G4/HDAC-IN-1
G4/HDAC-IN-1 (compound a6) is a G4/HDAC dual-targeting compound. G4/HDAC-IN-1 inhibits intracellular HDAC activity with an IC50 value of 1.1 μM, and induces G4 formation. G4/HDAC-IN-1 inhibits TNBC proliferation and tumor growth in TNBC xenograft model. G4/HDAC-IN-1 can be used for the research of cancer.
For research use only. We do not sell to patients.
- CAS No.: 3031784-60-5
- Formula: C36H49ClFN7O4
- Molecular Weight:698.27
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Storage:
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
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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HDAC8 0.03 μM (IC50) |
HDAC6 0.65 μM (IC50) |
HDAC1 1.26 μM (IC50) |
HDAC11 1.38 μM (IC50) |
HDAC4 2.64 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| BT-549 | IC50 |
6.5 μM
Compound: a6
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Cytotoxicity against human BT-549 cells harboring wild type BRCA1 and wild type BRCA2 assessed as reduction in cell viability
Cytotoxicity against human BT-549 cells harboring wild type BRCA1 and wild type BRCA2 assessed as reduction in cell viability
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[PMID: 36053318] |
| MDA-MB-231 | IC50 |
4.1 μM
Compound: a6
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Cytotoxicity against human MDA-MB-231 cells harboring wild type BRCA1 and wild BRCA2 assessed as reduction in cell viability
Cytotoxicity against human MDA-MB-231 cells harboring wild type BRCA1 and wild BRCA2 assessed as reduction in cell viability
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[PMID: 36053318] |
| MDA-MB-468 | IC50 |
3.3 μM
Compound: a6
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Cytotoxicity against human MDA-MB-468 cells harboring wild type BRCA1 and BRCA2 mutant reduction in assessed as cell viability
Cytotoxicity against human MDA-MB-468 cells harboring wild type BRCA1 and BRCA2 mutant reduction in assessed as cell viability
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[PMID: 36053318] |
| SUM-159-PT | IC50 |
7.4 μM
Compound: a6
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Cytotoxicity against human SUM159PT cells harboring wild type BRCA1 and wild type BRCA2 assessed as reduction in cell viability
Cytotoxicity against human SUM159PT cells harboring wild type BRCA1 and wild type BRCA2 assessed as reduction in cell viability
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[PMID: 36053318] |
G4/HDAC-IN-1 (0-10 μM; 1.5 h) shows HDAC inhibitory activity with an IC50 of 1.9 μM by determining nuclear extract and exhibits inhibitory activity on intracellular HDAC activity in MDA-MB-231 cells with an IC50 value of 1.1 μM[1]. G4/HDAC-IN-1 (0-50 μM) shows G4 binding activity with an IC50 of 0.4 μM[1]. G4/HDAC-IN-1 (0-10 μM; 1.5 h) inhibits HDAC1, HDAC8, HDAC4, HDAC6 and HDAC11 activities with IC50s of 1.26, 0.03, 2.64, 0.65 and 1.38 μM, respectively[1]. G4/HDAC-IN-1 (0-50 μM) binds with Pu22, HRAS and HTG21 sequences with KD values of 1.8, 3.6 and ＞10 μM, respectively[1]. G4/HDAC-IN-1 (1.25-5.0 μM; 48 h) dose-dependently increases DNA G4 level[1]. G4/HDAC-IN-1 (0-50 μM; overnight) inhibits cytotoxic activities of TNBC cell lines[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 cell line
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Concentration:1.25, 2.5 and 5.0 μM
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Incubation Time:48 hours
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Result:Increased the acetylation levels of HDAC1/2/3/8 substrate acetyl histone H3 (ac-H3), acetyl-histone H4 (ac-H4), and the HDAC6 substrate acetyl-α-tubulin (ac-Tub).
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Cell Line:TNBC cell lines
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Concentration:0-50 μM
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Incubation Time:Overnight
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Result:Showed cytotoxic activities to MDA-MB-231, MDA-MB-468, SUM159PT and BT549 with IC50s of 4.1, 3.3, 7.4 and 6.5 μM, respectively.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Five week-old female BALB/C mice with TNBC xenografts[1]
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Dosage:2.5 mg/kg
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Administration:Intraperitoneal injection; 2.5 mg/kg once daily; for 31 days
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Result:Showed well tolerance in vivo and exhibited potent antitumor activity.
Chemical Information
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CAS No. 3031784-60-5
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Molecular Weight 698.27
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Formula C36H49ClFN7O4
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SMILES
O=C(NCCCN(C)C)C1=CC=C(/C=C2CCN3C\2=NC4=C(C=C(F)C(N5CCN(CCCCCCCC(NO)=O)CC5)=C4)C3=O)C=C1.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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
G4/HDAC-IN-1 Related Classifications
HY-151263 Related Classifications
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