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G4/HDAC-IN-1
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。
G4/HDAC-IN-1图片
包装与价格：
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
G4/HDAC-IN-1 (compound a6) 是G4/HDAC双靶标化合物。G4/HDAC-IN-1 抑制胞内 HDAC 活性IC50值为 1.1 μM，并且诱导 G4 的形成。G4/HDAC-IN-1 抑制三阴性乳腺癌细胞的增殖，并且抑制肿瘤在异种移植模型中的生长。G4/HDAC-IN-1 可用于癌症的研究。
生物活性

G4/HDAC-IN-1 (compound a6) is aG4/HDACdual-targeting compound. G4/HDAC-IN-1 inhibits intracellularHDACactivity with anIC50value of 1.1 μM, and induces G4 formation. G4/HDAC-IN-1 inhibits TNBC proliferation and tumor growth in TNBC xenograft model. G4/HDAC-IN-1 can be used for the research ofcancer[1].

IC50& Target

HDAC8

0.03 μM (IC50)

HDAC6

0.65 μM (IC50)

HDAC1

1.26 μM (IC50)

HDAC11

1.38 μM (IC50)

HDAC4

2.64 μM (IC50)

体外研究
(In Vitro)

G4/HDAC-IN-1 (0-10 μM; 1.5 h) shows HDAC inhibitory activity with an IC50of 1.9 μM by determining nuclear extract and exhibits inhibitory activity on intracellular HDAC activity in MDA-MB-231 cells with an IC50value of 1.1 μM[1].
G4/HDAC-IN-1 (0-50 μM) shows G4 binding activity with an IC50of 0.4 μM[1].
G4/HDAC-IN-1 (0-10 μM; 1.5 h) inhibits HDAC1, HDAC8, HDAC4, HDAC6 and HDAC11 activities with IC50s of 1.26, 0.03, 2.64, 0.65 and 1.38 μM, respectively[1].
G4/HDAC-IN-1 (0-50 μM) binds with Pu22, HRAS and HTG21 sequences with KDvalues of 1.8, 3.6 and ＞10 μM, respectively[1].
G4/HDAC-IN-1 (1.25-5.0 μM; 48 h) dose-dependently increases DNA G4 level[1].
G4/HDAC-IN-1 (0-50 μM; overnight) inhibits cytotoxic activities of TNBC cell lines[1].

Western Blot Analysis[1]

Cell Line:MDA-MB-231 cell line
Concentration:1.25, 2.5 and 5.0 μM
Incubation Time:48 hours
Result:Increased the acetylation levels of HDAC1/2/3/8 substrate acetyl histone H3 (ac-H3), acetyl-histone H4 (ac-H4), and the HDAC6 substrate acetyl-α-tubulin (ac-Tub).

Cell Cytotoxicity Assay[1]

Cell Line:TNBC cell lines
Concentration:0-50 μM
Incubation Time:Overnight
Result:Showed cytotoxic activities to MDA-MB-231, MDA-MB-468, SUM159PT and BT549 with IC50s of 4.1, 3.3, 7.4 and 6.5 μM, respectively.
体内研究
(In Vivo)

G4/HDAC-IN-1 (2.5 mg/kg; i.p. once daily for 31 days) shows antitumor activity[1].

Animal Model:Five week-old female BALB/C mice with TNBC xenografts[1]
Dosage:2.5 mg/kg
Administration:Intraperitoneal injection; 2.5 mg/kg once daily; for 31 days
Result:Showed well tolerance in vivo and exhibited potent antitumor activity.
分子量

698.27

Formula

C36H49ClFN7O4

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.