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Tim-3 inhibitor ML-T7

Chemical Structure : Tim-3 inhibitor ML-T7

CAS No.: 459789-75-4

Tim-3 inhibitor ML-T7 (ML-T7)

Catalog No.: PC-21328Not For Human Use, Lab Use Only.

Tim-3 inhibitor ML-T7 is a potent small molecule inhibitor of T cell immunoglobulin and mucin-containing molecule 3 (Tim-3), binds to Tim-3 disrupts the interaction of Tim-3 with PtdSer and CEACAM1.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

Tim-3 inhibitor ML-T7 is a potent small molecule inhibitor of T cell immunoglobulin and mucin-containing molecule 3 (Tim-3), binds to Tim-3 disrupts the interaction of Tim-3 with PtdSer and CEACAM1.
ML-T7 targets the FG-CC' cleft of Tim-3, a highly conserved binding site of phosphatidylserine (PtdSer) and carcinoembryonic antigen–related cell adhesion molecule 1 (CEACAM1).
ML-T7 binds to hTim-3 and mTim-3 with Kd (dissociation constant) values of 6.98 and 7.40 μM, respectively.
ML-T7 blocks hTim-3 binding to CEACAM1-overexpressing Jurkat cells in a concentration-dependent manner and directly disrupts CEACAM1 binding to hTim-3 in SPR assay.
ML-T7 does not block Tim-3/galectin-9 interaction.
ML-T7 enhances TCR/STAT5 signaling and promotes CD8+ T cell antitumor activity through Tim-3.
ML-T7 directly potentiates the survival and prevents exhaustion of CD8+ cytotoxic T lymphocytes (CTLs), potentiates functions of DCs through both Tim-3 and Tim-4.
ML-T7 (50 mg/kg) exerts antitumor activity in preclinical syngeneic mouse models and humanized mice, potentiates anti–PD-1 therapy in vivo.

Physicochemical Properties

M.Wt 506.34
Formula C27H17Cl2NO5
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

5-(2,4-dichlorophenyl)-3-(p-tolyl)-3a,6a-dihydrospiro[furo[3,4-c]pyrrole-1,2'-indene]-1',3',4,6(3H,5H)-tetraone

References

1. Ma S, et al. Sci Transl Med. 2023 Nov 15;15(722):eadg6752.

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