Retaspimycin
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Retaspimycin是水溶性的氢醌盐酸盐类Hsp90抑制剂[1]。
Hsp90是Hsp家族的成员,该蛋白家族的其它成员有Hsp40、Hsp70等等。这些蛋白作为分子伴侣,参与许多细胞内进程。当细胞暴露于应激时,一些蛋白变得不稳定,积累形成聚集体,随后引起细胞凋亡。在这种情况下,Hsps帮助其客户蛋白正确折叠,并伴随它们被转运到正确的位置,从而防止细胞凋亡。Hsps是癌细胞发展所需的,在许多癌细胞中过表达。因此,Hsp的抑制剂被认为是癌症治疗的有吸引力的疗法。作为Hsp90的抑制剂,retaspimycin通过与Hsp90 N端的ATP结合口袋相结合而起作用[1]。
在RPMI-8826和MM1.S细胞中,retaspimycin导致Hsp90客户蛋白的降解,如c-RAF和Her2。Retaspimycin也引起Hsp70水平的增加。除此之外,retaspimycin阻止RPMI-8826细胞分泌免疫球蛋白轻链。在trastuzumab抗性的乳腺癌细胞中,retaspimycin有效引起Her2的降解,导致肿瘤生长抑制和细胞凋亡[1]。
Retaspimycin常与其它药物联合用于癌症治疗。在GIST-882(胃肠道间质瘤)异种移植小鼠中,retaspimycin与imatinib联合使用具有显著效应,引起66%的肿瘤消退。在GIST-PSW异种移植小鼠中,retaspimycin与imatinib或sunitinib联合治疗具有有效的抗肿瘤活性,减少肿瘤负荷。在GIST-PSW和GIST-882小鼠模型中,当单独使用时,retaspimycin分别减少84%和69%的肿瘤体积。而且,retaspimycin减少这两个模型中的有丝分裂活动。然而,retaspimycin的抗肿瘤效应没有imatinib或sunitinib或其组合治疗的效果好[2]。
参考文献:
1. Hanson B E, Vesole D H. Retaspimycin hydrochloride (IPI-504): a novel heat shock protein inhibitor as an anticancer agent. 2009.
2. Floris G, Debiec-Rychter M, Wozniak A, et al. The heat shock protein 90 inhibitor IPI-504 induces KIT degradation, tumor shrinkage, and cell proliferation arrest in xenograft models of gastrointestinal stromal tumors. Molecular cancer therapeutics, 2011, 10(10): 1897-1908.
Storage | Store at -20°C |
M.Wt | 587.7 |
Cas No. | 857402-23-4 |
Formula | C31H45N3O8 |
Synonyms | IPI-504;IPI504;IPI 504,Retaspimycin |
Solubility | Soluble in DMSO |
Chemical Name | [(3R,5S,6R,7S,8E,10S,11S,12Z,14E)-6,20,22-trihydroxy-5,11-dimethoxy-3,7,9,15-tetramethyl-16-oxo-21-(prop-2-enylamino)-17-azabicyclo[16.3.1]docosa-1(22),8,12,14,18,20-hexaen-10-yl] carbamate |
SDF | Download SDF |
Canonical SMILES | CC1CC(C(C(C=C(C(C(C=CC=C(C(=O)NC2=CC(=C(C(=C2O)C1)NCC=C)O)C)OC)OC(=O)N)C)C)O)OC |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
描述 | Retaspimycin是热休克蛋白90(HSP90)的小分子抑制剂。 | |||||
靶点 | HSP90 | |||||
IC50 |