2. Epigenetics
  3. Histone Methyltransferase
  4. MLL1-IN-1

MLL1-IN-1 是一种具有口服活性的 MLL1 抑制剂，IC50 = 0.043 μM。MLL1-IN-1 诱导 Menin 蛋白降解，抑制白血病细胞增殖。MLL1-IN-1 可在白血病小鼠中消退肿瘤。MLL1-IN-1 可用于 MLL1 相关白血病研究[1]。

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MLL1-IN-1

MLL1-IN-1 Chemical Structure

CAS No. : 3058433-50-1

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MLL1-IN-1 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 ASH1L/KMT2H SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 NSD3/WHSC1L1 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

MLL1-IN-1 is an orally active MLL1 inhibitor with an IC50 of 0.043 μM. MLL1-IN-1 induces Menin protein degradation and inhibits the proliferation of leukemia cells. MLL1-IN-1 can induce tumor regression in leukemia-bearing mice. MLL1-IN-1 is useful for research into MLL1-associated leukemia[1].

体外研究
(In Vitro)

MLL1-IN-1 (7 天) 抑制 MOLM-13、MV-4-11、OCI-AML3 细胞活力，IC50 分别为 0.04、0.035、0.047 μM[1]。

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

MLL1-IN-1 相关抗体:
体内研究
(In Vivo)

MLL1-IN-1 (30-200 mg/kg，p.o.，每日 2 次，14 天) 在 MV-4-11 皮下异种移植小鼠模型中消退肿瘤[1].
MLL1-IN-1 (30-200 mg/kg，p.o.，每日 1 次，21/90 天) 在 MOLM-13 皮下异种移植小鼠模型中消退肿瘤[1].
MLL1-IN-1 (150 mg/kg，p.o.，每日 1 次，21 天) 在 MLL-r AML 病人来源 PDX 小鼠模型中延长生存期[1].

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

Animal Model: Female CB17 SCID mice with MV-4-11 subcutaneous xenograft[1]
Dosage: 30, 100, 200 mg/kg
Administration: p.o., twice daily for 14 days
Result: Reduced tumors by 88%, with a 100% recurrence rate following drug discontinuation at a dose of 30 mg/kg. Reduced tumors by 97%/99%, with no recurrence observed 6 weeks after drug discontinuation at doses of 100/200 mg/kg.
分子量

589.74

Formula

C34H44FN5O3
CAS 号
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

MLL1-IN-1 相关分类

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  • 稀释计算器

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  • 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:

MLL1-IN-13058433-50-1Histone MethyltransferaseMLL1 inhibitorleukemiaMOLM-13 cellsMV-4-11 cellsOCI-AML3 cellsCB17 SCID miceInhibitorinhibitorinhibit

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