2. Epigenetics Apoptosis
  3. Histone Methyltransferase WDR5 Apoptosis Caspase
  4. HLC40

HLC40 是一种 MLL1 组蛋白甲基转移酶 (histone methyltransferase) 抑制剂，通过结合 WDR5 发挥作用，其 IC50 值为 0.82 μM。HLC40 可抑制癌细胞增殖、诱导细胞凋亡 (apoptosis) 并上调活化的 caspase-3 水平。HLC40 在小鼠 AML 异种移植模型中展现出抗肿瘤活性。

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HLC40

HLC40 Chemical Structure

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HLC40 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

查看 Caspase 亚型特异性产品:

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

HLC40 is a MLL1 histone methyltransferase inhibitor with an IC50 of 0.82 μM by binding to WDR5. HLC40 inhibits proliferation of cancer cells, induces apoptosis and upregulates cleaved caspase-3 levels. HLC40 exhibits antitumor efficacy in a murine AML xenograft model[1].

IC50 & Target[1]

Caspase 3

 

体外研究
(In Vitro)

HLC40 在体外无细胞生化实验中可强效抑制 MLL1 组蛋白甲基转移酶活性，其 IC50 为 0.82 μM[1]。
HLC40 可强效且选择性地抑制发生 MLL 重排的 AML 细胞系 MV4-11 和 MOLM-13 的增殖，其 IC50 值分别为 8.92 μM 和 7.07 μM；而对 MLL 野生型 K562 细胞的活性极低 (IC50 = 49.68 μM)[1]。
HLC40 在稳定转染的 HEK-293 细胞中对 CysLT1 受体表现出极弱的拮抗活性，其 IC50 = 5.28 μM[1]。
HLC40 (2.5-10 μM; 72 h) 可在 MLL 重排的 AML 细胞 MV4-11 和 MOLM-13 中诱导浓度依赖性凋亡，在 10 μM 浓度下 MV4-11 细胞的凋亡率最高可达 30.31%[1]。
HLC40 (0.625-10 μM; 24 h) 可激活 MOLM-13 MLL 重排急性髓系白血病 (AML) 细胞中的凋亡通路，表现为剪切型半胱天冬酶-3 (cleaved caspase-3) 的浓度依赖性上调[1]。
HLC40 (0.625-10 μM; 24 h) 以浓度依赖的方式抑制 MOLM-13 MLL 重排 AML 细胞中整体 H3K4 的单甲基化、双甲基化和三甲基化[1]。
HLC40 (20 μM; 2 h) 可直接与 MOLM-13 MLL 重排 AML 细胞内的 WDR5 结合，这一点可通过 WDR5 在高达 61 °C 的温度下呈现显著热稳定性得到证明[1]。
HLC40 (10 μM; 24 h) 可破坏 MV4-11 MLL 重排 AML 细胞中 WDR5 介导的转录激活，抑制增殖程序并上调细胞周期负调控因子[1]。

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

HLC40 相关抗体:

Apoptosis Analysis[1]

Cell Line: MV4-11, MOLM-13 leukemia cell lines
Concentration: 2.5, 5, 10 μM
Incubation Time: 72 h
Result: Induced statistically significant, concentration-dependent increases in apoptotic cells.
Ranged apoptosis rates from 17.67% to 30.31% in MV4-11 cells.

Western Blot Analysis[1]

Cell Line: MOLM-13 leukemia cell lines
Concentration: 0.625, 1.25, 2.5, 5, 10 μM
Incubation Time: 24 h
Result: Induced a clear concentration-dependent upregulation of cleaved caspase-3 levels.
Caused a pronounced, concentration-dependent reduction in H3K4me1/2/3 methylation marks.
Showed the most notable decrease observed at 5 μM where H3K4me1 and H3K4me3 levels were substantially suppressed.
药代动力学
(Parmacokinetics)
Species Dose Route T1/2 Cmax
Mice[1] 30 mg/kg i.p. 16.7 h 4138.19 ng/mL
体内研究
(In Vivo)

HLC40 (20-30 mg/kg；腹腔注射；每日一次；连续 21 天) 在小鼠 MV4-11 异种移植模型中展现出显著的剂量依赖性抗肿瘤功效，在 30 mg/kg 剂量下实现 49.1% 的肿瘤生长抑制率，且未观察到毒性[1]。

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

Animal Model: Acute myeloid leukemia mice (Female Balb/c-nu nude, 6-week injected with MV4-11 cells)[1]
Dosage: 20 mg/kg; 30 mg/kg
Administration: i.p.; daily; 20 days
Result: Exhibited dose-dependent tumor growth suppression.
Achieved 49.1% tumor weight growth inhibition (TGI) at 30 mg/kg compared to vehicle control.
Caused no significant body weight loss in any treatment group.
Showed no treatment-related tissue abnormalities in heart, liver, spleen, lung, and kidney relative to controls.
分子量

773.74

Formula

C38H33F6N3O6S
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

HLC40 相关分类

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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:

HLC40HLC 40HLC-40Histone MethyltransferaseWDR5ApoptosisCaspaseWD repeat protein-5WD40 repeat domain protein 5mll-rearranged leukemiahematologic malignanciesxenograft modelsMV4-11 cellsMOLM-13 cellsMLL1 complexCysLT1 receptorK562 cellsAML cellsInhibitorinhibitorinhibit

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