1. Metabolic Enzyme/Protease Epigenetics Cell Cycle/DNA Damage
  2. Epoxide Hydrolase HDAC
  3. sEH/HDAC6-IN-2

sEH/HDAC6-IN-2 是一种有效的双重可溶性环氧化物水解酶 (sEH) 和 HDAC6 抑制剂,对人类 sEH、小鼠 sEH 和 HDAC6IC50 分别为 0.9 nM、46.8 nM 和 8 nM。sEH/HDAC6-IN-2 可用于研究炎症疼痛。

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sEH/HDAC6-IN-2 Chemical Structure

sEH/HDAC6-IN-2 Chemical Structure

CAS No. : 3009011-58-6

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

sEH/HDAC6-IN-2 is a potent dual soluble epoxide hydrolase (sEH) and HDAC6 inhibitor with IC50s of 0.9 nM, 46.8 nM, and 8 nM for human sEH, mouse sEH, and HDAC6, respectively. sEH/HDAC6-IN-2 can be used for the study of inflammatory pain[1].

IC50 & Target[1]

HDAC6

0.008 μM (IC50)

Human sEh

0.0009 μM (IC50)

Mouse sEh

0.0468 μM (IC50)

HDAC8

0.062 μM (IC50)

HDAC11

0.464 μM (IC50)

HDAC2

0.492 μM (IC50)

HDAC1

1.151 μM (IC50)

HDAC3

1.276 μM (IC50)

体外研究
(In Vitro)

sEH/HDAC6-IN-2 对 HDAC6 的抑制活性具有明显的选择性(选择性指数:HDAC1/HDAC6 = 144,HDAC2/HDAC6 = 62,HDAC3/HDAC6 = 160,HDAC8/HDAC6 = 8,HDAC11/HDAC6 = 58)[1]
sEH/HDAC6-IN-2(化合物 28g;1-2 μM;24 小时)诱导 α-微管蛋白乙酰化增加,而不影响组蛋白 H3,表明选择性抑制 HDAC6[1]

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

Western Blot Analysis[1]

Cell Line: THP-1 cells
Concentration: 1 μM, 2 μM
Incubation Time: 24 h
Result: Induced acetylation of α-tubulin and histone H3.
体内研究
(In Vivo)

sEH/HDAC6-IN-2(compound 28g;30 mg/kg; 腹腔注射;一次)缓解小鼠福尔马林引起的炎症疼痛[1]
静脉和口服给药后 SD 大鼠中 sEH/HDAC6-IN-2 的药代动力学[1]
1.19

parameter iv (10 mg/kg) ig (50 mg/kg)
Tmax (h) 0.08 0.50
Cmax (μM) 7.87 6.63
t1/2 (h) 5.43 3.55
CL (L/h) 0.16 0.82
Vz (L) 1.28 4.20
AUC0-12h (μM·h) 12.29 15.01
AUC0-∞ (μM·h) 21.16 21.22
F (%) 24.42 -

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

Animal Model: Kunming mice (male, weighing 20-22 g) injected with 5% Formalin solution[1].
Dosage: 30 mg/kg
Administration: ip; once
Result: Exhibited an effective analgesic activity.
分子量

580.02

Formula

C27H32ClF2N5O5

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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产品名称:
sEH/HDAC6-IN-2
目录号:
HY-159171
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