jh1

NVP-BSK805 (BSK 805) is an ATP-competitive JAK2 inhibitor.

Ropsacitinib (PF-06826647) is a selective TYK2 inhibitor, which binds to TYK2 catalytically active JH1 domain (IC50: 17 nM).

SJH1-62B is a PROTAC (proteolysis-targeting chimera) designed to target the androgen receptor (AR).

SJH1-51B is an effective PROTAC degrader of BRD4, exhibiting antitumor properties.

TyK2-IN-2 is a selective inhibitor of TYK2 (IC50s: 7 nM, 0.1 μM, and 0.05 μM for TYK2 JH2, IL-23, and IFNα).

Tyk2-IN-5 is a selective and orally active inhibitor of Tyk2 JH2 (Ki: 0.086 nM for Tyk2 JH2; IC50: 25 nM for IFNα).

Tyk2-IN-7 is an inhibitor of TYK2 JH2, binds to the TYK2 JH2 domain (IC50: 0.00053 μM; Ki.app: 0.00007 μM).

NVP-BSK805 trihydrochloride is a potent ATP-competitive inhibitor of JAK2, exhibiting IC50 values of 0.48 nM, 31.63 nM, 18.68 nM, and 10.76 nM against JAK2 JH1, JAK1 JH1, JAK3 JH1, and TYK2 JH1, respectively.

GJH-166 is an analog of dopamine that has been shown to inhibit adrenergic transmission in canines.

JH-131e-153, a diacylglycerol (DAG)-lactone, serves as a small molecule activator for the C1 domain of Munc13-1, exhibiting an activation hierarchy of WT>I590≈R592A≈W588A. This compound's C1 domain shares sequence and structure homology with protein kinase C (PKC), with an activation preference of PKCα>Munc13-1>PKCε. JH-131e-153 is implicated in the modulation of neuronal processes and holds potential for research in neurodegenerative diseases [1].