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A 83-01 Chemical Structure
|Product name: A 83-01|
|Cat. No.: HY-10432|
A 83-01 is a selective inhibitor of TGF-β type I receptor ALK5 kinase, type I activin/nodal receptor ALK4 and type I nodal receptor ALK7 (IC50 values are 12, 45 and 7.5 nM respectively).
IC50 Value: 12 nM ( ALK5)
A 83-01 blocks phosphorylation of Smad2 and inhibits TGF-β-induced epithelial-to-mesenchymal transition. A 83-01 only weakly inhibits ALK-1, -2, -3, -6 and MAPK activity and is more potent than SB 431542.
in vitro: A-83-01, an inhibitor of TGF-β type I receptor, increased the expression of Myf5 and MyoD, and enhanced myotube formation . Microarray analysis of HM-1 cells treated with TGF-β1 and/or A-83-01 revealed that A-83-01 efficiently inhibited transcriptional changes that are induced by TGF-β1 . -83-01 treatment significantly increased these parameters within 24 h that was positively related to pericyte coverage and tumor cell proliferation. Furthermore, apparent diffusion coefficient (ADC) determined by diffusion-weighed imaging was decreased by A-83-01 treatment, suggesting the decrease of tumor interstitial fluid pressure. Vascular function of the tumor improved by A-83-01treatment well assessed on post-Gd-L-enhanced MR images .
in vivo: The targeting efficacy of single intravenous injections of F-SL combined with A-83-01 was evaluated by measurement of the biodistribution and the antitumor effect in mice bearing murine lung carcinoma M109. A-83-01 temporarily changed the tumor vasculature around 3 h post injection. A-83-01 induced 1.7-fold higher drug accumulation of F-SL in the tumor than liposome alone at 24 h post injection .
|M.Wt||421.52||Storage||Please store the product under the recommended conditions in the Certificate of Analysis.|
|Solvent & Solubility||
50 mM in DMSO
|1 mg||5 mg||10 mg|
|1 mM||2.3724 mL||11.8618 mL||23.7237 mL|
|5 mM||0.4745 mL||2.3724 mL||4.7447 mL|
|10 mM||0.2372 mL||1.1862 mL||2.3724 mL|
. Yamamura S, Matsumura N, Mandai M, 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.
A 77-01 is a potent inhibitor of TGF-(beta) type I receptor superfamily activin-like kinase ALK5 with IC50 of 25 nM.
EW-7197 is a highly potent, selective, and orally bioavailable TGF-(beta) receptor ALK4/ALK5 inhibitor with IC50 of 13 nM and 11 nM, respectively.
GW788388 is a potent and selective inhibitor of ALK5 with IC50 of 18 nM, also inhibits TGF-(beta) type II receptor and activin type II receptor activities, but does not inhibit BMP type II receptor.
ITD-1 is an inducer of TGF(beta) type II receptor degradation-1, is a potent and highly selective TGF(beta) pathway inhibitor (IC50 = 0.85 (mu)M).
LY364947 is a potent ATP-competitive inhibitor of TGF(beta)R-I with IC50 of 59 nM, exhibits 7-fold selectivity over TGF(beta)R-II.
LY2157299 is a potent TGF(beta) receptor I (T(beta)RI) inhibitor with IC50 of 56 nM.
R-268712 is a potent and selective inhibitor of ALK5 with an IC50 of 2.5 nM.
RepSox(E-616452; SJN 2511) is a potent and selective inhibitor of the TGF(beta)R-1/ALK5 with IC50 of 23 nM and 4 nM for ATP binding to ALK5 and ALK5 autophosphorylation, respectively.
SB525334 is a potent and selective inhibitor of TGF(beta) 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.
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