HJC0350

Alias: HJC 0350; HJC-0350; HJC0350

Cat No.:V1924 Purity: ≥98%

COA Product Data Instructions for use SDS

HJC0350 is a potent and selective antagonist/inhibitor of EPAC2 with IC50 of 0.3 μM, it exhibited no inhibition on Epac1.

HJC0350 Chemical Structure CAS No.: 885434-70-8
Product category: cAMP

This product is for research use only, not for human use. We do not sell to patients.

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Citations by Top Journals: Nature, Cell, Science, etc.

Top Publications Citing lnvivochem Products

Nature 2021, 597(7874):119-125.

Cell 2020,183:1202-1218.e25.

Science Adv 2022: 8, eabm9427.

Nature 597, 119–125 (2021)

Cell Stem Cell 2020,26(6):845-861.e12.

Science Trans Med 2023,15(701):eadd7872.

STTT 2023,8(1):91.

Cell Reports 2023,42(4):112313

Science Trans Med 2023, 15: eadd7872.

Cancer Cell 2021,39(4):529-547.e7.

Cancer Discov 2022,12(4):1106-1127.

Immunity 2023,56(3):620-634.e11.

J Am Chem Soc 2022,144:21831-21836.

Cell 2020,183:1202-1218.e25.

Science Adv 2022:8,eabm9427.

Nature 2021,597(7874):119-125.

Cell 2020,183:1202-1218.e25.

PNAS Nexus 2022,1(3):pgac063.

ACS Nano 2023,17(10):9110-9125.

Biomaterial 2023 Sep16:302:122333.

Purity & Quality Control Documentation

Current batch：

Purity: ≥98%

COA

MSDS

Instructions

Product Description
Bioactivity & Protocols
Physicochemical Properties
Solubility Data
Calculators
Biological Data

Product Description

HJC0350 is a potent and selective antagonist/inhibitor of EPAC2 with IC50 of 0.3 μM, it exhibited no inhibition on Epac1. Under both physiological and pathological conditions, the isoforms of exchange proteins directly activated by cAMP (EPAC), EPAC1 and EPAC2, react to the second messenger cAMP and control a host of intracellular functions. HJC 0350 competed with 8-NBD-cAMP in binding recombinant fusion protein EPAC2 with IC50 value of 0.3 μM and exhibited 133-fold more potent than cAMP, which competed with 8-NBD-cAMP in binding EPAC2 with IC50 value of 40 μM. HJC 0350 (25 μM) demonstrated EPAC2-specific antagonist properties as it inhibited EPAC2 GEF activity but had no effect on EPAC1-mediated Rap1-GDP exchange activity or cAMP-mediated PKA activation.

Biological Activity I Assay Protocols (From Reference)

Targets

EPAC2 ( IC50 = 0.3 µM )

ln Vitro

In vitro activity: HJC0350 is approximately 133 times more potent than cAMP and has an apparent IC50 value of 0.3 µM for competing with 8-NBD-cAMP binding of EPAC2. It is discovered that HJC0350 is an EPAC2-specific antagonist since it does not impede EPAC1-mediated Rap1-GDP exchange activity at 25 µM in the presence of equal concentrations of cAMP. When HEK293/EPAC2-FL cells are pretreated with 10 µM HJC0350, the 007-AM-induced decrease in FRET is completely blocked[1].

ln Vivo

Enzyme Assay

HJC 0350 is a potent and selective antagonist of EPAC2. HJC 0350 competed with 8-NBD-cAMP in binding recombinant fusion protein EPAC2 with IC50 value of 0.3 μM and exhibited 133-fold more potent than cAMP, which competed with 8-NBD-cAMP in binding EPAC2 with IC50 value of 40 μM. HJC 0350 (25 μM) inhibited EPAC2 GEF activity in the presence of 25 μM cAMP, but did not affect cAMP-mediated PKA activation or EPAC1-mediated Rap1-GDP exchange activity. This suggests that HJC 0350 is an EPAC2-specific antagonist.

Cell Assay

HJC 0350 (10 μM) completely inhibited the decrease of FRET in HEK293/EPAC2-FL cells induced by 007-AM (a membrane permeable EPAC selective cAMP analogue) in HEK293 cells expressing EPAC1- or EPAC2-based fluorescence resonance energy transfer (FRET) sensor (EPAC2-FL or EPAC1-FL). However, it had no effect on HEK293/EPAC1-FL cells.

Animal Protocol

References

[1]. Identification and characterization of small molecules as potent and specific EPAC2 antagonists. J Med Chem. 2013 Feb 14;56(3):952-62.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Physicochemical Properties

Molecular Formula

C15H19NO2S

Molecular Weight

277.38

Exact Mass

277.11

Elemental Analysis

C, 64.95; H, 6.90; N, 5.05; O, 11.54; S, 11.56

CAS #

885434-70-8

Related CAS #

885434-70-8

Appearance

Solid powder

SMILES

CC1=CC(=C(C(=C1)C)S(=O)(=O)N2C=C(C=C2C)C)C

InChi Key

AFZWZVLPIMHLSE-UHFFFAOYSA-N

InChi Code

InChI=1S/C15H19NO2S/c1-10-6-12(3)15(13(4)7-10)19(17,18)16-9-11(2)8-14(16)5/h6-9H,1-5H3

Chemical Name

2,4-dimethyl-1-(2,4,6-trimethylphenyl)sulfonylpyrrole

Synonyms

HJC 0350; HJC-0350; HJC0350

HS Tariff Code

2934.99.9001

Storage

Powder -20°C 3 years

4°C 2 years

In solvent -80°C 6 months

-20°C 1 month

Shipping Condition

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Solubility Data

Solubility (In Vitro)

DMSO: 33.3~52 mg/mL (120.2~187.5 mM)

Water: <1 mg/mL

Ethanol: <1 mg/mL

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.5 mg/mL (9.01 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

(Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	3.6052 mL	18.0258 mL	36.0516 mL
	5 mM	0.7210 mL	3.6052 mL	7.2103 mL
	10 mM	0.3605 mL	1.8026 mL	3.6052 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Mass

Concentration

Volume

Molecular Weight*

Calculate Reset

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

Calculate the Mass of a compound required to prepare a solution of known volume and concentration
Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?

Enter 350.26 in the Molecular Weight (MW) box
Enter 10 in the Concentration box and choose the correct unit (mM)
Enter 5 in the Volume box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

Calculate Reset

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:

Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
Enter 25 into the Concentration (End) box and select the correct unit (mM)
Enter 25 into the Volume (End) box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box

Molecular formula

Total molecular weight

g/mol

Calculate Reset

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4 c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
Click the “Calculate” button
The answer appears in the Volume (to add to vial) box

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)

Dosage mg/kg

Average weight of animals g

Dosing volume per animal μL

Number of animals

Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)

% DMSO

% Tween 80

% ddH₂O

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Calculation results

Working concentration： mg/mL；

Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O，mix and clarify.

Note： (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.

Biological Data

Relative potency of EPAC2 antagonist 20i(HJC0350).J Med Chem.2013 Feb 14;56(3):952-62.
Specificity of EPAC antagonists 1, 14c and 20i.J Med Chem.2013 Feb 14;56(3):952-62.
Effects of 20i on 007-AM mediated cellular activation of EPAC.J Med Chem.2013 Feb 14;56(3):952-62.
Effects of 20i on 8-Br-cAMP-AM mediated cellular activation of PKA.J Med Chem.2013 Feb 14;56(3):952-62.
J Med Chem.2013 Feb 14;56(3):952-62.