3065966-31-3
Chemical Structure
SKLB-0124
- CAS No.: 3065966-31-3
- Formula:C32H45N5O2
- Molecular Weight:531.73
IUPAC Name: 4-(2-((3r,5r,7r)-adamantan-1-yl)acetamido)-N-(4-(5-((methyl(2-(methylamino)ethyl)amino)methyl)pyridin-3-yl)phenyl)butanamide
InChIKey: DXVPSWFANZITSW-DFQGNTDCSA-N
SMILES: O=C(NCCCC(NC1=CC=C(C2=CN=CC(CN(C)CCNC)=C2)C=C1)=O)CC34C[C@H](C[C@@H]5C4)C[C@H](C5)C3
Biological Activity: SKLB-0124 is a selective PRMT6 degrader based on a hydrophobic labeling (HyT) method. SKLB-0124 is a selective PRMT6 degrader with DC50s of 15.4 μM and a 16.4 μM in HCC827 and MDA-MB-435 cells. SKLB-0124 does not degrade PRMT1 or PRMT8. SKLB-0124 exhibits an IC50 on PRMT6 of 1.6 μM. SKLB-0124 induces proteasome dependent degradation of PRMT6 and significantly inhibits the proliferation. SKLB-0124 effectively induces apoptosis and cell cycle arrest. SKLB-0124 can be used for the studies of lung cancer and breast cancer[1].
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SKLB-0124 | SKLB-0124 is a selective PRMT6 degrader based on a hydrophobic labeling (HyT) method. SKLB-0124 is a selective PRMT6 degrader with DC50s of 15.4 μM and a 16.4 μM in HCC827 and MDA-MB-435 cells. SKLB-0124 does not degrade PRMT1 or PRMT8. SKLB-0124 exhibits an IC50 on PRMT6 of 1.6 μM. SKLB-0124 induces proteasome dependent degradation of PRMT6 and significantly inhibits the proliferation. SKLB-0124 effectively induces apoptosis and cell cycle arrest. SKLB-0124 can be used for the studies of lung cancer and breast cancer. | |||||||||||||||||||||
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