adpkd

MR-L2 is a reversible and noncompetitive allosteric activator of long-isoform phosphodiesterase-4 (PDE4).

H2-Gamendazole is a novel compound for spermatogenesis inhibition and cancer therapy as an inhibitor of heat shock proteins and/or elongation factor 1 alpha, and is an Hsp90 regulator.

DM-4107 is a primary metabolite of Tolvaptan, primarily metabolized by the CYP3A4 enzyme in the liver. In SCHH cells, DM-4107 inhibits the human liver transport proteins NTCP, BSEP, MRP3, and MRP4, with IC50 values of 95.6, 119, 61.2, and 37.9 μM respectively, affecting bile acid transport. It is applicable for research on autosomal dominant polycystic kidney disease (ADPKD).

HDAC6-IN-43 (compound 26) is a potent inhibitor of HDACs. This compound effectively inhibits various HDACs, notably HDAC1, HDAC2, and HDAC6, with an IC50 of less than 150 nM, and demonstrates particularly high sensitivity to HDAC6 with an IC50 of 11 nM. HDAC6-IN-43 is utilized in the study of autosomal dominant polycystic kidney disease (ADPKD).

TBK1degrader-4 (Compound 30) is a molecular glue degrader targeting TBK1. It effectively inhibits cyst growth, reduces inflammation, and lowers levels of pro-inflammatory factors such as Ccl2, IFNβ, and IL-6. TBK1degrader-4 shows potential for research in autosomal dominant polycystic kidney disease (ADPKD).

DM-4103 is a primary metabolite of Tolvaptan, predominantly metabolized by the CYP3A4 enzyme in the liver. In SCHH cells, DM-4103 inhibits the human liver transport proteins NTCP, BSEP, MRP2, MRP3, and MRP4 with IC50 values of 16.3, 4.15, 51.0, 44.6, and 4.26 μM, respectively, and affects bile acid transport. DM-4103 is applicable for research in autosomal dominant polycystic kidney disease (ADPKD).

XYDC2050 (Compound 29) is a selective vasopressin V2 receptor (V2R) antagonist, with an IC50 of 27 nM and a Ki of 2.8 nM. It exhibits a Ki of 420.7 nM for V1R with a selectivity index of 162. XYDC2050 inhibits vasopressin-induced intracellular cyclic adenosine monophosphate (cAMP) accumulation with an IC50 of 12 nM. This compound can suppress kidney cyst growth, reduce kidney-to-body weight ratio, and decrease cyst area and cystic index, making it a candidate for autosomal dominant polycystic kidney disease (ADPKD) research.

Vasopressin V2 receptor antagonist 1 (Compound 4g) is a vasopressin V2 receptor (V2R) antagonist with a Ki of 3.8 nM, used in the treatment of autosomal dominant polycystic kidney disease (ADPKD).

CDK7-IN-20 is a potent, selective, and irreversible inhibitor of Cyclin-Dependent Kinase 7 (CDK7) with an IC50 value of 4 nM, exhibiting over 206-fold selectivity against related kinases [CDK1, CDK2, CDK3, CDK5, CDK6, CDK9, and CDK12]. It holds potential for research into autosomal dominant polycystic kidney disease (ADPKD).