2. PROTAC NF-κB Immunology/Inflammation Apoptosis Epigenetics Cell Cycle/DNA Damage
  3. PROTACs NF-κB NOD-like Receptor (NLR) Interleukin Related TNF Receptor HDAC
  4. PROTAC HDAC6 degrader 7

PROTAC HDAC6 degrader 7 是一种具有口服活性的，高效且选择性的 PROTAC 降解剂，靶向组蛋白去乙酰化酶 6 (HDAC6) (IC50 = 118 nM)。PROTAC HDAC6 degrader 7 可同时破坏 HDAC6 的催化结构域和锌指泛素结合结构域。PROTAC HDAC6 degrader 7 可抑制 NLRP3 炎症小体的组装和激活，并阻断 NF-κB 信号通路，从而减少关键炎症因子的转录和释放。PROTAC HDAC6 degrader 7 可降低 NLRP3、pro-IL-1β、TNF-α 和 IL-6 的 mRNA 水平。PROTAC HDAC6 degrader 7 可用于炎症性肠病 (IBD) 的研究。
(粉色: HDAC6 配体 (HY-179422)；蓝色: Cereblon 配体 (HY-W087383)；黑色: 连接子)。

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PROTAC HDAC6 degrader 7

PROTAC HDAC6 degrader 7 Chemical Structure

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PROTAC HDAC6 degrader 7 相关抗体

Top Publications Citing Use of Products

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

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NLRP3 NLRP1 NOD1 NOD2

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TNFRSF1A/CD120a TNFRSF3/CD18 TNFRSF4 TNFRSF5/CD40 TNFRSF6/Fas/CD95 TNFRSF7/CD27 TNFRSF8/CD30 TNFRSF9/4-1BB/CD137 TNFRSF12A/TWEAK TNFRSF16/NGF Receptor/CD271 TNFRSF18/GITR/CD357

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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

PROTAC HDAC6 degrader 7 is an orally active, highly efficient, and selective PROTAC degrader targeting histone deacetylase 6 (HDAC6) (IC50 = 118 nM). PROTAC HDAC6 degrader 7 can eliminate both the catalytic and zinc-finger ubiquitin-binding domain. PROTAC HDAC6 degrader 7 inhibits NLRP3 inflammasome assembly and activation, as well as blocks NF-κB signaling, thereby reducing the transcription and release of key inflammatory factors. PROTAC HDAC6 degrader 7 can reduce the mRNA levels of NLRP3, pro-IL-1β, TNF-α, and IL-6. PROTAC HDAC6 degrader 7 can be used for the study of inflammatory bowel disease (IBD)[1]. (Pink: HDAC6 ligand (HY-179422); Blue: Cereblon ligand (HY-W087383); Black: linker).

IC50 & Target

NF-κB

 

IL-6

 

NLRP3

 

HDAC6

118 nM (IC50)

体外研究
(In Vitro)

PROTAC HDAC6 degrader 7 (Compound 22f) (0-2 μM，12 小时) 在 MV4-11 细胞中表现出浓度依赖性的强效 HDAC6 降解活性 (DC50 = 13.4 nM)[1]。
PROTAC HDAC6 degrader 7 (25-200 nM，12 小时) 在 MV4-11 细胞中在 200 nM 浓度下仅对 IKZF1 产生轻微降解作用，但对 GSPT1 没有降解作用[1]。
PROTAC HDAC6 degrader 7 (0-2 μM) 对 HDAC6 具有高度特异性 (IC50 为 118 nM)，在 10 μM 浓度下对其他 HDAC 亚型没有明显的抑制作用[1]。
PROTAC HDAC6 degrader 7 (0.5 μM，0-24 小时) 可诱导 MV4-11 细胞中 HDAC6 的降解，该降解过程在 3 小时内启动，并在 12 小时内达到平衡。CRBN 配体和蛋白酶体抑制剂均可逆转这种降解，表明其作用机制是通过 CRBN 介导的泛素-蛋白酶体途径诱导 HDAC6 降解[1]。
PROTAC HDAC6 degrader 7 (0-6 μM，0-24 小时) 可呈时间依赖性地降解 J774A.1 细胞中的 HDAC6，其浓度依赖性半数致死浓度 (DC50) 为 9.20 nM[1]。
PROTAC HDAC6 degrader 7 (1.4-1000 nM，8 小时) 可呈浓度依赖性地显著抑制 LPS/ATP 刺激的 J774A.1 细胞中 IL-1β 的表达[1]。
PROTAC HDAC6 degrader 7 (40-200 nM，8 小时) 在低浓度下显著降低 J774A.1 细胞中成熟 IL-1β 和 p20 的水平，在高浓度下下调细胞内 NLRP3 和 pro-IL-1β 蛋白的表达[1]。
PROTAC HDAC6 degrader 7 (0.2-1 μM) 呈剂量依赖性地降低 Lipopolysaccharides (HY-D1056) (LPS) 诱导的 J774A.1 细胞中 NLRP3、pro-IL-1β、TNF-α 和 IL-6 的 mRNA 水平[1]。

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

PROTAC HDAC6 degrader 7 相关抗体:

Western Blot Analysis[1]

Cell Line: MV4-11 cells
Concentration: 25 nM, 50 nM, 100 nM, 200 nM
Incubation Time: 12 h
Result: Only IKZF1 was slightly degraded at 200 nM, but GSPT1 was not degraded.

ELISA Assay[1]

Cell Line: J774A.1 cells were pretreated 3 h followed by a 4.5 h pretreatment with LPS (1 μg/mL). Afterward, the cells were stimulated with ATP (5 mM) for 30 min
Concentration: 1.4 nM, 4.1 nM, 12.3 nM, 37 nM, 111 nM, 333 nM, 1000 nM
Incubation Time: 8 h
Result: Significantly inhibited IL-1β in LPS/ATP-stimulated J774A.1 cells in a concentration-dependent manner.
体内研究
(In Vivo)

PROTAC HDAC6 degrader 7 (Compound 22f) (2-10 mg/kg，口服，每日一次，持续 9 天) 可有效缓解 Dextran sulfate sodium salt (MW 5000) (HY-116282) (DSS) 诱导的小鼠急性结肠炎，并改善核心症状 (体重减轻、腹泻、便血) 和病理损伤 (结肠缩短、组织炎症浸润)[1]。

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

Animal Model: Male C57BL/6J mice (6-8 weeks old) were given an aqueous solution containing 2.5% (w/v) dextran sulfate sodium (DSS) for 9 days[1].
Dosage: 2 mg/kg, 10 mg/kg
Administration: P.o., once daily for 9 days
Result: The rate of weight loss was reduced.
Disease Activity Index (DAI) scores were significantly lowered.
The colon length in mice was significantly restored, approaching normal levels.
Mutual epithelial regeneration was promoted, inflammatory cell infiltration was reduced, and histopathological scores were significantly lowered.
The level of the inflammatory cytokine IL-1β was significantly lower than in the DSS model group, while the level of acetylated tubulin (Ac-tubulin), a specific substrate of HDAC6, was significantly upregulated.
分子量

851.00

Formula

C49H54N8O6
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 HDAC6 degrader 7 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

PROTAC HDAC6 degrader 7PROTACsNF-κBNOD-like Receptor (NLR)Interleukin RelatedTNF ReceptorHDACNuclear factor-κBNuclear factor-kappaBILTumor Necrosis Factor ReceptorTNFRHistone deacetylasesPROTACHDAC6 degradersNLRP3 inflammasomeNF-κB signalingUbiquitin-proteasome pathwayInhibitorinhibitorinhibit

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