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

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Application:	A TGF-β signaling blocker
CAS Number:	627536-09-8
Purity:	>97%
Molecular Weight:	352.8
Molecular Formula:	C₁₇H₁₀ClFN₆

Description

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 p38a at concentrations greater than 867 nM. Studies indicate that TGF-β RI 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.

Technical Information

Appearance:	Light yellow solid
Physical State:	Solid
Solubility:	Soluble in DMSO (>5 mg/ml).
Storage:	Store at 4° C
Boiling Point:	460.41 °C at 760 mmHg (Predicted)
Density:	1.49 g/cm³ (Predicted)
Refractive Index:	n²⁰_D 1.72 (Predicted)
IC50:	TGF-β RI/ALK5 kinase: EC₅₀50 = 48 nM; TGF-βRI: IC₅₀ = 49 nM; Hepatitis C virus: EC₅₀50 = 890 nM

Safety and Reference Information

WGK Germany:	3
PubChem CID:	10316032
SMILES:	Clc1ccc(F)c(c1)c1nc(Nc2ccncc2)c2nccnc2n1

For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.

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

SDS

Datasheet/SDS