polycystic kidney disease

BLU2864 is an orally active, highly selective, ATP-competitive PRKACA inhibitor with an IC50 of 0.3 nM, exhibiting anti-tumor activity and potential applications in cancer and polycystic kidney disease research [1] [2].

PPQ-102 (CFTR Inhibitor), an effective CFTR inhibitor, can completely inhibit CFTR chloride current (IC50: 90 nM).

BSc5367 is a potent inhibitor of the structural domain of Nek1 kinase with an IC50=11.5 nM. Nek1 is a NIMA-associated protein kinase tightly linked to cell cycle regulation, DNA repair, and microtubule regulation. BSc5367 can be used in studies related to amyotrophic lateral sclerosis (ALS), polycystic kidney disease (PKD), and several types of radiotherapy-resistant cancers.

AV457 is a potent and selective inhibitor of mTOR. It effectively suppresses cyst growth in polycystic kidney disease (PKD) organoids. AV457 reduces the protein expression of P-s6 and P-p70s6, but it does not decrease the protein expression of P-AKT.

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).

1. Steviol (NSC-226902), a natural sweetener, it inhibits proliferation of the gastrointestinal cancer cells intensively. 2. Steviol can induce a significant increase in CYP3A29 expression. 3. Steviol inhibits the proliferation of the human osteosarcoma U2OS cell line in a dose- and time-dependent manner. 4. Steviol can treat polycystic kidney disease, it slowed cyst growth, in part, by reducing AQP2 transcription, promoted proteasome, and lysosome-mediated AQP2 degradation.

Ibiglustat (Venglustat) succinate is an orally active, brain-penetrant inhibitor of glucosylceramide synthase (GCS) utilized in the investigation of Gaucher disease type 3, Parkinson's disease associated with GBA mutations, Fabry disease, GM2 gangliosidosis, and autosomal dominant polycystic kidney disease.

GFB-12811 is an orally active, selective, and potent CDK5 inhibitor, used in the study of autosomal dominant polycystic kidney disease.

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).

CYP4A11/CYP4F2-IN-2 (compound 15) serves as an orally administered inhibitor targeting CYP4A11/4F2, exhibiting IC50 values of 120 nM and 220 nM, respectively. This compound effectively suppresses 20-HETE production within the rat kidney and shows promise in mitigating the progression of diabetic nephropathy and autosomal dominant polycystic kidney disease [1].

Endo CNTinh-03 effectively inhibits the increase of cAMP and cGMP triggered by agonists such as G protein-coupled receptors, adenylate cyclase, and guanylate cyclase, with an IC50 of 4 μM. It also blocks the chloride ion currents induced by cholera toxin and Escherichia coli (STa) toxins, alleviates secretory diarrhea in mouse models, and prevents cyst growth in models of polycystic kidney disease.