TNG961 (TNG-961)

Chemical Structure : TNG961

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货号: PC-26588Not For Human Use, Lab Use Only.

TNG961 (TNG-961) is a potent, selective and oral CRBN-dependent HBS1L (GSPT3) molecular glue degrader with DC50 of 7 nM and Dmax of 98%, does not affect closely related GSPT1 protein, disrupts the HBS1L/PELO complex.

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生物&药学活性

TNG961 (TNG-961) is a potent, selective and oral CRBN-dependent HBS1L (GSPT3) molecular glue degrader with DC50 of 7 nM and Dmax of 98%, does not affect closely related GSPT1 protein, disrupts the HBS1L/PELO complex.
TNG961 selectively promotes ternary complex formation between Cullin 4A (Cul4A)-RING-box protein 1 (Rbx1)-DNA damage-binding protein (DDB1)-CRBN and HBS1L in a dose-dependent manner with AC50 of 14.7 nM, compared with an AC50 value > 10 µM for GSPT1.
TNG961 induces proximal association of HBS1L with a functional CRBN E3 ligase complex, with high selectivity over GSPT1.
TNG961 promotes ATP-dependent poly-ubiquitination of HBS1L, but not GSPT1.
TNG961 induces CRBN-dependent endogenous HBS1L degradation with proteome wide selectivity.
TNG961 inhibits viability of FOCAD-negative NCIH1755 cells with a potency of 100 nM, while does not affect FOCAD-reconstituted cells up to 10 uM.
TNG961 induces translational arrest and activation of the unfolded protein response (UPR) in FOCAD-negative, but not FOCAD-positive cells.
TNG961 induces tumor regressions across multiple FOCAD-negative xenograft models from diverse histologies and retained activity in tumors progressing on PRMT5 inhibitor treatment.

物理化学性质&存储条件

分子量	539.57
分子式	C28H24F3N3O3S
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	(R)-1-(6-(2,6-dioxopiperidin-3-yl)naphthalen-1-yl)-3-(2-(6-(trifluoromethyl)benzo[b]thiophen-2-yl)propan-2-yl)urea

参考文献

1. Nicholson HE, et al. Cancer Discov. 2026 Apr 19. doi: 10.1158/2159-8290.CD-26-0040.

TNG961 (TNG-961)

生物&药学活性

物理化学性质&存储条件

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TNG961 (TNG-961)

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