Hypothemycin – 1 mg

Brand:
Cayman
CAS:
76958-67-3
Storage:
-20
UN-No:
Non-Hazardous - /

Hypothemycin is a resorcylic acid lactone polyketide originally isolated from H. tricothecoides that has diverse biological activities, including fungicidal, kinase inhibitory, and anticancer properties.{45253,45254,45255,45256,45257,45258} It is active against the pathogenic fungi P. litchii, completely inhibiting spore germination when used at a concentration of 0.78 µg/ml.{45254} Hypothemycin inhibits MEK (IC50 = 15 nM) and other protein kinases containing a conserved cysteine residue in the ATP-binding domain, including ERK, PDGFR, VEGFR, PKD1, and MAPKAP5/MK5.{45255,45256} It also inhibits transforming growth factor β-activated kinase 1 (TAK1) in vitro (IC50 = 33 nM).{45257} Hypothemycin inhibits proliferation of cancer cell lines dependent on activating mutations, including A549, MV-4-11, and EOL1 cells (IC50s = 6, 0.006, and 0.0004 µM, respectively) and reduces tumor growth in Ma44 and HCT116 mouse xenograft models when administered at a dose of 25 mg/kg per day.{45256,45258}  

 

Available on backorder

SKU: 27913 - 1 mg Category:

Description

A resorcylic acid lactone polyketide with diverse biological activities; active against the fungi P. litchii, completely inhibiting spore germination when used at a concentration of 0.78 µg/ml; inhibits MEK (IC50 = 15 nM) and other protein kinases containing a conserved cysteine residue in the ATP-binding domain, including ERK, PDGFR, VEGF, PKD1, and MAPKAP5/MK5; inhibits TAK1 (IC50 = 33 nM); inhibits proliferation of A549, MV-4-11, and EOL1 cells (IC50s = 6, 0.006, and 0.0004 µM, respectively); reduces tumor growth in Ma44 and HCT116 mouse xenograft models at 25 mg/kg per day


Formal name: (1aR,3S,4S,6Z,9S,15bR)-1a,8,9,15b-tetrahydro-3,4,12-trihydroxy-14-methoxy-9-methyl-3H-oxireno[k][2]benzoxacyclotetradecin-5,11(2H,4H)-dione

Synonyms:  NSC 354462

Molecular weight: 378.4

CAS: 76958-67-3

Purity: ≥98%

Formulation: A solid


Product Type|Biochemicals|Kinase Inhibitors|CaMKs||Product Type|Biochemicals|Kinase Inhibitors|PDGFR Family||Product Type|Biochemicals|Kinase Inhibitors|PKD & PKG||Product Type|Biochemicals|Kinase Inhibitors|RAS/RAF/MEK/ERK/MAPK||Product Type|Biochemicals|Kinase Inhibitors|VEGFR Family||Product Type|Biochemicals|Natural Products|Microbial Metabolites||Product Type|Biochemicals|Natural Products|Polyketides||Product Type|Biochemicals|Pesticides|Fungicides||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling|ERK/MAPK Signaling||Research Area|Cancer|Cell Signaling|Growth Factor Receptor Signaling