Perforin-IN-1
Perforin-IN-1 is a perforin inhibitor that blocks perforin-mediated lysis of target cells by cytotoxic lymphocytes. Perforin-IN-1 achieves perforin inhibition in a mouse bone marrow transplantation model, protecting MHC-mismatched allogeneic bone marrow stem cell grafts from NK cell-mediated rejection. Perforin-IN-1 can be used for research on graft rejection.
For research use only. We do not sell to patients.
- CAS No.: 2378640-25-4
- Formula: C24H18F2N4O4S2
- Molecular Weight:528.55
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Jurkat | IC50 |
3.34 μM
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Inhibition of purified recombinant perforin-mediated lysis of Jurkat T lymphoma target cells measured by 51Cr release after 4 hrs incubation.
Inhibition of purified recombinant perforin-mediated lysis of Jurkat T lymphoma target cells measured by 51Cr release after 4 hrs incubation.
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31525966 |
In Vitro
Perforin-IN-1 (compound 16) exhibits low cLogP (2.84), high mouse and rat microsomal stability (100% and 100%), lower human microsomal stability (75%), and extremely high plasma protein binding (99.91%)[1].
Perforin-IN-1 (1.25-20 μM; 4-24 h) inhibits purified recombinant perforin-mediated lysis of Jurkat T lymphoma cells with an IC50 of 3.34 μM; blocks intact KHYG-1 NK cell-mediated lysis of K562 target cells with an IC50 of 4.43 μM; and exhibits low toxicity toward KHYG-1 NK cells, with cell viability of 90.6% at 10 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:Jurkat T lymphoma cells
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Concentration:20, 10, 5, 2.5, and 1.25 μM
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Incubation Time:30 min preincubation with recombinant perforin; 4 h incubation
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Result:Inhibited purified recombinant perforin-mediated lysis of Jurkat T lymphoma cells with an IC50 of 3.34 μM.
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Cell Line:KHYG-1 NK cells
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Concentration:10 μM
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Incubation Time:24 h
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Result:KHYG-1 NK cell viability was 90.6% at 10 μM.
Parmacokinetics
| Species | Dose | Route | T1/2 | AUC0-∞ |
|---|---|---|---|---|
| Mice[1] | 90 mg/kg | i.p. | 18.9 h | 42475 μM/L·h |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (wild-type recipients; donor bone marrow from BALB/c and B6.SJL-Ptprca mice (mixed at a 1:1 ratio, 24 × 106 cells total))[1]
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Dosage:125 mg/kg
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Administration:i.p.; at 0 h immediately before cell transfer and at 18 h after cell transfer
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Result:Demonstrated a 66% reduction of perforin activity, resulting in preservation of transplanted mismatched target cells.
In comparison to perforin knockout recipients, representing 100% perforin inhibition, a 66% reduction in perforin activity was observed as measured by survival of the transferred allogeneic cells.
Chemical Information
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CAS No. 2378640-25-4
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Molecular Weight 528.55
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Formula C24H18F2N4O4S2
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SMILES
FC1=CC(F)=CC=C1S(NC2=C(OC)N=CC(C3=CC=C(C4=CN=C(C(N(C)C5)=O)C5=C4)S3)=C2)(=O)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Perforin-IN-1 Related Classifications
HY-129387 Related Classifications
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