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Cat. No.: HY-183643

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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.

For research use only. We do not sell to patients.

Formula: C₂₈H₃₀ClN₇O₃
Molecular Weight:548.04

Storage:

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

RUVBL1/2-IN-1 Chemical Structure

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

All DNA/RNA Synthesis Isoforms :

In Vitro

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.

Cell Viability Assay^[1]

Cell Line:

Ramos human Burkitt lymphoma cells
Concentration:

0-3 μM
Incubation Time:

72 h
Result:

Inhibited Ramos cell viability with an EC₅₀ of 0.009 μM, representing the concentration required to reduce cell viability by 50% relative to untreated controls.

In Vivo

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.

Animal Model:

NOD.CB17-Prkdcscid/NCrCrl NOD-SCID mice (female, 4-5 weeks old, Burkitt lymphoma subcutaneous xenograft model with Ramos cells)^[1]
Dosage:

10 mg/kg (efficacy); 30 mg/kg (intolerability)
Administration:

p.o.; twice daily; 11 days
Result:

Achieved 84% tumor growth inhibition (TGI) at 10 mg/kg.
Caused no body weight loss at 10 mg/kg.
Triggered signs of intolerability starting at 30 mg/kg twice daily.

Chemical Information

Molecular Weight 548.04
Formula C₂₈H₃₀ClN₇O₃
SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage

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

Purity & Documentation

Handling Instructions (2659 KB)

References

[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. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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Biological Activity
- Description
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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RUVBL1/2-IN-1

All DNA/RNA Synthesis Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

RUVBL1/2-IN-1 Related Classifications

HY-183643 Related Classifications