Product Details
| Product Name:
Neflamapimod |
CAS No.:
209410-46-8 |
| Purity:
≥95% |
Supply Ability:
10g |
| Release date:
2024/11/17 |
Product Introduction
Bioactivity
| 名稱 | Neflamapimod |
| 描述 | Neflamapimod (VX-745) , a specific and effective inhibitor of p38α(IC50=10 nM), is 22-fold greater specificity against p38β and no inhibition activity to p38γ. |
| 細(xì)胞實(shí)驗(yàn) | BMSCs (5 × 104 cells/well) or MM cells (3 × 104 cells/well) are incubated in 96-well culture plates in the presence or absence of VX-745 for 48 hours at 37 °C. DNA synthesis is measured by [3H]-thymidine ([3H]TdR) uptake. Cells are pulsed with [3H]TdR (0.5 μCi/well [.0185 MBq]) during the last 8 hours of 48-hour cultures. Growth inhibition of both MM cells and BMSCs by VX-745 is also assessed by measuring 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) dye absorbance.(Only for Reference) |
| 激酶實(shí)驗(yàn) | Spectrophotometric coupled-enzyme assay: The IC50 for the inhibition of p38α and p38β homologs are obtained by a spectrophotometric coupled-enzyme assay. A fixed concentration of enzyme (15 nM of p38α or p38β) is incubated with VX-745 in DMSO for 10 min. at 30 °C in 0.1 M HEPES buffer, pH 7.5, containing 10% glycerol, 10 mM MgCl2, 2.5 mM phosphoenolpyruvate, 200 μM NADH, 150 μg/mL pyruvate kinase, 50 μg/mL lactate dehydrogenase, and 200 μM EGF receptor peptide (KRELVEPLTPSGEAPNQALLR). The reaction is initiated with 100 μM and 70 μM ATP for p38α and p38β assays, respectively. The decrease of absorbance at 340 nm is monitored to follow the rate of the reaction. IC50 is evaluated from the rate data as a function of the inhibitor concentration. |
| 體外活性 | Neflamapimod selectively inhibits p38α and p38β MAPK with IC50 of 10 nM and 220 nM, respectively, but not p38γ MAPK and a large panel of other kinases, with IC50 larger than 20 μM. In a human peripheral blood mononuclear cell (PBMC) assay, Neflamapimod provides IC50 of 56 and 52 nM for IL-1β and TNFα, respectively. Neflamapimod blocks IL-6 and IL-8 production induced by IL-1 and TNFα, and COX-2 synthesis mediated by LPS and IL-1β. [1-3] Neflamapimod (60 nM-20 μM) inhibits IL-6 and VEGF secretion in bone marrow stromal cells (BMSCs), without affecting their viability. Neflamapimod also inhibits TNF-α-induced IL-6 secretion in BMSCs. Neflamapimod inhibits both multiple myeloma (MM) cell proliferation and IL-6 secretion in BMSCs triggered by adherence of MM cells to BMSCs, suggesting that Neflamapimod can inhibit paracrine multiple myeloma (MM) cell growth in the BM milieu and overcome cell adhesion-related drug resistance. [4] |
| 體內(nèi)活性 | Neflamapimod is effective against adjuvant-induced arthritis (AA) in the rat with ED50 of 5 mg/kg. Histological scores for Neflamapimod in AA rats are 93% inhibition of bone resorption and 56% inhibition of inflammation. In the classical cartilage-induced arthritis model, Neflamapimod exhibits a dose-responsive decrease in severity score. [1-3] In a type II collagen-induced arthritis (CIA) mice model, Neflamapimod (2.5, 5, and 10 mg/kg) has 27%, 31%, and 44% improvement in the inflammatory scores, respectively, when compared to vehicle-treated mice. In addition, histological scores show a 32-39% protection of bone and cartilage erosion by Neflamapimod. [5] |
| 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 : 43.6 mg/mL (100 mM)
|
| 關(guān)鍵字 | Inhibitor | VX 745 | VX745 | Neflamapimod | Autophagy | inhibit | p38 MAPK |
| 相關(guān)產(chǎn)品 | Stavudine | Xylitol | Myricetin | Sodium 4-phenylbutyrate | Hydroxychloroquine | Guanidine hydrochloride | Taurine | Curcumin | Oxyresveratrol | Paeonol | Naringin | Gefitinib |
| 相關(guān)庫 | 高選擇性抑制劑庫 | 神經(jīng)退行性疾病化合物庫 | 疼痛相關(guān)化合物庫 | 經(jīng)典已知活性庫 | 激酶抑制劑庫 | 藥物功能重定位化合物庫 | 抑制劑庫 | 抗衰老化合物庫 | 已知活性化合物庫 | 抗癌藥物庫 |
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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Recommended supplier
| Product name |
Price |
|
Suppliers |
Update time |
|
|
$/ |
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Anhui Ruihan Technology Co., Ltd
|
2023-08-21 |
United States