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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- CAS No.: 3065966-31-3
- 화학식: C32H45N5O2
- 분자량:531.73
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
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All Histone Methyltransferase Isoforms
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Biological Activity
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PRMT6 15.4 nM (DC50) |
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.
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Cell Line:MDA-MB-435 cells and HCC827 cells
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Concentration:10 and 20 μM
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Incubation Time:3 d
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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.
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Cell Line:MDA-MB-435 cells and HCC827 cells
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Concentration:10 and 20 μM
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Incubation Time:6 d
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Result:Induced apoptosis in 78.41% of the HCC827 cells and 90.1% of the MDA-MB-435 cells at 20 μM.
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Cell Line:MDA-MB-435 cells and HCC827 cells
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Concentration:1.25, 2.5, 5, 10 and 20 μM
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Incubation Time:0.5, 1, 3, 5 and 7 d
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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.
| Species | Dose | Route | Tmax | T1/2 | C0 | AUC0-t | AUC0-∞ | MRT |
|---|---|---|---|---|---|---|---|---|
| Rat[1] | 1 mg/kg | i.v. | 0.033 h | 3.12 h | 559 ng/mL | 88.1 ng·h/mL | 113 ng·h/mL | 2.09 h |
Chemical Information
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CAS No. 3065966-31-3
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분자량 531.73
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화학식 C32H45N5O2
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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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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
SKLB-0124 Related Classifications
HY-178114 Related Classifications
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