H1667

Hypothemycin

from Hypomyces trichothecoides, ≥98% (HPLC)

• 同義詞: 3H-Oxireno[k][2]benzoxacyclotetradecin-5,11(2H,4H)-dione,1a,8,9,15b-tetrahydro-3,4,12-trihydroxy-14-methoxy-9-methyl-,(1aR,3S,4S,6Z,9S,15bR)-, NSC354462
• 經驗公式（希爾表示法）: C₁₉H₂₂O₈
• CAS號碼: 76958-67-3
• 分子量：: 378.37
• MDL號碼: MFCD08457932
• 分類程式碼代碼: 51111800
• PubChem物質ID: 329815176
• NACRES: NA.77

屬性

• 生物源: Hypomyces trichothecoides
• 品質等級: 200
• 化驗: ≥98% (HPLC)
• 溶解度: DMSO: soluble; acetone: soluble; deionized water: insoluble
• 儲存溫度: −20°C
• SMILES 字串: COc1cc(O)c2C(=O)O[C@@H](C)CC=CC(=O)[C@@H](O)[C@@H](O)CC3OC3c2c1
• InChI: 1S/C19H22O8/c1-9-4-3-5-12(20)17(23)14(22)8-15-18(27-15)11-6-10(25-2)7-13(21)16(11)19(24)26-9/h3,5-7,9,14-15,17-18,21-23H,4,8H2,1-2H3/b5-3-/t9-,14-,15+,17+,18+/m0/s1
• InChI 密鑰: SSNQAUBBJYCSMY-KNTMUCJRSA-N

描述

生化／生理作用

Hypothemycin, one of the highly oxygenated analogues in the group of 14-membered resorcylic acid lactones (RAL), has minor antifungal and cytotoxic activity and exhibits an in vitro anti-malarial activity with an IC₅₀ of 2.2 μg/mL. Hypothemycin is also reported to selectively and irreversibly inhibit protein kinases that contain a conserved cysteine residue (Cys¹⁶⁶) that is located within the ATP-binding domain. Though this group accounts for less then 10% of all identified kinases, there are several targets implicated in aberrant cellular proliferation such as ERKs, MEK, FMS-like tyrosine kinase protein (FLT), and platelet-derived growth factor receptors (PDGFR). In cell culture, hypothemycin displays potent cytotoxicity against cancer cell lines that are dependent on certain activating kinase mutations. Additionally, hypothemycin demonstrates significant tumor growth inhibition in at least three separate murine xenograft models. Hypothemycin also inhibits the production of several cytokines such as IL2, IL6, IFNγ, and TNFα.

安全資訊

• 象形圖: GHS07
• 訊號詞: Warning
• 危險聲明: H302
• 防範說明: P301 + P312 + P330
• 危險分類: Acute Tox. 4 Oral
• 儲存類別代碼: 11 - Combustible Solids
• 水污染物質分類（WGK）: WGK 3
• 閃點（°F）: Not applicable
• 閃點（°C）: Not applicable