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ALK5 Inhibitor I

ALX-270-448

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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). Suppresses invasion of MDA-MB-231 breast cancer cells in a matrigel invasion assay.

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Product Details

Alternative Name	TGF-β RI Kinase Inhibitor I, 3-(Pyridin-2-yl)-4-(4-quinonyl)]-1H-pyrazole
Appearance	Yellow to brown solid.
CAS	396129-53-6
Couple Target	TGF-beta receptor
Couple Type	Inhibitor
Formula	C₁₇H₁₂N₄
MW	272.3
Purity	≥97% (TLC)
Solubility	Soluble in DMSO or methanol.

Handling & Storage

Use/Stability	As indicated on product label or CoA when stored as recommended. 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.
Long Term Storage	-20°C
Shipping	Ambient Temperature

Regulatory Status	RUO – Research Use Only

Chemically defined conditions for long-term maintenance of pancreatic progenitors derived from human induced pluripotent stem cells: S. Konagaya, et al.; Sci. Rep. 9, 640 (2019), Abstract — Full Text
Closed-channel culture system for efficient and reproducible differentiation of human pluripotent stem cells into islet cells: K. Hirano, et al.; Biochem. Biophys. Res. Commun. 487, 344 (2017), Application(s): hiPSC line 253G1, Abstract
Emdogain-regulated gene expression in palatal fibroblasts requires TGF-βRI kinase signaling: A. Stähli, et al.; PLoS One 9, e105672 (2014), Abstract — Full Text
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
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

Last modified: May 29, 2024

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ALK5 Inhibitor I

ALX-270-448

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