Chemical Structure : KMG-1068
CAS No.:
KMG-1068
(KMG1068)
Catalog No.: 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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426.49
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Formula
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C21H22N4O4S
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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methyl 2-(2-(4,5-dimethyl-6-oxopyrimidin-1(6H)-yl)acetamido)-5-phenethylthiazole-4-carboxylate
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References
1. Seulki Park, et al. Eur J Med Chem. 2025 Apr 15:291:117642.
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