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CPTH2 hydrochloride
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。
CPTH2 hydrochloride Chemical Structure
CAS No. : 2108899-91-6
| 规格 |
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是否有货 |
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| 100 mg |
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询价 |
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| 250 mg |
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询价 |
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| 500 mg |
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询价 |
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* Please select Quantity before adding items.
CPTH2 hydrochloride 的其他形式现货产品:
CPTH2
| 生物活性 |
CPTH2 hydrochloride is a potent histone acetyltransferase (HAT) inhibitor. CPTH2 hydrochloride selectively inhibits the acetylation of histone H3 by Gcn5. CPTH2 hydrochloride induces apoptosis and decreases the invasiveness of a clear cell renal carcinoma (ccRCC) cell line through the inhibition of acetyltransferase p300 (KAT3B)[1][2].
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| IC50 & Target[1][2] |
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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].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
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. |
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| 分子量 |
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| Formula |
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| CAS 号 |
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis.
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| 参考文献 |
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[1]. Cocco E, et al. KAT3B-p300 and H3AcK18/H3AcK14 levels are prognostic markers for kidney ccRCC tumoraggressiveness and target of KAT inhibitor CPTH2. Clin Epigenetics. 2018 Apr 4;10:44.
[2]. Chimenti F, et al. A novel histone acetyltransferase inhibitor modulating Gcn5 network: cyclopentylidene-[4-(4′-chlorophenyl)thiazol-2-yl)hydrazone. J Med Chem. 2009 Jan 22;52(2):530-6.
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