2. PROTAC Epigenetics Cell Cycle/DNA Damage Apoptosis
  3. PROTACs HDAC Bcl-2 Family Apoptosis
  4. PROTAC HDAC3 degrader-1

PROTAC HDAC3 degrader-1 是一种选择性靶向 HDAC3 的 PROTAC 降解剂，其 DC50 为 30.73 nM。PROTAC HDAC3 degrader-1 可通过泛素-蛋白酶体系统诱导 HDAC3 降解。PROTAC HDAC3 degrader-1 可促进细胞凋亡 (apoptosis)、诱导 DNA 损伤，并下调抗凋亡蛋白 Mcl-1 和 Bcl-xL。PROTAC HDAC3 degrader-1 可用于急性髓系白血病的相关研究。
(粉色: HDAC3 配体 (HY-181768)；蓝色: VHL 配体 (HY-125845)；黑色: 连接子)。

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PROTAC HDAC3 degrader-1

PROTAC HDAC3 degrader-1 Chemical Structure

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PROTAC HDAC3 degrader-1 相关抗体

Top Publications Citing Use of Products

查看 PROTACs 亚型特异性产品:

查看所有亚型
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

查看 HDAC 亚型特异性产品:

查看所有亚型
HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

查看 Bcl-2 Family 亚型特异性产品:

查看所有亚型
Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3 Bad

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PROTAC HDAC3 degrader-1 is a selective PROTAC degrader targeting HDAC3 with a DC50 of 30.73 nM. PROTAC HDAC3 degrader-1 induces degradation of HDAC3 via the ubiquitin-proteasome system. PROTAC HDAC3 degrader-1 promotes apoptosis, induces DNA damage, and downregulates anti-apoptotic proteins Mcl-1 and Bcl-xL. PROTAC HDAC3 degrader-1 can be used for the research of acute myeloid leukemia[1]. (Pink: HDAC3 ligand (HY-181768); Blue: VHL ligand (HY-125845); Black: linker).

IC50 & Target[1]

HDAC3

30.73 nM (DC50)

Bcl-xL

 

Mcl-1

 

体外研究
(In Vitro)

PROTAC HDAC3 degrader-1 (b22) (20 nM, 200 nM; 12 h) 可诱导 MV4-11 细胞中 HDAC3 的降解，处理 12 h 后，20 nM 浓度下的降解率为 24.4%，200 nM 浓度下的降解率为 81.8%[1]。
PROTAC HDAC3 degrader-1 可在 THP-1 急性髓系白血病 (AML) 细胞中诱导 HDAC3 降解，其 DC50 为 143.1 nM[1]。
PROTAC HDAC3 degrader-1 (0.5-1000 nM; 24 h) 可在 MV4-11 细胞中诱导浓度依赖性的 HDAC3 降解，处理 24 h 后其 DC50 为 30.73 nM，最大降解效率达 82%[1]。
PROTAC HDAC3 degrader-1 (200 nM; 0.5-24 h) 可在 MV4-11 细胞中诱导时间依赖性 HDAC3 降解，在 200 nM 浓度下 8 h 内达到最大降解水平，且降解状态至少能维持 24 h[1]。
PROTAC HDAC3 degrader-1 (8-1000 nM; 12 h) 在 MV4-11 细胞中对 HDAC3 表现出相较于其他 HDAC 亚型 (HDAC1、HDAC2、HDAC4、HDAC6、HDAC11) 的高选择性降解作用，在最高 200 nM 的浓度下即可实现该效果；仅在以 ≥1000 nM 浓度处理 12 h 后，才会对 HDAC8 产生影响[1]。
PROTAC HDAC3 degrader-1 (48 小时) 对 MV4-11 AML 细胞表现出中等抗增殖活性，处理 48 h 后的 IC50 为 1.26 μM，并且对 Kasumi-1、THP-1、HL-7702 和 iBMDMs 细胞的细胞毒性显著降低[1]。
PROTAC HDAC3 degrader-1 (0.078-2.500 μM; 48 h) 可与 Venetoclax (HY-15531) 协同抑制 MV4-11 细胞增殖，处理 48 h 后所有测试浓度组合的 CI 值均小于 1[1]。
PROTAC HDAC3 degrader-1 (300-600 nM; 48 h) 与 Venetoclax 协同作用以促进 MV4-11 细胞的凋亡，联合处理 48 h 后凋亡率最高可达 88.90%[1]。
PROTAC HDAC3 degrader-1 (150-600 nM; 24 h) 与 Venetoclax 在 MV4-11 细胞中发挥协同作用，可下调抗凋亡蛋白 Mcl-1 和 Bcl-xL、增强 DNA 损伤 (γH2A.X 水平升高)，并在联合处理 24 h 后激活 caspase3 剪切；而单独使用 b22 对这些蛋白无显著影响[1]。

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

PROTAC HDAC3 degrader-1 相关抗体:

Western Blot Analysis[1]

Cell Line: MV4-11 acute myeloid leukemia (AML) cells
Concentration: 20 nM; 200 nM
Incubation Time: 12 h
Result: Induced 24.4% HDAC3 degradation at 20 nM.
Induced 81.8% HDAC3 degradation at 200 nM.

Western Blot Analysis[1]

Cell Line: MV4-11 cells
Concentration: 0.5, 1.4, 4.1, 12.3, 37.0, 111.1, 333.3, 1000 nM
Incubation Time: 24 h
Result: Induced concentration-dependent HDAC3 degradation with a DC50 of 30.73 nM and a maximum degradation efficiency (Dmax) of 82%.

Western Blot Analysis[1]

Cell Line: MV4-11 cells
Concentration: 200 nM
Incubation Time: 0.5, 1, 1, 2, 3, 4, 6, 8, 10, 12, 24 h
Result: Reached maximum HDAC3 degradation within 8 h of treatment.
Sustained degradation levels were maintained for at least 24 h.

Western Blot Analysis[1]

Cell Line: MV4-11 cells
Concentration: 8, 40, 200, 1000 nM
Incubation Time: 12 h
Result: Promoted efficient, dose-dependent degradation of HDAC3 specifically.
Showed no significant effects on HDAC1, HDAC2, HDAC4, HDAC6, or HDAC11 at concentrations up to 200 nM.
Caused a significant effect on HDAC8 only at concentrations ≥ 1000 nM.

Cell Proliferation Assay[1]

Cell Line: MV4-11 cells
Concentration: 2.500, 1.250, 0.625, 0.313, 0.156, 0.078 μM (PROTAC HDAC3 degrader-1); 0.031, 0.063, 0.125 μM (Venetoclax)
Incubation Time: 48 h
Result: Produced combination index (CI) values < 1 for all tested combinations with Venetoclax, indicating synergistic antiproliferative effects.
CI values ranged from 0.066 to 0.611 across the tested concentration combinations.

Apoptosis Analysis[1]

Cell Line: MV4-11 cells
Concentration: 300, 600 nM (PROTAC HDAC3 degrader-1 alone); 300, 600 nM (PROTAC HDAC3 degrader-1) + 30, 60 nM (Venetoclax) (HY-15531) (combined)
Incubation Time: 48 h
Result: Induced 11.40% apoptosis at 300 nM when used alone.
Induced 14.16% apoptosis at 600 nM when used alone.
Increased apoptosis rate to 63.10% when combined with 30 nM Venetoclax at 300 nM b22.
Increased apoptosis rate to 79.10% when combined with 30 nM Venetoclax at 600 nM.
Increased apoptosis rate to 69.50% when combined with 60 nM Venetoclax at 300 nM.
Increased apoptosis rate to 88.90% when combined with 60 nM Venetoclax at 600 nM.

Western Blot Analysis[1]

Cell Line: MV4-11 cells
Concentration: 150, 300, 600 nM (PROTAC HDAC3 degrader-1 alone); 150, 300, 600 nM (PROTAC HDAC3 degrader-1) + 30, 60 nM (Venetoclax) (combined)
Incubation Time: 24 h
Result: Did not significantly alter Mcl-1 or Bcl-xL protein levels when used alone.
Dose-dependently downregulated Mcl-1 and Bcl-xL when combined with Venetoclax.
Increased γH2A.X levels (a marker of DNA double-strand breaks) when combined with Venetoclax.
Reduced pro-caspase3 levels when combined with Venetoclax.
Synergistically increased cleaved caspase3 levels when combined with Venetoclax.
药代动力学
(Parmacokinetics)
Species Dose Route Cmax AUC0-inf T1/2 Vss CL
Mice[1] 2 mg/kg i.v. 1454.29 ng/mL 807.25 ng·h/mL 1.81 h 4.27 L/kg 45.64 mL/min/kg
体内研究
(In Vivo)

PROTAC HDAC3 degrader-1 (2 mg/kg; i.v.; single dose) 在雄性 ICR 小鼠中可产生中等水平的全身暴露，其终末半衰期为 1.81 h，总血浆清除率为 45.64 mL/min/kg[1]。

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

934.16

Formula

C50H63N9O7S
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

PROTAC HDAC3 degrader-1 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:

PROTAC HDAC3 degrader-1PROTACsHDACBcl-2 FamilyApoptosisHistone deacetylasesubiquitin-proteasome systemapoptosisKasumi-1 cellsDNA damageTHP-1 AML cellsBcl-xLMV4-11 cellsacute myeloid leukemiaMcl-1HDAC3Inhibitorinhibitorinhibit

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