SETDB1-IN-1
SETDB1-IN-1 is a SETDB1 inhibitor with an IC50 of 16 μM. SETDB1-IN-1 inhibits histone methyltransferase) activity via SAM-competitive and peptide-dependent mechanisms. SETDB1-IN-1 is applicable to research related to melanoma, lung cancer, liver cancer, breast cancer and prostate cancer.
For research use only. We do not sell to patients.
- CAS No.: 2585194-96-1
- Formula: C12H18ClFN6O2S
- Molecular Weight:364.83
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Histone Methyltransferase Isoforms
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Biological Activity
Description
In Vitro
SETDB1-IN-1 (Compound 7) exhibits limited selectivity in a panel of 16 purified methyltransferases, and shows potent inhibitory activity against SETDB1, SUV39H1, SUV39H2, PRMT7 and PRMT1[1].
SETDB1-IN-1 is a peptide-dependent, SAM-competitive inhibitor of purified recombinant SETDB1 (570-1291)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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CAS No. 2585194-96-1
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Molecular Weight 364.83
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Formula C12H18ClFN6O2S
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SMILES
NC1=NC=NC2=C1N=CN2[C@H]3[C@H](F)[C@H](O)[C@@H](CSCCN)O3.Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Liver Cancer Modeling
Liver cancer can be classified into primary liver cancer and secondary liver cancer. Secondary liver cancer is the metastatic liver cancer. Primary liver cancer includes hepatocellular carcinoma (HCC), intrahepatic cholangiocarcinoma (ICC) and fibrolamellar HCC, of which HCC is the most common form, accounting for approximately 90% of primary liver cancers[1]. HCC mouse models include chemical agent-induced models, transplanted tumor models, and genetic engineered models.
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Breast Cancer Modeling
Breast cancer is a heterogeneous cancer, and it has been distinguished into four subtypes: luminal A, luminal B, HER2-positive and basal-like. Molecular mutations, epigenetic alterations, hormone exposure and immune microenvironment are related to the progression of breast cancer.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)