1. Epigenetics
  2. Histone Methyltransferase
  3. DDO-2093

DDO-2093 is a potent MLL1-WDR5 protein-protein interaction inhibitor (IC50=8.6 nM; Kd=11.6 nM) with antitumor activity. DDO-2093 selectively inhibits the catalytic activity of MLL complex.

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (DDO-2093 dihydrochloride) usually boasts enhanced water solubility and stability.

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

DDO-2093 Chemical Structure

DDO-2093 Chemical Structure

CAS No. : 2250024-74-7

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Description

DDO-2093 is a potent MLL1-WDR5 protein-protein interaction inhibitor (IC50=8.6 nM; Kd=11.6 nM) with antitumor activity. DDO-2093 selectively inhibits the catalytic activity of MLL complex[1].

Cellular Effect
Cell Line Type Value Description References
HUVEC IC50
> 100 μM
Compound: 24; DDO-2093
Cytotoxicity against HUVEC assessed as reduction in cell viability after 24 hrs by MTT assay
Cytotoxicity against HUVEC assessed as reduction in cell viability after 24 hrs by MTT assay
[PMID: 34225179]
MOLM-13 GI50
9.9 μM
Compound: DDO-2093
Antiproliferative activity against human MOLM-13 cells assessed as inhibition of cell proliferation measured after 5 days by ATPlite assay
Antiproliferative activity against human MOLM-13 cells assessed as inhibition of cell proliferation measured after 5 days by ATPlite assay
[PMID: 34283608]
MOLM-13 IC50
9.9 μM
Compound: 24; DDO-2093
Antiproliferative activity against human MOLM-13 cells harboring MLL-AF9 fusion protein assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
Antiproliferative activity against human MOLM-13 cells harboring MLL-AF9 fusion protein assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
[PMID: 34225179]
MV4-11 GI50
8 μM
Compound: DDO-2093
Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell proliferation measured after 5 days by ATPlite assay
Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell proliferation measured after 5 days by ATPlite assay
[PMID: 34283608]
MV4-11 IC50
8 μM
Compound: 24; DDO-2093
Antiproliferative activity against human MV4-11 cells harboring MLL-AF4 fusion protein assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
Antiproliferative activity against human MV4-11 cells harboring MLL-AF4 fusion protein assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
[PMID: 34225179]
MV4-11 IC50
8000 nM
Compound: DDO-2093
Anti-proliferative activity against human MV4-11 cells harboring MLL-AF4 fusion protein assessed as inhibition of cell viability treated for 72 hrs by CCK-8 assay
Anti-proliferative activity against human MV4-11 cells harboring MLL-AF4 fusion protein assessed as inhibition of cell viability treated for 72 hrs by CCK-8 assay
[PMID: 35436124]
In Vitro

DDO-2093 (5 μM; pretreated 7 days) inhibits MLL-fusion protein dependent genes expression (HOXA9 and Meis1)[1].

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

Western Blot Analysis[1]

Cell Line: MV4-11 cells
Concentration: 1, 2.5, 5, and 10 μM
Incubation Time: 7 days
Result: Dose-dependently reduced the mono-, di-, and trimethylation of H3K4.
In Vivo

DDO-2093 (20-80 mg/kg; i.p.; every other day for 21 days) significantly suppresses the tumor size and weight in a dose-dependent manner[1].

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

Animal Model: Female nude mice (MV4-11 human leukemia cancer xenografts)[1]
Dosage: 20 mg/kg, 40 mg/kg and 80 mg/kg
Administration: Intraperitoneal injection; every other day for 21 days
Result: Had the tumor volume growth inhibition (GI) values were calculated to be 13.7%, 37.6% and 63.9% with doses of 20 mg/kg, 40 mg/kg and 80 mg/kg, respectively.
Molecular Weight

614.11

Formula

C29H37ClFN9O3

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CN(C2=CC=C(N3CCN(C)CC3)C(NC(C4=CC(N)=C(F)C(C)=C4Cl)=O)=C2)N=N1)NCCCN5CCOCC5

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
References
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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.

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Product Name:
DDO-2093
Cat. No.:
HY-132233
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