TH-6

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TH-6

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

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。

生物活性

TH-6 is a potentHDACinhibitor withIC₅₀s of 0.115, 0.135, 0.242, 0.138, 2.120 μM forHDAC1,HDAC2,HDAC3,HDAC6,HDAC8, respectively. TH-6 inhibits cell migration and invasion. TH-6 inducesapoptosisand 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)

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 IC₅₀value 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 t_1/2of 50.3 min^[1].

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 IC₅₀values 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].

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

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.