Description:
JNJ-39641160 (JNJ39641160) is a peripherally restricted, non-covalent, potent, selective, orally-available Cathepsin S (CatS) inhibitor with Ki of 38 nM (hCatS).JNJ-39641160 maintains a high selectivity against other closely related cysteine proteases including cathepsins B, C, F, V (L2), K, Z, C, or legumain and the aspartic proteases such as cathepsins E or D.JNJ-39641160 showed similar potency against human and monkey CatS enzymes, and it exhibited less, albeit significant, activity against mouse and dog CatS enzymes (Ki=160-207 nM).JNJ-39641160 is only weakly active against rat cathepsin S (Ki=9.6 uM). JNJ-39641160 induced accumulation of the p10Ii with an average IC50 of 294 ± 28 nM, showed similar potency in purified human PBMC with IC50 of 327 nM.JNJ-39641160 dose-dependently blocked the proteolysis of the invariant chain, and inhibited both T-cell activation and antibody production to a vaccine antigen in C57BL/6 mice.JNJ-39641160 fully reversed tactile allodynia in wild-type mice but was completely ineffective in the same model in CatS knockout mice.
Handling:
Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to 24 months.
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance,
we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one
month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at
least 1 hour.