2. Cell Cycle/DNA Damage Epigenetics Apoptosis
  3. Wee1 HDAC Apoptosis
  4. Wee1/HDAC-IN-1

Wee1/HDAC-IN-1 是一种双 Wee1/HDAC 抑制剂，对 Wee1、HDAC1、HDAC3 和 HDAC6 的 IC50 值分别为 1.2 nM、196 nM、156 nM 和 55 nM。Wee1/HDAC-IN-1 对 MV4-11 细胞表现出强的抗增殖活性，其 IC50 值为 0.076 μM。Wee1/HDAC-IN-1 选择性地结合到 Wee1 和 HDACs 的催化位点，干扰 DNA 损伤修复通路，并诱导 MV4-11 细胞凋亡 (apoptosis)。Wee1/HDAC-IN-1 可用于急性髓系白血病的研究。

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Wee1/HDAC-IN-1

Wee1/HDAC-IN-1 Chemical Structure

CAS No. : 3037071-29-4

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Wee1/HDAC-IN-1 相关抗体

Top Publications Citing Use of Products

查看 Wee1 亚型特异性产品:

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PKMYT1

查看 HDAC 亚型特异性产品:

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HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Wee1/HDAC-IN-1 is a dual Wee1/HDAC inhibitor with an IC50 of 1.2 nM for Wee1 and IC50 values of 196 nM for HDAC1, 156 nM for HDAC3, and 55 nM for HDAC6. Wee1/HDAC-IN-1 exhibits strong antiproliferative activity against MV4-11 cells with an IC50 of 0.076 μM. Wee1/HDAC-IN-1 selectively binds to Wee1 and HDACs. Wee1/HDAC-IN-1 interferes with DNA damage repair pathways and induces apoptosis in MV4-11 cells. Wee1/HDAC-IN-1 Wee1/HDAC-IN-1 can be used for the research of acute myeloid leukemia (AML)[1].

IC50 & Target[1]

Wee1

1.2 nM (IC50)

HDAC1

196 nM (IC50)

HDAC3

156 nM (IC50)

HDAC6

55 nM (IC50)

HDAC2

>2000 nM (IC50)

HDAC8

1295 nM (IC50)

HDAC10

1310 nM (IC50)

HDAC11

>2000 nM (IC50)

体外研究
(In Vitro)

Wee1/HDAC-IN-1 (Compound 23f) (72 h) 在不同类型的 AML 细胞中表现出强效的抗增殖活性。Wee1/HDAC-IN-1 对 MV4-11 细胞、THP-1 细胞和 HL-60 细胞的 IC50 值分别为 0.076 μM、0.773 μM 和 0.309 μM[1]。
Wee1/HDAC-IN-1 (10-75 nM；96 h) 具有诱导MV4-11细胞分化的能力[1]。
Wee1/HDAC-IN-1 (37.5-600 nM；72 h) 以剂量依赖的方式诱导 MV4-11细胞凋亡[1]。
Wee1/HDAC-IN-1 (19-1200 nM; 72 h) 以剂量依赖的方式降低 CDK1 的磷酸化水平，同时增加乙酰化组蛋白 H3 的表达。Wee1/HDAC-IN-1 可以以剂量依赖的方式促进 γH2A.X 的表达，γH2A.X 是 DNA 双链损伤的生物标志物[1]。

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

Wee1/HDAC-IN-1 相关抗体:

Apoptosis Analysis[1]

Cell Line: MV4-11
Concentration: 37.5, 75, 150, 300, 600 nM
Incubation Time: 72 h
Result: Induced cellapoptosis in a dose-dependent manner, with a notable increasein apoptosis (56.90%) observed at a concentration of 600 nM.

Western Blot Analysis[1]

Cell Line: MV4-11
Concentration: 19, 75, 300, 1200 nM
Incubation Time: 72 h
Result: Reduced the phosphorylation level of CDK1, increased the expression of acetylated histone H3, and promoted the expression of yH2A.X.

Cell Differentiation Assay[1]

Cell Line: MV4-11 cells
Concentration: 10, 25, 50, 75 nM
Incubation Time: 96 h
Result: Induced an increase in CD11b expression,indicating a certain differentiation-inducing ability.
体内研究
(In Vivo)

Wee1/HDAC-IN-1 (Compound 23f) (15-60 mg/kg；腹腔注射；每日一次；21 天) 抑制了在 BALB/c 裸鼠中皮下注射 MV4-11 细胞的肿瘤生长[1]。
Wee1/HDAC-IN-1 (150 mg/kg；尾静脉给药；单次注射) 在 ICR 小鼠 (18-20 g) 中显示了可接受的肝肾安全谱[1]。

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

Animal Model: BALB/c nude (female, 6-8 weeks old) were subcutaneous injection of MV4-11 cells, 1 × 107 cells/mouse[1]
Dosage: 15 mg/kg, 30 mg/kg, 60 mg/kg
Administration: Intraperitoneal; once daily; 21 days
Result: Tumor growth was significantly inhibited in a dose-dependent manner.
Median survival time was increased.
Induced significant morphological changes in tumor cells, including cell shrinkage, aggregation, and chromatin marginalization.
\r\nReduced the compensatory CHK1 activation caused by Wee1 inhibition.
Animal Model: ICR mice (18-20 g)[1]
Dosage: 120 mg/kg, 150 mg/kg
Administration: Tail vein injection; once
Result: No significant changes in biochemical parameters (ALT、AST and BUN) or morphological changes in major organs were observed, indicating acceptable hepatic and renal safety profiles and low potential toxicity.
分子量

629.75

Formula

C33H43N9O4
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

Wee1/HDAC-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?

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Keywords:

Wee1/HDAC-IN-13037071-29-4Wee1HDACApoptosisHistone deacetylasesMV4-11 cellsantitumor efficacyxenograft modelhistone deacetylase inhibitorsinhibitory activityCHK1acute myeloid leukemia (AML)dual-targeting compoundsInhibitorinhibitorinhibit

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