1. Cell Cycle/DNA Damage Epigenetics
  2. HDAC
  3. KTT-1

KTT-1 是一种动力学选择性且口服有效的 HDAC2 抑制剂。KTT-1 通过下调 c-Fos 表达,在早期阶段抑制破骨细胞分化。KTT-1 与 KTT-1 能有效抑制胶原诱导性关节炎 (CIA) 小鼠模型中的关节炎症状。KTT-1 可用于类风湿性关节炎和神经退行性疾病的研究。

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KTT-1

KTT-1 Chemical Structure

CAS No. : 2397562-26-2

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

KTT-1 is a kinetically selective and orally active HDAC2 inhibitor. KTT-1 exhibits high HDAC2-selectivity over HDAC1. KTT-1 inhibits osteoclast differentiation at an early stage by downregulating c-Fos expression. KTT-1 effectively suppresses arthritis symptoms in the collagen-induced arthritis (CIA) mouse model. KTT-1 can be used for the research of rheumatoid arthritis and neurodegenerative diseases[1][2].

IC50 & Target[1][2]

HDAC2

 

体外研究
(In Vitro)

KTT-1 (25-200 nM;骨髓来源的巨噬细胞 (BM 细胞)) 减少了破骨细胞的数量和关键破骨细胞分化基因的表达[1]
KTT-1 (25-100 nM;骨髓来源的巨噬细胞 (BMDMs)) 减少了 IL-1β 和 IL-6 的产生,而不影响 TNF-α 的产生[1]
KTT-1 (第 6 天,第 8 天,第 10 天;骨髓来源的巨噬细胞 (BM 细胞)) 改变了基因表达并阻止了破骨细胞的分化[1]

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

体内研究
(In Vivo)

KTT-1 (0.03 mg/mL (6 mg/kg/day);饮用水给药;连续 10 天) 减轻 CIA 模型中的关节炎严重程度[1]
KTT-1 (0.03 mg/mL (6 mg/kg/day);饮用水给药;22天) 缓解 CAIA 模型中的关节炎严重程度[1]

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

Animal Model: DBA/1JJmsSlc (male, 6-7 weeks old, collagen-induced arthritis (CIA) model)[1]
Dosage: 0.03 mg/mL (6 mg/kg/day)
Administration: Drinking water; 10 consecutive days
Result: Arthritis severity was significantly attenuated, as evidenced by reduced clinical scores and histological scores.
Showed markedly reduced synovial inflammation and immune cell infiltration, with preservation of normal joint architecture.
Animal Model: DBA/1JJmsSlc (male, 6-7 weeks old, collagen antibody-induced arthritis (CAIA) model)[1]
Dosage: 0.03 mg/mL (6 mg/kg/day)
Administration: Drinking water; 22 days
Result: Arthritis severity was significantly alleviated, as indicated by reduced clinical scores and improved body weight gain.
分子量

499.54

Formula

C26H21N5O4S

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
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  • 稀释计算器

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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.

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HY-179216
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