A 83-01 MedChemExpress (MCE)

Product Name	A 83-01
Synonyms	A83-01 A-83-01 A 83-01 A-83-01AB142092) ALK5 Inhibitor IV TGF inhibitor A-83-01 TGF-β RI Kinase Inhibitor IV Synonyms A83-01 A-83-01 A 83-01 A-83-01AB142092) ALK5 Inhibitor IV TGF inhibitor A-83-01 TGF-β RI Kinase Inhibitor IV 3-(6-Methyl-2-pyridinyl)-N-phenyl-4-(4-quinolinyl)-1H-pyrazole-1-carbothioamide 3-(6-methylpyridin-2-yl)-N-phenyl-4-(quinolin-4-yl)-1H-pyrazole-1-carbothioamide
CAS	909910-43-6
EINECS
Chemical Formula	C25H19N5S
Molecular Weight	421.52
inchi
Package	1 mg;5 mg;10 mg;25 mg;50 mg;100 mg
Price	Email to quote
Descriptions	A 83-01 A 83-01 MedChemExpress (MCE) HY-10432 909910-43-6 99.41% -20°C, protect from light, stored under nitrogen The compound is unstable in solutions, freshly prepared is recommended. Room temperature in continental US Descriptions A 83-01 A 83-01 MedChemExpress (MCE) HY-10432 909910-43-6 99.41% -20°C, protect from light, stored under nitrogen The compound is unstable in solutions, freshly prepared is recommended. Room temperature in continental US may vary elsewhere. A 83-01 is a potent inhibitor of TGF-β type I receptor ALK5 kinase, type I nodal receptor ALK4 and type I nodal receptor ALK7, with IC50s of 12 nM, 45 nM and 7.5 nM against the transcription induced by ALK5, ALK4 and ALK7, respectively. A 83-01 is a potent inhibitor of TGF-β type I receptor ALK5 kinase, ALK4 and ALK7, reduces the level of ALK-5-induced transcription with an IC50 of 12 nM in Mv1Lu cells, also blocks the ALK4-TD and ALK7-TD induced transcription with IC50s of 45 nM and 7.5 nM in R4-2 cells, and weakly suppresses that induced by constitutively active ALK-6, ALK-2, ALK-3, and ALK-1. A 83-01 (0.03-10 μM) potently prevents the growth-inhibitory effects of TGF-β, and completely inhibits the effect at 3 μM. A 83-01 (1-10 μM) inhibits TGF-β-induced Smad activation in HaCaT cells[1]. A 83-01 (1 μM) decreases cell motility, adhesion and invasion increased by TGF-β1 in HM-1 cells, but does not change cell proliferation[2]. A 83-01 (50, 150 and 500 μg/mouse, i.p.) significantly improves survival of the mice without body weight or neurobehavioral appearances[2]. A 83-01 (0.5 mg/kg, i.p.) shows a significantly strong antitumor effect in mice bearing M109 cells[3]. Mice[2] Female B6C3F1 mice used for the in vivo studies are maintained under specific pathogen-free conditions. To evaluate the effect of A 83-01 on the survival of mice bearing peritoneal dissemination, HM-1 cells (1×106) are injected into the abdominal cavity via the left flank of the mouse. Starting the next day, A 83-01 (150 μg/body) or vehicles (PBS with 0.5% DMSO) are injected into the abdominal cavity three times per week. Mice are euthanized before reaching the moribund state[2]. HM-1 cells are seeded into a 96-well plate and are incubated for 18 hr. A 83-01 (1 μM) or vehicle are then added for 12 hr followed by the addition of TGF-β1 (1 ng/mL) or vehicle for 60 hr. The number of viable cells in each well is examined using the WST-1 assay[2]. ALK5 12 nM (IC50) ALK4 45 nM (IC50) ALK7 7.5 nM (IC50) \| \| \| \| \| \| \| \| \| \| [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. [Content Brief] [2]. Yamamura S, et al. The activated transforming growth factor-beta signaling pathway in peritoneal metastases is a potential therapeutic target in ovarian cancer. Int J Cancer. 2012 Jan 1 130(1):20-8. [Content Brief] [3]. Taniguchi Y, et al. Enhanced antitumor efficacy of folate-linked liposomal Adriamycin with TGF-β type I receptor inhibitor. Cancer Sci. 2010 Oct 101(10):2207-13. [Content Brief]
Supplier Website	http://www.medchemexpress.com/A-83-01.html
Last Update	2025-10-14 16:03:33

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