RUVBL1/2-IN-1 

RUVBL1/2-IN-1 is an orally active RUVBL1/2 complex inhibitor with an EC₅₀ of 0.012 μM against human targets. RUVBL1/2-IN-1 impairs ATPase-related functions, thereby reducing nuclear MYC protein levels, impairing DNA damage response and inhibiting cancer cell proliferation. In a MYC-dependent Burkitt's lymphoma xenograft model, RUVBL1/2-IN-1 effectively inhibits tumor growth and suppresses the activity of RUVBL1^R117H mutant cells. RUVBL1/2-IN-1 has been applied in research related to MYC-dependent Burkitt's lymphoma^[1].

RUVBL1/2-IN-1 (compound 18) (0-10 μM; 72 h) inhibits HCT116 cell viability with an EC₅₀ of 0.020 μM^[1].
RUVBL1/2-IN-1 (compound 18) (0-3 μM; 72 h) inhibits Ramos cell viability with an EC₅₀ of 0.009 μM^[1].
RUVBL1/2-IN-1 (compound 18) (200 nM; 1 h) potently inhibits etoposide-induced p-CHK2 upregulation in HCT116 cells, showing greater potency than CB-6644 (HY-114429)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

RUVBL1/2-IN-1 (compound 18) (10-30 mg/kg; p.o.; twice daily; 11 days) delivers 84% tumor growth inhibition in a MYC-dependent Burkitt lymphoma Ramos xenograft model at a 10 mg/kg twice daily oral dose, with no observed body weight loss, while signs of intolerability emerge at doses starting at 30 mg/kg^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

548.04

C₂₈H₃₀ClN₇O₃

CN(C(C)=C(C1=O)NC(C23CC(CCCC2)(C3)NC(C4=CC(Cl)=NN5C4=NC(C)=C5)=O)=O)N1C6=CC=CC=C6

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Zheng L, et al. Rapid Optimization Enabled by Single-Molecule Tracking: Discovery of a Potent RUVBL1/2 Inhibitor to Evaluate the Targeting of MYC-Driven Cancers. J Med Chem. Published online April 22, 2026.