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HDAC-IN-45
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。
HDAC-IN-45图片
CAS NO:2421122-61-2
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
HDAC-IN -45 (Compound 14) 是一种小分子HDAC抑制剂,具有抗癌活性,也可与 Y303 残基形成氢键。HDAC-IN-45 (Compound 14) 对 HDAC1、2 和 3 亚型具有显著的抑制作用,IC50分别为 0.108、0.585 和 0.563 μM。
生物活性

HDAC-IN-45 (Compound 14) is a small moleculeHDACinhibitor and has anticancer activity, also can forms a hydrogen bond with residue Y303. HDAC-IN-45 (Compound 14) has substantial inhibitory effects towardsHDAC1, 2 and 3 isoforms withIC50values of 0.108, 0.585 and 0.563 μM respectively[1].

IC50& Target[1]

HDAC1

0.108 μM (IC50)

HDAC2

0.585 μM (IC50)

HDAC3

0.563 μM μM (IC50)

HDAC6

﹥10 μM (IC50)

HDAC8

6.81 μM (IC50)

体外研究
(In Vitro)

HDAC-IN-45 (Compound 14) suppresses the growth of triple-negative breast cancer cells MDA-MB-231 (IC50= 1.48 μM), MDA-MB-468 (IC50= 0.65 μM), and liver cancer cells HepG2 (IC50= 2.44 μM).
HDAC-IN-45 has equally virulent in the HDAC-sensitive cell lines (YCC11) and -resistant gastric cell lines (YCC3/7) and overcome HDACi resistance. HDAC-IN-45 has a high toxicity (IC50= 0.33 μM) in three leukemic cell lines, K-562, KG-1 and THP-1.
HDAC-IN-45 (Compound 14) has substantial inhibitory effects towards HDAC1, 2 and 3 isoforms withIC50values of 0.108, 0.585 and 0.563 μM respectively.
HDAC-IN-45 (Compound 14) can elevate acetylation level of histone H3 and expression of p21.
HDAC-IN-45 (Compound 14) exerts a dose-dependent upregulation of ac-H3K9 in MDA-MB-231 cells, triggers cell cycle arrest in G1 phase.
HDAC-IN-45 (Compound 14) exhibits a potent antitumor efficacy in xenograft mouse model[1].

Cell Proliferation Assay[1]

Cell Line:Triple-negative breast cancer cells; liver cancer cells; YCC11 and YCC3/7
Concentration:a series of concentration
Incubation Time:72 h
Result:Inhibited the cell growth viability of HepG2 and triple-negative breast cancer cells.

Cell Cytotoxicity Assay[1]

Cell Line:Three leukemic cell lines (K-562, KG-1 and THP-1); YCC3/7 and YCC11 cell lines
Concentration:a series of concentration
Incubation Time:72 h
Result:Showed a potent anti-cancer effect, exhibited high sensitivities and strong toxicities with IC50 values below micromolar in leukemic cell lines.

Western Blot Analysis[1]

Cell Line:MDA-MB-231 cells
Concentration:2 μM
Incubation Time:24 h
Result:Elevated acetylation level of histone H3 and expression of p21.

Cell Cycle Analysis[1]

Cell Line:MDA-MB-231cells
Concentration:4 μM
Incubation Time:24 h
Result:Arrested cell cycle in G1 and trigger apoptosis.
体内研究
(In Vivo)

HDAC-IN-45 (Compound 14) (25 mg/kg or 50mg/kg; i.p.; every day) exhibits a potent antitumor efficacy in human MDA-MB-231 breast cancer xenograft mouse model[1].

Animal Model:Human MDA-MB-231 breast cancer xenograft mouse model[1]
Dosage:25 mg/kg or 50mg/kg
Administration:25 mg/kg or 50mg/kg; i.p.; every day.
Result:Exhibited a potent antitumor efficacy.
分子量

502.93

Formula

C25H20ClFN8O

CAS 号

2421122-61-2

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.