TGF-beta RI Kinase Inhibitor VA TGF-β signaling blocker

TGF-β RI Kinase Inhibitor V (CAS 627536-09-8)

TGF-β RI Kinase Inhibitor V | CAS 627536-09-8 is rated 5.0 out of 5 by 1.
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Synonym: 2-(5-Chloro-2-fluorophenyl)pteridin-4-yl)pyridin-4-yl amine
Application: A TGF-β signaling blocker
CAS Number: 627536-09-8
Purity: >97%
Molecular Weight: 352.75
Molecular Formula: C17H10ClFN6
* Refer to Certificate of Analysis for lot specific data (including water content).
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TGF-β RI Kinase Inhibitor V is a selective and reversible inhibitor, which suppresses TGF-β RI/ALK5 signaling. It is known that TGF-β RI Kinase Inhibitor V also inhibits p38α at concentrations greater than 867 nM. Studies indicate that TGF-βRI Kinase Inhibitor V reduces the number of myofibroblasts at fibroblastic foci. In addition, this compound is effective in blocking autocrine and paracrine TGF-β signaling in glioma cells and restores the lytic activity of polyclonal natural killer cells against glioma cells. This inhibitor functions in suppressing the action of MAPKAP and PKD.


References

1. Ge, R., et al. 2006. Clin. Cancer Res. 12: 4315-4330. PMID: 16857807
2. Kapoun, A.M., et al. 2006. Mol. Pharmacol. 70: 518-531. PMID: 16707625
3. Jian, H., et al. 2006. Genes Dev. 20: 666-674. PMID: 16543220
4. Hayashi, T., et al. 2004. Clin. Cancer Res. 10: 7540-7546. PMID: 15569984
5. Uhl, M., et al. 2004. Cancer Res. 64: 7954-7961. PMID: 15520202

Appearance :
Light yellow solid
Physical State :
Solid
Solubility :
Soluble in DMSO (>5 mg/ml).
Storage :
Store at 4° C
Melting Point :
214.79° C (Predicted)
Boiling Point :
460.41° C at 760 mmHg (Predicted)
Density :
1.49 g/cm3 (Predicted)
Refractive Index :
n20D 1.72 (Predicted)
IC50 :
TGF-β RI/ALK5 kinase: EC5050 = 48 nM; TGF-βRI: IC50 = 49 nM; Hepatitis C virus: EC5050 = 890 nM
pK Values :
pKb: 4.56 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
PubChem CID :
10316032
MDL Number :
MFCD11519969
SMILES :
C1=CC(=C(C=C1Cl)C2=NC3=NC=CN=C3C(=N2)NC4=CC=NC=C4)F

Download SDS (MSDS)

Certificate of Analysis

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Rated 5 out of 5 by from Wang Wang, ZP. et al. (PubMed 24515103) used TGF- RI Kinase Inhibitor V to demonstrate that TGF- signaling participates in the maintenance of the primordial follicle pool in the mouse ovary. -SCBT Publication Review
Date published: 2015-07-18
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