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SKLB-0124 is a potent degrader of PRMT6, exhibiting DC50 values of 15.4 μM in HCC827 cells and 16.4 μM in MDA-MB-435 cells. It does not degrade PRMT1 or PRMT8. SKLB-0124 has an IC50 value of 1.6 μM for PRMT6. It induces proteasome-dependent degradation of PRMT6 and significantly inhibits cell proliferation. Additionally, SKLB-0124 effectively induces apoptosis and cell cycle arrest, making it suitable for research in lung cancer and breast cancer.
| Pack Size | Price | USA Stock | Global Stock | Quantity |
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| 10 mg | Inquiry | Inquiry | Inquiry | |
| 50 mg | Inquiry | Inquiry | Inquiry |
| Description | SKLB-0124 is a potent degrader of PRMT6, exhibiting DC50 values of 15.4 μM in HCC827 cells and 16.4 μM in MDA-MB-435 cells. It does not degrade PRMT1 or PRMT8. SKLB-0124 has an IC50 value of 1.6 μM for PRMT6. It induces proteasome-dependent degradation of PRMT6 and significantly inhibits cell proliferation. Additionally, SKLB-0124 effectively induces apoptosis and cell cycle arrest, making it suitable for research in lung cancer and breast cancer. |
| Targets&IC50 | PRMT6:15.4 nM (DC50) |
| In vitro | SKLB-0124 demonstrates non-acute degradation kinetics by degrading PRMT6 at an appropriate rate via the ubiquitin-proteasome system (UPS) pathway in MDA-MB-435 and HCC827 cells (1.25-20 μM, 0.5-7 d), without inducing a hook effect. It inhibits cell proliferation, with IC50 values of 6.66 μM and 5.68 μM for HCC827 and MDA-MB-435 cells, respectively, when used at concentrations of 0-10 μM for 6 days. At concentrations of 10-20 μM for 3 days, SKLB-0124 causes G0/G1 phase arrest in MDA-MB-435 and HCC827 cells in a concentration-dependent manner. Additionally, SKLB-0124 exhibits low toxicity towards normal HEK293 and HEK293T cells at concentrations ranging from 15-90 μM over 9 days. |
| Molecular Weight | 531.75 |
| Formula | C32H45N5O2 |
| Cas No. | 3065966-31-3 |
| Smiles | O=C(NC1=CC=C(C=C1)C=2C=NC=C(C2)CN(C)CCNC)CCCNC(=O)CC34CC5CC(CC(C5)C3)C4 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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