ESI-09

Name: ESI-09
Brand: MedChemExpress
SKU: HY-16704
Rating: 5.0 (6 reviews)

Cat. No.: HY-16704 Purity: 99.25%: FAQs
Data Sheet SDS COA Handling Instructions

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ESI-09 is a novel noncyclic nucleotide EPAC antagonist with IC₅₀ values of 3.2 and 1.4 μM for EPAC1 and EPAC2, respectively.

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

ESI-09 Chemical Structure

CAS No. : 263707-16-0

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 78	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 78	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 72	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 116	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 429	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 649	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 6 publication(s) in Google Scholar

4 Publications Citing Use of MCE ESI-09

Proliferation Assay

: ESI-09 purchased from MedChemExpress. Usage Cited in: Acta Biochim Biophys Sin (Shanghai). 2017 Jul 1;49(7):573-580. [Abstract]; PANC-1 cells treated with different concentrations of combination of CHIR99021 and ESI-09 (0, 1 μM+1 μM, 3 μM+3 μM, 5 μM+5 μM, and 10 μM+10 μM) for 48 h.

: ESI-09 purchased from MedChemExpress. Usage Cited in: J Neurosci. 2016 Oct 12;36(41):10560-10573. [Abstract]; The inhibition of Epac1 activity by ESI-09 reduces oligodendrocyte maturation.

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Biological Activity
Protocol
Purity & Documentation
References
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Description

ESI-09 is a novel noncyclic nucleotide EPAC antagonist with IC₅₀ values of 3.2 and 1.4 μM for EPAC1 and EPAC2, respectively.

IC₅₀ & Target

IC50: 3.2 μM (EPAC1), 1.4 μM (EPAC2)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
HeLa S3	IC₅₀	10.8 μM Compound: ESI-09	Inhibition of recombinant C-terminal FLAG/HA-tagged EPAC1 (unknown origin) expressed in retrovirus infected human HeLaS3 cells assessed as reduction in cAMP-mediated guanine nucleotide exchange factor activity in presence of C-terminal truncated Rap1B (1 Inhibition of recombinant C-terminal FLAG/HA-tagged EPAC1 (unknown origin) expressed in retrovirus infected human HeLaS3 cells assessed as reduction in cAMP-mediated guanine nucleotide exchange factor activity in presence of C-terminal truncated Rap1B (1	[PMID: 27190593]
HeLa S3	IC₅₀	4.4 μM Compound: ESI-09	Inhibition of recombinant C-terminal FLAG/HA-tagged EPAC2 (unknown origin) expressed in retrovirus infected human HeLaS3 cells assessed as reduction in cAMP-mediated guanine nucleotide exchange factor activity in presence of C-terminal truncated Rap1B (1 Inhibition of recombinant C-terminal FLAG/HA-tagged EPAC2 (unknown origin) expressed in retrovirus infected human HeLaS3 cells assessed as reduction in cAMP-mediated guanine nucleotide exchange factor activity in presence of C-terminal truncated Rap1B (1	[PMID: 27190593]

In Vitro

While cAMP competes with 8-NBD-cAMP binding with an IC₅₀ of 39 μM, ESI-09 shows an increased potency with an apparent IC₅₀ of 10 μM. ESI-09 inhibis cAMP-mediated EPAC2 and EPAC1 GEF activity with an IC₅₀ of 1.4 and 3.2μM, respectively. ESI-09 could fit well into the functional cAMP-binding pocket of EPAC1, establishing favorable hydrophobic and hydrogen bonding interactions with the protein’s active-site residues. ESI-09 inhibits 007-AM-stimulated Akt phosphorylation at T308 and S473 in a dose-dependent manner. ESI-09 inhibits pancreatic cancer cells AsPC-1 and PANC-1 migration. ESI-09 inhibits EPAC1-mediated adhesion of PDA cells on collagen I^[1]. Exposure to ESI-09 significantly reduces intracellular and total bacterial counts in HUVECs at 30 min postinfection with 10 multiplicities of infection (MOI) of R. australis compared with similarly infected controls^[2].

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

In Vivo

Treatment with ESI-09 dramatically protects WT mice against R. australis infection with much milder disease manifestations and significantly improves survival^[2].

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

Molecular Weight

330.77

Formula

C₁₆H₁₅ClN₄O₂

CAS No.

263707-16-0

Appearance

Solid

Color

Yellow to orange

SMILES

O=C(C1=NOC(C(C)(C)C)=C1)/C(C#N)=N/NC2=CC(Cl)=CC=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : ≥ 47 mg/mL (142.09 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	3.0232 mL	15.1162 mL	30.2325 mL
5 mM	0.6046 mL	3.0232 mL	6.0465 mL
10 mM	0.3023 mL	1.5116 mL	3.0232 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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 (7.56 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (7.56 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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.65%

Select Batch:

Data Sheet (275 KB) SDS (392 KB)

COA (246 KB) LCMS (93 KB)

Handling Instructions (2659 KB)

References

[1]. Almahariq M, et al. A novel EPAC-specific inhibitor suppresses pancreatic cancer cell migration and invasion. Mol Pharmacol. 2013 Jan;83(1):122-8. [Content Brief]

[2]. Gong B, et al. Exchange protein directly activated by cAMP plays a critical role in bacterial invasion during fatal rickettsioses. Proc Natl Acad Sci U S A. 2013 Nov 26;110(48):19615-20. [Content Brief]

Cell Assay ^[1]	INS-1 cells are plated in 96-well plates precoated with polylysine. After overnight incubation, the medium is replaced with Krebs-Ringer bicarbonate (KRB) containing 2.9 mM glucose. After an additional 2-hour incubation, the cells are treated with ESI-09 or DMSO vehicle as a control in fresh KRB containing 11.8 mM glucose for 10 minutes, followed by a 30-minute stimulation with 10 µM 007-AM. The supernatant is collected, and insulin is quantified using an Ultra Sensitive Rat Insulin ELISA kit from Crystal Chem Inc^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[2]	Mice: ESI-09 is dissolved in buffered saline containing 10% (vol/vol) ethanol and 10% (vol/vol) Tween-80. Thirty-three WT C57BL/6 mice are divided into four groups [11 mice (group A), 10 mice (group B), 6 mice each (groups C and D)]. Groups A and C are treated with the Epac-specific inhibitor ESI-09 [10 mg/kg ] via i.p. injection for 5 d before infection, whereas groups B and D are treated with vehicle, followed by i.v. inoculation of R. australis for groups A and B or mock inoculation for groups C and D. ESI-09 or vehicle treatment is continued for another 7 d until mice are killed on day 8. During the course of the experiments, animals are monitored daily for signs of illness and mortality^[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Almahariq M, et al. A novel EPAC-specific inhibitor suppresses pancreatic cancer cell migration and invasion. Mol Pharmacol. 2013 Jan;83(1):122-8. [Content Brief] [2]. Gong B, et al. Exchange protein directly activated by cAMP plays a critical role in bacterial invasion during fatal rickettsioses. Proc Natl Acad Sci U S A. 2013 Nov 26;110(48):19615-20. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.0232 mL	15.1162 mL	30.2325 mL	75.5812 mL
	5 mM	0.6046 mL	3.0232 mL	6.0465 mL	15.1162 mL
	10 mM	0.3023 mL	1.5116 mL	3.0232 mL	7.5581 mL
	15 mM	0.2015 mL	1.0077 mL	2.0155 mL	5.0387 mL
	20 mM	0.1512 mL	0.7558 mL	1.5116 mL	3.7791 mL
	25 mM	0.1209 mL	0.6046 mL	1.2093 mL	3.0232 mL
	30 mM	0.1008 mL	0.5039 mL	1.0077 mL	2.5194 mL
	40 mM	0.0756 mL	0.3779 mL	0.7558 mL	1.8895 mL
	50 mM	0.0605 mL	0.3023 mL	0.6046 mL	1.5116 mL
	60 mM	0.0504 mL	0.2519 mL	0.5039 mL	1.2597 mL
	80 mM	0.0378 mL	0.1890 mL	0.3779 mL	0.9448 mL
	100 mM	0.0302 mL	0.1512 mL	0.3023 mL	0.7558 mL

ESI-09 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.

Keywords:

ESI-09263707-16-0ESI09ESI 09Virus ProteaseInhibitorinhibitorinhibit

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ESI-09

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4 Publications Citing Use of MCE ESI-09

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Complete Stock Solution Preparation Table

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