JNJ-39641160
Modify Date: 2025-08-24 14:32:56
JNJ-39641160 structure
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Common Name | JNJ-39641160 | ||
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| CAS Number | 1049809-89-3 | Molecular Weight | 699.677 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C38H40Cl2N6O3 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of JNJ-39641160JNJ-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. |
| Name | JNJ-39641160 |
|---|
| 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. |
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| References | 1. William A Eckert 3rd, et al. Eur J Pharmacol. 2020 Aug 5;880:173171. |
| Molecular Formula | C38H40Cl2N6O3 |
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| Molecular Weight | 699.677 |