HDAC3 degrader-2
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.
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- CAS 番号: 3110847-73-6
- 分子式: C54H70N6O5
- 分子量:883.17
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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生物活性
製品説明
体外実験
HDAC3 degrader-2 (compound GS-1) (25-50 μM; 24 h) exhibits only extremely low cytotoxicity in HEK293 and L02 cells. After 24 h of treatment, the relative cell viability remains above 50% at both 25 μM and 50 μM concentrations[1].
HDAC3 degrader-2 (0-10 μM; 2-24 h) potently and selectively degrades HDAC3 in THP-1 cells, with a DC50 of 1.24 μM after 24 h of treatment, while exerting minimal effects on the levels of HDAC1 and HDAC2[1].
HDAC3 degrader-2 (5-20 μM; 24 h) inhibits the activation of NLRP3 inflammasome in THP-1-derived macrophages via selective degradation of HDAC3, reduces the levels of mature IL-1β and caspase-1, and suppresses ASC speck formation without altering the expression of inflammasome components[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:L02, HEK293
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Concentration:25 μM, 50 μM
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Incubation Time:24 h
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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.
Parmacokinetics
体内実験
HDAC3 degrader-2 (15 mg/kg; i.p.; daily; for 11 consecutive days) significantly ameliorates DSS (HY-116282C)-induced colitis in male C57BL/6 mice[1].
HDAC3 degrader-2 (7.5-15 mg/kg; i.p.; two administrations) exerts dose-dependent efficacy against acute gouty arthritis induced by Uric acid sodium (MSU) (HY-B2130A) in male C57BL/6 mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (male) treated LPS[1]
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Dosage:15 mg/kg
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Administration:i.p.; single dose
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Result:Achieved 80% survival at 84 hours.
Achieved 70% survival at 120 hours.
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Animal Model:C57BL/6 (male) treated DSS[1]
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Dosage:15 mg/kg
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Administration:i.p.; daily; 11 consecutive days
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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.
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Animal Model:C57BL/6 (male) treated MSU[1]
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Dosage:7.5-15 mg/kg
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Administration:i.p.; two doses (1 hour pre-MSU injection and 12 hours post-MSU injection)
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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.
化学情報
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CAS 番号 3110847-73-6
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分子量 883.17
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分子式 C54H70N6O5
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SMILES
C[C@]12[C@]3(C([C@@]4([H])[C@@](CC3)(CC[C@@](C)(C4)C(N5CCN(C6=CC=C(C=C6)NC(CCCCCC(NC7=C(C=CC=C7)N)=O)=O)CC5)=O)C)=CC([C@]1([H])[C@@]8([C@@](C(C)(C(C(C#N)=C8)=O)C)([H])CC2)C)=O)C
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
HDAC3 degrader-2 関連分類
HY-182051 関連分類
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