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首页-小分子抑制剂&激动剂-Others-Diacylglycerol Kinase (DGK)-BMS-986408
BMS-986408

Chemical Structure : BMS-986408

CAS No.: 2618418-12-3

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BMS-986408 (BMS 986408, BMS-408)

货号: PC-24873Not For Human Use, Lab Use Only.

BMS-986408 (BMS-408) is a potent, selective, DAG substrate competitive dual DGKα and DGKζ lipid kinase inhibitor with IC50 of 3 nM and 20 nM respectively, >100-fold selectivity for DGKα over DGKβ and DGKγ.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

BMS-986408 (BMS-408) is a potent, selective, DAG substrate competitive dual DGKα and DGKζ lipid kinase inhibitor with IC50 of 3 nM and 20 nM respectively, >100-fold selectivity for DGKα over DGKβ and DGKγ.
BMS-986408 inhibits DGKζ and DGKι with similar potency, shows no significant activity for Type II (DGKδ, DGKη, DGKκ), Type III (DGKε, or Type V (DGKθ) family members. BMS-986408 induces the translocation of both YFP-DGKα (EC50=0.026 µM) and YFP-DGKζ (EC50=0.008 µM) from cytoplasm to plasma membrane.
BMS-986408 also induces the degradation of both DGKα and DGKζ, which is ubiquitin and proteosome dependent.
BMS-986408 shows potent amplification of phospho-ERK in both CD4+ (EC50=0.008 µM) and CD8+ (EC50=0.012 µM) T cells and IL-2 production (Donor 1 EC50 0.019 µM; Donor 2 EC50 0.034 µM).
BMS-986408 amplified the antigen-specific activation of naïve mouse OT-1 CD8+ T cells by autologous BMDCs cross-presenting OVA, as measured by proliferation (EC50=0.015 µM) and IL-2 production (EC50=0.022 µM).
BMS-986408 also amplified the antigen specific killing of NY-ESO-1 antigen presenting SAOS-2 cells by human T cells transduced with NY-ESO-1 TCR (EC50=0.001 µM).
BMS-986408 binds to the accessory subdomain of the DGKα and DGKζ catalytic domain.
BMS-986408 broadly amplify T cell–mediated tumor immunity and invigorate both PD-1 immune checkpoint and CAR T-cell therapy.

物理化学性质&存储条件

分子量 511.59
分子式 C28H32F3N5O
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-((2S,5R)-2,5-diethyl-4-((S)-1-(4-(trifluoromethyl)phenyl)propyl)piperazin-1-yl)-1-methyl-2-oxo-1,2-dihydroquinazoline-6-carbonitrile

参考文献

1. Wichroski M, et al. Cancer Immunol Res. 2025 Jun 12. doi: 10.1158/2326-6066.CIR-25-0156.

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