1. Protein Tyrosine Kinase/RTK
    MAPK/ERK Pathway
    Stem Cell/Wnt
  2. VEGFR
    MEK
    FLT3
    PDGFR
    ERK
  3. Hypothemycin

Hypothemycin 

Cat. No.: HY-107417
Handling Instructions

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.

For research use only. We do not sell to patients.

Hypothemycin Chemical Structure

Hypothemycin Chemical Structure

CAS No. : 76958-67-3

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Description

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[1][2].

IC50 & Target[2]

VEGFR2

10 nM (Ki)

VEGFR1

70 nM (Ki)

MEK1

17 nM (Ki)

MEK2

38 nM (Ki)

FLT-3

90 nM (Ki)

PDGFRα

1.5 μM (Ki)

PDGFRβ

900 nM (Ki)

ERK1

8.4 μM (Ki)

ERK2

2.4 μM (Ki)

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[2].

In Vivo

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[1].

Animal Model: Adult female Balb/c mice (weighing 18–22 g) infected with T. brucei[1]
Dosage: 10 mg/kg
Administration: Administered once daily via intraperitoneal injection for 7 days.
Result: Showed a dose-dependent reduction in parasitemia in infected mice.
Prolonged survival of infected mice over 30 days, with a cure rate of 33%.
Molecular Weight

378.37

Formula

C₁₉H₂₂O₈

CAS No.

76958-67-3

SMILES

COC1=CC(O)=C(C(O[[email protected]@H](C)C/C=C\C2=O)=O)C([[email protected]@H](O3)[[email protected]@]3([H])C[[email protected]](O)[[email protected]@H]2O)=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

HypothemycinVEGFRMEKFLT3PDGFRERKVascular endothelial growth factor receptorMitogen-activated protein kinase kinaseMAPKKMAP2KCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3Platelet-derived growth factor receptorExtracellular signal regulated kinasesfungalpolyketidemultikinaseVEGFR2VEGFR1MEK1MEK2FLT-3PDGFRβPDGFRαERK1ERK2eosinophilicAMLmelanomaHUVECmastocytomaNSCLCInhibitorinhibitorinhibit

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Hypothemycin
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