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浙江省杭州市萧山区宁围街道传化科创大厦2幢6层

SB202190 (FHPI)

目录号
C152121
产品规格
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产品介绍

DESCRIPTION

Background


SB202190 is a selective p38 MAP kinase inhibitor with IC50s of 50 nM and 100 nM for p38α and p38β2, respectively. SB 202190 binds to the ATP pocket of the active recombinant human p38 kinase with a Kd of 38 nM. SB 202190 has anti-cancer activity and rescued memory deficits[1][2]. SB202190 induces autophagy[3]. 

M. W t

331.34

Formula

C20H14FN3O

CAS No

152121-30-7

Storage

Powder

- 20°C

3 years

4°C

2 year                                  C20H14FN3O

In solvent

-80°C

6 months                                     

 

-20°C 

1 month

Solubility

DMSO

100 mg/mL(301.80 mM; Need ultrasonic)

 

Ethanol

12 mg/mL(36.22 mM)

 

H2O

< 0.1 mg/mL(insoluble)

 


技术参数

BIOLOGICAL ALTIVITY

In Vitro

SB202190 (0-10 μM; 0-72 hours) 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 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, SB202190 (10 μM; 2 hours) abrogates phosphorylation of S6K1(T389) and S6(S235/236), but not AKT(S473), indicating that p38i selectively blocks mTORC1 signaling[2].

In Vivo

SB202190 (5 mg/kg; intraperitoneal injection; daily for 10-12 days) 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]. Nemoto S, et al. Induction of apoptosis by SB202190 through inhibition of p38beta mitogen-activated protein kinase. J Biol Chem. 1998 Jun 26;273(26):16415-20.

[3]. Grossi V, et al. Bay 43-9006 inhibits p38α activity in colorectal cancer cells and synergizes with the DFG-in inhibitor SB202190 to increase apoptotic response. Cancer Biol Ther. 2012 Dec;13(14):1471-81.

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