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Emricasan (IDN-6556) pan-Caspase inhibitor

Name: Emricasan (IDN-6556)
Brand: Selleck Chemicals
SKU: S7775
Availability: InStock
Rating: 5 (77 reviews)

Cat.No.S7775

Emricasan (IDN-6556, PF 03491390, PF-03491390) is a potent irreversible pan-caspase inhibitor and also functions as an inhibitor of Zika virus infection.

Chemical Structure

Molecular Weight: 569.50

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.93%

99.93

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Related Targets	Apoptosis related Ras STAT TNF-alpha Bcl-2 PD-1/PD-L1 Ferroptosis p53 RIP kinase c-RET MDM2/MDMX Myc Antifolate MRP IAP OXPHOS PERK FKBP Thymidylate Synthase ABC Transporter Heme Oxygenase PFKFB Pyroptosis Photosensitizer PKD Survivin Annexin A ASK Bcl-6 Nur77
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Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Activity Description	PMID
Jurkat E6-1	Function assay	Inhibition of Anti-Fas antibody-induced caspase-3 activity in human Jurkat E6-1 cells using Ac-DEVD-AMC substrate by fluorescence based assay, IC50 = 0.006 μM.	29650287
JFas	Function assay	Inhibitory concentration against JFas cells, IC50 = 0.025 μM.	16250635
THP-1	Function assay	Inhibitory concentration against THP-1 cells, IC50 = 0.27 μM.	16250635
A673	qHTS assay	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
Saos-2	qHTS assay	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	29435139
MG 63 (6-TG R)	qHTS assay	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells	29435139
NB1643	qHTS assay	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	29435139
SK-N-MC	qHTS assay	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	569.50	Formula	C₂₆H₂₇F₄N₃O₇	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	254750-02-2	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	PF 03491390, PF-03491390			Smiles	CC(C(=O)NC(CC(=O)O)C(=O)COC1=C(C(=CC(=C1F)F)F)F)NC(=O)C(=O)NC2=CC=CC=C2C(C)(C)C

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (175.59 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 25 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (8.78mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an 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 the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

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 addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	caspase ^[1]
In vitro	Emricasan (IDN-6556), also called PF-03491390, is an inhibitor of activated caspases with sub- to nanomolar activity in vitro. It shows neuroprotective activity for hNPCs but does not suppress ZIKV replication^[2].
In vivo	In the murine NASH model, stellate cell activation and hepatic fibrogenesis are attenuated by administration of Emricasan (IDN-6556), a pan-caspase inhibitor^[1]. It decreases liver injury but not metabolic derangement in NASH and also ameliorates inflammation. This compound is currently being evaluated in phase 2 clinical trials for the reduction of hepatic injury and liver fibrosis caused by chronic HCV infection^[2].
References	[1] https://pubmed.ncbi.nlm.nih.gov/24750664/ [2] https://pubmed.ncbi.nlm.nih.gov/27571349/

Applications

Methods	Biomarkers	Images	PMID
Growth inhibition assay	Cell viability		27571349

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT03205345	Unknown status	Decompensated Cirrhosis	Conatus Pharmaceuticals Inc.	June 28 2017	Phase 2
NCT01653899	Completed	Diabetes	University of Alberta\|Conatus Pharmaceuticals Inc.	June 2012	Phase 1\|Phase 2

Tech Support

Handling Instructions

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