spr inhibitor 3

SPR inhibitor 3 is an effective sepiapterin reductase inhibitor. SPR inhibitor 3 decreases neuropathic and inflammatory pain through a reduction of BH4 levels. SPR inhibitor 3 shows a high binding affinity to human SPR in a cell-free assay (IC50=74 nM) an

CSRM617 hydrochloride is a selective small-molecule inhibitor of the transcription factor ONECUT2 (OC2, a master regulator of androgen receptor), with a Kd of 7.43 µM in SPR assays, directly binding to the OC2-HOX domain. CSRM617 hydrochloride induces apoptosis through the appearance of cleaved Caspase-3 and PARP and is well tolerated in the mouse model of prostate cancer [1].

CSRM617 is a selective small molecule inhibitor of the transcription factor ONECUT2 (OC2, the main regulator of androgen receptor). The Kd in SPR analysis is 7.43 uM, which can directly bind to the OC2-HOX domain. CSRM617 induces apoptosis by cleaving the

USP7-IN-18 (Compound X21) serves as a novel USP7 inhibitor by directly suppressing enzyme activity and modulating downstream pathways, including the newly identified PCLAF target. At concentrations of 0.25-1 μM for 24 hours, it exhibits inhibitory effects. USP7-IN-18 effectively reduces proliferation in leukemia (RS4;11) and colon cancer (MC38/CT26.WT) cells at 0.01-100 μM over 72 hours. It demonstrates high selectivity for USP7 at 2.5 μM within 0.5 hours, surpassing eight other deubiquitinating enzymes. SPR analysis shows that at 1.95-2000 nM for 3 minutes, the compound binds the catalytic domain of USP7 with a KD value of 4.9 μM.

CHI3L1-IN-3 is a CHI3L1 inhibitor that binds to CHI3L1 with dissociation constants (Kd) of 13.76 μM and 13.5 μM as measured by MST and SPR assays, respectively. It demonstrates an extended plasma half-life and microsomal stability, along with a low intrinsic clearance rate. In three-dimensional multicellular glioblastoma (GBM) spheroid models, CHI3L1-IN-3 induces dose-dependent cytotoxicity, reduces spheroid mass, and inhibits cell migration. This compound is valuable for glioblastoma research.