SKLB06489
SKLB06489 is a selective and orally active inhibitor of type I PRMT enzymes, with IC50 values of 64.55 nM (PRMT1), 4.21 nM (PRMT6), and 51.27 nM (PRMT8). SKLB06489 inhibits cell proliferation, colony formation, DNA replication, and DNA damage repair in cancer cells. SKLB06489 induces G0/G1-phase cell cycle arrest and apoptosis in cancer cells. SKLB06489 enhances intracellular cholesterol efflux via ABCA1 and ABCG1 upregulation, disrupts cholesterol metabolic homeostasis, and suppresses tumor growth in subcutaneous xenograft models. SKLB06489 can be used for the research of triple-negative breast cancer (TNBC).
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- 화학식: C25H33N5O
- 분자량:419.56
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Protocol
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
IC50 & Target
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PRMT1 64.55 nM (IC50) |
PRMT6 4.21 nM (IC50) |
PRMT8 51.27 nM (IC50) |
In Vitro
SKLB06489 (40 μM; 8 h) selectively and stably binds to PRMT1 and PRMT6 in HEK293T cells, enhancing their thermal stability[1].
SKLB06489 (5-7 days) dose-dependently inhibits proliferation of MDA-MB-231, Hs578T, and BT549 TNBC cells with IC50 values in the low micromolar range[1].
SKLB06489 (2.5-20 μM; 12-14 days) dose-dependently inhibits colony formation in MDA-MB-231, Hs578T, and BT549 TNBC cells[1].
SKLB06489 (2.5-10 μM; 6 days) dose-dependently reduces ADMA levels in MDA-MB-231 and Hs578T TNBC cells, indicating inhibition of type I PRMT enzymatic activity in cells[1].
SKLB06489 (5-20 μM; 1-3 days) dose- and time-dependently inhibits DNA replication in MDA-MB-231, Hs578T, and BT549 TNBC cells[1].
SKLB06489 (10 μM; 24 h) impairs DNA damage repair in MDA-MB-231 and Hs578T TNBC cells, with a more pronounced effect than MS023 in Hs578T cells[1].
SKLB06489 (5-20 μM; 24 h) dose-dependently induces G0/G1 phase cell cycle arrest in MDA-MB-231, Hs578T, and BT549 TNBC cells[1].
SKLB06489 (5-20 μM; 72 h) dose-dependently induces apoptosis in MDA-MB-231, Hs578T, and BT549 TNBC cells[1].
SKLB06489 (10 μM; 4 days) upregulates ABCA1 and ABCG1 mRNA expression in MDA-MB-231 and Hs578T TNBC cells[1].
SKLB06489 (5-10 μM; 4 days) dose-dependently enhances cholesterol efflux (increasing medium cholesterol) and reduces intracellular cholesterol in MDA-MB-231 and Hs578T TNBC cells[1].
SKLB06489 (5-10 μM) upregulates ABCG1 protein levels in MDA-MB-231 and Hs578T TNBC 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:2.5 μM, 5 μM, 10 μM
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Incubation Time:6 days
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Result:Dose-dependently reduced ADMA levels without affecting PRMT1 or PRMT6 expression.
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Cell Line:MDA-MB-231, Hs578T, and BT549 cells
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Concentration:5 μM, 10 μM, 20 μM
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Incubation Time:24 h
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Result:Dose-dependently increased the proportion of cells in G0/G1 phase and decreased the proportion in S phase.
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Cell Line:MDA-MB-231, Hs578T, and BT549 cells
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Concentration:5 μM, 10 μM, 20 μM
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Incubation Time:72 h
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Result:Dose-dependently increased the percentage of apoptotic cells (early + late) in MDA-MB-231 (5.9% to 41.8% and 82.9%), Hs578T (20.7% to 68.4% and 79.9%), and BT549 (6.5% to 49.1% and 92.3%) cells at 10 and 20 μM, respectively.
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Cell Line:MDA-MB-231 and Hs578T cells
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Concentration:10 μM
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Incubation Time:4 days
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Result:Significantly upregulated ABCA1 (15.93-fold in MDA-MB-231, 13.90-fold in Hs578T) and ABCG1 (4.64-fold in MDA-MB-231, 3.79-fold in Hs578T) mRNA expression.
Parmacokinetics
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude (female, aged 4-5 weeks, 6-week-old) bearing DA-MB-231 cells[1]
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Dosage:40 mg/kg; 80 mg/kg
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Administration:i.g.; daily; 33 days
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Result:Dose-dependently suppressed tumor growth; had a tumor growth inhibition (TGI) value of 58.4% at 80 mg/kg; reduced tumor weight compared to vehicle control; increased cleaved caspase-3-positive cells; decreased Ki67-positive cells in tumor tissues.
- Somatic Cell Culture
- Breast Cancer Modeling
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Flow cytometric DNA-content cell-cycle staining
- Apoptosis Solutions
- Soft Agar Colony Formation Assay
- MTT Cell Proliferation Assay
- Genotoxicity/Mutagenicity Study
- Annexin V plus membrane-impermeant dye apoptosis staining
- BrdU Incorporation Assay
- CFSE Dye Dilution Proliferation Assay
- Dye-dilution cell tracking and proliferation staining
- Patient-Derived Orthotopic Xenograft (PDOX)
- CCK-8/WST-8 Cell Proliferation Assay
- Protocol for Cell Cycle
- Cell Counting-Based Growth Curve Assay
- Colony Formation (Clonogenic) Assay
- Cell Viability Determination by MTT Colorimetric Assay
- How to Select the Route of Administration for Mammals
- EdU Incorporation Assay (Click Chemistry-Based DNA Synthesis Measurement)
- Ki-67 Immunostaining Proliferation Assay
- PCNA Immunodetection Proliferation Assay
- Protocol for Cell Counting and Cell Density Analysis
- Patient-Derived Xenograft (PDX)
- Splenic/Portal-Vein Liver Metastasis Xenograft
- Subcutaneous Cell-Line-Derived Xenograft
- Orthotopic Cell-Line Xenograft
- Intraperitoneal/Peritoneal Dissemination Xenograft
Chemical Information
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분자량 419.56
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화학식 C25H33N5O
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SMILES
CNCCN(CC1=NNC2=CC=C(C=C21)C3=CC=C(C=C3)NC(C4CCCCC4)=O)C
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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)
SKLB06489 Related Classifications
HY-186045 Related Classifications
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