ALEXIS Biochemicals: ALK5 Inhibitor I

ALX-270-448

Revised 24-Jul-06

ALK5 Inhibitor I
SYNONYMS	TGF-β RI Kinase Inhibitor I 3-(Pyridin-2-yl)-4-(4-quinonyl)]-1H-pyrazole
PRODUCT LINE	Chemokines & Cytokines
PRODUCT CATEGORY	Transforming Growth Factor beta [TGFbeta] & Receptors / Related Products

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-270-448-M001		1 mg	30.00 USD
ALX-270-448-M005		5 mg	90.00 USD

Product Specification

FORMULA:	C₁₇H₁₂N₄
MW:	272.3
PURITY:	≥97% (¹H-NMR)
APPEARANCE:	Yellow to brown solid.
SOLUBILITY:	Soluble in DMSO or methanol.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
USE/STABILITY:	Stable for 2 years after receipt when stored at -20°C. Stock solutions are stable for up to 3 months when stored at -20°C.
HANDLING:	Protect from light.
HAZARD:	MAY BE CARCINOGENIC. HARMFUL.

Product Description

Cell permeable, potent, selective and ATP-competitive inhibitor of TGF-β RI kinase (IC₅₀=51nM). Displays ~15-fold greater selectivity over p38α MAPK (IC₅₀=740nM). Inhibits TGF-β-dependent cellular growth (IC₅₀=89nM in NIH 3T3 mouse fibroblasts) and transcription activation (IC₅₀=47nM in mink lung cells).

Product Specific Literature References

Synthesis and activity of new aryl- and heteroaryl-substituted pyrazole inhibitors of the transforming growth factor-beta type I receptor kinase domain: J.S. Sawyer, et al.; J. Med. Chem. 46, 3953 (2003) Abstract
Successful shape-based virtual screening: the discovery of a potent inhibitor of the type I TGFbeta receptor kinase (TbetaRI): J. Singh, et al.; Bioorg. Med. Chem. Lett. 13, 4355 (2003) Abstract

Further Categories Containing This Product:

MAPK Pathway Inhibitors

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