SA-VAT79531
SA-VA, an intracellular self-assembled PROTAC featuring azide and alkyne groups, selectively degrades VEGFR-2 and EphB4 proteins within U87 cells. This compound undergoes in situ conversion to active PROTAC via a copper-catalyzed click reaction utilizing endogenous copper present in tumor tissues. Additionally, SA-VA induces apoptosis and arrests cell cycle progression in the S phase [1].
PROTAC NSD3 degrader-1T81377
PROTAC NSD3 degrader-1 (compound 56) is a targeted degradation agent for the Nuclear receptor binding SET domain protein NSD3. It effectively induces the degradation of NSD3 in NCI-H1703 and A549 lung cancer cell lines, with DC50 values of 1.43 and 0.94 μM, respectively. Additionally, it hinders H3K36 methylation, triggers apoptosis, and arrests the cell cycle. Furthermore, PROTAC NSD3 degrader-1 diminishes the expression of NSD3-related genes, including CDC25A, ALDH1A1, and IGFBP.
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FMF-06-098-1T823852769753-07-1
FMF-06-098-1 is a multitargeted depressant capable of promoting the degradation of a wide array of kinases, including AAK1, ABL2, AURKA, AURKB, BUB1B, CDC7, CDK1, CDK12, CDK13, CDK2, CDK4, CDK6, CDK7, CDK9, CHEK1, CSNK1D, EPHA1, PAK, FGFR1, GAK, IRAK4, ITK, LIMK2, MAP4K2, MAP4K3, MAPK6, MAPK7, MARK4, MELK, PKN3, PLK4, PRKAA1, PTK2, PTK6, RPS6KA4, SGK2, STK35, TNK2, UHMK1, ULK1, and WEE1 [1].
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