AG-490
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.
AG-490是一种酪氨酸激酶抑制剂[1]。
作为酪氨酸激酶抑制剂家族的一员，AG-490对多种激酶具有抑制活性。该物质可在 ALL病人的B细胞前体中抑制过度活跃的JAK2，在嗜酸细胞中抑制细胞因子诱导的JAK2活化，并可在蕈样肉芽肿源性T细胞中抑制STAT3活化。AG-490也可靶向JAK3及其下游STAT和MAPK信号通路。在IL-2依赖的T细胞系D10中，AG-490可抑制IL-2诱导的细胞增殖，IC50值为25 μM，且不影响IL-2R链表达。该物质也可抑制IL-2调控的STAT5a和STAT5b磷酸化，IC50值为50 μM-70 μM。此外，AG-490可降低IL-2诱导的DNA结合，对STAT5a/5b、STAT1和STAT3的程度分别为78%、65%和65%。所有结果表明，AG-490可能为抑制免疫病理病情带来有益的临床疗法[1]。
参考文献：
[1] Wang L H, Kirken R A, Erwin R A, et al. JAK3, STAT, and MAPK signaling pathways as novel molecular targets for the tyrphostin AG-490 regulation of IL-2-mediated T cell response. The Journal of Immunology, 1999, 162(7): 3897-3904.
- 1. Huilan Wang, Xiushan Feng, et al. "Role and mechanism of the p-JAK2/p-STAT3 signaling pathway in follicular development in PCOS rats." Gen Comp Endocrinol. 2022 Oct 3;330:114138. PMID: 36202220
- 2. HONGMEI QU, QUN YU, et al. "HIF-3α affects preeclampsia development by regulating EVT growth via activation of the Flt-1/JAK/STAT signaling pathway in hypoxia." Mol Med Rep. 2021 Jan;23(1):68. PMID: 33215219
- 3. Fei S, Li W, et al. "Protective Effect of Alprostadil on Acute Pancreatitis in Rats via Inhibiting Janus Kinase 2 (JAK2)/STAT3 Signal Transduction Pathway." Med Sci Monit. 2019 Oct 13;25:7694-7701. PMID: 31606729
- 4. Xin M, Jin X, et al. "Dipeptidyl peptidase-4 inhibition prevents vascular aging in mice under chronic stress: Modulation of oxidative stress and inflammation." Chem Biol Interact. 2019 Oct 2:108842. PMID: 31586451
- 5. Zhou H, Sun Y, et al. "Paris saponin VII extracted from trillium tschonoskii suppresses proliferation and induces apoptosis of human colorectal cancer cells." J Ethnopharmacol. 2019 Jul 15;239:111903. PMID: 31047966
- 6. Lan H, Su Y, et al. "Melatonin protects circulatory death heart from ischemia/reperfusion injury via the JAK2/STAT3 signalling pathway." Life Sci. 2019 Jul 1;228:35-46. PMID: 31028804
- 7. MXinwei Feng1, Junfeng Lu2, et al. "Mycobacterium smegmatis Induces Neurite Outgrowth and Differentiation in an Autophagy-Independent Manner in PC12 and C17.2 Cells." Front. Cell. Infect. Microbiol., 19 June 2018.
- 8. Wang L, Zhang F, et al. "CAFs enhance paclitaxel resistance by inducing EMT through the IL 6/JAK2/STAT3 pathway." Oncol Rep. 2018 May;39(5):2081-2090. PMID: 29565447
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 294.3 |
| Cas No. | 133550-30-8 |
| Formula | C17H14N2O3 |
| Synonyms | Tyrphostin B42 |
| Solubility | insoluble in H2O; ≥14.7 mg/mL in DMSO; ≥4.73 mg/mL in EtOH with gentle warming and ultrasonic |
| Chemical Name | (E)-N-benzyl-2-cyano-3-(3,4-dihydroxyphenyl)prop-2-enamide |
| SDF | Download SDF |
| Canonical SMILES | C1=CC=C(C=C1)CNC(=O)C(=CC2=CC(=C(C=C2)O)O)C#N |
| 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。 |
| Description | AG-490是一种酪氨酸激酶抑制剂，对JAK2、EGFR和ErbB2的IC50值分别为约10 μM、0.1 μM和13.5 μM。 | |||||
| 靶点 | JAK2 | EGFR | ErbB2 | |||
| IC50 | ～10 μM | 0.1 μM | 13.5 μM | |||
质量控制和MSDS
- 批次:
化学结构
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