2. Epigenetics Apoptosis
  3. Histone Methyltransferase Apoptosis
  4. 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.

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SKLB-0124

SKLB-0124 Chemical Structure

CAS No. : 3065966-31-3

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SKLB-0124 Related Antibodies

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View All Histone Methyltransferase Isoform Specific Products:

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EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D ASH1L/KMT2H SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

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Description

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].

IC50 & Target[1]

PRMT6

15.4 nM (DC50)

In Vitro

SKLB-0124 (1.25-20 μM, 0.5-7 d) exhibits nonacute degradation kinetics, and achieved the degradation of PRMT6 with an appropriate rate in MDA-MB-435 cells and HCC827 cells through the cellular ubiquitin proteasome system (UPS) pathway and does not produce the hook effect[1].
SKLB-0124 (0-10 μM, 6 d) inhibits cell proliferation with IC50 of 6.66 and 5.68 μM against HCC827 and MDA-MB-435 cells[1].
SKLB-0124 (10-20 μM, 3 d) causes G0/G1 phase arrest in a concentration-dependent manner in MDA-MB-435 cells and HCC827 cells[1].
SKLB-0124 (15-90 μM, 9 d) has relatively low toxicity towards normal HEK293 and HEK293T cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

SKLB-0124 Related Antibodies

Cell Cycle Analysis[1]

Cell Line: MDA-MB-435 cells and HCC827 cells
Concentration: 10 and 20 μM
Incubation Time: 3 d
Result: Caused the G0/G1 arrest pattern in a concentration dependent manner, with a concomitant decrease of cells in other phases of the cell cycle.

Apoptosis Analysis[1]

Cell Line: MDA-MB-435 cells and HCC827 cells
Concentration: 10 and 20 μM
Incubation Time: 6 d
Result: Induced apoptosis in 78.41% of the HCC827 cells and 90.1% of the MDA-MB-435 cells at 20 μM.

Western Blot Analysis[1]

Cell Line: MDA-MB-435 cells and HCC827 cells
Concentration: 1.25, 2.5, 5, 10 and 20 μM
Incubation Time: 0.5, 1, 3, 5 and 7 d
Result: Significantly and dose-dependently reduced the expression of PRMT6 protein.
Observed that after 5 days of PRMT6 degradation, there was a significant degradation after 7 days.
Significantly degraded PRMT6 but did not degrade PRMT1 or PRMT8.
Molecular Weight

531.73

Formula

C32H45N5O2
CAS No.
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
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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SKLB-0124 Related Classifications

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Keywords:

SKLB-01243065966-31-3SKLB0124SKLB 0124Histone MethyltransferaseApoptosisAnticancer agentsHistone methylationHydrophobic tagging methodPRMT6Protein degraderInhibitorinhibitorinhibit

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