Product Details
| Product Name:
CNX-1351 |
CAS No.:
1276105-89-5 |
| Purity:
99.69% |
Supply Ability:
10g |
| Release date:
2024/11/16 |
Product Introduction
Bioactivity
| 名稱 | CNX-1351 |
| 描述 | CNX-1351 is a potent, isoform-selective, and targeted covalent inhibitor of PI3Kα. |
| 激酶實(shí)驗(yàn) | Biochemistry assay: The motor domains of KSP (amino acids 1–360) is expressed as in Escherichia coli BL21(DE3) as COOH-terminal 6-his fusion proteins. Bacterial pellets are lysed in a microfluidizer with a lysis buffer [50 mM Tris-HCl; 50 mM KCl, 10 mM imidazole, 2 mM MgCl2, 8 mM β-mercaptoethanol, 0.1 mM ATP (pH 7.4)], and proteins are purified using Ni-NTA agarose affinity chromatography, with an elution buffer consisting of 50 mM PIPES, 10% sucrose, 300 mM imidazole, 50 mM KCl, 2 mM MgCl2, mM β-mercaptoethanol, and 0.1 mM ATP (pH 6.8). Steady-state measurements of ATPase activity are performed with a pyruvate kinase–lactate dehydrogenase detection system that coupled the appearance of ADP with oxidation of NADH. Absorbance changes are monitored at 340 nm. All biochemical experiments are performed in PEM25 buffer [25 mM Pipes/KOH (pH 6.8), 2 mM MgCl2, 1 mM EGTA] supplemented with 10 μM SB 743921 for experiments involving microtubules. Rates of ADP release are measured in a stopped-flow apparatus; the decrease in fluorescence of MANT-ATP is monitored. Rates of Pi release are measured in a stopped-flow apparatus, using bacterial phosphate binding protein modified with 7-diethylamino-3-((((2 maleimidyl)ethyl)amino)carbonyl)coumarin (MDCC) dye. Ki estimates of KSP inhibitors are extracted from the dose–response curves, with explicit correction for enzyme concentration. Tubulin polymerization by measuring changes in absorbance at 340 nm is monitored. The assay is performed in 100-μL volumes in 96-well half-area microtiter plates, using a microplate reader with the incubation temperature set at 37 °C. |
| 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 : 5.73 mg/mL (9.99 mM)
|
| 關(guān)鍵字 | PI3K | Phosphoinositide 3-kinase | Inhibitor | inhibit | CNX-1351 | CNX1351 | CNX 1351 |
| 相關(guān)產(chǎn)品 | Myricetin | Erucic acid | Sapanisertib | (2S,3R,4S)-4-Hydroxyisoleucine | 3-Methyladenine | Duvelisib (R enantiomer) hydrochloride | Isoprenaline hydrochloride | Quercetin | Quercetin Dihydrate | Apilimod | LY294002 | Idelalisib |
| 相關(guān)庫 | 糖酵解化合物庫 | 經(jīng)典已知活性庫 | 激酶抑制劑庫 | 抗肥胖化合物庫 | 抗卵巢癌化合物庫 | 血管生成庫 | 抑制劑庫 | NO PAINS 化合物庫 | 抗衰老化合物庫 | 已知活性化合物庫 | 抗癌化合物庫 | 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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