A 83-01 [ALK5; ALK4; ALK7 Inhibitor]
[CAT#: MOD2005ZP65]
Selective TGF-βRI (ALK5), ALK4 and ALK7 inhibitor. Maintains human induced pluriA highly potent stem cell (hiPSC) self renewal.
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Description
83-01 is a selective inhibitor of TGF-βRI (ALK5), ALK4 and ALK7 (ICK values of ALK5, ALK4 and ALK7 are 12, 45 and 7.5 nM, respectively).
Reprogramming: A 83-01 can reprogram fibroblasts into neural stem cells and cardiomyocytes.
Differentiation: A 83-01 blocks SMAD2/3 phosphorylation and inhibits TGF-β-induced epithelial-to-mesenchymal transition
Maintenance/self-renewal: A 83-01 helps to maintain the homogeneity of iPSC and long-term self-renewal in vitro
Reprogramming: A 83-01 can reprogram fibroblasts into neural stem cells and cardiomyocytes.
Differentiation: A 83-01 blocks SMAD2/3 phosphorylation and inhibits TGF-β-induced epithelial-to-mesenchymal transition
Maintenance/self-renewal: A 83-01 helps to maintain the homogeneity of iPSC and long-term self-renewal in vitro
Synonyms
A83
Chemical Name
3-(6-Methyl-2-pyridinyl)-N-phenyl-4 -(4-quinolinyl)-1H-pyrazole-1-carbothioamide
Modulator Type
Inhibitor
Relevant Disease
Neurological Disorders
Assay Description
83-01 is an effective inhibitor of TGF-βI type receptor ALK5 kinase, ALK4 and ALK7, which can reduce the transcription level induced by ALK-5 in Mv1Lu cells, IC50 is 12 nM, and can also block ALK4-TD and ALK7- The IC50 induced by TD in R4-2 cells was 45 nM and 7.5 nM transcription, and weakly suppressed transcription induced by constitutively active ALK-6, ALK-2, ALK-3 and ALK-1. 83-01 (0.03-10 µM) effectively prevented the growth inhibitory effect of TGF-β, and completely inhibited the effect at 3 µM. 83-01 (1-10 µM) inhibited TGF-β-induced Smad activation in HaCaT cells [1]. TGF-β1 reduced 83-01 (1 µM) cell movement, adhesion and invasion in HM-1 cells, but did not change cell proliferation [2].
Reference
[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.
[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.
[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.
Assay Description
83-01 (50, 150 and 500 μg/mouse, intraperitoneal injection) can significantly improve the survival rate of mice without weight or neurobehavior appearance [1]. 83-01 (0.5 mg/kg, i.p.) has a strong antitumor effect on mice with M109 cells [2].
References
[1]. 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.
[2]. 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.
[2]. 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.
Molecular Weight
421.52
Form
Pale yellow solid
Chemical Formula
C25H19N5S
Source
Synthetic
SMILES
CC1=CC=CC(=N1)C2=NN(C=C2C3=CC=NC4=CC=CC=C34)C(=S)NC5=CC=CC=C5
Solubility
Soluble in DMSO (50mM)
IC50
IC50: 12 nM (ALK5, cell-based), 45 nM (ALK4 cell-based), 7.5 nM (ALK7 cell-based)
CAS NO.
909910-43-6
PubChem Substance ID
16218924
Purity
>98%
Storage
-20°C (protect from light)
Shipping
Room Temperature
Handling Advice
The compound is sensitive to light. Therefore, we recommend protecting solid materials and solutions from light.
According to reports, A 83-01 can be decomposed into A 77-01 in solution. Therefore, we recommend that you form a solution and use it immediately. Don't store solutions.
If the solution needs to be stored, the solution should be dispensed into sealed vials and stored at -20°C for up to one month.
According to reports, A 83-01 can be decomposed into A 77-01 in solution. Therefore, we recommend that you form a solution and use it immediately. Don't store solutions.
If the solution needs to be stored, the solution should be dispensed into sealed vials and stored at -20°C for up to one month.
Research Use Only
For research use only
For Research Use Only. Not For Clinical Use.
