SKLB-0124
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].
Product Specifications
CAS Number
[3065966-31-3]
UNSPSC
12352005
Target
Apoptosis; Histone Methyltransferase
Related Pathways
Apoptosis; Epigenetics
Field of Research
Cancer
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
Molecular Formula
C32H45N5O2
Molecular Weight
531.73
References & Citations
[1]Yang H, et al. Discovery of a first-in-class degrader for the protein arginine methyltransferase 6 (PRMT6) . Bioorg Chem. 2024 Jul;148:107439.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
PRMT6
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