应用；   An antifungal selective inhibitor of MEK  

CAS号码:   76958-67-3  

纯度:   ≥97%  

分子量:   378.37  

分子式:   C₁₉H₂₂O₈  

* 参考分析证明 大量特定数据 (包括水 含量).

介绍 技术信息 安全信息 安全技术说明书和分析证明书

Hypothemycin exhibits antifungal and cytotoxic activity against some tumor cell lines partly attributed to inhibition of Ras-inducible genes. Hypothemycin facilitates the ubiquitinylation process of cyclin D1. Hypothemycin has been identified as a potent and selective inhibitor of threonine/tyrosine-specific kinase, MEK, and other protein kinases that contain a conserved cysteine residue in the ATP-binding site in in vitro studies.

参考文献

1. Sonoda, H., et al., 1999. Suppression of oncogenic transformation by hypothemycin associated with accelerated cyclin D1 degradation through ubiquitin-proteasome pathway. Life sciences. 65(4): 381-94. PMID: 10421424
2. Tanaka, H., et al., 1999. Antitumor efficacy of hypothemycin, a new Ras-signaling inhibitor. Japanese journal of cancer research : Gann. 90(10): 1139-45. PMID: 10595743
3. Camacho, R., et al., 1999. Hypothemycin inhibits the proliferative response and modulates the production of cytokines during T cell activation. Immunopharmacology. 44(3): 255-65. PMID: 10598882
4. Zhao, A., et al., 1999. Resorcylic acid lactones: naturally occurring potent and selective inhibitors of MEK. The Journal of antibiotics. 52(12): 1086-94. PMID: 10695671
5. Schirmer, Andreas., et al., 2006. Targeted covalent inactivation of protein kinases by resorcylic acid lactone polyketides. Proceedings of the National Academy of Sciences of the United States of America. 103(11): 4234-9. PMID: 16537514
6. Winssinger, Nicolas., et al., 2007. Chemistry and biology of resorcylic acid lactones. Chemical communications (Cambridge, England). (1): 22-36. PMID: 17279252

物理状态 :

Solid

来源于 :

Phoma sp

溶解度 :

Soluble in DMSO (10 mg/ml), and acetone. Insoluble in water, methanol, and deionized water.

保存 :

Store at -20° C

熔点 :

251.29° C (Predicted)

沸点 :

~667.8° C at 760 mmHg (Predicted)

密度 :

~1.3 g/cm    ³ (Predicted)

折射率 :

n    ²⁰    _D 1.57 (Predicted)

IC50 :

Growth of HT29 cells: IC    ₅₀ = 0.08 mM; Growth of HCT116 cells: IC    ₅₀ = 0.90 mM

仅供科研使用。不可用于诊断或治疗。  

德国水公害等级 :

3

PubChem CID :

5477775

MDL 号码 :

MFCD08457932

SMILES :

CC1C/C=C/C(=O)C2C(O2)CC(C(C3=CC(=CC(=C3C(=O)O1)O)OC)O)O