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Product details

名称

Grp94 Inhibitor-1

分子类型

小分子

别名

Grp94 抑制剂-1

英文名称

Grp94 Inhibitor-1

货号

G650204-5mg

包装规格

5mg

浓度

≥98%

储存温度

-20°C储存

运输条件

超低温冰袋运输

产品介绍

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 )

生化机理

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。

CAS号

2234897-35-7

分子式

C22H28N2O2

分子量

352.47 g/mol

PubChem编号

137321151

Isomeric SMILES

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

IIUPAC Name

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

INCHI

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)

InChi Key

JMGDXIHGWTVBMX-UHFFFAOYSA-N

Smiles

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

PubChem CID

137321151

溶解性

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

氢键供体数Hydrogen Bond Donor Count

氢键受体数Hydrogen Bond Acceptor Count

可旋转键计数Rotatable Bond Count

精确质量Exact Mass

352.215 Da

单同位素质量Monoisotopic Mass

352.215 Da

拓扑极表面积Topological Polar Surface Area

75.400 Å²

重原子数Heavy Atom Count

形式电荷Formal Charge

复杂度Complexity

451.000

同位素原子数Isotope Atom Count

共价键合单元计数Covalently-Bonded Unit Count

XLogP3

4.700

Safety

「No Dangerous Attributes」

「No upstream and downstream information yet」

Technical Documents

「No technical documents」

Articles

「No related articles yet」

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