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Cat. No.: HY-190463

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OICR18704

OICR18704 is a selective, orally active, allosteric ClpP inhibitor with an IC₅₀ of 13.7 nM against hClpP. OICR18704 does not inhibit bacterial ClpP homologs. OICR18704 exerts anticancer effects on leukemia in a ClpP-dependent manner. OICR18704 can be used for research on acute myeloid leukemia.

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

Formula: C₂₄H₂₀ClF₃N₆O
Molecular Weight:500.90

Storage:

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

Data Sheet (283 KB)

OICR18704 Chemical Structure

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Use of MCE Products

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

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

Description

In Vitro

Anti-cancerProtein/Amino Acid MetabolismOthers

Anti-cancer

OICR18704 (120 h) reduces KOPN8 leukemia cell viability in a ClpP-dependent manner^[1].

Protein/Amino Acid Metabolism

OICR18704 (15-90 min) inhibits the Ac-WLA-AMC peptidase activity of hClpP with an IC₅₀ of 13.7 nM^[1].
OICR18704 (3 min) binds to hClpP in a cell-free DSF assay with an EC₅₀ of 0.49 µM^[1].
OICR18704 is more selective for hClpP than for bacterial ClpP and 63 proteases, and shows minimal binding to kinases except PRKCI^[1].

Others

OICR18704 (5 µM; 120 min) is highly permeable across Caco-2 monolayer cells with no efflux^[1].

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

Cell Viability Assay^[1]

Cell Line:

KOPN8 cells
Concentration:

increasing concentrations
Incubation Time:

120 h
Result:

Control shRNA KOPN8 cells were sensitive, whereas ClpP-depleted KOPN8 cells showed no additional loss of viability.

Parmacokinetics

Species	Dose	Route	Bioavailability	T_1/2	V_ss	Clearance (CL)	AUC_last
Mice^[1]	2 mg/kg	i.v.	/	48 h	0.16 L/kg	0.04 mL/min/kg	0.25 × 10^6 ng·h/mL
Mice^[1]	10 mg/kg	p.o.	88 %	/	/	/	/

In Vivo

Anti-cancer

OICR18704 (100 mg/kg; p.o.; 5 or 7 days until endpoint) reduces KOPN8 leukemia engraftment in both injected and non-injected femurs in NS-GF mice^[1].
OICR18704 (100 mg/kg; p.o.; 5 or 7 days until endpoint) delays OCI-AML2 tumor growth and reduces tumor weight in SCID mice^[1].

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

Animal Model:

NOD/SCID-GF (NS-GF; female, 8-10 weeks old)^[1]
Dosage:

100 mg/kg
Administration:

p.o. (oral gavage); 5 or 7 days until endpoint
Result:

At day 21, treated mice had 7.5% CD19+ cells in the injected right femur and 5.2% CD19+ cells in the non-injected left femur.

Animal Model:

SCID (male, 8-10 weeks old)^[1]
Dosage:

100 mg/kg
Administration:

p.o. (oral gavage); 5 or 7 days until endpoint
Result:

Delayed tumor growth.
At day 21, tumor weight in treated mice was 0.48 g.

Chemical Information

Molecular Weight 500.90
Formula C₂₄H₂₀ClF₃N₆O
SMILES

CC(N1C(C2=C(N=C1CN3CCN(CC3)C4=CC(C(F)(F)F)=C(C=C4)C#N)C=C(C=C2)Cl)=O)C#N
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (283 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Goncalves M M, et al. Allosteric inhibition of human mitochondrial ClpP by hijacking the dordaviprone (ONC201) binding site[J]. Nature Communications, 2026.

Calculators

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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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