Grp94 Inhibitor-1


Catalog No. Size PriceQuantity
M27783-C Contact sales@xcessbio.com for quotation $100Unavailable

Description

Grp94 Inhibitor-1 is a potent, selective Grp94 inhibitor with an IC50 value of 2 nM, and over 1000-fold selectivity to Grp94 against Hsp90α.

Product information

CAS Number: 2234897-35-7

Molecular Weight: 352.47

Formula: C22H28N2O2

Chemical Name: 4-[(4-hydroxycyclohexyl)amino]-4'-(propan-2-yl)-[1,1'-biphenyl]-3-carboxamide

Smiles: CC(C)C1C=CC(=CC=1)C1=CC(C(N)=O)=C(C=C1)NC1CCC(O)CC1

InChiKey: JMGDXIHGWTVBMX-UHFFFAOYSA-N

InChi: 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)

Technical Data

Appearance: Solid Power

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

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

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:

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.

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.

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

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