1. Cell Cycle/DNA Damage Epigenetics Apoptosis NF-κB Metabolic Enzyme/Protease Immunology/Inflammation
  2. HDAC Apoptosis Reactive Oxygen Species
  3. TH-6

TH-6 是一种有效的 HDAC 抑制剂,对 HDAC1、HDAC2、HDAC3、HDAC6、HDAC8 的 IC50 分别为 0.115、0.135、0.242、0.138、2.120 µM。TH-6 抑制细胞迁移和侵袭。TH-6 诱导细胞凋亡 (apoptosis)和细胞周期停滞在 G2/M 期。TH-6 显示出抗肿瘤活性。

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TH-6 Chemical Structure

TH-6 Chemical Structure

CAS No. : 3031349-25-1

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10 mM * 1 mL in DMSO ¥3477
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1 mg ¥1750
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5 mg ¥3680
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10 mg ¥5900
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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

TH-6 is a potent HDAC inhibitor with IC50s of 0.115, 0.135, 0.242, 0.138, 2.120 µM for HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, respectively. TH-6 inhibits cell migration and invasion. TH-6 induces apoptosis and cell cycle arrest at G2/M phase. TH-6 shows anti-tumor activity[1].

IC50 & Target[1]

HDAC1

0.115 μM (IC50)

HDAC2

0.135 μM (IC50)

HDAC3

0.242 μM (IC50)

HDAC6

0.138 μM (IC50)

HDAC8

2.120 μM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
H22 IC50
26 nM
Compound: TH-6
Antiproliferative activity against mouse H22 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
Antiproliferative activity against mouse H22 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
[PMID: 35926141]
HCT-116 IC50
28 nM
Compound: TH-6
Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
[PMID: 35926141]
HepG2 IC50
29 nM
Compound: TH-6
Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
[PMID: 35926141]
HFL1 IC50
13 nM
Compound: TH-6
Antiproliferative activity against human HFL1 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
Antiproliferative activity against human HFL1 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
[PMID: 35926141]
HUVEC IC50
0.271 μM
Compound: TH-6
Antiproliferative activity against HUVEC cells assessed as inhibition of cell growth measured after 24 hrs by MTT assay
Antiproliferative activity against HUVEC cells assessed as inhibition of cell growth measured after 24 hrs by MTT assay
[PMID: 35926141]
K562 IC50
0.018 μM
Compound: TH-6
Antiproliferative activity against human K562 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
Antiproliferative activity against human K562 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
[PMID: 35926141]
MCF7 IC50
27 nM
Compound: TH-6
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
[PMID: 35926141]
MDA-MB-231 IC50
30 nM
Compound: TH-6
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
[PMID: 35926141]
体外研究
(In Vitro)

TH-6 (0-2 µM) shows antiproliferative activities in cancer cell lines and normal human lung cells[1].
TH-6 (0-10 µM) inhibits tubulin polymerization with an IC50 value of 4.06 µM[1].
TH-6 (0.03, 0.1, 0.3 1 µM; 24 h) increases the expression of Ac-α-Tubulin and AC-Histone H3 in HepG2 cells[1].
TH-6 (7.5, 15, 30 nM) induces apoptosis and cell cycle arrest at G2/M phase[1].
TH-6 (0-30 nM) decreases the MMP and increase ROS levels of HepG2 cells in a dose-dependent manner[1].
TH-6 (7.5, 15, 30 nM; 48 h) inhibits cell migration and invasion in MDA-MB-231 cells and suppress the migration of HUVECs in a concentration-dependent manner[1].
TH-6 shows favorable liver microsomal stability in vitro with t1/2 of 50.3 min[1].

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

Cell Viability Assay[1]

Cell Line: K562, GepG2, HCT-116, MDA-MB-231, H22, MCF-7, HFL-1 cells
Concentration: 0-2 µM
Incubation Time:
Result: Showed antiproliferative activities with an IC50 values of 18, 29, 28, 30, 26, 27, 134 nM for K562, GepG2, HCT-116, MDA-MB-231, H22, MCF-7, HFL-1 cells, respectively.

Western Blot Analysis[1]

Cell Line: HepG2 cells
Concentration: 0.03, 0.1, 0.3 1 µM
Incubation Time: 24 h
Result: Increased the intracellular levels of HDAC6 substrate acetyl-α-tubulin and the HDAC1/2/3 substrate acetyl-histone H3 in a dose-dependent manner.

Cell Cycle Analysis[1]

Cell Line: HepG2 cells
Concentration: 7.5, 15, 30 nM
Incubation Time:
Result: Induced cell cycle arrest at G2/M phase with decreased the expression of Cdc2, Cdc25c, and Cyclin B1 proteins in a dose dependent manner.

Apoptosis Analysis[1]

Cell Line: HepG2 cells
Concentration: 7.5, 15, 30 nM
Incubation Time:
Result: Showed an accumulation of apoptotic cells from 27.04 to 50.54% and upregulated the expression of the pro-apoptotic protein (Bax and Bad) and downregulated the expression of the antiapoptotic protein (Bcl-2 and Bcl-xL) in a dose-dependent manner.
体内研究
(In Vivo)

TH-6 (10, 20 mg/kg; i.v.; daily for 21 days) shows anti-tumor activity in mouse[1].
TH-6 (20 mg/kg) shows antivascular activity and a good cardiovascular safety profile in mouse[1].

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

Animal Model: 4-5 weeks, 18-22 g female ICR mice (H22 allograft mouse model)[1]
Dosage: 10, 20 mg/kg
Administration: I.v.; daily for 21 days
Result: Reduced tumor weights at day 21 by 82% and did not affect body weight during treatment, indicating the low toxicity.
分子量

429.44

Formula

C22H24FN3O5

CAS 号
性状

固体

颜色

Light yellow to khaki

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
细胞实验: 

DMSO 中的溶解度 : 50 mg/mL (116.43 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.3286 mL 11.6431 mL 23.2861 mL
5 mM 0.4657 mL 2.3286 mL 4.6572 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3286 mL 11.6431 mL 23.2861 mL 58.2153 mL
5 mM 0.4657 mL 2.3286 mL 4.6572 mL 11.6431 mL
10 mM 0.2329 mL 1.1643 mL 2.3286 mL 5.8215 mL
15 mM 0.1552 mL 0.7762 mL 1.5524 mL 3.8810 mL
20 mM 0.1164 mL 0.5822 mL 1.1643 mL 2.9108 mL
25 mM 0.0931 mL 0.4657 mL 0.9314 mL 2.3286 mL
30 mM 0.0776 mL 0.3881 mL 0.7762 mL 1.9405 mL
40 mM 0.0582 mL 0.2911 mL 0.5822 mL 1.4554 mL
50 mM 0.0466 mL 0.2329 mL 0.4657 mL 1.1643 mL
60 mM 0.0388 mL 0.1941 mL 0.3881 mL 0.9703 mL
80 mM 0.0291 mL 0.1455 mL 0.2911 mL 0.7277 mL
100 mM 0.0233 mL 0.1164 mL 0.2329 mL 0.5822 mL
Help & FAQs
  • 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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TH-6
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HY-149029
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