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Cdk4 inhibitor is a cell-permeable, asymmetrical indolocarbazole that exhibits antiproliferative activity by blocking cyclin D1/Cdk4 with an IC50 of 0.8 μM. It also inhibits the activity of other Cdk's only at much higher concentrations (IC50 = 520 nM and 2.1 μM for Cdk2/E and Cdk1/B, respectively). Cdk4 inhibitor can inhibit tumor cells growth in HCT-116 and NCI-H460 cells (IC50 < 3.0 μM). Synonyms: 2-Bromo-12,13-dihydro-5H-indolo[2,3-a]pyrrolo[3,4-c]carbazole-5,7(6H)-dione. Grades: ≥90%. CAS No. 546102-60-7. Molecular formula: C20H10BrN3O2. Mole weight: 404.22.
Cdk4 Inhibitor III - CAS 265312-55-8
The Cdk4 Inhibitor III, also referenced under CAS 265312-55-8, controls the biological activity of Cdk4. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications. Group: Fluorescence/luminescence spectroscopy.
Cdk4 Inhibitor II, NSC 625987 - CAS 141992-47-4
The Cdk4 Inhibitor II, NSC 625987, also referenced under CAS 141992-47-4, controls the biological activity of Cdk4. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications. Group: Fluorescence/luminescence spectroscopy.
Cdk4 Inhibitor V (4-(((4-Hydroxy-5-propoxy-pyridin-2-ylmethyl)-amino)-methylene)-6-iodo-4H-isoquinoline-1,3-dione)
A cell-permeable pyridinylmethylamino-isoquinoline dione compound that acts as a potent, ATP-binding site targeting and reversible inhibitor of Cdk4/D1 activity with selectivity over Cdk2/E and Cdk1/B (IC50=0.03, 1.6 and 25.3uM, respectively). Shown to block the phosphorylation of Rb and induce growth arrest in HCT116 and MCF-7 cells (IC50=0.73 and 0.88uM). Displays desirable metabolic stability in rat liver microsomes and in the presence of NADPH and UDPGA cofactors (t1/2 > 30mins). Group: Biochemicals. Grades: Highly Purified. CAS No. 943746-57-4. Pack Sizes: 5mg. Molecular Formula: C??H??IN?O?. US Biological Life Sciences.
Worldwide
Cdk4 Inhibitor V - CAS 943746-57-4
The Cdk4 Inhibitor V, also referenced under CAS 943746-57-4, controls the biological activity of Cdk4. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications. Group: Fluorescence/luminescence spectroscopy.
CDK4/6 Inhibitor IV
Cdk4/6 inhibitor IV is a cell-permeable triaminopyrimidine inhibitor for Cdk4/cyclin D1 with IC50 values of 1.5 μM and Cdk6/cyclin D1 with IC50 values of 5.6 μM. It exhibits blocking of pRb phosphorylation at Ser780 and Ser795. Cdk4/6 inhibitor IV can suppresses tumor growth in Xenograft mouse model. Synonyms: CINK4; Cyclin-dependent kinase 4/6 Inhibitor IV. Grades: ≥98%. CAS No. 359886-84-3. Molecular formula: C27H32N6O. Mole weight: 456.6.
Cdk4/6 Inhibitor IV - CAS 359886-84-3
The Cdk4/6 Inhibitor IV, also referenced under CAS 359886-84-3, controls the biological activity of Cdk4/6. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications. Group: Fluorescence/luminescence spectroscopy.
10Z-Hymenialdisine
10Z-Hymenialdisine is a pan kinase inhibitor (IC50 values are 6, 10, 22, 28, 35, 40, 70, 80, 100, 470, 500, 600, 700 and 700 nM for MEK1, GSK-3β, Cdk1/cyclin B, Cdk5/p25, CK1, Cdk2/cyclin A, Cdk2/cyclin E, ASK-γ, Cdk3/cyclin E, Erk1, PKCγ, Cdk4/cyclin D1, Cdk6/cyclin D2 and PKCα, respectively). 10Z-Hymenialdisine inhibits NF-κB activation and suppresses inflammatory gene expression. Synonyms: Hymenialdisine; (Z)-Hymenialdisine; 4-(2-amino-4-oxo-1H-imidazol-5(4H)-ylidene)-2-bromo-4,5,6,7-tetrahydropyrrolo[2,3-c]azepin-8(1H)-one. Grades: ≥97% by HPLC. CAS No. 82005-12-7. Molecular formula: C11H10BrN5O2. Mole weight: 324.13.
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.
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
1,4-Bis(4-nitrophenyl)piperazine
An impurity of Palbociclib, a selective inhibitor of cyclin-dependent kinases CDK4 and CDK6. Palbociclib is developed for the treatment of ER-positive and HER2-negative breast cancer. Synonyms: 1,4-Bis(4-nitrophenyl)piperazine; 16264-05-4; Piperazine, 1,4-bis(4-nitrophenyl)-EINECS 240-371-8UNII-P6TE7B2EYY. CAS No. 16264-05-4. Molecular formula: C16H16N4O4. Mole weight: 328.328.
An impurity of Palbociclib which is a selective inhibitor of the cyclin-dependent kinases CDK4 and CDK6. Synonyms: Palbociclib Impurity 25. Grades: >95%. CAS No. 2488840-59-9. Molecular formula: C24H29N7O4. Mole weight: 479.54.
1-?(6-?Nitro-?3-?pyridinyl)?piperazine
1-?(6-?Nitro-?3-?pyridinyl)?piperazine is a reagent used in the preparation of highly potent and orally bioavailable 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amine cyclin-dependant kinases as anticancer agents. Also is an impurity of Palbociclib (P139900), an experimental drug for the treatment of breast cancer being developed by Pfizer. It is a selective inhibitor of the cyclin-dependent kinases CDK4 and CDK6. Group: Biochemicals. Grades: Highly Purified. CAS No. 775288-71-6. Pack Sizes: 25mg, 50mg. Molecular Formula: C9H12N4O2. US Biological Life Sciences.
1-? (Benzyloxycarbonyl) ?pyrrolidine-?3-?carboxylic Acid is a reagent used in the synthesis of cyclin-dependent kinase 4-inhibitors (CDK4) for cancer treatments. Also used towards the discovery of a potent inhibitor of poly(ADP-ribose) polymerase (PARP) for the treatment of cancer pased upon benzimidazole carboxamide moieties. Group: Biochemicals. Grades: Highly Purified. CAS No. 188527-21-1. Pack Sizes: 100mg, 250mg. Molecular Formula: C13H15NO4, Molecular Weight: 249.26. US Biological Life Sciences.
Worldwide
1-Boc-4-(6-aminopyridin-3-yl)piperazine-d4
1-Boc-4-(6-aminopyridin-3-yl)piperazine-d4 is an intermediate in synthesizing Palbociclib-d4 (P139901), an isotope labelled compound of Palbociclib (P139900). Palbociclib (P139900) is an experimental drug for the treatment of breast cancer being developed by Pfizer. It is a selective inhibitor of the cyclin-dependent kinases CDK4 and CDK6. Group: Biochemicals. Grades: Highly Purified. CAS No. 1808106-94-6. Pack Sizes: 25mg, 50mg. Molecular Formula: C14H18D4N4O2. US Biological Life Sciences.
Worldwide
1-Piperazin-N-oxide Palbociclib
1-Piperazin-N-oxide Palbociclib is a derivative compound of Palbociclib (P139900). Palbociclib (also known as compound number PD-0332991) is an experimental drug for the treatment of breast cancer being developed by Pfizer. It is a selective inhibitor of the cyclin-dependent kinases CDK4 and CDK6. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 1mg, 2.5mg. Molecular Formula: C24H29N7O3, Molecular Weight: 463.53. US Biological Life Sciences.
2,7-Diazaspiro[3.5]nonane-7-carboxylic Acid tert-Butyl Ester is a reagent in the synthesis of RET kinase inhibitors. In addition it is used in the preparation of CDK4/6 inhibitors. Group: Biochemicals. Grades: Highly Purified. CAS No. 896464-16-7. Pack Sizes: 100mg, 250mg. Molecular Formula: C12H22N2O2, Molecular Weight: 226.32. US Biological Life Sciences.
2-? Chloro-? 8-? cyclopentyl-? 5-? methyl-? 8H-? pyrido [2, ? 3-? d] ? pyrimidin-? 7-? one is an impurity of Palbociclib (P139900),(also known as compound number PD-0332991) is an experimental drug for the treatment of breast cancer being developed by Pfizer. It is a selective inhibitor of the cyclin-dependent kinases CDK4 and CDK6. Group: Biochemicals. Grades: Highly Purified. CAS No. 1013916-37-4. Pack Sizes: 250mg, 1g. Molecular Formula: C13H14ClN3O, Molecular Weight: 263.72. US Biological Life Sciences.
Worldwide
3-ATA
3-ATA is a selective cyclin-dependent kinase 4 (CDK4) inhibitor. Group: Biochemicals. Grades: Highly Purified. CAS No. 129821-08-5. Pack Sizes: 1mg, 2.5mg. Molecular Formula: C13H10N2OS, Molecular Weight: 242.3. US Biological Life Sciences.
Worldwide
5-bromo-4-chloro-N-cyclopentylpyrimidin-2-amine
An impurity of Palbociclib, a selective inhibitor of cyclin-dependent kinases CDK4 and CDK6. Palbociclib is developed for the treatment of ER-positive and HER2-negative breast cancer. Synonyms: 5-Bromo-4-chloro-N-cyclopentylpyrimidin-2-amine; 1823404-28-9; CS-0011349; D87404; 5-?Bromo-?4-?chloro-?N-?cyclopentylpyrimidin?-?2-?amine. CAS No. 1823404-28-9. Molecular formula: C9H11BrClN3. Mole weight: 276.56.
An impurity of Palbociclib which is a selective inhibitor of the cyclin-dependent kinases CDK4 and CDK6. Synonyms: Palbociclib Impurity 27; Pyrido(2,3-d)pyrimidin-7(8H)-one, 6-acetyl-2-amino-8-cyclopentyl-5-methyl-. CAS No. 571189-64-5. Molecular formula: C15H18N4O2. Mole weight: 286.33.
An impurity of Palbociclib which is a selective inhibitor of the cyclin-dependent kinases CDK4 and CDK6. Synonyms: Palbociclib Impurity 26; Pyrido[2,3-d]pyrimidin-7(8H)-one, 6-acetyl-8-cyclopentyl-5-methyl-2-[[5-(4-methyl-1-piperazinyl)-2-pyridinyl]amino]-. CAS No. 571189-51-0. Molecular formula: C25H31N7O2. Mole weight: 461.57.
An impurity of Palbociclib, a selective inhibitor of cyclin-dependent kinases CDK4 and CDK6. Palbociclib is developed for the treatment of ER-positive and HER2-negative breast cancer. Synonyms: 4-[6-[(6-bromo-8-cyclopentyl-5-methyl-7-oxo-2-pyrido[2,3-d]pyrimidinyl)amino]-3-pyridinyl]-1-piperazinecarboxylic acid tert-butyl ester; tert-butyl 4-[6-[(6-bromo-8-cyclopentyl-5-methyl-7-oxopyrido[2,3-d]pyrimidin-2-yl)amino]pyridin-3-yl]piperazine-1-carboxylate. CAS No. 571188-82-4. Molecular formula: C27H34BrN7O3. Mole weight: 584.51.
6-Desacetyl-6-Bromo Palbociclib
An impurity of Palbociclib, a selective inhibitor of cyclin-dependent kinases CDK4 and CDK6. Palbociclib is developed for the treatment of ER-positive and HER2-negative breast cancer. Synonyms: 6-Bromo-8-cyclopentyl-5-methyl-2-[(5-piperazin-1-ylpyridin-2-yl)amino]pyrido[2,3-d]pyrimidin-7-one; Pyrido-[2,3-d]-pyrimidin-7-one 41. CAS No. 851067-56-6. Molecular formula: C22H26BrN7O. Mole weight: 484.402.
6-Desacetyl-6-Bromo Palbociclib Hydrochloride
An impurity of Palbociclib, a selective inhibitor of cyclin-dependent kinases CDK4 and CDK6. Palbociclib is developed for the treatment of ER-positive and HER2-negative breast cancer. Synonyms: 6-bromo-8-cyclopentyl-5-methyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one hydrochloride. CAS No. 850918-83-1. Molecular formula: C22H27ClBrN7O. Mole weight: 520.86.
6-Desacetyl Palbociclib
An impurity of Palbociclib, a selective inhibitor of cyclin-dependent kinases CDK4 and CDK6. Palbociclib is developed for the treatment of ER-positive and HER2-negative breast cancer. Synonyms: Pyrido[2,3-d]pyriMidin-7(8H)-one, 8-cyclopentyl-5-Methyl-2-[[5-(1-piperazinyl)-2-pyridinyl]aMino]-; Pyrido-[2,3-d]-pyrimidin-7-one 38. CAS No. 571190-22-2. Molecular formula: C22H27N7O. Mole weight: 405.506.
6-Desacetyl Palbociclib Hydrochloride
An impurity of Palbociclib, a selective inhibitor of cyclin-dependent kinases CDK4 and CDK6. Palbociclib is developed for the treatment of ER-positive and HER2-negative breast cancer. Synonyms: 8-cyclopentyl-5-methyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one hydrochloride. CAS No. 571189-66-7. Molecular formula: C22H28ClN7O. Mole weight: 441.96.
An impurity of Palbociclib which is a selective inhibitor of the cyclin-dependent kinases CDK4 and CDK6. Synonyms: Pyrido[2,3-d]pyrimidin-7(8H)-one, 8-cyclopentyl-5-methyl-2,6-bis[[5-(1-piperazinyl)-2-pyridinyl]amino]; Palbociclib Impurity G. CAS No. 2458234-37-0. Molecular formula: C31H39N11O. Mole weight: 581.73.
Abemaciclib
Abemaciclib is a potent and selective inhibitor of cyclin-dependent kinases, CDK4 and CDK6, as a method to inhibit the proliferation of cancer cells. Group: Biochemicals. Grades: Highly Purified. CAS No. 1231929-97-7. Pack Sizes: 5mg, 10mg. Molecular Formula: C27H32F2N8, Molecular Weight: 506.59. US Biological Life Sciences.
Worldwide
Abemaciclib
Abemaciclib is an orally available cyclin-dependent kinase (CDK) inhibitor that targets the CDK4 (cyclin D1) and CDK6 (cyclin D3) cell cycle pathway, with potential antineoplastic activity. It is used for the treatment of advanced or metastatic breast cancers. Synonyms: LY-2835219; LY 2835219; LY2835219; Verzenio; N-[5-[(4-ethylpiperazin-1-yl)methyl]pyridin-2-yl]-5-fluoro-4-(7-fluoro-2-methyl-3-propan-2-ylbenzimidazol-5-yl)pyrimidin-2-amine. Grades: ≥98%. CAS No. 1231929-97-7. Molecular formula: C27H32F2N8. Mole weight: 506.61.
Abemaciclib
Abemaciclib (LY2835219) is a selective CDK4/6 inhibitor with IC 50 values of 2 nM and 10 nM for CDK4 and CDK6, respectively. Uses: Scientific research. Group: Signaling pathways. Alternative Names: LY2835219. CAS No. 1231929-97-7. Pack Sizes: 5 mg; 10 mg; 50 mg; 100 mg; 200 mg; 500 mg; 1 g. Product ID: HY-16297A.
Abemaciclib-[d5]
Labelled Abemaciclib. Abemaciclib is an orally available cyclin-dependent kinase (CDK) inhibitor that targets the CDK4 (cyclin D1) and CDK6 (cyclin D3) cell cycle pathway, with potential antineoplastic activity. It is used for the treatment of advanced or metastatic breast cancers. Synonyms: N-[5-[(4-Ethyl-1-piperazinyl)methyl]-2-pyridinyl]-5-fluoro-4-[4-fluoro-2-methyl-1-(1-methylethyl)-1H-benzimidazol-6-yl]-2-pyrimidinamine-d5; N-(5-((4-ethylpiperazin-1-yl)methyl)pyridin-2-yl)-5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazol-6-yl)pyrimidin-2-amine-d5. Grades: > 98%. CAS No. 1809251-51-1. Molecular formula: C27H27D5F2N8. Mole weight: 511.62.
Abemaciclib-[d7]
Labelled Abemaciclib. Abemaciclib is an orally available cyclin-dependent kinase (CDK) inhibitor that targets the CDK4 (cyclin D1) and CDK6 (cyclin D3) cell cycle pathway, with potential antineoplastic activity. It is used for the treatment of advanced or metastatic breast cancers. Synonyms: N-(5-((4-ethylpiperazin-1-yl)methyl)pyridin-2-yl)-5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazol-6-yl)pyrimidin-2-amine-d7. Grades: > 98%. Molecular formula: C27H25D7F2N8. Mole weight: 513.64.
abemaciclib mesylate
Abemaciclib mesylate is a CDK inhibitor with selectivity for CDK4 and CDK6. It was approved for the treatment of advanced or metastatic breast cancers. Uses: The treatment of advanced or metastatic breast cancers. Synonyms: Verzenio; LY2835219; LY 2835219; LY-2835219; UNII-KKT462Q807; Abemaciclib methanesulfonate; N-(5-((4-ethylpiperazin-1-yl)methyl)pyridin-2-yl)-5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazol-6-yl)pyrimidin-2-amine methanesulfonate. CAS No. 1231930-82-7. Molecular formula: C28H36F2N8O3S. Mole weight: 602.706.
Abemaciclib metabolite M18 hydrochloride
Abemaciclib metabolite M18 (LSN3106729) hydrochloride, the metabolite of Abemaciclib (HY-16297A), is a CDK inhibitor with antitumor activity. Abemaciclib metabolite M18 hydrochloride and a CRBN ligand have been used to design PROTAC CDK4/6 degrader [1] [2]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: LSN3106729 hydrochloride. CAS No. 2704316-82-3. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-126534A.
Abemaciclib metabolite M2
Abemaciclib metabolite M2 (LSN2839567) is a metabolite of Abemaciclib, acts as a potent CDK4 and CDK6 inhibitor, with IC50s of 1.2 and 1.3 nM, respectively. Anti-cancer activity[1][2]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: LSN2839567. CAS No. 1231930-57-6. Pack Sizes: 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-128669.
Abemaciclib methanesulfonate
Abemaciclib methanesulfonate (LY2835219 methanesulfonate) is a selective CDK4/6 inhibitor with IC 50 s of 2 nM and 10 nM for CDK4 and CDK6, respectively [1] [2] [3]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: LY2835219 methanesulfonate. CAS No. 1231930-82-7. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg; 100 mg; 200 mg; 500 mg. Product ID: HY-16297.
AG-012986
AG-012986 is a multitargeted cyclin-dependent kinase (CDK) inhibitor active against CDK1, CDK2, CDK4/6, CDK5, and CDK9, with selectivity over a diverse panel of non-CDK kinases. AG-012986 showed antiproliferative activities in vitro with IC(50)s of <100 nmol/L in 14 of 18 tumor cell lines. In vivo, significant antitumor efficacy induced by AG-012986 was seen (tumor growth inhibition,>83.1%) in 10 of 11 human xenograft tumor models. AG-012986 also showed dose-dependent retinoblastoma Ser(795) hypophosphorylation, cell cycle arrest, decreased Ki-67 tumor staining, and apoptosis in conjunction with antitumor activity. Synonyms: AG 012986; AG012986; Benzamide, 4-((4-amino-5-(2,6-difluorobenzoyl)-2-thiazolyl)amino)-N-((1R)-2-(dimethylamino)-1-methylethyl)-. Grades: >98%. CAS No. 486414-35-1. Molecular formula: C22H23F2N5O2S. Mole weight: 459.51.
AG-024322
AG-24322 is a second generation CDK inhibitor. AG-024322 is a potent inhibitor of CDK1, CDK2, and CDK4 that produces cell-cycle arrest and antitumor activity in preclinical models. Synonyms: AG-24322; AG 24322; AG24322. Grades: 98%. CAS No. 837364-57-5. Molecular formula: C23H20F2N6. Mole weight: 418.44.
AMG 925
AMG-925 is a potent, selective, and bioavailable FLT3/cyclin-dependent kinase 4 (CDK4) dual kinase inhibitor. AMG 925 inhibited AML xenograft tumor growth by 96% to 99% without significant body weight loss. The antitumor activity of AMG 925 correlated with the inhibition of STAT5 and RB phosphorylation, the pharmacodynamic markers for inhibition of FLT3 and CDK4, respectively. In addition, AMG 925 was also found to inhibit FLT3 mutants (e.g., D835Y) that are resistant to the current FLT3 inhibitors (e.g., AC220 and sorafenib). AMG 925, which combines inhibition of two kinases essential for proliferation and survival of FLT3-mutated AML cells, may improve and prolong clinical responses. Synonyms: AMG925; AMG-925; AMG 925; FLX925; FLX-925; FLX 925. Grades: >98%. CAS No. 1401033-86-0. Molecular formula: C26H29N7O2. Mole weight: 471.55.
AT7519
AT7519 (AT7519M) as a potent inhibitor of CDKs , with IC 50 s of 210, 47, 100, 13, 170, and <10 nM for CDK1, CDK2, CDK4 to CDK6, and CDK9, respectively. Uses: Scientific research. Group: Signaling pathways. Alternative Names: AT7519M. CAS No. 844442-38-2. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg; 100 mg. Product ID: HY-50940.
AT7519 Hydrochloride
AT7519 Hydrochloride is a potent inhibitor of CDKs , with IC 50 s of 210, 47, 100, 13, 170, and <10 nM for CDK1, CDK2, CDK4 to CDK6, and CDK9, respectively. Uses: Scientific research. Group: Signaling pathways. CAS No. 902135-91-5. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg; 100 mg. Product ID: HY-50943.
AT7519 TFA
AT7519 (AT7519M) TFA as a potent inhibitor of CDKs , with IC 50 s of 210, 47, 100, 13, 170, and <10 nM for CDK1, CDK2, CDK4 to CDK6, and CDK9, respectively. Uses: Scientific research. Group: Signaling pathways. Alternative Names: AT7519M TFA. CAS No. 1431697-85-6. Pack Sizes: 5 mg; 10 mg; 50 mg; 100 mg. Product ID: HY-50940A.
AZD8421
AZD8421 is a selective CDK2 inhibitor (IC50 = 9 nM) as well as achieving CDK family selectivity in cells versus key off-targets (CDK1, CDK4/6, CDK9), AZD8421 had no significant kinase inhibition outside the CDK family. AZD8421 inhibits cancer cell proliferation by inhibiting pRB phosphorylation, inducing cell cycle arrest in G1/S phase and senescence. AZD8421 can be studied in research for breast cancer and ovarian cancer[1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 3047321-53-6. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg. Product ID: HY-158106.
BMS-265246
BMS-265246 is a potent and selective CDK1/2 inhibitor with IC50 of 6 nM/9 nM. It is 25-fold more selective for CDK1/2 than CDK4. Synonyms: BMS265246; BMS-265246; BMS 265246. Grades: >98%. CAS No. 582315-72-8. Molecular formula: C18H17F2N3O2. Mole weight: 345.34.
BMS-265246
BMS-265246 is a potent and selective pyra-zolopyridine based inhibitor of cdk2/cyclinE, cdk1/cyclinB and cdk4/ cyclinD. Group: Biochemicals. Alternative Names: (4-Butoxy-1H-pyrazolo[3, 4-b]pyridin-5-yl) (2, 6-difluoro-4-methylphenyl) methanone. Grades: Highly Purified. CAS No. 582315-72-8. Pack Sizes: 5mg. US Biological Life Sciences.
Worldwide
Bohemine
Bohemine is a purine analogue and is a synthetic and selective CDK inhibitor with IC50s of 4.6 μM, 83 μM, and 2.7 μM for Cdk2/cyclin E, Cdk2/cyclin A, and Cdk9/cyclin T1, respectively. Bohemine also inhibits ERK2 with an IC50 of 52 μM and has less inhibitory effect on CDK1, CDK4 and CDK6. Bohemine has a broad spectrum anti-cancer activities. Uses: Designed for use in research and industrial production. Product Category: Inhibitors. CAS No. 189232-42-6. Molecular formula: C18H24N6O. Mole weight: 340.42. Purity: ≥97%. Product ID: ACM189232426. Alfa Chemistry ISO 9001:2015 Certified. Categories: Bohemanella.
CA224
CA224 (Compound 1) is a selective and orally active Cdk4 - cyclin D1 inhibitor with an IC 50 of 6.2 μM. CA224 induces cell apoptosis and shows antitumor activity [1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 883561-04-4. Pack Sizes: 5 mg; 10 mg; 25 mg. Product ID: HY-111207.
CDK4/6-IN-15
CDK4/6-IN-15 is an orally active and selective CDK4/6 inhibitor. CDK4/6-IN-15 potently inhibits cancer cells growth. CDK4/6-IN-15 arrests cell cycle at G1 phase and suppresses retinoblastoma tumour suppressor protein (Rb) phosphorylation at S780 and E2 factor (E2F)-regulated gene expression [1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 2078047-99-9. Pack Sizes: 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-142076.
CDK4-IN-1
CDK 4/6 Inhibitor is a part of a group of compounds that exhibits selective inhibitory properties towards Cyclin-Dependent Kinases 4 & 6. These compounds are most commonly used to treat patients with breast cancer. Synonyms: CDK4 IN 1; LEE011 analog; CDK4-IN-1; CDK4IN-1; CDK4-IN1; CDK4IN1; CDK4 IN 1; 4-[5-Chloro-3-(1-methylethyl)-1H-pyrazol-4-yl]-N-[5-[4-(dimethylamino)-1-piperidinyl]-2-pyridinyl]-2-pyrimidinamine. Grades: >98%. CAS No. 1256963-02-6. Molecular formula: C22H29ClN8. Mole weight: 440.97.
CDK9-IN-1
Among CDKs, CDK9 is a validated pathological target in HIV infection, inflammation and cardiac hypertrophy; however selective CDK9 inhibitors are still not available. We present a selective inhibitor family of CDK9 based on the 4-phenylamino-6- phenylpyrimidine nucleus. We show a convenient synthetic method to prepare a useful intermediate and its derivatisation resulting in novel compounds. The CDK9 inhibitory activity of the derivatives was measured in specific kinase assay and the CDK inhibitory profile of the best ones (IC50 > 100nM) was determined. The most selective compounds had high selectivity over CDK1, 2, 3, 5, 6, 7 and showed at least one order of magnitude higher inhibitory activity over CDK4 inhibition. The most selective molecules were examined in cytotoxicity assays and their ability to inhibit HIV-1 replication was determined in cellular assays. Synonyms: CDK9-IN-1; CDK9 IN 1. Grades: >98%. CAS No. 1415559-43-1. Molecular formula: C26H21N5O4S. Mole weight: 499.54.
Crozbaciclib
Crozbaciclib (CDK4/6/1 Inhibitor) is a CDK4/6 inhibitor with IC 50 s of 3 and 1 nM, respectively. Uses: Scientific research. Group: Signaling pathways. Alternative Names: CDK4/6/1 Inhibitor. CAS No. 2099128-41-1. Pack Sizes: 5 mg; 10 mg. Product ID: HY-112280.
Crozbaciclib fumarate
Crozbaciclib fumarate is a CDK4/6 inhibitor with IC 50 s of 3 and 1 nM, respectively. Uses: Scientific research. Group: Signaling pathways. CAS No. 2567494-39-5. Pack Sizes: 5 mg; 10 mg; 25 mg. Product ID: HY-112280A.
CVT-313
A cell-permeable purine analog that acts as a potent, selective, reversible, and ATP-competitive inhibitor of Cdk2 (IC50 = 0.5 μM for Cdk2/A and Cdk2/E; 4.2 μM for Cdk1/B; 215 μM for Cdk4/D1). Inhibits other kinases only at much higher concentrations (IC50 > 1.25 mM for MAPK, PKA, and PKC). Shown to induce tumor cells growth arrest (IC50 = ~1.25-20 μM) in vitro and prevent neointima formation in vivo. Synonyms: CVT 313; NG 26; CVT313; NG26; NG-26; NG26. Grades: 95%. CAS No. 199986-75-9. Molecular formula: C20H28N6O3. Mole weight: 400.47.
Dalpiciclib
Dalpiciclib (SHR-6390) is an orally active and highly selective inhibitor of CDK4 and 6 with IC 50 values of 12.4 nM and 9.9 nM, respectively [1] [2]. Dalpiciclib shows antitumor activity against breast cancer and esophageal squamous cell carcinoma [1] [2] [3] [4]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: SHR-6390. CAS No. 1637781-04-4. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg. Product ID: HY-114338.
Dalpiciclib hydrochloride
Dalpiciclib (SHR-6390) hydrochloride is an orally active and highly selective inhibitor of CDK4 and 6 with IC 50 values of 12.4?nM and 9.9?nM, respectively [1] [2]. Dalpiciclib hydrochloride shows antitumor activity against breast cancer and esophageal squamous cell carcinoma [1] [2] [3] [4]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: SHR-6390 hydrochloride. CAS No. 2891598-76-6. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-114338A.
Ebvaciclib
PF-06873600 is a selective and orally bioavailable inhibitor of cyclin-dependent kinase (CDK), with Ki values of 0.09 nM, 0.13 nM and 0.16 nM for CDK2, CDK4 and CDK6, respectively. PF-06873600 has potential antineoplastic activity[1][2]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: PF-06873600. CAS No. 2185857-97-8. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-114177.
Fascaplysin, Synthetic - CAS 114719-57-2
A cell-permeable red pigment, originally isolated from marine sponge, that acts as a potent, ATP-competitive inhibitor of Cdk4/D1 (IC?? = 0.35 μM). Group: Fluorescence/luminescence spectroscopy.
Flavopiridol
Flavopiridol (Alvocidib) is a broad spectrum and competitive inhibitor of CDKs , inhibiting CDK1, CDK2, CDK4 with IC 50 s of 30, 170, 100 nM, respectively. Uses: Scientific research. Group: Signaling pathways. Alternative Names: HMR-1275; Alvocidib; L86-8275. CAS No. 146426-40-6. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg; 100 mg. Product ID: HY-10005.
Flavopiridol Hydrochloride
Flavopiridol Hydrochloride (Alvocidib Hydrochloride) is a broad inhibitor of CDK , competing with ATP to inhibit CDKs including CDK1, CDK2, CDK4 with IC 50 s of 30, 170, 100 nM, respectively. Uses: Scientific research. Group: Signaling pathways. Alternative Names: Alvocidib Hydrochloride; L86-8275 Hydrochloride; HMR-1275 Hydrochloride. CAS No. 131740-09-5. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg; 100 mg. Product ID: HY-10006.
GGTI-2418
GGTI-2418 is a synthetic peptidomimetic inhibitor of geranylgeranyltransferase I (GGTase I) that appears to induce apoptosis by downregulating several pivotal oncogenic and tumor survival pathways. GGTase I catalyzes the lipid posttranslational modification which is required for the function of Rho GTPases (frequently found aberrantly activated in human cancer). GGTase I inhibitors block Rho function in cancer cells and induce a G1 phase cell cycle arrest by a mechanism involving induction of the CDK inhibitors p21waf and p27kip, CDK2 and CDK4 inhibition and hypophoshorylation of the tumor suppressor Rb. GGTase I inhibitors also induce apoptosis by a mechanism involving downregulation of the expression of survivin and suppression of the activation of PI3K/Akt. Synonyms: GGTI 2418; GGTI-2418; GGTI 2418. CAS No. 501010-06-6. Molecular formula: C23H31N5O4. Mole weight: 441.532.
GSK-3 Inhibitor IX ((2Z,3E)-6-Bromoindirubin-3-oxime)
A cell-permeable bis-indolo (indirubin) compound that acts as a highly potent, selective, reversible, and ATP-competitive inhibitor of GSK-3a/b (IC50=5nM). Its specificity has been tested against various Cdk's (IC50=83, 300, 320, and 10,000nM for Cdk5/p25, Cdk2/A, Cdk1/B, and Cdk4/D1, respectively) as well as many other commonly studied kinases (IC50≥10uM), including MAP kinases, PKA, PKC isoforms, PKG, CK, and IRTK. Inhibition of GSK by BIO has been shown to result in the activation of Wnt-signaling pathway and sustained pluripotency in human and murine ESCs (embryonic stem cells). Reported to maintain self-renewal in human and mouse embryonic stem cells. Also induces the differentiation of neonatal cardiomyocytes. Group: Biochemicals. Grades: Highly Purified. CAS No. 667463-62-9. Pack Sizes: 1mg, 10mg. US Biological Life Sciences.
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HZ1
Anticancer agent 241 (HZ1) is an orally active first-in-class cyclin-dependent kinase like 3 (CDKL3) -specific inhibitor. Anticancer agent 241 shows a strong tumor-suppressing effect, and has the potential to overcome the resistance of CDK4/6 inhibitor [1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 3030492-40-8. Pack Sizes: 5 mg; 10 mg; 25 mg; 50 mg. Product ID: HY-161847.
Indirubin
Indirubin is an inhibitor of GSK-3β and cyclin-dependent kinases (CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E, CDK4/cyclin D1, CDK5/p35). Also, Indirubin is a specific Aryl Hydrocarbon receptor (AHR) ligand. Uses: Antibiotics, antineoplastic. Synonyms: Indirubin; C.I. 73200, Couroupitine B, Indigo red, Indigopurpurin, NSC 105327; NSC-105327; NSC105327; Indigopurpurin; Couroupitine B; [2,3'-Biindolinylidene]-2',3-dione; 3-(1,3-Dihydro-3-oxo-2H-indol-2-ylidene)-1,3-dihydro-2H-indol-2-one. Grades: >98%. CAS No. 479-41-4. Molecular formula: C16H10N2O2. Mole weight: 262.268.
LEE011 hydrochloride
CDK4/6 inhibitor LEE011 specifically inhibits CDK4 and 6, thereby inhibiting retinoblastoma (Rb) protein phosphorylation. Inhibition of Rb phosphorylation prevents CDK-mediated G1-S phase transition, thereby arresting the cell cycle in the G1 phase, suppressing DNA synthesis and inhibiting cancer cell growth. Overexpression of CDK4/6, as seen in certain types of cancer, causes cell cycle deregulation.Treatment with LEE011 significantly reduced proliferation in 12 of 17 human neuroblastoma-derived cell lines by inducing cytostasis at nanomolar concentrations (mean IC50=307 ± 68 nmol/L in sensitive lines). LEE011 caused cell-cycle arrest and cellular senescence that was attributed to dose-dependent decreases in phosphorylated RB and FOXM1, respectively. Responsiveness of neuroblastoma xenografts to LEE011 translated to the in vivo setting in that there was a direct correlation of in vitro IC50 values with degree of subcutaneous xenograft growth delay. Synonyms: 7-cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxamide hydrochloride; Ribociclib hydrochloride; LEE011; LEE-011 LEE 011. Grades: >98%. CAS No. 1211443-80-9. Molecular formula: C23H31ClN8O. Mole weight: 471.0.
LEE011 succinate
LEE011 is an orally bioavailable and highly specific CDK4/6 (cyclin-dependent kinase 4/6) inhibitor. LEE011 in combination with LGX818 (a V600E BRAF specific inhibitor) or BYL719 (a PIK3CA specific inhibitor) leads to robust anti-tumor activity in melanoma and breast cancer tumor models. Synonyms: Ribociclib succinate; LEE 011 succinate; LEE-011 succinate. Grades: >98%. CAS No. 1374639-75-4. Molecular formula: C27H36N8O5. Mole weight: 552.63.
Lerociclib
Lerociclib (G1T38) is a potent and selective inhibitor of CDK4/6 , with IC 50 s of 1 nM, 2 nM for CDK4/CyclinD1 and CDK6/CyclinD3, respectively. Uses: Scientific research. Group: Signaling pathways. Alternative Names: G1T38. CAS No. 1628256-23-4. Pack Sizes: 5 mg; 10 mg; 25 mg; 50 mg. Product ID: HY-112272.
Lerociclib
Lerociclib is a novel, selective, and orally bioavailable CDK4/6 inhibitor with biochemical IC50 values of 1 nM, 2 nM and 28 μnM for CDK4, CDK6 and CDK9 respectively. Synonyms: G1T38. CAS No. 1628256-23-4. Molecular formula: C26H34N8O. Mole weight: 474.60.
Lerociclib dihydrochloride
Lerociclib dihydrochloride (G1T38 dihydrochloride) is a potent and selective inhibitor of CDK4 / CDK6 , with IC 50 s of 1 nM and 2 nM for CDK4 / CyclinD1 and CDK6 / CyclinD3 , respectively. Uses: Scientific research. Group: Signaling pathways. Alternative Names: G1T38 dihydrochloride. CAS No. 2097938-59-3. Pack Sizes: 5 mg; 10 mg; 50 mg; 100 mg. Product ID: HY-112272A.
Methyl-13C, d3 Toluenesulfonate
Methyl-13C, d3 Toluenesulfonate is the labelled version of Methyl Toluenesulfonate which was used to prepare rhodacyanine dyes as antimalarials. It was also used to synthesize of fascaplysin derivatives with CDK4 inhibitory activities. Group: Biochemicals. Grades: Highly Purified. CAS No. 1781628-74-7. Pack Sizes: 25mg, 50mg. Molecular Formula: C713CH7D3O3S, Molecular Weight: 190.24. US Biological Life Sciences.
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