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SB 202190 hydrochloride

Names

[ CAS No. ]:
350228-36-3

[ Name ]:
SB 202190 hydrochloride

[Synonym ]:
4-[4-(4-Fluorophenyl)-5-(4-pyridinyl)-1H-imidazol-2-yl]phenol hydrochloride (1:1)
SB 202190 Hydrochloride
Phenol, 4-[4-(4-fluorophenyl)-5-(4-pyridinyl)-1H-imidazol-2-yl]-, hydrochloride (1:1)
4-[4-(4-fluorophenyl)-5-pyridin-4-yl-1,3-dihydroimidazol-2-ylidene]cyclohexa-2,5-dien-1-one,hydrochloride
4-[4-(4-Fluorophenyl)-5-(pyridin-4-yl)-1H-imidazol-2-yl]phenol hydrochloride (1:1)

Biological Activity

[Description]:

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[1][2]. SB202190 hydrochloride induces autophagy[3].

[Related Catalog]:

Signaling Pathways >> Apoptosis >> Apoptosis
Research Areas >> Cancer
Signaling Pathways >> Autophagy >> Autophagy
Signaling Pathways >> MAPK/ERK Pathway >> p38 MAPK
Research Areas >> Neurological Disease

[Target]

p38α:50 nM (IC50)

p38β2:100 nM (IC50)


[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[1]. 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)[2]. 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[2].

[In Vivo]

SB 202190 (5 mg/kg; intraperitoneal injection; daily for 10-12 days) hydrochloride shows inhibition of tumor cell survival and tumor growth[2].

[References]

[1]. Davies SP, et al. Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem J. 2000 Oct 1;351(Pt 1):95-105.

[2]. Yang S, et al. Protective effects of p38 MAPK inhibitor SB202190 against hippocampal apoptosis and spatial learning and memory deficits in a rat model of vascular dementia. Biomed Res Int. 2013;2013:215798.

Chemical & Physical Properties

[ Molecular Formula ]:
C20H15ClFN3O

[ Molecular Weight ]:
367.80

[ Exact Mass ]:
367.088776

[ PSA ]:
61.80000

[ LogP ]:
5.45240

[ Storage condition ]:
2-8°C

Safety Information

[ Hazard Codes ]:
Xi

[ Risk Phrases ]:
36/37/38

[ Safety Phrases ]:
26-36/37

Related Compounds