ZAP-180013

Cas No.:	873080-25-2
Chemical Name:	5-Chloro-N-(4-chlorobenzyl)-2-(ethylsulfonyl)-N-(furan-2-ylmethyl)pyrimidine-4-carboxamide
Synonyms:	5-Chloro-N-[(4-chlorophenyl)methyl]-2-(ethylsulfonyl)-N-(2-furanylmethyl)-4-pyrimidinecarboxamide;5-chloro-N-(4-chlorobenzyl)-2-(ethylsulfonyl)-N-(furan-2-ylmethyl)pyrimidine-4-carboxamide;STK911200;ZAP 180013;ST50173581;5-chloro-N-(4-chlorobenzyl)-2-(ethylsulfonyl)-N-(2-furylmethyl)pyrimidine-4-carboxamide;[5-chloro-2-(ethylsulfonyl)pyrimidin-4-yl]-N-[(4-chlorophenyl)methyl]-N-(2-fur ylmethyl)carboxamide
SMILES:	ClC1=C([H])N=C(N=C1C(N(C([H])([H])C1=C([H])C([H])=C([H])O1)C([H])([H])C1C([H])=C([H])C(=C([H])C=1[H])Cl)=O)S(C([H])([H])C([H])([H])[H])(=O)=O
Formula:	C19H17Cl2N3O4S
M.Wt:	454.3270
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	ZAP-180013 is a zeta-chain-associated protein kinase 70 (ZAP-70) inhibitor with an IC50 of 1.8 μM. ZAP-180013 inhibits the interaction of ZAP-70 SH2 domain with immunoreceptor tyrosine-based activation motif (ITAMs)[1].
Target:	IC50: 1.8 μM (ZAP-70)[1]
In Vitro:	ZAP-70 is a critical molecule in the transduction of T cell antigen receptor signaling and the activation of T cells. Upon activation of the T cell antigen receptor, ZAP-70 is recruited to the intracellular ζ-chains of the T cell receptor, where ZAP-70 is activated and colocalized with its substrates. Inhibitors of ZAP-70 could potentially function as treatments for autoimmune diseases or organ transplantation. ZAP-180013 disrupts the interaction between ZAP-70 and the T cell antigen receptor. The IC50s in both FP and TR-FRET assays for ZAP-180013 are 9.6 μM and 16.841 μM, respectively[1].
References:	[1]. Patrick R Visperas, et al. Identification of Inhibitors of the Association of ZAP-70 With the T Cell Receptor by High-Throughput Screen. SLAS Discov. 2017 Mar;22(3):324-331.