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

Curated Selection

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