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Abelson murine leukemia viral oncogene homolog 1 also known as ABL1 is a protein that, in humans, is encoded by the ABL1 gene (previous symbol ABL) located on chromosome 9. c-Abl is sometimes used to refer to the version of the gene found within the mammalian genome, while v-Abl refers to the viral gene. Human abelson murine leukemia viral oncogene homolog 1 (abl-1) (genbank accession no. nm_007313), amino acids 248-531 with t334i mutation and n-terminal his-tag, mw = 33 kda, expressed in a baculovirus-infected sf9 cell expression system. Group: Enzymes. Synonyms: ABL1; JTK7; c-ABL; p150; AblKinase; ABL; bcr/abl; c-ABL1; v-abl. AblKinase. Mole weight: mol wt 33 kDa. Stability: -70°C. Form: aqueous solution. Source: Baculovirus infected Sf9 cells. Species: Human. ABL1; JTK7; c-ABL; p150; AblKinase; ABL; bcr/abl; c-ABL1; v-abl. Cat No: NATE-0013.
BMP Inhibitor III, LDN-212854 (Abl Inhibitor V, LDN212854, Bone Morphogenetic Protein Inhibitor III, PDGFR Tyrosine Kinase Inhibitor XXIV, RIP2 Inhibitor I, RIPK2 Inhibitor I, 5-(6-(4-(Piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyrimidin-3-yl)quinoline)
A cell-permeable pyrazolopyrimidinyl quinoline that is superior to Dorsomorphin and DMH1 as an ATP-site-targeting, ALK1/2 inhibitor (IC50 = 2.40 and 1.30nM, respectively; [ATP] = 6uM) with respect to both potency and selectivity over ALK3/4/5 (IC50 = 0.858, 2.133, and 9.276uM, respectively). Also a potent RIPK2 inhibitor (IC50 = 6nM) with reduced potency against ABL1/c-abl, PDGFR-beta, ALK3, and PDGFR-alpha (IC50 = 40, 68, 85.8, and 650nM, respectively) and little inhibitory activity toward a panel of more than 190 kinases. Effectively inhibits ALK2- and ALK3-mediated C2C12 osteogenic differentiation (IC50 = 10 and 40.5nM, respectively) in vitro and prevents constitutively active ALK2 Q207D mutant-induced heterotopic ossification in mice (6mg/kg/12h via i.p.) in vivo. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 5mg. Molecular Formula: C??H??N?. US Biological Life Sciences.
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1-Naphthyl PP1
1-Naphthyl PP1 (1-NA-PP 1) is a selective inhibitor of src family kinases and Protein Kinase D. 1-Naphthyl PP1 inhibits v-Src and c-Fyn, c-Abl, CDK2 and CAMK II with IC 50 s of 1.0, 0.6, 0.6, 18 and 22 μM, respectively [1] [2] [3]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: 1-NA-PP 1. CAS No. 221243-82-9. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-13941.
1-Naphthyl PP1
Selective inhibitor of src family kinases v-Src and c-Fyn as well as the tyrosine kinase c-Abl. (IC50 values are 1.0, 0.6, 0.6, 18 and 22 uM for v-Src, c-Fyn, c-Abl, CDK2 and CAMK II respectively). Preferentially inhibits mutant over wild-type kinases (IC50 values are 1.5 vs 1000 nM for I338G v-src and v-src respectively). Group: Biochemicals. Grades: Highly Purified. CAS No. 221243-82-9. Pack Sizes: 10mg, 50mg. Molecular Formula: C19H19N5. US Biological Life Sciences.
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1-Naphthyl PP1 hydrochloride
1-Naphthyl PP1 hydrochloride (1-NA-PP 1 hydrochloride) is a selective inhibitor of src family kinases. 1-Naphthyl PP1 hydrochloride inhibits v-Src and c-Fyn, c-Abl, CDK2 and CAMK II with IC 50 s of 1.0, 0.6, 0.6, 18 and 22 μM, respectively [1]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: 1-NA-PP 1 hydrochloride. CAS No. 956025-47-1. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-13941B.
1-Naphthyl PP1 hydrochloride
1-Naphthyl PP1 hydrochloride is a selective inhibitor of src family kinases, including v-Src and c-Fyn, tyrosine kinase c-Abl and CAMK II with IC50 values of 1.0, 0.6, 0.6, 18 and 22 μM for v-Src, c-Fyn, c-Abl, CDK2 and CAMK II respectively. It was considerably more potent and showed distinct substituent effects at the pyrazolopyrimidine core. It was cell-active, and potently blocked prostate cancer cell proliferation by inducing G2/M arrest. Uses: 1-naphthyl pp1 hydrochloride could potently block prostate cancer cell proliferation by inducing g2/m arrest. Synonyms: 1-Tert-butyl-3-(naphthalen-1-yl)-1H-pyrazolo[3,4-d]pyriMidin-4-aMine hydrochloride;1-NA-PP 1 hydrochloride. Grades: >98 %. CAS No. 956025-47-1. Molecular formula: C19H20ClN5. Mole weight: 353.85.
2-Amino-5-bromobenzothiazole
2-Amino-5-bromobenzothiazole is a chemical reagent used in the synthesis of pharmacologically active agents such as Ablkinase inhibitors for treatment of abnormal cell growth diseases or cytotoxic/anticancer agents. Group: Biochemicals. Grades: Highly Purified. CAS No. 20358-03-6. Pack Sizes: 1g, 5g. Molecular Formula: C7H5BrN2S, Molecular Weight: 229.1. US Biological Life Sciences.
This product is a potent inhibitor of Ablkinases and was developed for the treatment of chronic myeloid leukemia (CML). It works by blocking the activity of the Bcr-Abl fusion protein, which drives the growth of CML cells. Clinical trials have shown promising results, with high rates of complete remission and durable responses in patients with CML who were resistant or intolerant to previous treatments. Synonyms: PMO-BzC. Grades: 97%. CAS No. 956139-21-2. Molecular formula: C37H37ClN5O5P. Mole weight: 698.15.
Abl Cytosolic Substrate
Abl Cytosolic Substrate is a substrate for Abelson tyrosine kinase (Abl). Synonyms: L-Lysine, L-α-glutamyl-L-alanyl-L-isoleucyl-L-tyrosyl-L-alanyl-L-alanyl-L-prolyl-L-phenylalanyl-L-alanyl-L-lysyl-L-lysyl-; L-Lysine, N2-[N2-[N2-[N-[N-[1-[N-[N-[N-[N-(N-L-α-glutamyl-L-alanyl)-L-isoleucyl]-L-tyrosyl]-L-alanyl]-L-alanyl]-L-prolyl]-L-phenylalanyl]-L-alanyl]-L-lysyl]-L-lysyl]-; L-α-Glutamyl-L-alanyl-L-isoleucyl-L-tyrosyl-L-alanyl-L-alanyl-L-prolyl-L-phenylalanyl-L-alanyl-L-lysyl-L-lysyl-L-lysine; Glu-Ala-Ile-Tyr-Ala-Ala-Pro-Phe-Ala-Lys-Lys-Lys. Grades: ≥95%. CAS No. 168202-46-8. Molecular formula: C64H101N15O16. Mole weight: 1336.58.
Abl Cytosolic Substrate acetate
Abl Cytosolic Substrate acetate is a substrate for Abelson tyrosine kinase (Abl). Synonyms: Glu-Ala-Ile-Tyr-Ala-Ala-Pro-Phe-Ala-Lys-Lys-Lys acetate salt; L-α-Glutamyl-L-alanyl-L-isoleucyl-L-tyrosyl-L-alanyl-L-alanyl-L-prolyl-L-phenylalanyl-L-alanyl-L-lysyl-L-lysyl-L-Lysine acetate salt. Grades: ≥95%. CAS No. 2918768-10-0. Molecular formula: C64H101N15O16.C2H4O2. Mole weight: 1396.63.
A cell-permeable furopyrimidine that acts as a potent, ATP-binding site-targeting, Ack1-selective inhibitor (IC50 = 22nM) and effectively prevents receptor-mediated Ack1 activation (by >90% in MEF & LAPC4 cultures; 16h 800nM), while exhibiting much reduced potency against Lyn, Lck, Abl1 and BTK (IC50 ≥346.7nM) and no inhibitory activity toward 25 other kinases. Shown to completely inhibit EGF-induced, but not androgen DHT- (dihydrotestosterone) stimulated, AR transcription activity in serum- and androgen-deprived prostate cancer LAPC4 cutlures. Effectively inhibits androgen-independent LNCaP prostate cancer growth both in vitro (by 60%; 72h 8uM) and in castrated mice in vivo (4mg/kg/96h injections on day 7/11/15/19/23/27 post tumor transplant). Group: Biochemicals. Grades: Highly Purified. CAS No. 873305-35-2. Pack Sizes: 10mg. US Biological Life Sciences.
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AIM-100
AIM-100 is a potent and selective Ack1 tyrosine kinase with IC50 value of 24 nM. AIM-100, not only inhibited Ack1 activation but also able to suppress pTyr267-AR phosphorylation, binding of AR to PSA, NKX3.1, and TMPRSS2 promoters, and inhibit AR transcription activity. Ack1 tyrosine kinase activation correlates with pancreatic cancer progression. Ack1 inhibitors hold promise for therapeutic intervention to inhibit pancreatic tumor growth. Group: Others. Alternative Names: AIM-100; AIM 100; AIM100. CAS No. 873305-35-2. Molecular formula: C23H21N3O2. Mole weight: 371.44. Appearance: Solid powder. Purity: >98%. IUPACName: N-[[(2S)-oxolan-2-yl]methyl]-5,6-diphenylfuro[2,3-d]pyrimidin-4-amine. Canonical SMILES: C12=NC=NC (NC[C@H]3OCCC3)=C1C (C4=CC=CC=C4)=C (C5=CC=CC=C5)O2. Catalog: ACM873305352.
AP23464
AP23464 is a potent adenosine 5'-triphosphate (ATP)-based inhibitor of Src and Ablkinases. It displays antiproliferative activity against a human CML cell line and Bcr-Abl-transduced Ba/F3 cells with an IC50=14 nM. Synonyms: AP-23464; AP 23464; (4-((2-cyclopentyl-9-(3-hydroxyphenethyl)-9H-purin-6-yl)amino)phenyl)dimethylphosphine oxide. Grades: >98%. CAS No. 845895-51-4. Molecular formula: C30H38N5O2P. Mole weight: 475.53.
Asciminib
Asciminib, also known as ABL-001, is a potent and selective allosteric Bcr-Abl inhibitor. Asciminib inhibits Ba/F3 cell growth with an IC50 of 0.25 nM. Uses: Tyrosine kinase inhibitors. Synonyms: ABL-001; ABL 001; ABL001; N-[4-[chloro(difluoro)methoxy]phenyl]-6-[(3R)-3-hydroxypyrrolidin-1-yl]-5-(1H-pyrazol-5-yl)pyridine-3-carboxamide. CAS No. 1492952-76-7. Molecular formula: C20H18ClF2N5O3. Mole weight: 449.843.
At9283
AT9283 is a multi-targeted kinase inhibitor with potent activity against Aurora A/B, JAK2/3, Abl (T315I) and Flt3 (IC50s ranging from 1 to 30 nM). AT9283 inhibits growth and survival of multiple solid tumors in vitro and in vivo. Group: Inhibitors. Alternative Names: 1-Cyclopropyl-3-(3-(5-(morpholinomethyl)-1H-benzo[d]imidazol-2-yl)-1H-pyrazol-4-yl)urea;1-Cyclopropyl-3-(3-(5-(morpholinomethyl)-1H-benzo[d]imidazol-2-yl)-1H-pyrazol-4-yl)ureaAT9283;AT9283, >=98%;N-cyclopropyl-N-[3-[5-(4-morpholinylmethyl)-1H-benzimidazol-2-yl]-1H-pyrazol-4-yl]Urea;Urea, N-cyclopropyl-N-[3-[6-(4-morpholinylmethyl)-1H-benzimidazol-2-yl]-1H-pyrazol-4-yl]-. CAS No. 896466-04-9. Molecular formula: C19H23N7O2. Mole weight: 381.438. Purity: 0.997. Density: 1.45. Catalog: ACM896466049.
AT9283
AT-9283 is a broad spectrum kinase inhibitor that potently inhibits Aurora A, Aurora B, JAK2, JAK3, and c-ABL (IC50= 3, 3, 1.2, 1.1, and 4 nM, respectively). It also potently (IC50 = <1 μM) inhibits serine/threonine kinases as well as receptor and non-receptor tyrosine kinases. Synonyms: AT9283; AT 9283; AT-9283. Grades: >98%. CAS No. 896466-04-9. Molecular formula: C19H23N7O2. Mole weight: 381.43.
AT9283
AT9283 is a multi-targeted kinase inhibitor with potent activity against Aurora A/B , JAK2/3 , Abl (T315I) and Flt3 ( IC 50 s ranging from 1 to 30 nM). AT9283 inhibits growth and survival of multiple solid tumors in vitro and in vivo [1] [2]. Uses: Scientific research. Group: Signaling pathways. CAS No. 896466-04-9. Pack Sizes: 10 mM * 1 mL; 2 mg; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-50514.
AT-9283 L-lactate
AT9283 is a multikinase inhibitor, is also a small-molecule inhibitor of several kinases with potential antineoplastic activity. AT9283 binds to and inhibits Aurora kinases A and B, JAK2 (Janus kinase 2) and the kinase BCR-ABL, which may result in the inhibition of cellular division and proliferation and the induction of apoptosis in tumor cells that overexpress these kinases. Synonyms: AT 9283; AT9283. CAS No. 896466-76-5. Molecular formula: C19H23N7O2. Mole weight: 471.52.
AZD0424
AZD0424 is an orally bioavailable small molecule tyrosine kinase inhibitor. It targets both Abl and Src kinases with potential antineoplastic activity. It selectively inhibits both Src and Ablkinase activity and may result in the inhibition of tumor growth in susceptible tumor cells. Uses: Azd0424 has the inhibition of tumor growth in tumor cells. Synonyms: AZD 0424; AZD-0424; 1-(4-(2-((4-((6-chloro-[1,3]dioxolo[4,5-b]pyridin-7-yl)amino)-5-isopropoxyquinazolin-7-yl)oxy)ethyl)piperazin-1-yl)ethan-1-one; 7-(2-(4-Acetylpiperazin-1-yl)ethoxy)-4-(5-chloro-2,3-methylenedioxypyridin-4-ylamino)-5-isopropoxyquinazoline. Grades: 98%. CAS No. 692054-06-1. Molecular formula: C25H29ClN6O5. Mole weight: 528.99.
Bafetinib
A substituted benzamide derivative structurally related to STI-571 (Imatinib Mesylate). It was identified as highly potent Bcr-Ablkinase inhibitor. Group: Biochemicals. Alternative Names: N-[3- ([4, 5'-Bipyrimidin]-2-ylamino) -4-methylphenyl]-4-[[ (3S) -3- (dimethylamino) -1-pyrrolidinyl]methyl]-3- (trifluoromethyl) benzamide; INNO 406; NS 187. Grades: Highly Purified. CAS No. 859212-16-1. Pack Sizes: 1mg. US Biological Life Sciences.
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BCR-ABL1-IN-1
BCR-ABL1-IN-1 is a potent, orally active, and specific inhibitor of ABLkinase. BCR-ABL1-IN-1 has potential for elucidating the role of ABLkinases in the brain in non-clinical studies [1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 1488090-21-6. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-145887.
Bosutinib Isomer Methanoate
Bosutinib Isomer is the 3,5-dichloro-4-methoxy isomer of Bosutinib. It has been reported that this compound has been offered incorrectly as Bosutinib (B676095) C&E News 90 (21) 2012 34-35 and Levinson NM, Boxer SG (2012) Structural and Spectroscopic Analysis of the Kinase Inhibitor Bosutinib and an Isomer of Bosutinib Binding to the Abl Tyrosine Kinase Domain. PLoS ONE 7(4): e29828. doi:10. 1371/journal. pone. 0029828. Group: Biochemicals. Alternative Names: 4-[(3,5-Dichloro-4-methoxyphenyl)amino]-6-methoxy-7-[3-(4-methyl-1-piperazinyl)propoxy]-3-quinolinecarbonitrile Methanoate. Grades: Highly Purified. Pack Sizes: 10mg. US Biological Life Sciences.
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Casein Kinase II from Human, Recombinant
The Casein kinase 2 (EC 2.7.11.1) is a serine/threonine-selective protein kinase that is a tetramer of two alpha subunits and two beta subunits. The alpha subunits have the catalytic kinase domain. Casein kinase 2 has been implicated in cell cycle control, DNA repair, regulation of the circadian rhythm and other cellular processes. Casein kinase ii (ck2) is a constitutively active serine/threonine protein kinase composed of two 44 kda catalytic α-subunits and two 26 kda regulatory β-subunits in an α2β2 configuration to form stable heterotetramers. ck2 holoenzyme undergoes autophosphorylation at two serine residues (s2/s3) of its β-subunit. recen... ck2 is able to phosphorylate, under special circumstances, tyrosyl residues in proteins. ck2 is implicated in a variety of cellular functions. Group: Enzymes. Synonyms: EC 2.7.11.1; Casein Kinase II; CK2; CK II; Casein Kinase 2. CAS No. 9026-43-1. CK. Mole weight: a-subunit (45 kDa), b-subunit (25 kDa). The apparent molecular weight of the a-subunit estimated by SDS-PAGE is about 42 kDa. Activity: 859,000 units/mg. Storage: at -80°C. Avoid repeated freeze/thaw cycles. Form: 350 mM NaCl, 20 mM Tris-HCl (pH 7.5 25°C), 1 mM Na2EDTA, 2 mM DTT and 0.1% Triton X-100. Source: E. coli. Species: Human. EC 2.7.11.1; Casein Kinase II; CK2; CK II; Casein Kinase 2. Cat No: NATE-1271.
CGP 76030
CGP76030 is a ual-specific Src and Ablkinase inhibitor, inhibit growth and survival of cells expressing imatinib mesylate-resistant Bcr-Ablkinases. Uses: Ual-specific src and ablkinase inhibitor. Synonyms: CGP-76030; CGP76030; CGP76030; CGP-076030. 7-(4-(2-((2-methoxyethyl)amino)ethoxy)phenyl)-5-(3-methoxyphenyl)-7H-Pyrrolo(2,3-d)pyrimidin-4-amine. Grades: ≥98%. CAS No. 497152-38-2. Molecular formula: C24H27N5O3. Mole weight: 433.5.
CGP77675
CGP77675 is an orally active and potent inhibitor of Src family kinases. CGP77675 inhibits phosphorylation of peptide substrates and autophosphorylation of purified Src ( IC 50 s of 5-20 and 40 nM, respectively), and also inhibits Src, EGFR, KDR, v-Abl, and Lck with IC 50 s of 5-20, 40, 20, 150, 1000, 310, and 290 nM, respectively. Anticancer activity [1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 234772-64-6. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-W062835.
CHMFL-ABL-053
CHMFL-ABL-053 is a potent and orally available inhibitor of BCR-ABL (IC50 = 70 nM) without inhibitory activity against c-KIT kinase that is a common target of BCR-ABL inhibitors currently used. A pharmacokinetic study revealed that it had 4.3h of half-life and 24% bioavailability in rats. It is developed for the treatment of chronic myeloid leukemia (CML). Uses: The treatment of chronic myeloid leukemia (cml). Synonyms: CHMFL-ABL-053; CHMFL-ABL053; CHMFL-ABL 053. 2 - ((3-Amino-4-methylphenyl)amino) - N - (2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide. CAS No. 1808287-83-3. Molecular formula: C28H26F3N7O2. Mole weight: 549.56.
CRT0066101 hydrochloride
CRT0066101 is an inhibitor of all three PKD isoforms (IC50s = 1, 2.5, and 2 nM for PKD1, PKD2, and PKD3, respectively). It exhibits selectivity for PKD against a panel of >90 protein kinases, including PKCα, PKBα, MEK, ERK, c-Raf, c-Src, and c-Abl. Synonyms: Phenol, 2-[4-[[(2R)-2-aminobutyl]amino]-2-pyrimidinyl]-4-(1-methyl-1H-pyrazol-4-yl)-, hydrochloride (1:3); (R)-2-(4-((2-Aminobutyl)amino)pyrimidin-2-yl)-4-(1-methyl-1H-pyrazol-4-yl)phenol trihydrochloride; 2-(4-{[(2R)-2-Aminobutyl]amino}pyrimidin-2-yl)-4-(1-methyl-1H-pyrazol-4-yl)phenol trihydrochloride. Grades: ≥95%. CAS No. 1781742-22-0. Molecular formula: C18H22N6O.3HCl. Mole weight: 447.79.
CZC-8004
CZC-8004 is an aminopyrimidine which is a pan-kinase inhibitor that binds a range of tyrosine kinases, including ABL, BTK, FAK, FER, JAK1, SRC, SYK, TEC, TNK1, TYK2, and YES. Synonyms: Dianilinopyrimidine-01; CZC-00008004. Grades: ≥98%. CAS No. 916603-07-1. Molecular formula: C17H16FN5. Mole weight: 309.3.
Dasatinib-d8
Dasatinib-d 8 is a deuterium labeled Dasatinib. Dasatinib is a dual Bcr-Abl and Src family tyrosine kinase inhibitor. Uses: Scientific research. Group: Isotope-labeled compounds. Alternative Names: BMS-354825-d8. CAS No. 1132093-70-9. Pack Sizes: 500 μg; 1 mg. Product ID: HY-10181S.
Dasatinib Monohydrate
Dasatinib Monohydrate is a novel, potent and multi-targeted inhibitor that targets Abl, PDGFR, ephrin receptors, Src, c-Kit, and other Src-family kinases (LCK, HCK, FYN, and others). Uses: Antineoplastic agents. Synonyms: BMS-354825 Monohydrate; BMS 354825 Monohydrate; BMS354825 Monohydrate; N-(2-chloro-6-methylphenyl)-2-((6-(4-(2-hydroxyethyl)piperazin-1-yl)-2-methylpyrimidin-4-yl)amino)thiazole-5-carboxamide hydrate. Grades: >98%. CAS No. 863127-77-9. Molecular formula: C22H28ClN7O3S. Mole weight: 506.02.
DPH
DPH is a potent cell permeable c-Abl activator. It binds and alters the conformation of the myristoyl binding site of c-Abl tyrosine kinase. DPH exhibits potent enzymatic and cellular activity that stimulates the activation of c-Abl and may be used in c-Abl tyrosine kinase-mediated cell signaling studies. Synonyms: 5-(3-(4-fluorophenyl)-1-phenyl-1H-pyrazol-4-yl)imidazolidine-2,4-dione; 5-[3-(4-fluorophenyl)-1-phenylpyrazol-4-yl]imidazolidine-2,4-dione; MLS000036279; SMR000041163; 5-[3-(4-fluorophenyl)-1-phenyl-1H-pyrazol-4-yl]imidazolidine-2,4-dione; Oprea1_189167; cid_660311; CHEMBL1311135; SCHEMBL13740728; BDBM66241; DTXSID30349772; HMS2301N21; DPH, >=98% (HPLC); AKOS002169217; AKOS016293917; CS-0251; NCGC00020328-05; HY-12070; F83225; A913925; 5-[3-(4-fluorophenyl)-1-phenyl-pyrazol-4-yl]hydantoin; 5-[3-(4-fluorophenyl)-1-phenyl-1h-pyrazol-4-yl]-2,4-imidazolidinedione; 5-[3-(4-fluorophenyl)-1-phenyl-4-pyrazolyl]imidazolidine-2,4-dione; 5-[3-(4-fluorophenyl)-1-phenyl-pyrazol-4-yl]imidazolidine-2,4-dione. Grades: >98%. CAS No. 484049-04-9. Molecular formula: C18H13FN4O2. Mole weight: 336.32.
eCF506
eCF506 is a potent and highl selective inhibitor towards Src tyrosine kinase with a 1000-fold selectivity over ABL. eCF506 inhibits SRC at subnanomolar concentration (IC50 < 0.5 nM). It is said that eCF506 is the first drug candidate of a second generation of Src inhibitors that will not only help to understand the complexity of some cancers but also the development of safer combination therapies. Synonyms: eCF506; eCF-506; eCF 506.; tert-butyl N-[4-[4-amino-1-[2-[4-(dimethylamino)piperidin-1-yl]ethyl]pyrazolo[3,4-d]pyrimidin-3-yl]-2-methoxyphenyl]carbamate; eCF506; Derivative 11a; GTPL9186; derivative 11a [PMID: 27115835]; tert-butyl N-[4-(4-amino-1-{2-[4-(dimethylamino)piperidin-1-yl]ethyl}-1H-pyrazolo[3,4-d]pyrimidin-3-yl)-2-methoxyphenyl]carbamate. Grades:>98%. CAS No. 1914078-41-3. Molecular formula: C26H38N8O3. Mole weight: 510.643.
Flumatinib
Flumatinib is a multi-kinase inhibitor of c-Abl, PDGFRβ and c-Kit with IC50 values of 1.2 nM, 307.6 nM and 2662 nM respectively. It can predominantly inhibit the autophosphorylation of Bcr-Abl in K562 cell in vitro. It can inhibit the phosphorylation of c-Kit in Mo7e cell and the phosphorylation of PDGFR in Swiss3T3 cell in higher concentration. It has no or little effect on other tyrosine kinase including EGFR?KDR?c-Src andHER2. It can reduce the expression of C-MYC, HIF-1 α and VEGF in U266 cell line in a time- and dose-dependent manners. It effectively overcame the drug resistance of certain KIT mutants with activation loop mutations. It was developed by Jiangsu Hansoh Pharmaceutical Co., Ltd. and is currently in Phase III clinical trials in China for the treatment of chronic myelogenous leukemia (CML). Uses: Flumatinib is used for the treatment of chronic myelogenous leukemia (cml). Synonyms: 4-[(4-methylpiperazin-1-yl)methyl]-N-(6-methyl-5-{[4-(pyridin-3-yl)pyrimidin-2-yl]amino}pyridin-3-yl)-3-(trifluoromethyl)benzamide; HH-GV678; HHGV678; HH GV678; 4-[(4-Methyl-1-piperazinyl)methyl]-N-(6-methyl-5-{[4-(3-pyridinyl)-2-pyrimidinyl]amino}-3-pyridinyl)-3-(trifluoromethyl)benzamide. Grades: >98%. CAS No. 895519-90-1. Molecular formula: C29H29F3N8O. Mole weight: 562.59.
Flumatinib Mesylate
Flumatinib mesylate, a derivative of imatinib, is a multi-kinase inhibitor for c-Abl, PDGFRβ and c-Kit. It is currently in Phase I and II clinical trials in China for the treatment of chronic myelogenous leukemia (CML). It effectively overcomes drug resistance of certain KIT mutants. It can reduce the expression of C-MYC, HIF-1 α and VEGF in U266 cell line in a time- and dose-dependent manners. Synonyms: HH-GV-678 mesylate. Grades: >98%. CAS No. 895519-91-2. Molecular formula: C30H33F3N8O4S. Mole weight: 658.69.
FTI-277
FTI-277, a peptide mimetic of the COOH-terminal Cys-Val-Ile-Met of K-Ras4B that inhibited potently FTase in vitro (IC50 = 500 pM) and was highly selective for FTase over geranylgeranyltransferase I (GGTase I) (IC50 = 50 nM). FTI-277, the methyl ester derivative of FTI-276, was extremely potent (IC50 = 100 nM) at inhibiting H-Ras, but not the geranylgeranylated Rap1A processing in whole cells. Treatment of H-Ras oncogene-transformed NIH 3T3 cells with FTI-277 blocked recruitment to the plasma membrane and subsequent activation of the serine/threonine kinase c-Raf-1 in cells transformed by farnesylated Ras (H-RasF), but not geranylgeranylated, Ras (H-RasGG). FTI-277 induced accumulation of cytoplasmic non-farnesylated H-Ras that was able to bind Raf and form cytoplasmic Ras/Raf complexes in which Raf kinase was not activated. Furthermore, FTI-277 blocked constitutive activation of mitogen-activated protein kinase (MAPK) in H-RasF, but not H-RasGG, or Raf-transformed cells. FTI-277 also inhibited oncogenic K-Ras4B processing and constitutive activation of MAPK, but the concentrations required were 100-fold higher than those needed for H-Ras inhibition. The results demonstrate that FTI-277 blocks Ras oncogenic signaling by accumulating inactive Ras/Raf complexes in the cytoplasm, hence preventing constitutive activation of the MAPK cascade. Uses: Radiation-sensitizing agents. Synonyms: FTI-277; FTI 277; FTI277. CAS No. 170006-73-2. Molecular formula: C22H29N3O3S2. Mole weight: 447.612.
Ganetespib
Ganetespib, also known as STA-9090, is a synthetic small-molecule inhibitor of heat shock protein 90 (Hsp90) with potential antineoplastic activity. Hsp90 inhibitor STA-9090 binds to and inhibits Hsp90, resulting in the proteasomal degradation of oncogenic client proteins, the inhibition of cell proliferation and the elevation of heat shock protein 72 (Hsp72); it may inhibit the activity of multiple kinases, such as c-Kit, EGFR, and Bcr-Abl, which as client proteins depend on functional Hsp90 for maintenance. Hsp90, a 90 kDa molecular chaperone upregulated in a variety of tumor cells, plays a key role in the conformational maturation, stability and function of "client" proteins within the cell, many of which are involved in signal transduction, cell cycle regulation and apoptosis, including kinases, transcription factors and hormone receptors. Hsp72 exhibits anti-apoptotic functions; its up-regulation may be used as a surrogate marker for Hsp90 inhibition. Synonyms: STA-9090; STA 9090; STA9090. Grades: >98%. CAS No. 888216-25-9. Molecular formula: C20H20N4O3. Mole weight: 364.40.
GNF-2
GNF-2 is a Bcr-Abl inhibitor that binds to the myristoyl binding pocket, an allosteric site distant from the active site, stabilizing the inactive form of the kinase. Thus, it can selectively inhibit Bcr-Abl phosphorylation (IC50 = 267 nM) without affecting native c-Abl or a panel of 63 additional kinases. Synonyms: GNF2; GNF-2; GNF 2. Grades: 98.73%. CAS No. 778270-11-4. Molecular formula: C18H13F3N4O2. Mole weight: 374.32.
GNF-7
GNF-7 is a type-II T315I inhibitor. GNF-7 inhibits Ack1 and germinal center kinase (GCK). GNF-7 is among the first type-II inhibitors capable of inhibiting T315I to be described and will serve as a valuable lead to design the third generation Bcr-Ablkinase inhibitors. Uses: Protein kinase inhibitors. Synonyms: GNF7; GNF 7; N-(4-methyl-3-(1-methyl-7-((6-methylpyridin-3-yl)amino)-2-oxo-1,4-dihydropyrimido[4,5-d]pyrimidin-3(2H)-yl)phenyl)-3-(trifluoromethyl)benzamide. Grades: 98%. CAS No. 839706-07-9. Molecular formula: C28H24F3N7O2. Mole weight: 547.54.
Hck from Human, Recombinant
Hck is a member of the Src family of non-receptor associated protein tyrosine kinases (PTK). Hck has been shown to associate with and be activated by Bcr-Abl, which is a protein-tyrosine kinase that is expressed in chronic myelogenous leukemia. Group: Enzymes. Synonyms: Hck; HCK; tyrosine-protein kinase HCK; JTK9; p59Hck; p61Hck. Hck. Mole weight: mol wt 58 kDa. Storage: -70°C. Form: buffered aqueous glycerol solution; Solution in 50 mM Tris pH 7.5, containing 0.05 mM EDTA, 1mM DTT, 100 mM NaCl, 0.05% NP-40, and 50% glycerol. Source: Baculovirus infected insect cells. Species: Human. Hck; HCK; tyrosine-protein kinase HCK; JTK9; p59Hck; p61Hck. Cat No: NATE-0334.
Herbimycin A
Herbimycin A, an ansamycin antibiotic , acts as a Src family kinase inhibitor. Herbimycin A binds to the SH domain and inhibits the activity of p60 v-src and p210 BCR-ABL Herbimycin A inhibits Hsp90 and impairs recovery from heat shock. Herbimycin A exhibits antiangiogenic activity in endothelial cells in vitro. Uses: Scientific research. Group: Natural products. CAS No. 70563-58-5. Pack Sizes: 1 mg; 2.5 mg; 500 μg; 100 μg. Product ID: HY-108486.
Herbimycin A (Antibiotic TAN 420F, (15R)-17-Demethoxy-15-methoxy-11-O-methyl-geldanamycin)
Benzoquinone ansamycin antibiotic. Herbicidal compound. Potent, selective, irreversible and cell permeable protein tyrosine kinase inhibitor. Inhibitor of v-Src, Yes, Fps, Ros, Bcr-Abl and ErbB oncogene products. Antitumor compound. Antiangiogenic. Inhibits NF-kappaB activation and phosphorylation of phospholipase C-gamma1. Inhibitor of heat shock protein 90 (Hsp90). Binds Hsp90 and destabilizes client proteins leading to their ubiquitination and proteasomal degradation. Increases the sensitivity of certain cancer cells to chemotherapeutic agents. Neuroprotective. Antiparasitic, antischistosomal agent. Antiviral. Increase microtubules sensitivity to cold in plants. Group: Biochemicals. Grades: Highly Purified. CAS No. 70563-58-5. Pack Sizes: 100ug, 1mg. Molecular Formula: C30H42N2O9. US Biological Life Sciences.
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HS 38
HS 38 is an ATP-competitive inhibitor of DAPK (IC50 = 200 nM) and ZIPK (Kd = 280 nM). It also inhibits PIM3 kinase (IC50 = 200 nM) with no significant effect on Src or Ablkinases. HS 38 regulates programmed cell death and phosphorylation of non-muscle and smooth muscle myosin. Synonyms: HS 38; HS38; HS-38; 2-[[1-(3-Chlorophenyl)-4,5-dihydro-4-oxo-1H-pyrazolo[3,4-d]pyrimidin-6-yl]thio]propanamide. Grades: ≥98% by HPLC. CAS No. 1030203-81-6. Molecular formula: C14H12CIN5O2S. Mole weight: 349.8.
Imatinib
Imatinib (STI571) is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL , v-Abl , PDGFR and c-kit kinase activity. Imatinib (STI571) works by binding close to the ATP binding site, locking it in a closed or self-inhibited conformation, therefore inhibiting the enzyme activity of the protein semicompetitively [1] [2] [3] [4]. Imatinib also is an inhibitor of SARS-CoV and MERS-CoV [5]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: STI571; CGP-57148B. CAS No. 152459-95-5. Pack Sizes: 10 mM * 1 mL; 200 mg; 500 mg; 1 g; 5 g. Product ID: HY-15463.
A deuterated tyrosine kinase inhibitor. Highly specific for BCR-ABL, the enzyme associated with chronic myelogenous leukemia (CML) and certain forms of acute lymphoblastic leukemia (ALL). Group: Biochemicals. Alternative Names: Imatinib-d8 Methanesulfonate, STI-571-d8, CGP-57148B-d8, Glivec-d8. Grades: Highly Purified. Pack Sizes: 500ug. US Biological Life Sciences.
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Imatinib free base
Imatinib is a tyrosine kinase inhibitor with antineoplastic activity. Imatinib binds to an intracellular pocket located within tyrosine kinases (TK), thereby inhibiting ATP binding and preventing phosphorylation and the subsequent activation of growth receptors and their downstream signal transduction pathways. This agent inhibits TK encoded by the bcr-abl oncogene as well as receptor TKs encoded by the c-kit and platelet-derived growth factor receptor (PDGFR) oncogenes. Imatinib was approved for medical use in the United States in 2001. Group: Inhibitors. Alternative Names: CGP 57148; CGP57148; CGP-57148; CGP57148B; CGP-57148B; CGP 57148B; STI571; STI-571; STI 571. CAS No. 152459-95-5. Molecular formula: C29H31N7O. Mole weight: 493.62. Appearance: White to off-white to brownish or yellowish tinged crystalline powder. Purity: >98%. IUPACName: N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)-4-((4-methylpiperazin-1-yl)methyl)benzamide. Canonical SMILES: O=C (NC1=CC=C (C)C (NC2=NC=CC (C3=CC=CN=C3)=N2)=C1)C4=CC=C (CN5CCN (C)CC5)C=C4. Catalog: ACM152459955.
Imatinib, Free base
An inhibitor of the bcr-abl tyrosine kinase. It acts by binding to the ATP binding site of bcr-abl. Imatinib also stimulates the entry of the bcr-abl tyrosine kinase into the nucleus, where it cannot perform its anti-apoptopic functions. It inhibits EOL-1 cell viability (IC50=0.5nm), phosphorylation of a fusion protein (IC50=30nm), and viability of BaF3 cells expressing Rhe-PDGFRa in the absence of IL-3 (IC50 =0.17nm). Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 100ug, 1g. US Biological Life Sciences.
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Imatinib Mesylate
Imatinib Mesylate (STI571 Mesylate) is a tyrosine kinases inhibitor that inhibits c-Kit , Bcr-Abl , and PDGFR ( IC 50 =100 nM) tyrosine kinases. Uses: Scientific research. Group: Signaling pathways. Alternative Names: STI571 Mesylate; CGP-57148B Mesylate. CAS No. 220127-57-1. Pack Sizes: 10 mM * 1 mL; 200 mg; 500 mg; 1 g; 5 g. Product ID: HY-50946.
Imatinib, Methanesulfonate Salt (STI-571, CGP-57148B)
A tyrosine kinase inhibitor. Highly specific for BCR-ABL, the enzyme associated with chronic myelogenous leukemia (CML) and certain forms of acute lymphoblastic leukemia (ALL). Imatinib inhibits bcr-abl tyrosine kinase activity, upon which some types of tumor cells depend for growth. Imatinib acts by binding to the ATP binding site of bcr-abl and competitively inhibiting its tyrosine kinase activity. Imatinib is selective for bcr-abl, but it also targets several other kinases (c-kit and PDGF-R). (1). Group: Biochemicals. Alternative Names: 4- [ (4-Methyl-1-piperazinyl) methyl] -N- [4-methyl-3- [ [4- (3-pyridinyl) -2-pyrimidinyl] amino] phenyl] benzamide Methanesulfonate; CGP 57148B; Imatinib Mesilate; Imatinib Methanesulfonate; Imatinib Mesylate; STI 571; Bcr-abl Inhibitor IV; Abl Inhibitor V, PDGFR Tyrosine Kinase Inhibitor XXIV, c-Kit Inhibitor IV. Grades: Highly Purified. CAS No. 220127-57-1. Pack Sizes: 25mg, 1g, 5g, 10g. US Biological Life Sciences.
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KB SRC 4
KB SRC 4 is a cell-permeable, potent and highly selective c-Src inhibitor with Kd value of 86 nM and Ki value of 44 nM, which is a key signaling kinase in cancer. It displays no inhibition on c-Abl up to 125 μM and is selective between Src family members. It inhibits cell growth in 4T1 mammary carcinoma tumor cells. It has antitumor activity and may be a promising therapeutic potential in the treatment of cancers. Synonyms: 1-[3-[1-([1,1'-Biphenyl]-3-ylmethyl)-1H-1,2,3-triazol-5-yl]phenyl]-3-(4-chlorophenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine. Grades: ≥98% by HPLC. CAS No. 1380088-03-8. Molecular formula: C32H23ClN8. Mole weight: 555.03.
Kw-2449
KW-2449 is a multi-targeted kinase inhibitor of FLT3, ABL, ABLT315I and Aurora kinase with IC50s of 6.6, 14, 4 and 48 nM, respectively. Group: Inhibitors. CAS No. 1000669-72-6. Molecular formula: C20H20N4O. Mole weight: 332.4. Purity: >99%. Catalog: ACM1000669726.
λ Protein phosphatase
λ Protein phosphatase is a serine/threonine phosphatase encoded by bacteriophage Lambda. λ Protein phosphatase is activated with requirement for divalent cations, such as Mn 2+. λ Protein phosphatase is able to dephosphorylate casein, adenovirus E1A protein, and the α subunit of phosphorylase kinase [1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 401941-75-1. Pack Sizes: 10 KU. Product ID: HY-E70373.
MAPK/MAK/MRK overlapping kinase (11-20)
MAPK/MAK/MRK overlapping kinase (11-20) is a 10-aa peptide. MAPK/MAK/MRK overlapping kinase is able to phosphorylate several exogenous substrates and to undergo autophosphorylation.
MAPK/MAK/MRK overlapping kinase (32-40)
MAPK/MAK/MRK overlapping kinase (32-40) is a 9-aa peptide. MAPK/MAK/MRK overlapping kinase is able to phosphorylate several exogenous substrates and to undergo autophosphorylation.
MAPK/MAK/MRK overlapping kinase (352-360)
MAPK/MAK/MRK overlapping kinase (352-360) is a 9-aa peptide. MAPK/MAK/MRK overlapping kinase is able to phosphorylate several exogenous substrates and to undergo autophosphorylation.
A cell-permeable di hydropyridopyrimidine-carboxamide compound that acts as a potent and reversible inhibitor of Mirk/Dyrk1B and Dyrk1A kinases (IC50 = 68 and 22nM). Exhibits very high selectivity for Mirk/Dyrk1B compared to Abl, Flt3, and MARK1 (64, 56 and 73% inhibition at 10uM, respectively) and a panel of 46 other kinases. Shown to induce activation of caspase-3 and sensitize tumor cells to the action of gemcitabine and cisplatin, possibly by de-stabilizing p27. Preferentially increases cycling in Mirk-elevated quiescent pancreatic cancer cells (SU86.86, Panc1, AsPc1, and SW620 at ~1uM). Also, shown to increase level of superoxides in quiescent pancreatic tumor cells (Panc1, SU86.86, and AsPc1) by blocking SOD2 and SOD3 activities. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg. US Biological Life Sciences.
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N-Desmethyl Imatinib (CGP-74588)
A metabolite of Imatinib, a tyrosine kinase inhibitor which is highly specific for BCR-ABL, the enzyme associated with chronic myelogenous leukemia (CML) and certain forms of acute lymphoblastic leukemia (ALL). Group: Biochemicals. Alternative Names: N-Desmethyl Gleevec, CGP-74588. Grades: Highly Purified. CAS No. 404844-02-6. Pack Sizes: 500ug. US Biological Life Sciences.
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N-Desmethyl Imatinib-d8
A deuterated metabolite of N-Desmethyl Imatinib, a tyrosine kinase inhibitor which is highly specific for BCR-ABL, the enzyme associated with chronic myelogenous leukemia (CML) and certain forms of acute lymphoblastic leukemia (ALL). Group: Biochemicals. Alternative Names: N-Desmethyl Gleevec-d8. Grades: Highly Purified. Pack Sizes: 250ug. US Biological Life Sciences.
Worldwide
NG25
Type II inhibitor of TAK1 (MAP3K7) and MAP4K2 (GCK) with nanomolar potency for a wider range of kinases (IC50 values 13 nM, 22 nM, 56 nM, 75 nM, 82 nM, 102 nM, 113 nM, and 149 nM for LYN, MAP4K2, CSK, Abl, FER, p38α, SRC, and TAK1, repectively). At 0.1 μM NG25 shows strong inhibition of TAK1, Lck, MAP4K2, p38α, Abl, YES1, and OSR1. NG 25 potently inhibited the activation of IKKβ by TLR7 and TLR9 agonists and prevented the secretion of type 1 IFNs induced by these ligands in Gen2.2 cells. Synonyms: NG 25; NG-25. Grades: >98%. CAS No. 1315355-93-1. Molecular formula: C29H30F3N5O2. Mole weight: 537.58.
NG 25 trihydrochloride
NG 25 trihydrochloride is a type II inhibitor of TAK1 (MAP3K7) and MAP4K2 (GCK) with nanomolar potency for multiple kinases including TAK1, Lck, MAP4K2, p38α, Abl, YES1, and OSR1. NG 25 potently inhibits the activation of IKKβ by TLR7 and TLR9 agonists, and prevents the secretion of type 1 IFNs induced by these ligands in Gen2.2 cells. Synonyms: NG 25 trihydrochloride; NG25 trihydrochloride; NG-25 trihydrochloride. Grades: 98%. CAS No. 2108554-00-1. Molecular formula: C29H30F3N5O2.3HCl. Mole weight: 646.96.
Nilotinib
Nilotinib is an orally available Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity. Uses: Scientific research. Group: Signaling pathways. Alternative Names: AMN107. CAS No. 641571-10-0. Pack Sizes: 10 mM * 1 mL; 100 mg; 200 mg; 500 mg. Product ID: HY-10159.
Nilotinib hydrochloride
Nilotinib is an orally bioavailable Bcr-Abl tyrosine kinase inhibitor displaying antineoplastic activity. It is promisingly used for the treatment of chronic myelogenous leukemia (CML). Uses: Tyrosine kinase inhibitors. Synonyms: AMN-107 HCl; 4-methyl-N-(3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl)-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)benzamide hydrochloride. CAS No. 923288-95-3. Molecular formula: C28H22F3N7O·HCl. Mole weight: 565.98.
Nilotinib monohydrochloride monohydrate
Nilotinib monohydrochloride monohydrate is an orally bioavailable aminopyrimidine-derivative Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity. It binds to and stabilizes the inactive conformation of the kinase domain of the Abl protein of the Bcr-Abl fusion protein, resulting in the inhibition of the Bcr-Abl-mediated proliferation of Philadelphia chromosome-positive (Ph+) chronic myeloid leukemia (CML) cells. It also inhibits the receptor tyrosine kinases platelet-derived growth factor receptor (PDGF-R) and c-kit, a receptor tyrosine kinase mutated and constitutively activated in most gastrointestinal stromal tumors (GISTs). Uses: Tyrosine kinase inhibitors. Synonyms: AMN-107; AMN 107; AMN107; Tasigna. Grades: >98%. CAS No. 923288-90-8. Molecular formula: C28H25ClF3N7O2. Mole weight: 583.99.
non-specific protein-tyrosine kinase
Unlike EC 2.7.10.1, receptor protein-tyrosine kinase, this protein-tyrosine kinase does not have a transmembrane domain. In the human genome, 32 non-specific protein-tyrosine kinases have been identified and these can be divided into ten families. Group: Enzymes. Synonyms: ABL; ABL1; ABL2; ABLL; ACK1; ACK2; AGMX1; ARG; ATK; ATP:protein-tyrosine O-phosphotransferase (ambi. Enzyme Commission Number: EC 2.7.10.2. FAK. Storage: Store it at +4 ?C for short term. For long term storage, store it at -20 ?C?-80 ?C. Form: Liquid or lyophilized powder. EXWM-3127; non-specific protein-tyrosine kinase; EC 2.7.10.2; ABL; ABL1; ABL2; ABLL; ACK1; ACK2; AGMX1; ARG; ATK; ATP:protein-tyrosine O-phosphotransferase (ambiguous); BLK; Bmk; BMX; BRK; Bruton's tyrosine kinase; Bsk; BTK; BTKL; CAKb; Cdgip; CHK; CSK; CTK; CYL; cytoplasmic protein tyrosine kinase; EMT; ETK; Fadk; FAK; FAK2; FER; Fert1/2; FES; FGR; focal adhesion kinase; FPS; FRK; FYN; HCK; HCTK; HYL; IMD1; ITK; IYK; JAK1; JAK2; JAK3; Janus kinase 1; Janus kinase 2; Janus kinase 3; JTK1; JTK9; L-JAK; LCK; LSK; LYN; MATK; Ntk; p60c-src protein tyrosine kinase; PKB; protein-tyrosine kinase (ambiguous); PSCTK; PSCTK1; PSCTK2; PSCTK4; PSCTK5; PTK2; PTK2B; PTK6; PYK2; RAFTK; RAK; Rlk; Sik; SLK; SRC; SRC2; SRK; SRM; SRMS; STD; SYK; SYN; Tck; TEC; TNK1; Tsk; TXK; TYK2; TYK3; YES1; YK2; ZAP70. Cat No: EXWM-3127.
NVP-BHG712
NVP-BHG712 / BHG-712 inhibits EphB4 kinase activity in the low nanomolar range in cellular assays showed high selectivity for targeting the EphB4 kinase when profiled against other kinases in biochemical as well as in cell based assays. It also shows activity against c-Raf, c-Src and c-Abl with IC50 of 0.395 μM, 1.266 μM and 1.667 μM, respectively. Group: Fluorinated apis. Alternative Names: BHG-712. CAS No. 940310-85-0. Molecular formula: C26H20F3N7O. Mole weight: 503.48. Appearance: White to off-white solid powder. Purity: >98%. IUPACName: 4-methyl-3-[ (1-methyl-6-pyridin-3-ylpyrazolo[3, 4-d]pyrimidin-4-yl)amino]-N-[3- (trifluoromethyl)phenyl]benzamide. Catalog: OFC940310850.
NVP-BHG712
NVP-BHG712 is a EphB4 kinase inhibitor and BCR-ABL inhibitor. NVP-BHG712, which inhibits EphB4 kinase activity in the low nanomolar range in cellular assays showed high selectivity for targeting the EphB4 kinase when profiled against other kinases in biochemical as well as in cell based assays. Furthermore, NVP-BHG712 shows excellent pharmacokinetic properties and potently inhibits EphB4 autophosphorylation in tissues after oral administration. In vivo, NVP-BHG712 inhibits VEGF driven vessel formation, while it has only little effects on VEGF receptor (VEGFR) activity in vitro or in cellular assays. The data shown here suggest a close cross talk between the VEGFR and EphR signaling during vessel formation. In addition to its established function in vascular remodeling and endothelial arterio-venous differentiation, EphB4 forward signaling appears to be an important mediator of VEGF induced angiogenesis since inhibition of EphB4 forward signaling is sufficient to inhibit VEGF induced angiogenesis. Synonyms: NVP BHG712; NVP BHG-712; NVP BHG 712; BHG-712; BHG712; BHG 712. CAS No. 940310-85-0. Molecular formula: C26H20F3N7O. Mole weight: 503.489.
ON 146040
ON 146040 was highly potent in killing hematologic tumor cells with IC50 values in the 150 to 1,000 nM range. In biochemical testing, ON 146040 inhibited PI3K α/δ isoforms (IC50 ? 14 and 20 nM, respectively) without having a major effect on β/γ isoforms (IC50 ? 3 and 1 μM, respectively). ON 146040 was also found to inhibit Abl1 and several mutant versions of this kinase (IC50 < 150 nM), although the compound was not found to be active against the T315I mutant. Following treatment with ON 146040, STAT3 and STAT5 phosphorylation were down-regulated in leukemia and myeloma cells. Synonyms: ON-146040; ON146040. Grades:>98%. CAS No. 1404231-34-0. Molecular formula: C24H23N7O3S. Mole weight: 489.55.
Paeciloquinone A
It is produced by the strain of Paecilomyces carneus P-177. It can inhibit the epidermal growth factor receptor protein tyrosine kinase. Paeciloquinone A inhibits the V-abl protein tyrosine kinase with IC50 of 0.59 μmol/L. Synonyms: 9,10-Anthracenedione, 1,3,6,8-tetrahydroxy-2-(tetrahydro-2-oxo-3-furanyl)-. CAS No. 162797-33-3. Molecular formula: C18H12O8. Mole weight: 356.28.
Paeciloquinone C
It is produced by the strain of Paecilomyces carneus P-177. It can inhibit the epidermal growth factor receptor protein tyrosine kinase. Paeciloquinone C inhibits the V-abl protein tyrosine kinase with IC50 of 0.56 μmol/L. Synonyms: 1,3,6,8-tetrahydroxy-2-(hydroxymethyl)-anthraquinone; 2-Hydroxymethyl-1,3,6,8-tetrahydroxy-anthrachinone. CAS No. 92439-42-4. Molecular formula: C15H10O7. Mole weight: 302.23.
PD166326
PD166326 is a pyridopyrimidine-type inhibitor of receptor tyrosine kinases , with IC 50 s of 6 nM and 8 nM for Src and Abl , respectively. PD166326 exhibits antileukemic activity [1] [2]. Uses: Scientific research. Group: Signaling pathways. CAS No. 185039-91-2. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-118144.
PD-173952
A Bcr-Abl tyrosine kinase inhibitor used in treatment research for chronic myelegenous leukemia (CML). Group: Biochemicals. Alternative Names: 6- (2, 6-Dichlorophenyl) -8-methyl-2-[[4- (4-morpholinyl) phenyl]amino]pyrido[2, 3-d]pyrimidin-7 (8H) -one. Grades: Highly Purified. CAS No. 305820-75-1. Pack Sizes: 10mg. US Biological Life Sciences.
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