Hypothemycin

Description

APIM050171: Hypothemycin, a fungal polyketide, is a multikinase inhibitor with Kis of 10/70 nM, 17/38 nM, 90 nM, 900 nM/1.5 μM, and 8.4/2.4 μM for VEGFR2/VEGFR1, MEK1/MEK2, FLT-3, PDGFRβ/PDGFRα, and ERK1/ERK2, respectively.

Background Information: A resorcylic acid lactone polyketide. It is a kinase inhibitor targeting mitogen-activated protein (MAP) kinase pathways at four levels: mitogen receptors, MAP kinase kinase (MEK)1/2 and ERK1/2, and certain downstream ERK substrates.

Target: ERK2

Ki: 2.4 μM

In Vitro: Hypothemycin inhibits eosinophilic EOL1 cell carrying mutations in FIP1L1-PDGFRα, acute myeloid leukemia MV-4-11 cell carrying mutations in FLT3-ITD, melanoma COLO829 cell carrying mutations in BRAF V600E, HUVEC cell carrying mutations in VEGFR, mastocytoma P815 cell carrying mutations in c-KIT D814Y, NSCLC A459 cell carrying mutations in KRAS, and ovarian SKOV-3 cell carrying mutations in HER2 with IC50s of 0.4 nM, 6 nM, 50 nM, 70 nM, 370 nM, 6.0 μM, and 7.0 μM, respectively.[1]

In Vitro: Hypothemycin (10 mg/kg) kills T. brucei in infected mice, completely curing the infection in one third of animals, although high doses of Hypothemycin (>10 mg/kg) leads to side effects.[2]

CAS No.: 76958-67-3

IUPAC/Chemical Name: (1aR,3S,4S,9S,15bR,Z)-3,4,12-trihydroxy-14-methoxy-9-methyl-3,4,8,9-tetrahydro-1aH-benzo[c]oxireno[2,3-e][1]oxacyclotetradecine-5,11(2H,15bH)-dione

Molecular Formula: C₁₉H₂₂O₈

Molecular Weight: 378.4

Purity: >96% (HPLC)
QC: 13C, 1H-NMR, MS and HPLC

Solubility: Soluble in DMSO, Acetone, Alcohols. Insoluble in water

Storage: Store at 0 °C (short term), -20 °C (long term), Desiccated

Note: Please contact for COA, Spectra, and SDS information.

Reference:
[1]. Hypothemycin, a fungal natural product, identifies therapeutic targets in Trypanosoma brucei
[2]. Targeted covalent inactivation of protein kinases by resorcylic acid lactone polyketides

 

Additional information

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Size	1 mg, 10 mg, 25 mg, 5 mg

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