2. Apoptosis Epigenetics Cell Cycle/DNA Damage
  3. Apoptosis HDAC
  4. HDAC-IN-73

HDAC-IN-73 (compound P-503) 是一种组蛋白脱乙酰酶 (HDAC) 抑制剂。HDAC-IN-73 对 HDAC1 和 HDAC6 的 IC50s 值分别为 0.17、0.49 µM。值得注意的是，HDAC-IN-73 对 HDAC6 的抑制效力增强，其疗效是 PsA (HY-N2150) 的 9 倍 (IC50=3.9 µM)。HDAC-IN-73 具有有效的抗增殖活性，诱导细胞凋亡，并导致细胞在 G2 / M 期停滞。HDAC-IN-73具有用于结肠癌等癌症研究的潜力[1] 。

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HDAC-IN-73 Chemical Structure

HDAC-IN-73 Chemical Structure

CAS No. : 2323571-16-8

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HDAC-IN-73 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

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

HDAC-IN-73 (compound P-503) is a histone deacetylase (HDAC) inhibitor. HDAC-IN-73 shows IC50s values of 0.17, 0.49 µM for HDAC1 and HDAC6, respectively. Notably, HDAC-IN-73's inhibitory potency against HDAC6 is heightened, exhibiting a 9-fold greater efficacy than PsA (HY-N2150) (IC50=3.9 μM). HDAC-IN-73 shows potent antiproliferative activity, induces apoptosis, and causes cell cycle arrest at G2 / M phase. HDAC-IN-73 has the potential to be used for the research of cancer such as colon cancer [1].

IC50 & Target[1]

HDAC1

0.17 μM (IC50)

HDAC6

0.49 μM (IC50)

体外研究
(In Vitro)

HDAC-IN-73 (compound P-503) (0-10 µM; 48 h)可抑制 HCT116 细胞的增殖，IC50 值为 0.24 µM，而 PsA 的IC50 值为 3.05 µM[1]。
与PsA相比，HDAC-IN-73 (0.25-2 µM; 24 h) 可以增加 HCT116 细胞中组蛋白 H3 或 α - 微管蛋白的乙酰化水平[1]。
HDAC-IN-73 (0.1-0.2 µM; 24 h) 可诱导 HCT116 细胞凋亡，并具有优于 PsA 的促凋亡作用[1]。
HDAC-IN-73 (0.2-0.4 µM; 48 h) 可在 G2 / M 期诱导 HCT116 细胞周期停滞，而 PsA 增加 G1 期的比例[1]。

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

HDAC-IN-73 相关抗体:

Apoptosis Analysis[1]

Cell Line: HCT116 cells
Concentration: 0.2, 0.4 µM
Incubation Time: 48 hours
Result: Induced apoptosis with 71.94 % of apoptotic cells (both early and late apoptotic cells) at define concentration of 0.4 μM, compared with PsA (56.5 %, 4 μM) .

Cell Cycle Analysis[1]

Cell Line: HCT116 cells
Concentration: 0.1, 0.2 µM
Incubation Time: 24 hours
Result: Induced cell cycle arrest at G2 / M phase while PsA increased proportion of G1 phase. HDAC-IN-73 with 0.1 μM and 0.2 μM can lead to 47.92 % and 74.56 % of the cells in G2 / M phase, respectively.

Western Blot Analysis[1]

Cell Line: HCT116 cells
Concentration: 0.25, 0.5, 1, 2 µM
Incubation Time: 24 hours
Result: Increased the acetylation levels of histone H3 or α-tubulin in a dose dependent manner comparing with PsA.
体内研究
(In Vivo)

HDAC-IN-73 (compound P-503) (5 mg/kg; i.p.; every 2 days for 26 days) 在 HCT116 异种移植模型中剂量为 5 mg/kg 时有显著的抗肿瘤活性，但也存在更高的毒性，HDAC-IN-73的安全性和毒性剂量需要进一步研究[1]。

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

Animal Model: 6 weeks, Female nude mice (BALB/c-nu) (HCT116 xenograft model)[1]
Dosage: 5 mg/kg
Administration: I.p.; every 2 days for 26 days
Result: Reduced the tumor volume (p < 0.0001) and the tumor weight (p < 0.01). Exhibited the significant loss of body weight which has the same trend with the group of negative control. Inhibited the tumor growth (TGI = 74.6 %) , while the TGI of SAHA (10 mg/kg, positive control) and PsA (10 mg/kg) were 13.1 % and 36.1 %, respectively.
Existed high toxicity, 2 mice died during the medication. Western blot tests showed that the acetylation levels of histone H3 or α-tubulin in tumor tissues were up-regulated.
分子量

758.18

Formula

C22H24Br2N4O6Se2
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

HDAC-IN-73 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • Do most proteins show cross-species activity?

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Keywords:

HDAC-IN-732323571-16-8ApoptosisHDACHistone deacetylasesHCT116 cellHDAC inhibitorHDAC1HDAC6HCT116 xenograft modelCancerColon cancerInhibitorinhibitorinhibit

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