|
受注：045-509-1970 |
技術サポート：[email protected] 平日9:00〜18:00 1営業日以内にご連絡を差し上げます |
化学情報
|
Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
| 化学式 | C26H30N6O3 |
|||
| 分子量 | 474.55 | CAS No. | 1234480-50-2 | |
| Solubility (25°C)* | 体外 | DMSO | 80 mg/mL warmed with 50ºC water bath (168.58 mM) | |
| Water | Insoluble | |||
| Ethanol | Insoluble | |||
|
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
||||
溶剤液（一定の濃度）を調合する
生物活性
| 製品説明 | XMD8-92 is a potent and selective dual inhibitor of big map kinase (BMK1, ERK5) and bromodomain-containing proteins (BRDs, BET) with Kd of 80 nM and 170 nM for ERK5 and BRD4(1), respectively. |
|---|---|
| in vitro | XMD8-92, via inhibition of BMK1 activation, significantly induces p21 expression in cells, and mediates suppression of cancer cell proliferation. [1] XMD8-92 markedly abrogates the inhibitive effects of hydroxysafflor yellow A (HSYA) on hepatic stellate cell (HSC) activation, and blockes the HSYA-mediated MEF2C down-regulation. [2] |
| in vivo | XMD8-92 (50 mg/kg i.p.) significantly inhibit the growth of the xenografted human or syngeneic mouse tumors by blocking tumor cell proliferation and tumor-associated angiogenesis. [1] XMD8-92 inhibits pancreatic tumor xenograft growth by significant downregulation of DCLK1 and several of its downstream targets. [3] |
プロトコル(参考用のみ)
| キナーゼアッセイ | KiNativ Profiling Method | |
|---|---|---|
| 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 allowed for precise determination of % inhibition at each point. A manuscript describing the details of this targeted mass spectrometry approach is in preparation. | ||
| 動物実験 | 動物モデル | Nod/Scid mice bearing HeLa xenograft, C57Bl/6 mice bearing LL/2 xenograft |
| 投薬量 | ~50 mg/kg twice a day | |
| 投与方法 | i.p. | |
参考
カスタマーフィードバック
-
, , Int J Oncol, 2017, 51(1):91-103
-
Data from [Data independently produced by , , Oncotarget, 2014, 5(10): 3145-58]
-
Data from [Data independently produced by , , J Cell Physiol, 2014, 229(7): 856-67]
Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：
| GLP-1(7-36) protected against oxidative damage and neuronal apoptosis in the hippocampal CA region after traumatic brain injury by regulating ERK5/CREB [ Mol Biol Rep, 2024, 51(1):313] | PubMed: 38374452 |
| Protective effects of macrophage-specific integrin α5 in myocardial infarction are associated with accentuated angiogenesis [ Nat Commun, 2023, 10.1038/s41467-023-43369-x] | PubMed: 37985764 |
| Extracellular signal-Regulated Kinase 5 (ERK5) is required for the Yes-associated protein (YAP) co-transcriptional activity [ Cell Death Dis, 2023, 14(1):32] | PubMed: 36650140 |
| Extracellular signal-Regulated Kinase 5 (ERK5) is required for the Yes-associated protein (YAP) co-transcriptional activity [ Cell Death Dis, 2023, 14(1):32] | PubMed: 36650140 |
| Endothelial activation and fibrotic changes are impeded by laminar flow-induced CHK1-SENP2 activity through mechanisms distinct from endothelial-to-mesenchymal cell transition [ Front Cardiovasc Med, 2023, 10:1187490] | PubMed: 37711550 |
| Endothelial activation and fibrotic changes are impeded by laminar flow-induced CHK1-SENP2 activity through mechanisms distinct from endothelial-to-mesenchymal cell transition [ Front Cardiovasc Med, 2023, 10:1187490] | PubMed: 37711550 |
| Identification of a Novel ERK5 (MAPK7) Inhibitor, MHJ-627, and Verification of Its Potent Anticancer Efficacy in Cervical Cancer HeLa Cells [ Curr Issues Mol Biol, 2023, 45(7):6154-6169] | PubMed: 37504304 |
| Glucose Starvation or Pyruvate Dehydrogenase Activation Induce a Broad, ERK5-Mediated, Metabolic Remodeling Leading to Fatty Acid Oxidation [ Cells, 2022, 11(9)1392] | PubMed: 35563698 |
| ERK5 Is a Major Determinant of Chemical Sarcomagenesis: Implications in Human Pathology [ Cancers (Basel), 2022, 14(14)3509] | PubMed: 35884568 |
| Establishment and characterization of immortalized sweat gland myoepithelial cells [ Sci Rep, 2022, 12(1):7] | PubMed: 34997030 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。