SB 202190 hydrochloride

SB-202190 hydrochloride is an inhibitor of p38 MAP kinases, inhibiting p38α (SAPK2A, MAPK14) and p38β (SAPK2B, MAPK11). It directly binds to the ATP binding pocket of p38 MAP kinases and has been used to elucidate the roles of p38 MAP kinases in inflammatory cytokine expression, nicotine-induced receptor expression, and HIV-mediated depressive disorder. SB 202190 hydrochloride is a selective p38 MAP kinase inhibitor with IC50s of 50 nM and 100 nM for p38α and p38β2, respectively. SB 202190 hydrochloride binds to the ATP pocket of the active recombinant human p38 kinase with a Kd of 38 nM. SB 202190 hydrochloride has anti-cancer activity. SB202190 hydrochloride induces autophagy.

Product information

CAS Number: 350228-36-3

Molecular Weight: 367.80

Formula: C20H15ClFN3O

Chemical Name: 4-[4-(4-fluorophenyl)-5-(pyridin-4-yl)-1H-imidazol-2-yl]phenol hydrochloride

Smiles: Cl.OC1C=CC(=CC=1)C1NC(=C(N=1)C1C=CC(F)=CC=1)C1C=CN=CC=1

InChiKey: XOQSUTIMRLPFPB-UHFFFAOYSA-N

InChi: InChI=1S/C20H14FN3O.ClH/c21-16-5-1-13(2-6-16)18-19(14-9-11-22-12-10-14)24-20(23-18)15-3-7-17(25)8-4-15;/h1-12,25H,(H,23,24);1H

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: To be determined

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

SB 202190 (0-10 μM; 0-72 hours) hydrochloride attenuates growth of a subgroup of CRC cell lines such as RKO, CACO2 and SW480 in a dose- and time-dependent manner. SB 202190 hydrochloride strongly inhibited colony formation and anchorage-independent growth (10 μM for 7-10 days) and elevated apoptotic cell death (10 μM for 72 h) in this same subset of CRC lines (RKO, CACO2 and SW480). In RKO, CACO2 and SW480 cells, SB 202190 (10 μM; 2 hours) hydrochloride abrogates phosphorylation of S6K1(T389) and S6(S235/236), but not AKT(S473), indicating that p38i selectively blocks mTORC1 signaling.

In Vivo:

SB 202190 (5 mg/kg; intraperitoneal injection; daily for 10-12 days) hydrochloride shows inhibition of tumor cell survival and tumor growth.

References:

1. Fu, X., Lawson, M.A., Kelley, K.W., et al. HIV-1 Tat activates indoleamine 2, 3 dioxygenase in murine organotypic hippocampal slice cultures in a p38 mitogen-activated protein kinase-dependent manner. J. Neuroinflammation 8(88), 1-12 (2011).
2. Fox, T., Coll, J.T., Xie, X., et al. A single amino acid substitution makes ERK2 susceptible to pyridinyl imidazole inhibitors of p38 MAP kinase. Protein Sci. 7(11), 2249-2255 (1998).

Products are for research use only. Not for human use.