t863

T-863(DGAT-1 inhibitor) is an orally active, selective and potent DGAT1 (Acyl-CoA:diacylglycerol acyltransferase 1) inhibitor that interacts with the acyl-CoA binding site of DGAT1, and inhibits triacylglycerol synthesis in cells. IC50 value: Target: DGAT1 T863 (DGAT-3) causes weight loss, reduction in serum and liver triglycerides, and improved insulin sensitivity in obese mice.

CFT8634 is an orally active and selective degrader targeting BRD9, with effects on the proliferation of SMARCB1-deficient cancer cell lines. CFT8634 induces the formation of a ternary complex with BRD9 and E3 ligase, inducing BRD9 ubiquitination and subsequent degradation by the proteasome.

(S,R)-CFT8634 is a selective and orally active BRD9 protein degrader with potential for researching BRD9-mediated disorders, such as abnormal cellular proliferation [1].