2. Apoptosis
  3. Caspase
  4. IDN-7314

IDN-7314 is a pan-Caspase inhibitor with an IC50 of 0.2-7 nM against all tested Caspases. IDN-7314 abrogates Jo2-induced caspase-3/7 activity. IDN-7314 reduces the procoagulant activity of tissue factor in hepatocytes. IDN-7314 is applicable to research related to chemically induced hepatitis, fulminant liver failure and apoptotic liver injury.

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IDN-7314

IDN-7314 Chemical Structure

CAS No. : 254750-11-3

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IDN-7314 Related Antibodies

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Description

IDN-7314 is a pan-Caspase inhibitor with an IC50 of 0.2-7 nM against all tested Caspases. IDN-7314 abrogates Jo2-induced caspase-3/7 activity. IDN-7314 reduces the procoagulant activity of tissue factor in hepatocytes. IDN-7314 is applicable to research related to chemically induced hepatitis, fulminant liver failure and apoptotic liver injury[1][2].

IC50 & Target[1]

Caspase 3

 

Caspase-7

 

In Vitro

IDN-7314 is a potent pan-caspase inhibitor, with IC50 values of 0.2-7 nM for all tested caspases[1].
IDN-7314 (100 nM) abolishes Jo2-induced caspase-3/7 activity and significantly reduces hepatocyte tissue factor procoagulant activity and release of tissue factor-positive microvesicles[2].

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

IDN-7314 Related Antibodies
In Vivo

IDN-7314 (10 mg/kg; i.p.) potently inhibits galactosamine-induced hepatocellular apoptosis and caspase-3 activation in female Sprague-Dawley rats, with 76-71% reductions in apoptotic hepatocytes depending on treatment schedule, but only modestly reduces plasma ALT levels and oncotic cell death in this model[1].
IDN-7314 (3 mg/kg; i.p.; single dose) inhibits caspase activation, prevents procoagulant changes, and reduces hepatocellular injury in Mus musculus (mice) with Fas-induced apoptotic liver injury[2]. Wait, no-wait, the original text uses "mice" not the Latin name. Let me correct that to follow the original content strictly:\n\nIDN-7314 (3 mg/kg; i.p.; single dose) inhibits caspase activation, prevents procoagulant changes, and reduces hepatocellular injury in mice with Fas-induced apoptotic liver injury[2].\n\nWait, rechecking: "Fas" is an English target name, so it should be bold. Citations get superscript. No other entities here-no Latin species name used (the text says "mice" not the Latin binomial, so we don't alter that), no gene symbols, chemical formulas, etc. That's correct.

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

Animal Model: Sprague-Dawley (female, 150-200 g, chemical-induced hepatitis model)[1]
Dosage: 10 mg/kg (6-hour observation group); 10 mg/kg (24-hour two-dose group); 10 mg/kg (24-hour pretreatment group)
Administration: i.p.; two doses at 3 and 4.5 hours post-galactosamine (6-hour group); two doses at 3 and 6 hours post-galactosamine (24-hour two-dose group); three doses 30 minutes pre-galactosamine, 3 and 6 hours post-galactosamine (24-hour pretreatment group)
Result: Reduced the percentage of apoptotic hepatocytes by 76% (from 5.0 ± 0.34% to baseline-like levels) at 6 hours post-galactosamine.
Reduced hepatic and plasma caspase-3 activities to control levels at 6 hours post-galactosamine.
Prevented procaspase-3 processing to its active fragment at 6 hours post-galactosamine.
Did not reduce plasma ALT activities at 6 hours post-galactosamine.
Had no significant effect on oncotic cell counts at 6 hours post-galactosamine.
Reduced plasma ALT levels by 57% (p < 0.05) at 24 hours post-galactosamine (two-dose schedule).
Reduced hepatocellular oncosis by 24% (p > 0.05) at 24 hours post-galactosamine (two-dose schedule).
Reduced hepatic and plasma caspase-3 activities to baseline at 24 hours post-galactosamine (two-dose schedule).
Reduced the percentage of apoptotic hepatocytes by 71% (from 7.3 ± 1.1% to 2.1 ± 0.4%) at 24 hours post-galactosamine (three-dose pretreatment schedule).
Had no significant effect on plasma ALT activities or oncotic cell counts at 24 hours post-galactosamine (three-dose pretreatment schedule).
Animal Model: Sprague-Dawley (female, 150-200 g, chemical-induced hepatitis model)[1]
Dosage: 10 mg/kg
Administration: i.p.; two doses at 3 and 4.5 hours post-galactosamine/endotoxin injection
Result: Reduced hepatic caspase-3 activities from 194 ± 33 ΔF/min/mg protein to baseline 16 ± 5 ΔF/min/mg protein.
Reduced plasma caspase-3 activities from 12.9 ± 1.5 ΔF/min/mg protein to baseline 0.2 ± 0.2 ΔF/min/mg protein.
Reduced the percentage of apoptotic hepatocytes by 80% (from 7.33 ± 0.32% to 1.50 ± 0.29%).
Reduced plasma ALT activities by 50% (from 708 ± 54 IU/L to 359 ± 34 IU/L).
Reduced the percentage of oncotic hepatocytes by 33% (from 2.35 ± 0.22% to 1.58 ± 0.13%).
Animal Model: C57BL/6J (male, 8-12 weeks old, Fas-induced apoptotic liver injury model)[2]
Dosage: 3 mg/kg
Administration: i.p.; single dose (administered 1 hour after Jo2 injection)
Result: Attenuated Jo2-induced hepatic cleaved caspase-3 levels.
Abolished Jo2-induced increases in plasma alanine aminotransferase (ALT) activity.
Eliminated Jo2-induced hepatic sinusoidal congestion/hemorrhage.
Completely prevented Jo2-induced increases in plasma TF-positive microvesicle levels.
Blocked Jo2-induced increases in plasma thrombin-antithrombin (TAT) levels.
Attenuated Jo2-induced hepatic fibrin(ogen) β chain accumulation.
Abolished Jo2-induced hepatic cleaved caspase-3 staining and dramatically reduced hepatic fibrin(ogen) deposition.
Molecular Weight

549.38

Formula

C22H17F6N3O7
CAS No.
SMILES

O(CC([C@@H](NC([C@@H](NC(C(NC1=C(F)C=CC=C1F)=O)=O)C)=O)CC(O)=O)=O)C2=C(F)C(F)=CC(F)=C2F
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Purity & Documentation
References
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IDN-7314 Related Classifications

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  • 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:

IDN-7314254750-11-3IDN7314IDN 7314Caspasechemical-induced hepatitiscaspase-7hepatocellular apoptosiscaspase-3female Sprague-Dawley ratsprimary mouse hepatocytesapoptotic liver injuryfulminant hepatic failurehepatocytescaspasesInhibitorinhibitorinhibit

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