Successful, we will reply to you quickly.OK
Please select the quantity.OK
Your message is being sent, please wait.Close
Send mail failed, please send again!Close
Products are for research use only. Not for human use. We do not sell to patients.
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.
LY2109761 is a novel selective TGF-(beta) receptor type I/II (T(beta)RI/II) dual inhibitor with Ki of 38 nM and 300 nM, respectively; shown to negatively affect the phosphorylation of Smad2.
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.