SKLB06329
SKLB06329 is a potent selective Type I PRMTs inhibitor. SKLB06329 shows good selectivity for PRMT6 (IC50 = 3.86 nM) over Type II/III PRMTs (PRMT5/7) and shows no significant inhibition against various lysine methyltransferases (PKMTs). SKLB06329 significantly inhibits the proliferation of triple-negative breast cancer (TNBC) cells, induces apoptosis, and suppresses the expression of asymmetric dimethylarginine (ADMA) within cells. SKLB06329 can be used for triple-negative breast cancer research.
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- 화학식: C20H25N5O2S
- 분자량:399.51
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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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- References
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Help & FAQs
All Histone Methyltransferase Isoforms
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Biological Activity
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PRMT6 3.86 nM (IC50) |
SKLB06329 (compound B9) (6 days) inhibits the proliferation of TNBC cells, with IC50 values of 29.94 μM (MDA-MB-231) and 3.93 μM (Hs578T), with efficacy comparable to MS023 (HY-19615)[1].
SKLB06329 forms hydrogen bonds with several amino acids in PRMT1, including Glu65, Met164, and Tyr170, and thus it potently inhibits type I PRMTs[1].
SKLB06329 (5-40 μM) significantly inhibits colony formation in MDA-MB-231 and Hs578T cells, with reduction in colony numbers and decreased cell density per colony even at 5 μM[1].
SKLB06329 (10-80 μM, 6 days) potently induces apoptosis, and inhibits ADMA expression in a concentration-dependent manner in TNBC (MDA-MB-231 and Hs578T) cells, indicating it inhibits the methylation function of type I PRMTs intracellularly[1].
SKLB06329 (0-80 μM, 6 days) exhibits a PRMT1-dependent anti-proliferative effect in MDA-MB-231 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-231 and Hs578T cells
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Concentration:10, 20, 40 and 80 μM
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Incubation Time:6 days
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Result:Induced apoptosis of MDA-MB-231 and Hs578T cells.
The apoptosis inducing effect was more pronounced in Hs578T cells.
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Cell Line:MDA-MB-231 and Hs578T cells
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Concentration:10, 20, 40 and 80 μM
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Incubation Time:6 days
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Result:Significantly reduced ADMA expression compared with that in the control group.
Reduced ADMA expression in a concentration-dependent manner.
Significantly reduced levels of H4R3me2a and H3R2me2a in MDA-MB-231 and Hs578T cells.
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Cell Line:PRMT1-knockdown (shPRMT1) MDA-MB-231 cells
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Concentration:0, 20, 40 and 80 μM
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Incubation Time:6 days
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Result:Showed a significant sensitivity decrease in PRMT1-knockdown (shPRMT1) MDA-MB-231 cells compared to the control group.
| Species | Dose | Route | T1/2 | Cmax | AUC0-t | AUC0-∞ | CL |
|---|---|---|---|---|---|---|---|
| Mice[1] | 2 mg/kg | i.v. | 2.91 h | 6290 ng/mL | 2057 ng·h/mL | 2092 ng·h/mL | 485 mL/h/kg |
Chemical Information
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분자량 399.51
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화학식 C20H25N5O2S
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SMILES
CN(CC1=NNC2=CC=C(C=C21)C3=CC=C(C=C3)NS(=O)(C4CC4)=O)CCN
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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)
SKLB06329 Related Classifications
HY-178274 Related Classifications
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