Perforin-IN-2 is a benzenesulfonamide perforin inhibitor that can reduce transplant rejection during allogeneic bone marrow/stem cell transplantation. The binding rate of Perforin-IN-2 to plasma proteins is 99.8%. Perforin-IN-2 requires a higher concentration (＞900 μM) to achieve the best perforin inhibition effect in vivo. Perforin-IN-2 can effectively inhibit the lytic activity of recombinant perforin on Jurkat T (IC50=6.65 μM) leukemia cells, and can also inhibit the death of K562 leukemia target cells.

Physicochemical Properties

CAS #	1567836-70-7
PubChem CID	73295278
Appearance	Light yellow to yellow solid powder
Hydrogen Bond Donor Count	1
Hydrogen Bond Acceptor Count	8
Rotatable Bond Count	5
Heavy Atom Count	35
Complexity	907
Defined Atom Stereocenter Count	0
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)

Biological Activity

References

[1].Preclinical Activity and Pharmacokinetic/Pharmacodynamic Relationship for a Series of Novel Benzenesulfonamide Perforin Inhibitors. ACS Pharmacol Transl Sci. 2022 May 31;5(6):429-439.

Solubility Data

Solubility (In Vitro)

DMSO :~33.33 mg/mL (~65.80 mM; with sonication (<80°C))

Solubility (In Vivo)

Solubility in Formulation 1: 2.5 mg/mL (4.94 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one),clear solution; with ultrasonication. 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 and add it to 900 μL corn oil and mix well.  (Please use freshly prepared in vivo formulations for optimal results.)