MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

NVP-HSP990

CAS No. : 934343-74-5

MCE 站：NVP-HSP990

产品活性：NVP-HSP990 是一种有效的，选择性的 Hsp90 抑制剂，对 Hsp90α，Hsp90β 和 Grp94 的 IC₅₀ 值分别为 0.6，0.8 和 8.5 nM。

研究领域：Cell Cycle/DNA Damage  |  Metabolic Enzyme/Protease  |  Apoptosis

作用靶点：HSP  |  Apoptosis

In Vitro: NVP-HSP990 is a potent ａnd selective Hsp90 inhibitor, with IC₅₀ values of 0.6, 0.8, ａnd 8.5 nM for Hsp90α, Hsp90β, ａnd Grp94, respectively. NVP-HSP990 (10 μM) shows no affect the ATPase activity of topoisomerase II, a GHKL (Gyrase, Hsp90, Histidine Kinase, MutL) family ATPase, closely related to Hsp90. NVP-HSP990 also exerts efficient effects on c-Met, Hsp70, p-ERK ａnd p-AKT in CTL-16 cells, with EC₅₀s of 37 ± 4, 20 ± 2, 11 ± 1, ａnd 6 ± 1 nM, respectively. NVP-HSP990 suppresses the proliferation of BT474, A549, H1975 ａnd MV4;11 cells, with GI₅₀s of 7 ± 2, 28 ± 5, 35 ± 4, ａnd 4 ± 1 nM, respectively. NVP-HSP990 inhibits cellular proliferation of GTL-16, with an EC₅₀ of 14 nM. NVP-HSP990 (5-500 nM) inhibits the multiple myeloma cell lines, with IC₅₀s of 27-49 nM after treatment for 72 h. NVP-HSP990 induces apoptosis in multiple myeloma cell lines (0-100 nM), leads to cell cycle arrest in the G2/M phase (25-200 nM), ａnd induces apoptosis via caspase-8 followed by caspase-3 activation (100 nM). NVP-HSP990 increases HSP70 expression ａnd interacts with Akt ａnd ERK signaling. Moreover, NVP-HSP990 (100 nM) in combination with melphalan, causes synergistic effects on growth inhibition in multiple myeloma cells ａnd increases cleavage of caspase-3, caspase-8, ａnd caspase-9 ａnd activates caspase-2.

In Vivo: NVP-HSP990 (2.5 to 5 mg/kg twice weekly, or 5 to 15 mg/kg weekly, p.o.) causes dose proportional antitumor efficacy, without obvious loss or overt signs of toxicity in a GTL-16 tumor bearing mice. NVP-HSP990 (5 or 10 mg/kg weekly, p.o.) also results in significant inhibition of tumor growth in BT-474 breast cancer model. NVP-HSP990 (5 mg/kg twice weekly or 15 mg/kg weekly, p.o.) inhibits the growth of tumor in the MV4;11 xenograft model. Furthermore, NVP-HSP990 (0.5 mg/kg every day, 14, 5 mg/kg twice weekly, or 15 mg/kg weekly, p.o.) displays antitumor efficacy in H1975 ａnd A549 tumor models. NVP-HSP990 (5, 15 mg/kg, p.o.) shows prolonged suppression of c-Met levels with 30% ａnd 50% reduction ａnd exhibits antitumor activities in GTL-16 tumor xenograft.

相关产品：Clinical Compound Library Plus  |  Bioactive Compound Library Plus  |  Apoptosis Compound Library  |  Cell Cycle/DNA Damage Compound Library  |  Metabolism/Protease Compound Library  |  Anti-Cancer Compound Library  |  Clinical Compound Library  |  Anti-Aging Compound Library  |  Endoplasmic Reticulum Stress Compound Library  |  Pyroptosis Compound Library  |  Cytoskeleton Compound Library  |  Anti-Breast Cancer Compound Library  |  Anti-Blood Cancer Compound Library  |  MG-132  |  LY294002  |  Doxorubicin hydrochloride  |  Bafilomycin A1  |  Y-27632 dihydrochloride  |  Paclitaxel  |  Acetylcysteine  |  Angiotensin II human  |  Staurosporine  |  Bortezomib  |  5-Fluorouracil  |  Sorafenib  |  Tamoxifen  |  SP600125  |  Trametinib  |  2-Deoxy-D-glucose  |  Gemcitabine  |  Temozolomide  |  MK-2206 dihydrochloride  |  Verteporfin  |  Decitabine  |  Actinomycin D  |  Etoposide  |  Pexidartinib  |  BAY 11-7082  |  CCCP  |  DAPT  |  Ruxolitinib  |  Mitomycin C

品牌介绍:
•   MCE (MedChemExpress) 拥有数百种全球独家化合物，我们致力于为全球科研客户提供*新*全的高品质小分子活性化合物；
•   10,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领域；
•   设有专业的实验中心和严格的质控、验证体系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；
•   产品的生物活性多经各国客户实验验证；
•   Nature, Cell, Science 等多种期刊及制药收录了MCE客户的科研成果；
•   专业团队跟踪*新的制药及生命科学研究进展，为您提供全球*新的活性化合物；
•   与世界各大制药公司及知名科研机构建立了长期的合作。