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CPTH2 hydrochloride
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。
CPTH2 hydrochloride图片
CAS NO:2108899-91-6
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
CPTH2 hydrochloride 是有效的组蛋白乙酰基转移酶 (HAT) 抑制剂。CPTH2 hydrochloride 选择性地抑制Gcn5对组蛋白 H3 的乙酰化。CPTH2 hydrochloride 通过抑制乙酰转移酶p300 (KAT3B)诱导凋亡 (apoptosis) 并降低透明细胞肾癌 (ccRCC) 细胞系的侵袭性。
生物活性

CPTH2 hydrochloride is a potenthistone acetyltransferase(HAT)inhibitor. CPTH2 hydrochloride selectively inhibits the acetylation of histone H3 byGcn5. CPTH2 hydrochloride inducesapoptosisand decreases the invasiveness of a clear cell renal carcinoma (ccRCC) cell line through the inhibition ofacetyltransferase p300 (KAT3B)[1][2].

IC50& Target[1][2]

GCN5

 

体外研究
(In Vitro)

CPTH2 (100 μM; 12, 24, 48 hours) hydrochloride causes a decrease in cell proliferation after as early as 12 h with a further significant reduction after 48 h stimulation[1].
CPTH2 (100 μM; 12 or 48 hours) hydrochloride causes a comparable drop of the activity in both cell lines[1].
CPTH2 (100 μM; 48 hours) hydrochloride produces a drastic increase in apoptotic/dead cell population after 48 h[1].
CPTH2 (100 μM; 12, 24, 48 hours) hydrochloride shows a reduced acetylation of both global AcH3 histone and H3AcK18[1].
CPTH2 (100 μM; 24, 48 hours) hydrochloride is capable to counteract invasion and migration of ccRCC-786-O cells in culture[1].
CPTH2 (0.2, 0.5, 1 mM) hydrochloride inhibits the growth of a GCN5 deleted strain and a single catalytic mutant E173H[2].
CPTH2 (0.6, 0.8 mM; for 24 hours) hydrochloride inhibits histone H3 acetylation in yeast cell cultures[2].
CPTH2 hydrochloride inhibits the Gcn5p dependent functional network[2].

Cell Proliferation Assay[1]

Cell Line:Papillary thyroid (K1) and clear cell Renal Cell Carcinoma (ccRCC-786-O) cell lines
Concentration:100 μM
Incubation Time:12, 24, 48 hours
Result:Caused a decrease in cell proliferation after as early as 12 h with a further significant reduction after 48 h stimulation.

Cell Viability Assay[1]

Cell Line:K1 and ccRCC-786-O cell lines
Concentration:100 μM
Incubation Time:24 hours (K1 cell) and 48 hours (ccRCC-786-O cell)
Result:Caused a comparable drop of the activity in both cell lines.

Apoptosis Analysis[1]

Cell Line:ccRCC-786-O cells
Concentration:100 μM
Incubation Time:48 hours
Result:Produced a drastic increase in apoptotic/dead cell population after 48 h.

Western Blot Analysis[1]

Cell Line:ccRCC-786-O cells
Concentration:100 μM
Incubation Time:12, 24, 48 hours
Result:Showed a reduced acetylation of both global AcH3 histone and H3AcK18.
分子量

328.26

Formula

C14H15Cl2N3S

CAS 号

2108899-91-6

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.