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AMG-548 hydrochloride (864249-60-5 free base)

Catalog No. T10298 CAS T10298

Synonyms: AMG-548 hydrochloride

AMG-548 hydrochloride is an orally active and selective p38α inhibitor (Ki: 0.5 nM) and shows slightly selective over p38β (Ki: 36 nM) and <1000 fold selective against p38γ/p38δ. It is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50: 3 nM).

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AMG-548 hydrochloride (864249-60-5 free base) Chemical Structure

AMG-548 hydrochloride (864249-60-5 free base), CAS T10298

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Description	AMG-548 hydrochloride is an orally active and selective p38α inhibitor (Ki: 0.5 nM) and shows slightly selective over p38β (Ki: 36 nM) and >1000 fold selective against p38γ/p38δ. It is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50: 3 nM).
Targets&IC50	p38β:3.6 nM (ki), JNK3:61 nM (ki), JNK1:11480 nM (ki), JNK2:39 nM (ki), p38α (dog):5.0 nM (ki), p38α:0.5 nM (ki), p38δ:2600 nM (ki), p38γ:4100 nM (ki)

Synonyms	AMG-548 hydrochloride
Molecular Weight	498.02
Formula	C29H28ClN5O
CAS No.	T10298

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

1. Lee MR, et al. MAP kinase p38 inhibitors: clinical results and an intimate look at their interactions with p38alphaprotein. Curr Med Chem. 2005;12(25):2979-94. 2. Verkaar F, et al. Inhibition of Wnt/β-catenin signaling by p38 MAP kinase inhibitors is explained by cross-reactivity with casein kinase Iδ/ɛ. Chem Biol. 2011 Apr 22;18(4):485-94.

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Keywords

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