脂肪原/ONX 0914/AG-CR1-3674-M005/5毫克
商品编号：
AG-CR1-3674-M005
品牌：
Adipogen Inc
市场价：
¥2400.00
美元价：
1440.00
产品分类：
其他试剂
公司分类：
Other_reagents
联系Q Q：
3392242852
电话号码：
4000-520-616
电子邮箱：
info@ebiomall.com
商品介绍
| Product Details | |
|---|---|
| Synonyms | N-[2-(4-Morpholinyl)acetyl]-L-alanyl-O-methyl-N-[(1S)-2-[(2R)-2-methyl-2-oxiranyl]-2-oxo-1-(phenylmethyl)ethyl]-L-tyrosinamide; PR-957 |
| Product Type | Chemical |
| Properties | |
| Formula | C31H40N4O7 |
| MW | 580.7 |
| CAS | 960374-59-8 |
| Purity Chemicals | ≥98% |
| Appearance | White solid. |
| Solubility | Soluble in DMSO (30mg/ml), ethanol (20mg/ml) or DMF. Poorly soluble in aqueous solutions. |
| Other Product Data | Note: Warming and sonication may be required when dissolving the compound in the solvent of choice. |
| InChi Key | WQAVPPWWLLVGFK-VTNASVEKSA-N |
| Shipping and Handling | |
| Shipping | AMBIENT |
| Short Term Storage | +4°C |
| Long Term Storage | -20°C |
| Handling Advice | Keep cool and dry. |
| Use/Stability | Stable for at least 2 years after receipt when stored at -20°C. |
| Documents | |
| MSDS |
 Download PDF |
| Product Specification Sheet | |
| Datasheet |
Download PDF |
- Potent and selective 20S immunoproteasome inhibitor.
- Targets the β5i subunit [LMP7] of the 20S immunoproteasome (IC50=73nM) and with minimal cross-reactivity to the chymotrypsin-like β5 subunit of the constitutive 20S proteasome (IC50=1.04µM).
- Potent anti-inflammatory and anticancer agent. Inhibits production of pro-inflammatory cytokines and can induce apoptosis in vitro.
- Inhibits presentation of LMP7-specific, MHC-I-restricted antigens in vitro and in vivo, which consequently blocks production of interleukin-23 (IL-23) by activated monocytes and IFN-γ and IL-2 by T cells. Can also inhibit IL-17-producing T cells under TH17-polarizing conditions in vitro and reduce TH1 and TH17 cell differentiation in vivo.
- Shown to attenuate disease progression in several experimental models of autoimmune disorders, such as rheumatoid arthritis, inflammatory bowel disease and lupus, as well as in some hematologic malignancies and other cancer types.
Product References
- A selective inhibitor of the immunoproteasome subunit LMP7 blocks cytokine production and attenuates progression of experimental arthritis: T. Muchamuel, et al.; Nat. Med. 15, 781 (2009)
- Prevention of experimental colitis by a selective inhibitor of the immunoproteasome: M. Basler, et al.; J. Immunol. 185, 634 (2010)
- Immunoproteasome-specific inhibitors and their application: M. Basler & M. Groettrup; Methods Mol. Biol. 832, 391 (2012)
- Prophylactic and therapeutic efficacies of a selective inhibitor of the immunoproteasome for Hashimoto's thyroiditis, but not for Graves' hyperthyroidism, in mice: Y. Nagayama, et al.; Clin. Exp. Immunol. 168, 268 (2012)
- Immunoproteasome subunit LMP7 deficiency and inhibition suppresses Th1 and Th17 but enhances regulatory T cell differentiation: K.W. Kalim, et al.; J. Immunol. 189, 4182 (2012)
- Inhibition of the immunoproteasome ameliorates experimental autoimmune encephalomyelitis: M. Basler, et al.; EMBO Mol. Med. 6, 226 (2014)
- Interferon-γ-induced upregulation of immunoproteasome subunit assembly overcomes bortezomib resistance in human hematological cell lines: D. Niewerth, et al.; J. Hematol. Oncol. 7, 7 (2014)
- Bortezomib-resistant mutant proteasomes: structural and biochemical evaluation with carfilzomib and ONX 0914: E.M. Huber, et al.; Structure 23, 407 (2015)
- Inhibition of the Immunoproteasome Subunit LMP7 with ONX 0914 Ameliorates Graft-versus-Host Disease in an MHC-Matched Minor Histocompatibility Antigen-Disparate Murine Model: J. Zilberberg, et al.; Biol. Blood Marrow Transplant 21, 1555 (2015)
- PR-957, a selective inhibitor of immunoproteasome subunit low-MW polypeptide 7, attenuates experimental autoimmune neuritis by suppressing Th17-cell differentiation and regulating cytokine production: H. Liu, et al.; FASEB J. 31, 1756 (2017)
- Inhibition and deficiency of the immunoproteasome subunit LMP7 suppress the development and progression of colorectal carcinoma in mice: J. Koerner, et al.; Oncotarget (Epub ahead of print) (2017)
品牌介绍
Adipogen公司由三个子公司组成，分别是Adipogen,Inc.(韩国),AdipogenSA(瑞士)和 AdipogenCorporation(美国圣地亚哥)。总部设在美国，运营总部在瑞士利斯塔尔。Adipogen公司专门从事生命科学研究试剂的开发，如癌症、免疫、炎症、代谢疾病（糖尿病、肥胖）、干细胞和神经退行性疾病等领域。其重点关注开发创新优质的ELISA试剂盒。另外，也可提供抗体和蛋白产品，Adipogen拥有自己的化学实验室，致力于开发创新型小分子化合物。
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