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首页-抗体药物偶连体和PROTACs-PROTAC-KMG-1068
KMG-1068

Chemical Structure : KMG-1068

CAS No.:

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KMG-1068 (KMG1068)

货号: PC-24420Not For Human Use, Lab Use Only.

KMG-1068 is a selective GSPT1/2-targeting molecular glue degrader, binds CRBN through a non-IMiD mechanism, induces proteasomal degradation of GSPT1/2 with DC50 of 126.7 nM for GSPT1 and 42.2 nM for GSPT2 in Jurkat cells.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

KMG-1068 is a selective GSPT1/2-targeting molecular glue degrader, binds CRBN through a non-IMiD mechanism, induces proteasomal degradation of GSPT1/2 with DC50 of 126.7 nM for GSPT1 and 42.2 nM for GSPT2 in Jurkat cells.
KMG-1068 potently inhibits cell proliferation with GI50 value of0.8 uM in HEK293T cells and 0.2 uM in Jurkat cells.
KMG-1068 forms a ternary complex with the CRBN and GSPT1/2.
KMG-1068 binds to the IMiD binding site of CRBN, similar to pomalidomide, and effectively induces the degradation of GSPT1 and GSPT2.
KMG-1068 selectively induces proteasomal degradation of GSPT1 and GSPT2 via a CRL4-dependent mechanism.

物理化学性质&存储条件

分子量 426.49
分子式 C21H22N4O4S
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

methyl 2-(2-(4,5-dimethyl-6-oxopyrimidin-1(6H)-yl)acetamido)-5-phenethylthiazole-4-carboxylate

参考文献

1. Seulki Park, et al. Eur J Med Chem. 2025 Apr 15:291:117642.

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