, and may increase or maintain tryptophan levels important to T cell function. Tryptophan depletion is associated with immunosuppression involving T cell arrest and anergy. Synonyms: NLG8189; NLG 8189; NLG-8189; D-1MT; 1-methyl-D-tryptophan; H-D-Trp(Me)-OH. Grades: > 98%. CAS No. 110117-83-4. Molecular formula: C12H14N2O2. Mole weight: 218.25. | |
| JH295 | JH295 is an irreversible, cysteine-targeted inhibitor of the human centrosomal kinase, Nek2. JH295 irreversibly inhibited cellular Nek2 without affecting the mitotic kinases, Cdk1, Aurora B, or Plk1. Moreover, JH295 did not perturb bipolar spindle assembly or the spindle assembly checkpoint. To our knowledge, JH295 is the first small molecule shown to inactivate Nek2 kinase activity in cells. Synonyms: JH 295; JH-295; 3-[(2-Ethyl-4-methyl-1H-imidazole)-5-ylmethylene]-5-[(1-oxo-2-propynyl)amino]-1H-indole-2(3H)-one. CAS No. 1311143-71-1. Molecular formula: C18H16N4O2. Mole weight: 320.35. | |
| K-858 | K-858 is a novel inhibitor of mitotic kinesin Eg5 and antitumor agent, induces cell death in cancer cells. K858 blocked centrosome separation, activated the spindle checkpoint, and induced mitotic arrest in cells accompanied by the formation of monopolar spindles. Synonyms: K-858; K 858; K858. Grades: 98%. CAS No. 72926-24-0. Molecular formula: C13H15N3O2S. Mole weight: 277.34. | |
| Lirilumab | A fully humanized monoclonal antibody against killer-cell immunoglobulin-like receptors (KIR), with potential immune checkpoint inhibitory and antineoplastic activities. Upon administration, lirilumab binds to KIR, thereby preventing the binding of KIR ligands to KIR on natural killer (NK) cells. By blocking these inhibitory receptors, NK cells become activated and attack cancer cells leading to tumor cell death. KIR, a member of the immunoglobulin superfamily, is expressed on the surface of NK cells. Synonyms: Anti-KIR (1-7F9); Anti-KIR monoclonal antibody - Innate Pharma; BMS-986015; BMS 986015; BMS986015; IPH-21; IPH 21; IPH21; IPH-2101; IPH2102; IPH 2102;LIRI; NN 1975; NN1975; NN-1975. CAS No. 1000676-41-4. | |
| LY2606368 dihydrochloride | The dihydrochloride salt form of LY2606368 which also known as prexasertib, is an inhibitor of checkpoint kinase 1 and has potential effect in antineoplastic. It is still under Phase II clinical trial against breast cancer and some other sorts of cancers. Uses: The dihydrochloride salt form of ly2606368 which also known as prexasertib, is an inhibitor of checkpoint kinase 1 and has potential effect in antineoplastic. Synonyms: UNII-9RFT476U2L; 9RFT476U2L; LY2606368 (dihydrochloride); 1234015-54-3; HY-18174A; CS-3507; CS 3507; CS3507; LY2606368; LY 2606368; LY-2606368. Grades: 98%. CAS No. 1234015-54-3. Molecular formula: C18H21Cl2N7O2. Mole weight: 438.31. | |
| Malformin A1 | Peptide antibiotic. Antibcaterial. Plant growth stimulator. Induces root curvature and malformation in plants. Mycotoxin. Prevents interleukin-1 (IL-1) induced endothelial changes by inhibition of protein synthesis. Inhibitor of interleukin-1 beta (IL1 beta) binding to its receptor. Enhancer of cellular fibrinolytic activity. Disrupts the cell cycle at the G2 checkpoint of cancer cells, leading to sensitization of the cancer cells to anti-cancer reagents. Anticancer compound. Cytotoxic against several cancer cell lines. Antimalarial and antitrypanosomal. Inhibitor of BRAF-mutated melanoma cell lines. Group: Biochemicals. Grades: Highly Purified. CAS No. 3022-92-2. Pack Sizes: 250ug, 1mg. Molecular Formula: C??H??N?O?S?. US Biological Life Sciences. | Worldwide |
| Malformin C | Peptide antibiotic. Induces root curvature and malformation in plants. Antibacterial, antimalarial and antitrypanosomal. Disrupts the cell cycle at the G2 checkpoint of cancer cells, leading to sensitization of the cancer cells to anti-cancer reagents.Malformin C is a bicyclic pentapeptide containing L-leucine, D-isoleucine, L-valine, and two D-cysteines coupled with a disulfide-bond bridge. Malformins A1 and C, originally isolated from the culture broth of Aspergillus niger FKI-2342, were found to abrogate the bleomycin-induced G2 arrest in Jurkat cells with IC50 values of 480nM and 0.9nM, respectively. Malformins may be promising candidates as anti-cancer agents. Source:Synthetic. Originally isolated from Aspergillus niger FKI-2342. Group: Biochemicals. Grades: Highly Purified. CAS No. 59926-78-2. Pack Sizes: 250ug, 1mg. Molecular Formula: C23H39N5O5S2. US Biological Life Sciences. | Worldwide |
| MEDI0680 | A humanized immunoglobulin (Ig) G4 monoclonal antibody directed against the negative immunoregulatory human cell surface receptor programmed cell death 1 (PD-1), a transmembrane protein in the Ig superfamily expressed on T cells. MEDI0680 has potential immune checkpoint inhibitory and antineoplastic activities because it binds to and inhibits PD-1 and its downstream signaling pathways. Synonyms: AMP-514; AMP 514; AMP514; MEDI 0680; MEDI-0680; MEDI0680. | |
| Mirin | Mirin is an MRN-ATM pathway inhibitor, inhibiting MRN-dependent activation of ATM without affecting ATM protein kinase activity and Mre11-associated exonuclease activity. Mirin also inhibits the G2/M checkpoint and homology-dependent repair in mammalian cells. Synonyms: 2-amino-5-[(4-hydroxyphenyl)methylidene]-1,3-thiazol-4-one. Grades: ≥95%. CAS No. 299953-00-7. Molecular formula: C10H8N2O2S. Mole weight: 220.3. | |
| Mirin | Mirin is a potent Mre11-Rad50-Nbs1 (MRN) complex inhibitor. Mirin prevents MRN-dependent activation of ATM (IC 50 =12 μM) without affecting ATM protein kinase activity, and it inhibits Mre11-associated exonuclease activity. Mirin abolishes the G2/M checkpoint and homology-dependent repair in mammalian cells. Mirin prevents ATM activation in response to DNA double-strand breaks (DSBs) and blocks homology-directed repair (HDR) in mammalian cells [1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 299953-00-7. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg; 100 mg. Product ID: HY-117693. | |
| MK-1775 | MK-1775, also known as AZD-1775, is a WEE1 inhibitor and a small-molecule inhibitor of the tyrosine kinase WEE1 with potential antineoplastic sensitizing activity. MK-1775 selectively targets and inhibits WEE1, a tyrosine kinase that phosphorylates cyclin-dependent kinase 1 (CDC2) to inactivate the CDC2/cyclin B complex. Inhibition of WEE1 activity prevents the phosphorylation of CDC2 and impairs the G2 DNA damage checkpoint. This may lead to apoptosis upon treatment with DNA damaging chemotherapeutic agents. Unlike normal cells, most p53-deficient or mutated human cancers lack the G1 checkpoint as p53 is the key regulator of the G1 checkpoint and these cells rely on the G2 checkpoint for DNA repair to damaged cells. Annulment of the G2 checkpoint may therefore make p53-deficient tumor cells more vulnerable to antineoplastic agents and enhance their cytotoxic effect. Synonyms: MK-1775; MK1775; MK 1775; AZD1775; AZD-1775; AZD 1775; adavosertib. 1-[6-(2-hydroxypropan-2-yl)pyridin-2-yl]-6-[4-(4-methylpiperazin-1-yl)anilino]-2-prop-2-enylpyrazolo[3,4-d]pyrimidin-3-one. Grades: >98%. CAS No. 955365-80-7. Molecular formula: C27H32N8O2. Mole weight: 500.607. | |
| Monalizumab | Monalizumab (IPH2201) is an immune checkpoint inhibitor targeting Natural Killer Group 2A ( NKG2A ). Monalizumab, a humanized anti-NKG2A blocking mAb, increases IFN-γ production, thereby promoting NK cell effector functions. Monalizumab can be used for the research of head and neck squamous cell carcinoma (HNSCC) [1] [2]. Uses: Scientific research. Group: Inhibitory antibodies. Alternative Names: IPH2201. CAS No. 1228763-95-8. Pack Sizes: 1 mg; 5 mg. Product ID: HY-P99032. | |
| Monalizumab | Monalizumab is a first-in-class immune checkpoint inhibitor that targets Natural Killer Group 2A (NKG2A). Monalizumab increased degranulation and IFN-γ production by NKG2A+ NK cell against HLA-E+ target cells, thereby promoting NK cell effector functions. Synonyms: IPH2201. CAS No. 1228763-95-8. | |
| Monastrol | Monastrol is a kinesin Eg5 inhibitor. Induction of apoptosis by monastrol is independent of the spindle checkpoint. Monastrol binds to the KSP-ADP complex, forming a KSP-ADP-monastrol ternary complex, which cannot bind to microtubules productively and cannot undergo further ATP-driven conformational changes. Uses: Antimitotic agents. Synonyms: DL-Monastrol; (S)-Monastrol; (+/-)-Monastrol; 4-(3-Hydroxyphenyl)-6-methyl-2-thioxo-1,2,3,4-tetrahydro-4H-pyrimidin-5-carboxylic Acid Ethyl Ester. CAS No. 254753-54-3. Molecular formula: C14H16N2O3S. Mole weight: 292.36. | |
| MPDL3280A | A human, Fc optimized, monoclonal antibody directed against the protein ligand PD-L1 (programmed cell death-1 ligand 1), with potential immune checkpoint inhibitory and antineoplastic activities. Atezolizumab binds to PD-L1, blocking its binding to and activation of its receptor programmed death 1 (PD-1) expressed on activated T-cells, which may enhance the T-cell-mediated immune response to neoplasms and reverse T-cell inactivation. In addition, by binding to PD-L1, atezolizumab also prevents binding of this ligand to B7.1 expressed on activated T cells, which further enhances the T-cell-mediated immune response. PD-L1 is overexpressed on many human cancer cell types and on various tumor-infiltrating immune cells. PD-L1 binding to PD-1 on T-cells suppresses the immune system and results in increased immune evasion. PD-1, a transmembrane protein, is a negative regulator of the immune system that limits the expansion and survival of CD8+ T cells. The Fc region of atezolizumab is modified in such a way that it does not induce either antibody-dependent cytotoxicity (ADCC) or complement-dependent cytotoxicity (CDC). Synonyms: Atezolizumab; RG 7446; RO 5541267; RG7446; RO5541267; RG-7446; RO-5541267; TECENTRIQ. CAS No. 1380723-44-3. Molecular formula: C37H62N4O2S. Mole weight: 627. | |
| MPI-0479605 | MPI-0479605 is a potent and selective ATP competitive inhibitor of Mps1. Cells treated with MPI-0479605 undergo aberrant mitosis, resulting in aneuploidy and formation of micronuclei. In cells with wild-type p53, this promotes the induction of a postmitotic checkpoint characterized by the ATM- and RAD3-related-dependent activation of the p53-p21 pathway. In both wild-type and p53 mutant cells lines, there is a growth arrest and inhibition of DNA synthesis. Subsequently, cells undergo mitotic catastrophe and/or an apoptotic response. In xenograft models, MPI-0479605 inhibits tumor growth, suggesting that drugs targeting Mps1 may have utility as novel cancer therapeutics. Synonyms: MPI-0479605; MPI 0479605; MPI0479605. Grades: 0.98. CAS No. 1246529-32-7. Molecular formula: C22H29N7O. Mole weight: 407.522. | |
| Mps1-IN-2 | Small-molecule inhibitor of Mps1 kinase (IC50 values 145 nM) with greater than 1000-fold selectivity relative to the 352-member kinase panel, with the major exceptions of Gak and Plk1 (Ambit essay Kd values 12 nM, 140 nM, and 61 nM for Mps1, Gak, and Plk1, respectively). Mps1-IN-2 induces bypass of a checkpoint-mediated mitotic arrest and provides a unique tool to investigate the combined inhibition of Plk1 and Mps1. Synonyms: Mps1-IN-2. Grades: >98%. CAS No. 1228817-38-6. Molecular formula: C26H36N6O3. Mole weight: 480.6. | |
| MPS1 Inhibitor, NMS-P715 ( (N- (2, 6-diethylphenyl) -1-methyl-8- ({4-[ (1-methylpiperidin-4-yl) carbamoyl]-2- (trifluoromethoxy) phenyl}amino) -4, 5-dihydro-1H-pyrazolo[4, 3-h]quinazoline-3-carboxamide) ) | An orally bioavailable, ATP-competitive, pyrazolo-quinazoline, MPS1 inhibitor (IC50=182nM, Ki=0.99nM) that is shown to act in a reversible and time-dependent manner. It demonstrates selectivity for MPS1 against a panel of 60 kinases, displaying activity against only three kinases, CK2, MELK, and NEK6 (<10uM), but not against other mitotic kinases including PLK1, CDK1, Aurora A, Aurora B, or the SAC kinase BUB1, in an in vitro kinase assay. It promotes massive SAC (spindle assembly checkpoint) override (EC50=65nM) in nocodazole-arrested U20S cells and elicits a reduction in the G1 and G2/M phase of the cell cycle in A2780 ovarian cancer cells, similar to RNAi-mediated MPS1 silencing. In addition, it is shown to inactivate SAC, delocalize kinetochore components, and inhibit the proliferation of select cancer cell lines (IC50 ~1uM), without marked activity among a panel of 127 normal cell lines. Also, it inhibits A2780 tumor xenograft growth in mice (90mg/kg/day, o.s., in vivo) by 53% wit Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 5mg. US Biological Life Sciences. | Worldwide |
| MPS1/TTK Inhibitor | MPS1/TTK inhibitor is an inhibitor of monopolar spindle 1 (MPS1/TTK), a dual-specificity kinase playing an essential role in mitotic spindle checkpoint signaling that is overexpressed in certain cancerous tumors. Synonyms: N-(2,6-diethylphenyl)-4,5-dihydro-8-[[2-methoxy-4-(4-methyl-1-piperazinyl)phenyl]amino]-1-methyl-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide. Grades: ≥98%. CAS No. 1202055-39-7. Molecular formula: C33H40N8O2. Mole weight: 580.72. | |
| N-Desmethyl Dovitinib | Dovitinib derivative; a benzimidazole quinolinone for inhibiting a checkpoint kinase 1 and its use in combination therapy for cancer. Group: Biochemicals. Alternative Names: 4-Amino-5-fluoro-3-[6-(1-piperazinyl)-1H-benzimidazol-2-yl]-. Grades: Highly Purified. CAS No. 668432-44-8. Pack Sizes: 1mg. US Biological Life Sciences. | Worldwide |
| Neihulizumab | Neihulizumab (ALTB-168) is an immune checkpoint agonistic antibody that binds to human CD162 (PSGL-1) , leading to downregulation of activated T-cells. Neihulizumab can be uesd for steroid-refractory acute graft-versus-host-disease (SR-aGVHD), psoriasis, psoriatic arthritis and ulcerative colitis research [1]. Uses: Scientific research. Group: Inhibitory antibodies. Alternative Names: ALTB-168; Anti-PSGL1/CD162 Reference Antibody (neihulizumab). CAS No. 2158362-38-8. Pack Sizes: 1 mg; 5 mg; 10 mg. Product ID: HY-P99378. | |
| nivolumab | Nivolumab, marketed as Opdivo, is a humanized IgG4 anti-PD-1 monoclonal antibody used to treat cancer. Nivolumab works as a checkpoint inhibitor, blocking a signal that would have prevented activated T cells from attacking the cancer, thus allowing the immune system to clear the cancer. Synonyms: Opdivo; ONO-4538; BMS-936558; MDX1106; ONO4538; BMS936558; MDX 1106; ONO 4538; BMS 936558; MDX-1106. CAS No. 946414-94-4. | |
| NSC 109555 dimesylate | NSC 109555 is a potent and selective inhibitor of checkpoint kinase 2 (Chk2), displaying no effect against other kinases. It inhibits H1 phosphorylation and attenuates mitochondrial ATP synthesis. NSC 109555 can be used in cancer therapy. Synonyms: DDUG; NCI C04808; Carbanilide, 4,4'-diacetyl-, 4,4'-bis(amidinohydrazone), dimethanesulfonate. CAS No. 15427-93-7. Molecular formula: C19H24N10O·2CH3SO3H. Mole weight: 600.7. | |
| PD0166285 | PD0166285 is a potent Wee1 inhibitor and Chk1 inhibitor with activity at nanomolar concentrations. This G2 checkpoint abrogation by PD0166285 was demonstrated to kill cancer cells, there at a toxic highest dose of 0.5 muM in some cell lines for exposure periods of no longer than 6 hours. The deregulated cell cycle progression may have ultimately damaged the cancer cells. We herein report one of the mechanism by which PD0166285 leads to cell death in the B16 mouse melanoma cell line. Synonyms: PD166285; 6-(2,6-dichlorophenyl)-2-((4-(2-(diethylamino)ethoxy)phenyl)amino)-8-methylpyrido[2,3-d]pyrimidin-7(8H)-one; 6-(2,6-Dichlorophenyl)-2-[4-(2-diethylaminoethoxy)phenylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one; Pyrido[2,3-d]pyrimidin-7(8H)-one, 6-(2,6-dichlorophenyl)-2-[[4-[2-(diethylamino)ethoxy]phenyl]amino]-8-methyl-. Grades: ≥98%. CAS No. 185039-89-8. Molecular formula: C26H27Cl2N5O2. Mole weight: 512.44. | |
| PD0407824 | PD0407824 is a potent and selective inhibitor of checkpoint kinase Chk1 and WEE1 with IC50s of 47 and 97 nM, respectively. It is a BMP chemical sensitizer that increases cell sensitivity to subthreshold amounts of BMP4. It has potential anticancer activity. Synonyms: PD 407824; 9-Hydroxy-4-phenylpyrrolo[3,4-c]carbazole-1,3(2H,6H)-dione; Pyrrolo[3,4-c]carbazole-1,3(2H,6H)-dione, 9-hydroxy-4-phenyl-. Grades: ≥98%. CAS No. 622864-54-4. Molecular formula: C20H12N2O3. Mole weight: 328.32. | |
| PD 166285 dihydrochloride | PD 166285, a novel protein tyrosine kinase inhibitor of a new structural class, is a potent inhibitor of the tyrosine kinases c-Src, Flg (fibroblast growth factor receptor 1, FGFR1), and PDGFRβ (platelet-derived growth factor receptor β) (IC50 values are 8.4, 39.3 and 98.3 nM respectively). PD 166285 also inhibits the checkpoint kinases Wee1 and MYT1 (Myt1), abolishes Cdc2 phosphorylation in numerous tumor cell lines, and abrogates the G2 checkpoint. Synonyms: PD 166285 dihydrochloride; PD166285 dihydrochloride; PD-166285 dihydrochloride6-(2,6-Dichlorophenyl)-2-[[4-[2-(diethylamino)ethoxy]phenyl]amino]-8-methylpyrido[2,3-d]pyrimidin-7(8H)-one dihydrochloride. Grades: ≥99% by HPLC. CAS No. 212391-63-4. Molecular formula: C26H27Cl2N5O2.2HCl. Mole weight: 585.35. | |
| PF-03814735 | PF-03814735 is an orally bioavailable, ATP-competitive, reversible small-molecule Aurora kinase inhibitor with potential antineoplastic activity. Aurora kinase inhibitor PF-03814735 binds to and inhibits Aurora kinases A and B, which may result in the inhibition of cellular division and proliferation in tumor cells that overexpress these kinases. Aurora kinases are serine-threonine kinases that play essential roles in mitotic checkpoint control during mitosis. Synonyms: PF03814735; PF-03814735; PF 03814735. Grades: >98%. CAS No. 942487-16-3. Molecular formula: C23H25F3N6O2. Mole weight: 474.48. | |
| PF 477736 | Selective checkpoint kinase 1 (Chk1) inhibitor (Ki values are 0.49 and 47 nM for Chk1 and Chk2 respectively). Abrogates cell cycle arrest at S and G2-M checkpoints; sensitizes cells to DNA damage. Group: Biochemicals. Grades: Highly Purified. CAS No. 952021-60-2. Pack Sizes: 10mg. Molecular Formula: C??H??N?O?. US Biological Life Sciences. | Worldwide |
| PF-477736 | PF-477736 is a proprietary compound targeting cell cycle checkpoint kinase 1 (chk1) with potential chemopotentiation activity. Chk1 inhibitor PF-477736 inhibits chk1, an ATP-dependent serine-threonine kinase that is a key component in the DNA replication-monitoring S/G2 checkpoint system. By overriding the last checkpoint defense against DNA damaging agent-induced lethal damage, chk1 inhibitor PF-477736 may potentiate the antitumor efficacy of various chemotherapeutic agents against tumor cells with intrinsic checkpoint defects. Synonyms: PF-477736; PF-477736; PF-477736; PF-00477736; PF00477736; PF 00477736. CAS No. 952021-60-2. Molecular formula: C22H25N7O2. Mole weight: 419.489. | |
| Pidilizumab | A humanized, immunoglobulin (Ig) G1 monoclonal antibody directed against human inhibitory receptor programmed cell death 1 (PD-1; PDCD1), with potential immune checkpoint inhibitory and antineoplastic activities. Pidilizumab binds to PD-1 and blocks the interaction between PD-1 and its ligands, PD-1 ligand 1 (PD-L1) and PD-1 ligand 2 (PD-L2). This prevents the activation of PD-1 and its downstream signaling pathways. This may restore immune function through the activation of natural killer (NK) cells and cytotoxic T-lymphocytes (CTLs) against tumor cells. PD-1, an inhibitory receptor belonging to the B7-receptor family expressed on activated T-lymphocytes, B-cells and NK cells, negatively regulates T-cell activation and effector function when activated by its ligands; it plays an important role in tumor evasion from host immunity. Synonyms: CT-011; MDV 9300; CT 011; MDV9300; CT011; MDV-9300. CAS No. 1036730-42-3. | |
| Poloxin | Poloxin is the first small-molecule inhibitor specifically targeting the function of the Plk1 PBD. Poloxin induces centrosome fragmentation and abnormal spindle and chromosome misalignment, which activate the spindle assembly checkpoint and prolong mitosis. Notably, centrosomal fragmentation induced by Poloxin is partially attributable to dysfunctional Kizuna, a key substrate of Plk1 at centrosomes. Moreover, Poloxin strongly inhibits proliferation of a panel of cancer cells by inducing mitotic arrest, followed by a surge of apoptosis. More important, we report, for the first time to our knowledge, that the PBD inhibitor, Poloxin, significantly suppresses tumor growth of cancer cell lines in xenograft mouse models by lowering the proliferation rate and triggering apoptosis in treated tumor tissues. Targeting the PBD by Poloxin is a powerful approach for selectively inhibiting Plk1 function in vitro and in vivo. Synonyms: Poloxin. Grades: 0.98. CAS No. 321688-88-4. Molecular formula: C18H19NO3. Mole weight: 297.354. | |
| Prexasertib | Prexasertib (LY2606368) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a K i of 0.9 nM and an IC 50 of <1 nM. Prexasertib inhibits CHK2 (IC 50 =8 nM) and RSK1 (IC 50 =9 nM). Prexasertib causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib shows potent anti-tumor activity [1] [2]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: LY2606368. CAS No. 1234015-52-1. Pack Sizes: 10 mM * 1 mL; 1 mg; 5 mg; 10 mg; 50 mg; 100 mg. Product ID: HY-18174. | |
| Prexasertib dihydrochloride | Prexasertib dihydrochloride (LY2606368 dihydrochloride) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a K i of 0.9 nM and an IC 50 of <1 nM. Prexasertib dihydrochloride inhibits CHK2 (IC 50 =8 nM) and RSK1 (IC 50 =9 nM). Prexasertib dihydrochloride causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib dihydrochloride shows potent anti-tumor activity [1] [2]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: LY2606368 dihydrochloride. CAS No. 1234015-54-3. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-18174A. | |
| proTAME | proTAME is a cell-permeable prodrug of N-4-tosyl-L-arginine methyl ester (TAME), which is an inhibitor of the anaphase-promoting complex/cyclosome (APC/C) suppressing its activation by Cdc20 and Cdh1. It induces mitotic arrest by activating the spindle assembly checkpoint (SAC). Synonyms: Pro-N-4-tosyl-L-arginine methyl ester; Methyl (2S) -5- [bis [ (2-phenylacetyl) oxymethoxycarbonylamino] methylideneamino] -2- [ (4-methylphenyl) sulfonylamino] pentanoate. Grades: ≥90%. CAS No. 1362911-19-0. Molecular formula: C34H38N4O12S. Mole weight: 726.75. | |
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