PCI-34051 NEW
| Price | $55 | $97 | $195 |
| Package | 5mg | 10mg | 25mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-07 |
Product Details
| Product Name: PCI-34051 | CAS No.: 950762-95-5 |
| Purity: 99.14% | Supply Ability: 10g |
| Release date: 2024/11/07 |
Product Introduction
Bioactivity
| 名稱 | PCI-34051 |
| 描述 | PCI-34051 is an effective and selective HDAC8 inhibitor (IC50: 10 nM). |
| 細胞實驗 | Cell lines: A549 cell line,Ovcar-3 cell line. Concentrations: 5 μM. Incubation Time: 24 hours. Method: Tumor cell lines and human umbilical vein endothelial cells are cultured for at least two doubling times,and growth is monitored at the end of PCI-34051 exposure using an Alamar Blue fluorometric cell proliferation assay as recommended by the manufacturer.PCI-34051 is assayed in triplicate wells in 96-well plates.The concentration required to inhibit cell growth by 50% (GI50) and 95% confidence intervals are estimated from the nonlinear regression using a four-parameter logistic equation. |
| 激酶實驗 | Histone deacetylase activity:For PCI-34051 characterization, measurements are performed in a reaction volume of 100 μL using 96-well assay plates in a fluorescence plate reader. For each isozyme. The HDAC protein in reaction buffer (50 mM HEPES, 100 mM KCl, 0.001% Tween-20, 5% dimethyl sulfoxide, pH7.4, supplemented with bovine serum albumin at concentrations of 0-0.05%) is mixed with PCI-34051 at various concentrations and allowed to incubate for 15 min. Trypsin is added to a final concentration of 50 nM, and acetyl-Gly-Ala-(N-acetyl-Lys)-amino-4-methyl coumarin is added to a final concentration of 25-100 μM to initiate the reaction. After a 30 min lag time, the fluorescence is measured over a 30 min time frame using an excitation wavelength of 335 nm and a detection wavelength of 460 nm. The increase in fluorescence with time is used as the measure of the reaction rate. |
| 體外活性 | PCI-34051 has a good potency for HDAC8 (Ki: 10 nM). PCI-34051 has high specificity (about 5-fold) for HDAC8 relative to the other class I HDACs including HDAC1. PCI-34051 has higher 200-fold selectivity than HDAC1/6 and higher 1000-fold selectivity than HDAC2/3//10. PCI-34051 inhibits ovarian tumor line OVCAR-3 (GI50: 6 μM) and 15% cell death. Neither significant tubulin nor histone acetylation is observed in the sensitive cell lines treated with PCI-34051 (<25 μM) at 24 hours nor at earlier time points. PCI-34051 induces caspase-dependent apoptosis. When caspase-3 activity is measured at various times after treatment with 5 μM PCI-34051, increasing levels of activity are observed from 12 to 24 to 48 hours. PCI-34051 does not stimulate Bid cleavage. While J.RT3-T.5 and P116 are sensitive to PCI-34051, the PLCγ1-deficient J.gamma1 line shows a marked decrease in the extent of PCI-34051-induced apoptosis. Furthermore, steady-state calcium levels strongly influence the apoptosis induced by PCI-34051. PCI-34051 induces cytochrome c release from mitochondria. |
| 體內(nèi)活性 | Administration of PCI-34051 and Dexamethasone reduces eosinophilic inflammation and airway hyperresponsiveness in asthma, thereby mitigating airway remodeling [2]. |
| 存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 15 mg/mL (50.62 mM) 1eq. NaOH : 5.9 mg/mL (20 mM) |
| 關(guān)鍵字 | PCI34051 | Apoptosis | inhibit | HDAC | Histone deacetylases | Inhibitor | PCI-34051 |
| 相關(guān)產(chǎn)品 | Stavudine | Sodium 4-phenylbutyrate | Tributyrin |
| 相關(guān)庫 | 高選擇性抑制劑庫 | 經(jīng)典已知活性庫 | 表觀遺傳庫 | 抑制劑庫 | 抗衰老化合物庫 | 已知活性化合物庫 | 抗癌活性化合物庫 |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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