382115
Histone Acetyl Transferase Inhibitor VII, CTK7A
The Histone Acetyl Transferase Inhibitor VII, CTK7A controls the biological activity of Histone Acetyl Transferase. This small molecule/inhibitor is primarily used for Cell Structure applications.
别名:
Histone Acetyl Transferase Inhibitor VII, CTK7A, HAT Inhibitor VII, p300/CBP Inhibitor V, PCAF Inhibitor III, Sodium-4-(3,5-bis(4-hydroxy-3-methoxystyryl)-1H-pyrazol-1-yl)benzoate, HBC, Na, Sodium-4-(3,5-bis(4-hydroxy-3-methoxystyryl)-1H-pyrazol-1-yl)benzoate, HBC, Na, HAT Inhibitor VII, p300/CBP Inhibitor V, PCAF Inhibitor III
质量水平
方案
≥99% (HPLC)
表单
powder
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
protect from light
颜色
tan
溶解性
DMSO: 100 mg/mL
运输
ambient
储存温度
−20°C
SMILES字符串
OC1=CC=C(C=C1OC)/C=C/C2=CC(/C=C/C3=CC=C(O)C(OC)=C3)=NN2C4=CC=C(C=C4)C(O[Na])=O
相关类别
一般描述
A cell-permeable and water soluble hydrazinobenzoylcurcumin (HBC) compound that acts as a selective, reversible and mixed mode inhibitor of p300/CBP and PCAF histone acetyltransferases (IC50 ≤ 25 and 50 µM, respectively) with minimal activity towards other histone modifying enzymes like, G9a, CARM1, HDAC1, SIRT2 and TIP60 (IC50 >100 µM). Blocks the autoacetylation of p300 and PCAF and histone acetylation, downregulates cyclin E expression and induces senescence-like growth arrest at 100 µM in KB cells. Further, suppresses tumor growth in xenograft oral tumor nude mouse model (100 mg/kg, i.p., b.i.d.) and reduces H3K14 and H3K9 acetylation levels. Reported to potently inhibit bFGF-induced bovine aortic endothelial cells (BAECs) invasion and tube formation with an IC50 of 0.93 µM and binds to Ca2+/calmodulin with high-affinity (Kd = 8.11 µM) and antagonize its functions in HCT15 cells.
包装
Packaged under inert gas
其他说明
Arif, M., et al. 2010. Chem. Biol.17, 903.
Shim, J.S., et al. 2004. Chem. Biol.11, 1455.
Shim, J.S., et al. 2002. Bioorg. Med. Chem. Biol.10, 2439.
Shim, J.S., et al. 2004. Chem. Biol.11, 1455.
Shim, J.S., et al. 2002. Bioorg. Med. Chem. Biol.10, 2439.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
免责声明
Toxicity: Standard Handling (A)
储存分类代码
11 - Combustible Solids
WGK
WGK 2
闪点(°F)
Not applicable
闪点(°C)
Not applicable
Vignesh Ramesh et al.
EMBO molecular medicine, 15(12), e17836-e17836 (2023-09-28)
The epithelial-to-mesenchymal transition (EMT) plays a central role in the development of cancer metastasis and resistance to chemotherapy. However, its pharmacological treatment remains challenging. Here, we used an EMT-focused integrative functional genomic approach and identified an inverse association between short-chain
Johanna Diener et al.
Nature communications, 12(1), 5056-5056 (2021-08-22)
Melanoma cells rely on developmental programs during tumor initiation and progression. Here we show that the embryonic stem cell (ESC) factor Sall4 is re-expressed in the Tyr::NrasQ61K; Cdkn2a-/- melanoma model and that its expression is necessary for primary melanoma formation.
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