A CXCR4 antagonist (IC50s = 8 and 11 nM for the human and rat receptors

IT1t (hydrochloride) – 10 mg

Brand:
Cayman
CAS:
1092776-63-0
Storage:
-20
UN-No:
Non-Hazardous - /

IT1t is a chemokine (C-X-C motif) receptor 4 (CXCR4) antagonist (IC50s = 8 and 11 nM for the human and rat receptors, respectively).{48774} It is selective for CXCR4 over human ether-a-go-go-related gene potassium channels (hERG/Kv11.1; IC50 = 13,240 nM). IT1t inhibits calcium mobilization induced by chemokine (C-X-C-motif) ligand 12 (CXCL12) in CEM cells (IC50 = 1.1 nM) and decreases CXCL12-induced migration of Jurkat cells (IC50 = 79.1 nM).{48774,50131} It inhibits replication of the HIV-1 strain NL4-3 in MT-4 cells and isolated human peripheral blood mononuclear cells (PBMCs) stimulated with phytohemagglutinin (PHA; IC50s = 14.2 and 19 nM, respectively).{50131} IT1t (20 µM) reduces tumor growth in an MDA-MB-231-B zebrafish xenograft model.{50133}  

 

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SKU: 28434 - 10 mg Category:

Description

A CXCR4 antagonist (IC50s = 8 and 11 nM for the human and rat receptors, respectively); selective for CXCR4 over hERG/Kv11.1 (IC50 = 13,240 nM); inhibits CXCL12-induced calcium mobilization in CEM cells (IC50 = 1.1 nM) and decreases CXCL12-induced migration of Jurkat cells (IC50 = 79.1 nM); inhibits replication of the HIV-1 strain NL4-3 in MT-4 cells and isolated PHA-stimulated PBMCs; reduces tumor growth in an MDA-MB-231-B zebrafish xenograft model at 20 µM

Formal name: N,N′-dicyclohexyl-carbamimidothioic acid, (5,6-dihydro-6,6-dimethylimidazo[2,1-b]thiazol-3-yl)methyl ester, dihydrochloride

Synonyms: 

Molecular weight: 479.6

CAS: 1092776-63-0

Purity: ≥95%

Formulation: A crystalline solid

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