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Hypothemycin

Catalog No. T15542 CAS 76958-67-3

Hypothemycin is a fungal polyketide and is a multikinase inhibitor (Kis: 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).

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Hypothemycin, CAS 76958-67-3

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Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Hypothemycin is a fungal polyketide and is a multikinase inhibitor (Kis: 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).
Targets&IC50	MEK2:38 nM (ki), PDGFRβ:900 nM （ki）, PDGFRα:1.5 μM （ki）, ERK2:2.4 μM （ki）, FLT-3:90 nM （ki）, MEK1:17 nM (ki), ERK1:8.4 μM （ki）, VEGFR1:70 nM (ki), VEGFR2:10 nM (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, and melanoma COLO829 cell carrying mutations in BRAF V600E. It has an IC50s of 0.4 nM, 6 nM, and 50 nM, respectively. Hypothemycin also inhibits 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 (IC50s: 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. However, it completely curing the infection in one third of animals, although high doses of Hypothemycin (>10 mg/kg) leads to side effects.

Molecular Weight	378.37
Formula	C19H22O8
CAS No.	76958-67-3

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Schirmer A, et al. Targeted covalent inactivation of protein kinases by resorcylic acid lactone polyketides. Proc Natl Acad Sci U S A. 2006 Mar 14;103(11):4234-9. 2. Nishino M, et al. Hypothemycin, a fungal natural product, identifies therapeutic targets in Trypanosoma brucei. Elife. 2013 Jul 9;2:e00712.

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Hypothemycin 76958-67-3 Others Inhibitor inhibitor inhibit

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