CCF642 NEW
| Price | $30 | $43 | $77 |
| Package | 1mg | 2mg | 5mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-11 |
Product Details
| Product Name: CCF642 | CAS No.: 346640-08-2 |
| Purity: 98.82% | Supply Ability: 10g |
| Release date: 2024/11/11 |
Product Introduction
Bioactivity
| 名稱(chēng) | CCF642 |
| 描述 | CCF642 (AC1LYELL) is a novel PDI-inhibiting compound with antimyeloma activity. |
| 激酶實(shí)驗(yàn) | Inhibition of CB-839 on rHu-GAC: The enzymatic activity is measured in assay buffer containing 50 mM Tris-Acetate pH 8.6, 150 mM K2HPO4 , 0.25 mM EDTA, 0.1 mg/mL bovine serum albumin, 1 mM DTT, 2 mM NADP+ and 0.01% Triton X-100. To measure inhibition, the inhibitor (prepared in DMSO) is first pre-mixed with glutamine and glutamate dehydrogenase (GDH) and reactions are initiated by the addition of rHu-GAC. Final reactions contains 2 nM rHu-GAC, 10 mM glutamine, 6 units/mL GDH and 2% DMSO. Generation of NADPH is monitored by fluorescence (Ex340/Em460 nm) every minute for 15 minutes on a SpectraMax M5e plate reader. Relative fluorescence units (RFU) are converted to units of NADPH concentration (μM) using a standard curve of NADPH. Each assay plate incorporates control reactions that monitores the conversion of glutamate (1 to 75 μM) plus NADP+ to α-ketoglutarate plus NADPH by GDH. Under these assay conditions, up to 75 μM glutamate is stoichiometrically converts to α-ketoglutarate/NADPH by GDH. Initial reaction velocities are calculated by fitting the first 5 minutes of each progress curve to a straight line. Inhibition curves are fitted to a four-parameter dose response equation of the form: % activity = Bottom + (Top-Bottom)/(1+10^((LogIC50-X)*HillSlope)). |
| 體外活性 | In vitro, CCF642 inhibits PDI reductase activity about 100-fold more potently than the structurally distinct established inhibitors PACMA 31 and LOC14. Computational modeling suggests a novel covalent binding mode in active-site CGHCK motifs. CCF642 causes acute ER stress in multiple myeloma cells accompanied by apoptosis-inducing calcium release[1]. |
| 體內(nèi)活性 | CCF642 displays potent efficacy in an aggressive syngeneic mouse model of multiple myeloma and prolongs the lifespan of C57BL/KaLwRij mice engrafted with 5TGM1-luc myeloma, an effect comparable to the first-line multiple myeloma therapeutic bortezomib[1]. |
| 存儲(chǔ)條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 11.11 mg/mL (29.36 mM), Sonication is recommended. |
| 關(guān)鍵字 | calcium | Inhibitor | PDI | apoptosis | isomerases | disulfide | CCF 642 | myeloma | protein | multiple | release | CCF-642 | CCF642 | stress | inhibit | anti-multiple |
| 相關(guān)庫(kù) | 經(jīng)典已知活性庫(kù) | 內(nèi)質(zhì)網(wǎng)應(yīng)激化合物庫(kù) | 血液病分子庫(kù) | 抑制劑庫(kù) | 已知活性化合物庫(kù) | 共價(jià)抑制劑庫(kù) | 抗代謝疾病化合物庫(kù) |
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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$30.00 / 5mg
Recommended supplier
| Product name | Price | Suppliers | Update time | |
|---|---|---|---|---|
| $/ |
Anhui Ruihan Technology Co., Ltd
|
2023-08-21 |
United States- Since: 2011-01-07
- Address: 36?Washington?Street, Wellesley?Hills
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