G-quadruplex ligand 6
G-quadruplex ligand 6 is a G-quadruplex ligand targeting the c-MYC promoter with anti-tumor activity. G-quadruplex ligand 6 forms a non-covalent complex with Pu22, a G-quadruplex model of the c-MYC promoter, with a microscopic dissociation constant Kd of 0.202 μM. G-quadruplex ligand 6 selectively inhibits tumor cell proliferation, blocks the binding of transcription factors by stabilizing the G-quadruplex in the c-MYC promoter, and thereby regulates the expression of proto-oncogenes. G-quadruplex ligand 6 can be used in the research of pancreatic cancer, non-small cell lung cancer, colorectal cancer, and triple-negative breast cancer.
For research use only. We do not sell to patients.
- Formula: C18H22ClN5O2
- Molecular Weight:375.85
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Storage:
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
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
G-quadruplex ligand 6 (C-1305) exists in four protonated forms with distinct spectral characteristics, has three macroscopic pKa values of 1.59, 7.87 and 9.49, and maintains a stable dominant protonated state under NMR and near-physiological pH conditions[1].
G-quadruplex ligand 6 forms a Pu22:C-1305 complex with the c-MYC promoter G-quadruplex model DNA Pu22 at a binding ratio of 1:2, with submicromolar-level affinity. The microscopic dissociation constants at the two binding sites of Pu22 are both 0.202 μM[1].
G-quadruplex ligand 6 (72 h) potently inhibits the viability of Panc-1, MIA PaCa-2, H460, A549, HCT116 and MDA-MB-231 cancer cell lines, with IC50 values ranging from 1.09 μM to 2.15 μM; in contrast, it exhibits significantly lower toxicity against human normal cell lines, with IC50 values of 7.1-9.0 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Molecular Weight 375.85
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Formula C18H22ClN5O2
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SMILES
C[NH+](CCCNC1=CCC2N=NN3C4=C(C(C1=C23)=O)C=C(C=C4)O)C.[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)
G-quadruplex ligand 6 Related Classifications
HY-183984 Related Classifications
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