2. Cell Cycle/DNA Damage Epigenetics Immunology/Inflammation Apoptosis
  3. HDAC NOD-like Receptor (NLR) Caspase Interleukin Related
  4. HDAC3 degrader-2

HDAC3 degrader-2 是一种选择性 HDAC3 降解剂。HDAC3 degrader-2 通过降解 HDAC3 抑制 NLRP3 炎症小体的活化，进而减少 IL-1β 与 caspase-1 的成熟。HDAC3 degrader-2 具有抗炎活性。HDAC3 degrader-2 可用于内毒素休克、结肠炎、痛风性关节炎的相关研究。

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HDAC3 degrader-2

HDAC3 degrader-2 Chemical Structure

CAS No. : 3110847-73-6

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HDAC3 degrader-2 相关抗体

Top Publications Citing Use of Products

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

查看 NOD-like Receptor (NLR) 亚型特异性产品:

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NLRP3 NLRP1 NOD1 NOD2

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

查看 Interleukin Related 亚型特异性产品:

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IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

HDAC3 degrader-2 is a selective HDAC3 degrader. HDAC3 degrader-2 inhibits the activation of the NLRP3 inflammasome by degrading HDAC3, thereby reducing the maturation of IL-1β and caspase-1. HDAC3 degrader-2 exhibits anti-inflammatory activity. HDAC3 degrader-2 can be used in research related to endotoxin shock, colitis and gouty arthritis[1].

体外研究
(In Vitro)

HDAC3 degrader-2 (compound GS-1) (25-50 μM; 24 h) 在 HEK293 和 L02 细胞中仅表现出极低的细胞毒性，经 24 h 处理后，25 μM 和 50 μM 浓度下的相对细胞存活率均保持在 50% 以上[1]。
HDAC3 degrader-2 (0-10 μM; 2-24 h) 可强效且选择性地降解 THP-1 细胞中的 HDAC3，处理 24 h 后的 DC50 为 1.24 μM，而对 HDAC1 和 HDAC2 的水平影响极小[1]。
HDAC3 degrader-2 (5-20 μM; 24 h) 可通过选择性降解 HDAC3 抑制 THP-1 来源巨噬细胞中 NLRP3 炎症小体的活化，降低成熟 IL-1β 和 caspase-1 的水平并抑制 ASC 斑点形成，且不会改变炎症小体组分的表达[1]。

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

HDAC3 degrader-2 相关抗体:

Cell Cytotoxicity Assay[1]

Cell Line: L02, HEK293
Concentration: 25 μM, 50 μM
Incubation Time: 24 h
Result: Resulted in 94.29±1.07% relative cell viability in HEK293 cells and 86.65±3.54% relative cell viability in L02 cells at 25 μM.
Resulted in 69.98±3.37% relative cell viability in HEK293 cells and 77.45±3.06% relative cell viability in L02 cells at 50 μM.
药代动力学
(Parmacokinetics)
Species Dose Route T1/2 Tmax Cmax AUC0-t AUC0-∞ MRT0-t MRT0-∞ F
Rat[1] 5 mg/kg i.v. 2.82 h 0.0833 h 9473 ng/mL 3094 ng·h/mL 3133 μg·h/mL 0.354 h 0.513 h /
Rat[1] 15 mg/kg i.p. 4.55 h 6.67 h 1222 ng/mL 15322 ng·h/mL 15772 ng·h/mL 7.23 h 7.95 h 67.2 %
体内研究
(In Vivo)

HDAC3 degrader-2 (15 mg/kg；腹腔注射；单次给药) 对 C57BL/6 雄性小鼠的 LPS (HY-D1056) 诱导内毒素休克具有强效保护作用[1]。
HDAC3 degrader-2 (15 mg/kg；腹腔注射；每日；连续 11 天) 可显著改善 C57BL/6 雄性小鼠中 DSS (HY-116282C) 诱导的结肠炎[1]。
HDAC3 degrader-2 (7.5-15 mg/kg；腹腔注射；两次给药) 对 C57BL/6 雄性小鼠中 Uric acid sodium (MSU) (HY-B2130A) 诱导的急性痛风性关节炎表现出剂量依赖性疗效[1]。

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

Animal Model: C57BL/6 (male) treated LPS[1]
Dosage: 15 mg/kg
Administration: i.p.; single dose
Result: Achieved 80% survival at 84 hours.
Achieved 70% survival at 120 hours.
Animal Model: C57BL/6 (male) treated DSS[1]
Dosage: 15 mg/kg
Administration: i.p.; daily; 11 consecutive days
Result: Restored colon length.
Significantly attenuated weight loss.
Reduced the disease activity index (DAI) score.
Improved mucosal integrity.
Reduced epithelial damage.
Partially restored crypt architecture and goblet cell abundance.
Degraded HDAC3 protein in colon tissues.
Suppressed the expression of activated caspase-1 and IL-1β.
Animal Model: C57BL/6 (male) treated MSU[1]
Dosage: 7.5-15 mg/kg
Administration: i.p.; two doses (1 hour pre-MSU injection and 12 hours post-MSU injection)
Result: Suppressed joint swelling.
Maintained 100% survival in mice treated with 15 mg/kg dose without observable adverse effects.
Resulted in minimal inflammatory infiltration, no crystal deposition, and no tissue damage in treated joints.
分子量

883.17

Formula

C54H70N6O5
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

HDAC3 degrader-2 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:

HDAC3 degrader-23110847-73-6HDACNOD-like Receptor (NLR)CaspaseInterleukin RelatedHistone deacetylasesILTHP-1 cellscaspase-1THP-1-derived macrophagesNLRP3 inflammasomeIL-1βHDAC3L02C57BL/6 male miceHEK293Lys367Inhibitorinhibitorinhibit

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