GL-4512 | LILRB4 inhibitor | Probechem Biochemicals

Chemical Structure : GL-4512

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GL-4512 (GL4512)

货号: PC-27380Not For Human Use, Lab Use Only.

GL-4512 a potent, small molecule direct modulator of leukocyte immunoglobulin-like receptor B4 (LILRB4, ILT3/CD85k) with SPR KD of 39.2 nM for binding to immobilized LILRB4 protein, inhibits LILRB4-SCG2 interaction with IC50 of 37 nM in TR-FRET assays, inhibits LILRB4-mediated immunosup pressive signaling pathways relevant to tumor immune evasion.

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生物&药学活性

GL-4512 a potent, small molecule direct modulator of leukocyte immunoglobulin-like receptor B4 (LILRB4, ILT3/CD85k) with SPR KD of 39.2 nM for binding to immobilized LILRB4 protein, inhibits LILRB4-SCG2 interaction with IC50 of 37 nM in TR-FRET assays, inhibits LILRB4-mediated immunosup pressive signaling pathways relevant to tumor immune evasion.
GL-4512 demonstrates cellular engagement of LILRB4 with EC50 of 53 nM,
GL-4512 shows direct binding to recombinant human LILRB4 extracellular do main protein with MST KD of 18.1 nM.
GL-4512 attenuated SCG2-induced phosphorylation of both SHP1 and SHP2 with IC50 values of 101 nM and 141 nM in LILRB4-expressing THP-1 derived macrophage-like cells respectively.
GL-4512 markedly suppressed p-STAT3 levels in a dose-de pendent manner (IC50 = 76.3 nM) in SCG2 stimulation induced substantial phosphorylation of STAT3 in LILRB4-expressing cells.
GL-4512 restores anti-tumor immune function across colorectal cancer and AML co-culture systems.
GL-4512 demonstrates cross-species LILRB4 engagement (KD=32.5 nM, recombinant murine LILRB4) and suppresses CT26 tumor progression in vivo (20 mg/kg by oral gavage once daily for 21 days).

物理化学性质&存储条件

分子量	425.57
分子式	C21H23N5OS2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	4-methyl-N-(2-methyl-4-(thiomorpholinomethyl)phenyl)-2-(pyrimidin-2-yl)thiazole-5-carboxamide

参考文献

1. Abdel-Rahman SA, et al. ACS Chem Biol. 2026 Jul 26. doi: 10.1021/acschembio.6c00486.

GL-4512 (GL4512)

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物理化学性质&存储条件

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GL-4512 (GL4512)

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