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Home > Inhibitors & Agonists > TGF-beta/Smad > TGF beta Receptor (TGFBR)

A77-01

  Cat. No.:  DC8020   Featured
Chemical Structure
607737-87-1
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More than 5000 active chemicals with high quality for research!
Field of application
A 77-01 is a potent inhibitor of TGF-β type I receptor superfamily activin-like kinase ALK5 with IC50 of 25 nM.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 607737-87-1
Chemical Name: 4-[3-(6-Methyl-2-pyridinyl)-1H-pyrazol-4-yl]-quinoline
Synonyms: 4-[3-(6-methyl-2-pyridinyl)-1h-pyrazol-4-yl]-quinoline;4-[5-(6-methylpyridin-2-yl)-1H-pyrazol-4-yl]quinoline;A 77-01;A-77-01;AC-13924;AG-G-20931;CHEBI:311956;CHEMBL129677;CTK5B2230;SureCN376179;4-(3-(6-Methylpyridin-2-yl)-1H-pyrazol-4-yl)quinoline;C18H14N4;4-(5-(6-methylpyridin-2-yl)-1H-pyrazol-4-yl)quinoline;4-[3-(6-methylpyridin-2-yl)-1H-pyrazol-4-yl]quinoline;4-[3-(6-Methyl-2-pyridinyl)-1H-pyrazol-4-yl]quinoline;4-[3-(6-Methyl-pyridin-2-yl)-1H-pyrazol-4-yl]-quinoline;BCP13726
SMILES: N1([H])C(C2=C([H])C([H])=C([H])C(C([H])([H])[H])=N2)=C(C([H])=N1)C1=C([H])C([H])=NC2=C([H])C([H])=C([H])C([H])=C12
Formula: C18H14N4
M.Wt: 286.3306
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: A 77-01 is a potent inhibitor of TGF-β type I receptor superfamily activin-like kinase ALK5 with IC50 of 25 nM. IC50 Value: 25 nM [1]Target: ALK5A-77-01 is a close analogue of A-83-01(Axon 1421) and has a very similar biological profile of A-83-01. A-83-01 is found to decompose to A-77-01 under certain circumstances and A-77-01 is likely an active component or metabolite of its prodrug A-83-01.
References: [1]. Tojo M, et al. The ALK-5 inhibitor A-83-01 inhibits Smad signaling and epithelial-to-mesenchymal transition by transforming growth factor-beta. Cancer Sci. 2005 Nov;96(11):791-800.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
DC7739 SD-208 SD-208 is a potent, orally active ATP-competitive transforming growth factor-β receptor 1 (TGF-βRI) inhibitor (IC50= 49 nM)
DC6312 SB525334 SB525334 is a potent and selective inhibitor of TGFβ receptor I (ALK5) with IC50 of 14.3 nM, is 4-fold less potent to ALK4 than ALK5 and inactive to ALK2, 3, and 6.
DC5189 SB-431542 SB431542 is a potent and selective inhibitor of ALK5 with IC50 of 94 nM, 100-fold more selective for ALK5 than p38 MAPK and other kinases.
DC7259 Repsox（ALK5 Inhibitor II） RepSox(E-616452; SJN 2511) is a potent and selective inhibitor of the TGFβR-1/ALK5 with IC50 of 23 nM and 4 nM for ATP binding to ALK5 and ALK5 autophosphorylation, respectively.
DC7587 ML347 ML347 is a selective BMP receptor inhibitor with IC50 of 32 nM for ALK2, >300-fold selectivity over ALK3. Also inhibits ALK1 activity with IC50 of 46 nM
DC10675 LY3200882 LY3200882 is a novel, highly selective TGFβRI small molecule inhibitor.
DC6306 LY2157299(Galunisertib) LY2157299 is a potent TGFβ receptor I (TβRI) inhibitor with IC50 of 56 nM. Phase 2.
DC7914 LDN-214117 LDN-214117 is a potent and selective ALK2 inhibitor with IC50 of 22 nM; > 100 fold selectivity for ALK5; also inhibits BMP6(IC50=100 nM).
DC7742 K02288 K02288 is a potent, and selective type I BMP receptor inhibitor with IC50 of 1.1, 1.8, 6.4 nM for ALK2, ALK1 and ALK6, showing weaker inhibition on other ALKs (3, 4, 5) and ActRIIA.
DC8028 ITD-1 ITD-1 is a novel and highly selective TGFβ pathway inhibitor. ITD-1 molecule turns stem cells into heart cells.
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