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

DDO-2093 是一种有效的 MLL1 和 WDR5 蛋白-蛋白相互作用抑制剂 (IC50=8.6 nM; Kd=11.6 nM)，具有抗肿瘤活性。DDO-2093 选择性抑制 MLL 复合物的催化活性。

在相同的摩尔浓度下，化合物盐形式与游离形式有相同的生物活性，但盐形式 DDO-2093 dihydrochloride 通常具有更好的水溶性和稳定性。

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DDO-2093 Chemical Structure

DDO-2093 Chemical Structure

CAS No. : 2250024-74-7

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DDO-2093 的其他形式现货产品:

Customer Review

Other Forms of DDO-2093:

DDO-2093 相关抗体

Top Publications Citing Use of Products

查看 Histone Methyltransferase 亚型特异性产品:

查看所有亚型
EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

细胞效力
(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]
体外研究
(In Vitro)

DDO-2093 (5 μM；预处理 7 天) 抑制 MLL 融合蛋白依赖性基因表达 (HOXA9 和 Meis1)[1]。

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

DDO-2093 相关抗体:

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.
体内研究
(In Vivo)

DDO-2093 (20-80 mg/kg；腹腔注射；每隔一天，持续 21 天) 以剂量依赖性方式显著抑制肿瘤大小和重量[1]。

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.
分子量

614.11

Formula

C29H37ClFN9O3
CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

DDO-2093 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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:

DDO-20932250024-74-7DDO2093DDO 2093Histone MethyltransferaseMLL1WDR5antitumorcatalyticcomplexMV4-11leukemiacancerInhibitorinhibitorinhibit

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目录号：
HY-132233
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