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 K_d 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^[1].

G-quadruplex ligand 6 (C-1305) exists in four protonated forms with distinct spectral characteristics, has three macroscopic pK_a 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.

375.85

C₁₈H₂₂ClN₅O₂

C[NH+](CCCNC1=CCC2N=NN3C4=C(C(C1=C23)=O)C=C(C=C4)O)C.[Cl-]

Room temperature in continental US; may vary elsewhere.

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• [1]. Pakuła J, et al. Reframing Triazoloacridinone C-1305 as a G-Quadruplex Pharmacophore. J Phys Chem B. 2026;130(20):5142-5151.