Grp94 Inhibitor-1

小分子

Grp94 抑制剂-1

Grp94 Inhibitor-1

G650204-5mg

5mg

≥98%

-20°C储存

超低温冰袋运输

Grp94 Inhibitor-1 is a potent, selective Grp94 inhibitor with an IC 50 value of 2 nM, and over 1000-fold selectivity to Grp94 against Hsp90α In Vitro Grp94-specific clients include a subset of integrin subunits such as integrin α2 and integrin αL. Their maturation and trafficking to the cell surface are dependent on the Grp94 chaperone function but have no association with cytoplasmic Hsp90α. Grp94 Inhibitor-1 (1-5 μM; 36 hours) significantly downregulated the cell surface expression levels of integrin α2 and integrin αL in a dose-dependent manner in panc1 cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: Panc1 cells Concentration: 1 μM; 2.5 μM; 5 μM Incubation Time: 36 hours Result: Decreased integrin α2 and integrin αL protein expression. In Vivo Grp94 Inhibitor-1 (intraperitoneal injection,qid.; coadminbistration 10 mg/kg or 30 mg/kg; 8 days) does not attenuate the colon shortening, but decreases disease activity index (DAI) scores. It also TNFα and IL-6 levels in the serum and colonic tissues and significantly reduces the p65 expression in colonic tissues, especially those in the 30 mg/kg dose group . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: C57BL/6 mice (male, 20-22 g) Dosage: 10 mg/kg or 30 mg/kg Administration: Intraperitoneal injection,qid.; coadminbistration 10 mg/kg or 30 mg/kg Result: Decreased disease activity index (DAI) scores in UC mices. Form:Solid IC50& Target:GRP94 2 nM (IC 50 )

Grp94 抑制剂-1 是一种强效、选择性的 Grp94 抑制剂，其 IC 50 值为 2 nM，对 Grp94 的选择性超过 Hsp90α 的 1000 倍。

2234897-35-7

C22H28N2O2

352.47 g/mol

137321151

CC(C)C1=CC=C(C=C1)C2=CC(=C(C=C2)NC3CCC(CC3)O)C(=O)N

2-[(4-hydroxycyclohexyl)amino]-5-(4-propan-2-ylphenyl)benzamide

1S/C22H28N2O2/c1-14(2)15-3-5-16(6-4-15)17-7-12-21(20(13-17)22(23)26)24-18-8-10-19(25)11-9-18/h3-7,12-14,18-19,24-25H,8-11H2,1-2H3,(H2,23,26)

JMGDXIHGWTVBMX-UHFFFAOYSA-N

CC(C)C1=CC=C(C=C1)C2=CC(=C(C=C2)NC3CCC(CC3)O)C(=O)N

137321151

DMSO : 250 mg/mL (709.28 mM; Need ultrasonic)

3

3

5

352.215 Da

352.215 Da

75.400 Ų

26

0

451.000

0

1

4.700