1. Apoptosis
  2. Caspase
  3. Heptelidic acid

Heptelidic acid  (Synonyms: Koningic acid)

Cat. No.: HY-120838 Purity: ≥97.0%
COA Handling Instructions

Heptelidic acid (Koningic acid) is a sesquiterpene antibiotic. Heptelidic acid inhibits Etoposide-induced apoptosis via downregulation of caspases. Koningic acid (KA) is a specific GAPDH inhibitor with an IC50of 90 μM.

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

Heptelidic acid Chemical Structure

Heptelidic acid Chemical Structure

CAS No. : 57710-57-3

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Based on 1 publication(s) in Google Scholar

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Description

Heptelidic acid (Koningic acid) is a sesquiterpene antibiotic[1]. Heptelidic acid inhibits Etoposide-induced apoptosis via downregulation of caspases[2]. Koningic acid (KA) is a specific GAPDH inhibitor with an IC50of 90 μM[3].

IC50 & Target[2]

Caspase-3

 

In Vitro

Heptelidic acid is a sesquiterpene antibiotic, found in the culture filtrate of three different strains of fungi isolated from soil samples. Heptelidic acid produces organisms, fermentation, isolation and characterization[1].
Heptelidic acid inhibits Etoposide-induced apoptosis in human leukemia U937 cells[2].Heptelidic acid inhibits caspase- 3 induction in U937 cells with an IC50 value of 40 μM after 8 h of Etoposide treatment[2].
Heptelidic acid (Koningic acid; KA), a natural product obtained from the Trichoderma fungus, can directly bind to the active site of human GAPDH. The expression of T. koningii KAr-GAPDH successfully rescued cell viability in human cells treated with Heptelidic acid. HEK293T cells expressing T. koningii KAr-GAPDH exhibited complete cell viability after treatment with 0-200 μM Heptelidic acid with the IC50=5 μM[3].

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

Cell Viability Assay[3]

Cell Line: HEK293T cells expressing KAr-GAPDH or EV (top left)
Concentration: 0.1, 1, 10, 100, 1000 μM
Incubation Time: 24 hours
Result: IC50=5 μM.
In Vivo

Heptelidic acid (Koningic acid; KA) is bioavailable and induces dynamic changes to glycolysis in vivo[3].

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

Animal Model: 6-week old female Foxn1nu mice bearing BT-474 tumor[3]
Dosage: 1, 2.5, 5, and 10 mg/kg
Administration: Daily intraperitoneal (IP) injections, 24 hours
Result: 1 mg/kg was determined to be the maximum tolerated dose (MTD) based upon behavioral monitoring and adverse events at higher doses (hemolysis, hematuria, and anemia).
Molecular Weight

280.32

Formula

C15H20O5

CAS No.
Appearance

Solid

Color

Colorless to off-white

SMILES

O=C(C1=C[C@@]2([H])[C@]([C@@]3(OC3)CC[C@@H]2C(C)C)([H])C(OC1)=O)O

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 : ≥ 30 mg/mL (107.02 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.5674 mL 17.8368 mL 35.6735 mL
5 mM 0.7135 mL 3.5674 mL 7.1347 mL
View the Complete Stock Solution Preparation Table

* 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.

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: ≥97.0%

References

Complete Stock Solution Preparation Table

* 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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.5674 mL 17.8368 mL 35.6735 mL 89.1838 mL
5 mM 0.7135 mL 3.5674 mL 7.1347 mL 17.8368 mL
10 mM 0.3567 mL 1.7837 mL 3.5674 mL 8.9184 mL
15 mM 0.2378 mL 1.1891 mL 2.3782 mL 5.9456 mL
20 mM 0.1784 mL 0.8918 mL 1.7837 mL 4.4592 mL
25 mM 0.1427 mL 0.7135 mL 1.4269 mL 3.5674 mL
30 mM 0.1189 mL 0.5946 mL 1.1891 mL 2.9728 mL
40 mM 0.0892 mL 0.4459 mL 0.8918 mL 2.2296 mL
50 mM 0.0713 mL 0.3567 mL 0.7135 mL 1.7837 mL
60 mM 0.0595 mL 0.2973 mL 0.5946 mL 1.4864 mL
80 mM 0.0446 mL 0.2230 mL 0.4459 mL 1.1148 mL
100 mM 0.0357 mL 0.1784 mL 0.3567 mL 0.8918 mL
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Heptelidic acid Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Heptelidic acid
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