XMD8-92 NEW
| Price | $48 | $68 | $133 |
| Package | 5mg | 10mg | 25mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-17 |
Product Details
| Product Name: XMD8-92 | CAS No.: 1234480-50-2 |
| Purity: 98.19% | Supply Ability: 10g |
| Release date: 2024/11/17 |
Product Introduction
Bioactivity
| 名稱 | XMD8-92 |
| 描述 | XMD8-92 is an effective and specific BMK1/ERK5 inhibitor (Kd: 80 nM). |
| 激酶實(shí)驗(yàn) | KiNativ profiling of XMD8-92 is carried out with both an ATP and ADP acylphosphate-desthiobiotin with the following modifications. HeLa cell lysates (5 mg/mL total protein) are incubated in the presence of XMD8-92 at 50 μM, 10 μM, 2 μM, 0.8 μM, and 0 μM for 15 minutes prior to addition of the ATP or ADP acylphosphate probe (5 μM final probe concentration). All reactions are performed in duplicate. Probe reactions proceeded for 10 minutes and the reaction stopped by the addition of urea and processed for MS analysis. Samples are analyzed by LC-MS/MS on a linear ion trap mass spectrometer using a time segmented "target list" designed to collect MS/MS spectra from all kinase peptide-probe conjugates that can be detected in HeLa cell lysates. This target list is generated and validated by prior exhaustive analysis of HeLa lysates. Up to four characteristic fragment ions for each kinase peptide-probe conjugate are used to extract signals for each kinase, and a comparison of inhibitor treated to control (untreated) lysates allow for precise determination of % inhibition at each point. A manuscript describing the details of this targeted mass spectrometry approach is in preparation[1]. |
| 體外活性 | XMD8-92 significantly inhibits the growth of pancreatic tumor xenografts by downregulating DCLK1 and several of its downstream targets. At a dose of 50 mg/kg, administered intraperitoneally (i.p.), XMD8-92 blocks tumor cell proliferation and tumor-associated angiogenesis, resulting in significant suppression of tumor growth in both xenografted human and syngeneic mouse models. |
| 體內(nèi)活性 | Hydroxysafflor yellow A (HSYA) inhibits the activation of hepatic stellate cells, while XMD8-92 can significantly block this inhibition and prevent the HSYA-mediated downregulation of MEF2C. By inhibiting the activation of BMK1, XMD8-92 significantly induces the expression of p21 in cells and inhibits the proliferation of cancer cells. |
| 存儲(chǔ)條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 19 mg/mL (40 mM) |
| 關(guān)鍵字 | Extracellular signal regulated kinases | XMD-8-92 | bFGF | Inhibitor | promyelocytic | XMD8 92 | protein | cancer | XMD892 | Epigenetic Reader Domain | inhibit | leukemia | ERK | XMD8-92 | HMEC |
| 相關(guān)產(chǎn)品 | TBHQ | ABBV-744 | Notoginsenoside R1 | 3-methyl-1,2,3,4-tetrahydroquinazolin-2-one | (+)-JQ-1 | Lidocaine | Astragaloside IV | Curcumin | Lidocaine hydrochloride | Honokiol | Tauroursodeoxycholate | Naphthol AS-E |
| 相關(guān)庫(kù) | 高選擇性抑制劑庫(kù) | DNA 損傷和修復(fù)分子庫(kù) | 疼痛相關(guān)化合物庫(kù) | 經(jīng)典已知活性庫(kù) | 激酶抑制劑庫(kù) | 抗卵巢癌化合物庫(kù) | 抑制劑庫(kù) | 抗衰老化合物庫(kù) | 已知活性化合物庫(kù) | 抗癌活性化合物庫(kù) |
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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United States- Since: 2011-01-07
- Address: 36?Washington?Street, Wellesley?Hills
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