Cat. No.: HY-107417

Hypothemycin

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Based on 1 Customer Validation

Hypothemycin, a fungal polyketide, is a multikinase inhibitor with K_is 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.

Purity: 98.0%
CAS No.: 76958-67-3
Formula: C₁₉H₂₂O₈
Molecular Weight:378.37

Storage:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

Hypothemycin Chemical Structure

CAS No.: 76958-67-3

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

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)

All VEGFR Isoforms :

All MEK Isoforms :

All PDGFR Isoforms :

All ERK Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	1 μM Compound: 17	Cytotoxicity against human A549 cells after 72 hrs by MTT assay Cytotoxicity against human A549 cells after 72 hrs by MTT assay	[PMID: 28749671]
COLO-829	IC₅₀	0.15 μM Compound: hypothemycin	Cytotoxicity against human COLO829 cells Cytotoxicity against human COLO829 cells	[PMID: 17067161]
HeLa	IC₅₀	1 μM Compound: 17	Cytotoxicity against human HeLa cells after 72 hrs by MTT assay Cytotoxicity against human HeLa cells after 72 hrs by MTT assay	[PMID: 28749671]
HT-29	IC₅₀	5.9 μM Compound: hypothemycin	Cytotoxicity against human HT-29 cells Cytotoxicity against human HT-29 cells	[PMID: 17067161]
Jurkat	IC₅₀	>1 μM Compound: HY	Cytotoxicity in human Jurkat cells assessed as inhibition of cellular viability after 72 hrs by CellTiter-Glo luminescent assay Cytotoxicity in human Jurkat cells assessed as inhibition of cellular viability after 72 hrs by CellTiter-Glo luminescent assay	[PMID: 30742435]
MCF7	IC₅₀	16.3 μM Compound: 7	Cytotoxicity against human MCF7 cells after 72 hrs by MTS assay Cytotoxicity against human MCF7 cells after 72 hrs by MTS assay	[PMID: 21513293]
MCF7	IC₅₀	3.3 μM Compound: 17	Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 28749671]
MDA-MB-435	IC₅₀	1.9 μM Compound: HPO	Cytotoxicity against human MDA-MB-435 cells assessed as reduction in cell viability measured after 72 hrs by celltiter-blue cell viability assay Cytotoxicity against human MDA-MB-435 cells assessed as reduction in cell viability measured after 72 hrs by celltiter-blue cell viability assay	[PMID: 35834411]
MV4-11	IC₅₀	15 nM Compound: HY	Cytotoxicity in human MV4-11 cells assessed as inhibition of cellular viability incubated for 72 hrs by CellTiter-Blue assay Cytotoxicity in human MV4-11 cells assessed as inhibition of cellular viability incubated for 72 hrs by CellTiter-Blue assay	[PMID: 30742435]
NCI-H460	IC₅₀	4.3 μM Compound: 7	Cytotoxicity against human H460 cells after 72 hrs by MTS assay Cytotoxicity against human H460 cells after 72 hrs by MTS assay	[PMID: 21513293]
OVCAR-3	IC₅₀	2.6 μM Compound: HPO	Cytotoxicity against human OVCAR-3 cells assessed as reduction in cell viability measured after 72 hrs by celltiter-blue cell viability assay Cytotoxicity against human OVCAR-3 cells assessed as reduction in cell viability measured after 72 hrs by celltiter-blue cell viability assay	[PMID: 35834411]
SF-268	IC₅₀	12.7 μM Compound: 7	Cytotoxicity against human SF268 cells after 72 hrs by MTS assay Cytotoxicity against human SF268 cells after 72 hrs by MTS assay	[PMID: 21513293]
SK-OV-3	IC₅₀	0.07 μM Compound: hypothemycin	Cytotoxicity against human SKOV3 cells Cytotoxicity against human SKOV3 cells	[PMID: 17067161]
THP-1	IC₅₀	>1 μM Compound: HY	Cytotoxicity in human THP1 cells assessed as inhibition of cellular viability after 72 hrs by CellTiter-Glo luminescent assay Cytotoxicity in human THP1 cells assessed as inhibition of cellular viability after 72 hrs by CellTiter-Glo luminescent assay	[PMID: 30742435]

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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%.

Chemical Information

CAS No. 76958-67-3
Appearance Solid
Molecular Weight 378.37
Formula C₁₉H₂₂O₈
Color White to off-white
SMILES

COC1=CC(O)=C(C(O[C@@H](C)C/C=C\C2=O)=O)C([C@@H](O3)[C@@]3([H])C[C@H](O)[C@@H]2O)=C1
Structure Classification
- Phenols
- Monophenols
- Antibiotics
- Macrolide Antibiotics
Initial Source
- Microorganisms
Hypomyces trichothecoides
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (264.29 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.6429 mL

13.2146 mL

26.4292 mL

5 mM

0.5286 mL

2.6429 mL

5.2858 mL

10 mM

0.2643 mL

1.3215 mL

2.6429 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (6.61 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (6.61 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.61 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[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. [Content Brief]

[2]. Nishino M, et al. Hypothemycin, a fungal natural product, identifies therapeutic targets in Trypanosoma brucei. Elife. 2013 Jul 9;2:e00712. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.6429 mL	13.2146 mL	26.4292 mL	66.0729 mL
	5 mM	0.5286 mL	2.6429 mL	5.2858 mL	13.2146 mL
	10 mM	0.2643 mL	1.3215 mL	2.6429 mL	6.6073 mL
	15 mM	0.1762 mL	0.8810 mL	1.7619 mL	4.4049 mL
	20 mM	0.1321 mL	0.6607 mL	1.3215 mL	3.3036 mL
	25 mM	0.1057 mL	0.5286 mL	1.0572 mL	2.6429 mL
	30 mM	0.0881 mL	0.4405 mL	0.8810 mL	2.2024 mL
	40 mM	0.0661 mL	0.3304 mL	0.6607 mL	1.6518 mL
	50 mM	0.0529 mL	0.2643 mL	0.5286 mL	1.3215 mL
	60 mM	0.0440 mL	0.2202 mL	0.4405 mL	1.1012 mL
	80 mM	0.0330 mL	0.1652 mL	0.3304 mL	0.8259 mL
	100 mM	0.0264 mL	0.1321 mL	0.2643 mL	0.6607 mL

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Hypothemycin

Macrocyclic Compound Library

MCE Bioactive Compound Library

Natural Product Library Plus

All VEGFR Isoforms

All MEK Isoforms

All PDGFR Isoforms

All ERK Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Hypothemycin

Macrocyclic Compound Library

MCE Bioactive Compound Library

Natural Product Library Plus

All VEGFR Isoforms

All MEK Isoforms

All PDGFR Isoforms

All ERK Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Hypothemycin Related Classifications

HY-107417 Related Classifications