hDHODH-IN-11

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hDHODH-IN-11 is a potent human dihydroorotate dehydrogenase (hDHODH) inhibitor with an IC₅₀ value of 7.2 nM. hDHODH-IN-11 has low cytotoxicity. hDHODH-IN-11 can be used in research of acute myeloid leukemia (AML).

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

hDHODH-IN-11 Chemical Structure

CAS No. : 2396653-34-0

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Description

IC₅₀ & Target

IC50: 7.2 nM (hDHODH)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
THP-1	EC₅₀	110 nM Compound: 4	Induction of apoptosis in human THP-1 cells measured after 3 days by Annexin-V-FITC staining based FACS analysis Induction of apoptosis in human THP-1 cells measured after 3 days by Annexin-V-FITC staining based FACS analysis	[PMID: 36162075]
THP-1	EC₅₀	74 nM Compound: 4	Induction of cell differentiation in human THP-1 cells measured for 2 days by flow cytometric analysis Induction of cell differentiation in human THP-1 cells measured for 2 days by flow cytometric analysis	[PMID: 36162075]
U-937	EC₅₀	452 nM Compound: 4	Induction of apoptosis in human U-937 cells measured after 3 days by Annexin-V-FITC staining based FACS analysis Induction of apoptosis in human U-937 cells measured after 3 days by Annexin-V-FITC staining based FACS analysis	[PMID: 36162075]
U-937	EC₅₀	61 nM Compound: 4	Induction of cell differentiation in human U-937 cells measured for 2 days by flow cytometric analysis Induction of cell differentiation in human U-937 cells measured for 2 days by flow cytometric analysis	[PMID: 36162075]

In Vitro

hDHODH-IN-11 (0.1 and 1 μM; 72 h; THP1 and U937 cells) has low cytotoxicity, pro-apoptotic and pro-differentiating abilities^[1].
hDHODH-IN-11 (0.1 μM; 72 h; THP1 and MV4-11 cells) with Dipyridamole (HY-B0312) results in synergistic effect and demonstrates a good pro-apoptotic activity^[1].

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

In Vivo

hDHODH-IN-11 (20 mg/kg; i.p.; daily, for 13 d; Balb/c mice with AML xenografts) reduces the leukemic burden and tumor weight^[1].

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

Animal Model:	Balb/c mice with AML xenografts^[1]
Dosage:	20 mg/kg
Administration:	Intraperitoneal injection; daily, for 13 days
Result:	Reduced the leukemic burden and tumor weight.

Molecular Weight

401.46

Formula

C₂₄H₂₃N₃O₃

CAS No.

2396653-34-0

SMILES

O=C(C1=C2C=CC=CN2N=C1O)NC3=CC(C)=C(OC4=CC=CC=C4)C=C3C(C)C

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]. Sainas S, et, al. Targeting Acute Myelogenous Leukemia Using Potent Human Dihydroorotate Dehydrogenase Inhibitors Based on the 2-Hydroxypyrazolo[1,5-a]pyridine Scaffold: SAR of the Aryloxyaryl Moiety. J Med Chem. 2022 Oct 13;65(19):12701-12724.

hDHODH-IN-11 Related Classifications

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The dilution calculator equation

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This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

hDHODH-IN-112396653-34-0Dihydroorotate DehydrogenaseDHODHlow cytotoxicityacute myeloid leukemiaTHP1U937DipyridamoleInhibitorinhibitorinhibit

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