MCE 的所有產品僅用作科學研究或藥證申報，我們不為任何個人用途提供產品和服務。

Retaspimycin Hydrochloride

CAS No. : 857402-63-2

產品活性：Retaspimycin Hydrochloride is a potent inhibitor of Hsp90 with EC₅₀s of 119 nM for both Hsp90 and Grp9.

研究領域：Cell Cycle/DNA Damage  |  Metabolic Enzyme/Protease

作用靶點：HSP

In Vitro: Retaspimycin (IPI-504) is a novel and highly soluble analog of 17AAG, an inhibitor of Hsp90. Retaspimycin can abrogate both the unfolded protein response element (UPRE) and ERSE-driven luciferase activity in non-treated U266 and MM.1s cells as well as in Tunicamycin (Tm)-treated cells. The IC₅₀s for the inhibition of reporter gene activity by Retaspimycin are 196±56 nM in U266 and 472±177 nM in MM.1s for UPRE-luc activity and 213±140 nM for the ERSE-driven activity in MM.1s cells. Retaspimycin treatment leads to a dose-dependent decrease of p50ATF6 with EC₅₀ of 237 nM, consistent with the reporter-gene assay. The level of sXBP1 is decreased in the presence of Retaspimycin with an apparent EC₅₀ between 300 nM and 1 μM. Incubation of Retaspimycin (IPI-504) potently suppresses both Akt and MAPKs phosphorylation in both sensitive and Trastuzumab-resistant cells. Total levels of Akt decreased in all 4 cell lines (BT474, SKBR-3, HCC1569, and HCC1569) in a dose-dependent manner. However, levels of total MAPKs are not significantly altered with Retaspimycin treatment.

In Vivo: Retaspimycin (IPI-504) and Trastuzumab independently induce tumor regression of Trastuzumab-sensitive BT474 cell-derived xenografts. Xenografts derived from BT474R cells continue to grow in the presence of Trastuzumab but are still sensitive to Retaspimycin. When used in combination, Retaspimycin and Trastuzumab add only marginal benefits to Retaspimycin monotherapy. Retaspimycin (100 mg/kg) as a single agent is more efficacious than Trastuzumab in inhibiting tumor growth in HCC1569 xenografts. The combination is not significantly superior to Retaspimycin used as a single agent.

相關產品：Covalent Screening Library Plus  |  Drug Repurposing Compound Library Plus  |  Clinical Compound Library Plus  |  Bioactive Compound Library Plus  |  Cell Cycle/DNA Damage Compound Library  |  Metabolism/Protease Compound Library  |  Anti-Cancer Compound Library  |  Clinical Compound Library  |  Anti-Aging Compound Library  |  Drug Repurposing Compound Library  |  Covalent Screening Library  |  Endoplasmic Reticulum Stress Compound Library  |  Pyroptosis Compound Library  |  Cytoskeleton Compound Library  |  Rare Diseases Drug Library  |  Anti-Prostate Cancer Compound Library  |  Membrane Protein-targeted Compound Library  |  Hsp90-IN-17  |  Palmitic acid  |  HSP90-IN-18  |  Paeoniflorin  |  Pimitespib  |  Debio 0932  |  KU-177  |  AMP-PCP disodium  |  Tamoxifen  |  JG-231  |  MPC-0767  |  HDAC6/HSP90-IN-1  |  Retaspimycin  |  Onalespib  |  HM03  |  EC144  |  2-Hexyl-4-pentynoic acid  |  Cucurbitacin D  |  NCT-58  |  MKT-077  |  Cemdomespib  |  6BrCaQ-C10-TPP  |  Rocaglamide  |  Novobiocin  |  Aminohexylgeldanamycin hydrochloride  |  Gedunin  |  KBU2046  |  HSF1A

熱門產品線：重組蛋白  |  化合物庫  |  天然產物  |  熒光染料  |  PROTAC  |  同位素標記物  |  寡核苷酸  |  抗體  |  點擊化學

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Fluorescent Dye  |  PROTAC  |  Isotope-Labeled Compounds  |  Oligonucleotides  |  Antibodies  |  Click Chemistry

品牌介紹:
•   MCE (MedChemExpress) 擁有200 多種*僅有化合物庫，我們致力于為*科研客戶提供前沿的高品質小分子活性化合物；
•   50,000 多種高選擇性抑制劑、激動劑涉及各熱門信號通路及疾病領；
•   產品種類涵蓋各種重組蛋白，多肽，常用試劑盒 ，更有 PROTAC、ADC 等特色產品，廣泛應用于新藥研發、生命科學等科研項目；
•   提供虛擬篩選，離子通道篩選，代謝組學分析檢測分析，藥物篩選等專業技術服務；
•   設有專業的實驗中心和嚴格的質控、驗證體系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各項質檢報告，確保產品的高純度、高品質；
•   產品的生物活性多經各國客戶實驗驗證；
•   Nature, Cell, Science 等多種頂級期刊及制藥 Patent 收錄了MCE客戶的科研成果；
•   專業團隊跟蹤新的制藥及生命科學研究進展，為您提供*新的活性化合物；
•   與世界各大制藥公司及*科研機構建立了長期的合作。