pkd

PKD-IN-1 is an inhibitor of PKD.

N-Cyclohexyl-4-[1-(1-piperazinyl)-2,6-naphthyridin-3-yl]-2-pyridinamine is a novel 2,6-naphthyridine identified by high throughput screen (HTS) as a dual protein kinase C D (PKC PKD) inhibitor[1].

CRT0066101 dihydrochloride is an effective and selective PKD inhibitor (IC50s: 1, 2.5 and 2 nM for PKD1, 2, and 3).

CID755673 is an effective and specific cell-active inhibitor for PKD (IC50: 182 nM); exhibits selective PKD1 inhibition when compared with PLK1, AKT, CAMKIIα, CAK, and PKC isoforms.

PKD-IN-1 dihydrochloride is an inhibitor of PKD.

BPKDi is a potent and selective inhibitor of PKD (protein kinase D).

Mepyramine maleate (Pyrilamine maleate) is a histamine H1 antagonist. It has mild hypnotic properties and some local anesthetic action and is used for allergies (including skin eruptions) both parenterally and locally. It is a common ingredient of cold remedies.

CID-797718 is a protein kinase D1 (PKD1) inhibitor.

AQW051 (VQW-765) is an orally active alpha-7 nicotinic acetylcholine receptor (α7-nAChR) specific activator that interacts with recombinant human α7-nAChR expression (pKD value 7.56). Alpha7-nachr is considered an attractive target for the treatment of cognitive impairments associated with neurological disorders, so VQW-051 is often used in studies of anxiety disorders and acute anxiety.

kb-NB77-78 is an analog of CID797718, which is a by-product of the synthesis of the parental compound, CID755673(PKD1 inhibitor).

ARC 239 dihydrochloride is a selective α2B adrenoceptor antagonist with pKD values of 8.8, 6.7, and 6.4 at α2B, α2A, and α2D receptors respectively (pKD values are 8.8, 6.7, and 6.4 at α2B, α2A, and α2D receptors respectively).

PROTAC EED degrader-2 is a PROTAC targeting EED (pKD of 9.27) and an inhibitor of polycomb repressive complex 2 (PRC2) with a pIC50 of 8.11.

CID 2011756 is an ATP-competitive and specific PKD1 inhibitor.

β-adrenoceptor and 5-HT1A 1B receptor antagonist

1-NM-PP1 (PP1 Analog II) is a cell-permeable PP1 analog that acts as a potent and selective inhibitor of mutant kinases over their wild-type progenitors.

RX821002 is a potent and selective antagonist of α2-adrenoceptor with low affinity for imidazoline sites. RX821002 displays selectivity for the α2D over the α2A subtypes (pKd values are 9.7 and 8.2 respectively).

CRT5, a pyrazine benzamide, is a potent and selective PKD inhibitor. It inhibits VEGF-induced phosphorylation of three PKD substrates (IC50s = 1, 2, and 1.5 nM for PKD1, PKD2, and PKD3, respectively), histone deacetylase 5, CREB (cAMP-response-element-binding protein), and HSP27 (heat-shock protein 27) at Ser82. Additionally, CRT5 decreases VEGF-induced endothelial migration, proliferation, and tubulogenesis[1].

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.

Protein kinase D (PKD), a serine threonine protein kinase activated by diacylglycerol downstream of PKC signaling, has three human isoforms that modulate cell proliferation, survival, invasion, and protein transport. CRT0066101 acts as an inhibitor of these three PKD isoforms, with IC50 values of 1, 2.5, and 2 nM for PKD1, PKD2, and PKD3, respectively. It demonstrates selectivity for PKD over a range of more than 90 protein kinases, including PKCα, PKBα, MEK, ERK, c-Raf, c-Src, and c-Abl. This specificity allows CRT0066101 to inhibit cell proliferation, induce apoptosis, and notably reduce the viability of pancreatic cancer cells both in vitro and in vivo.

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.

kb NB 142-70 is a selective protein kinase D (PKD) inhibitor with IC50 values of 28.3 nM, 58.7 nM, and 53.2 nM for PKD1, PKD2, and PKD3 respectively.

GSK8814 is a selective and ATAD2 2B bromodomain chemical probe and inhibitor (binding constant pKd=8.1 and a pKi=8.9 in BROMOscan). GSK8814 displays 500-fold selectivity for ATAD2 over BRD4 BD1. GSK8814 binds to ATAD2 and BRD4 BD1 (pIC50s: 7.3 and 4.6).

(S,R,S)-AHPC-O-Ph-PEG1-NH2 (VH032-O-Ph-PEG1-NH2) is an E3 ligase ligand-linker conjugate that combines a VHL ligand for the E3 ubiquitin ligase with a PROTAC linker; it is used in PROTAC EED degrader-1, targeting EED with a potency (pKD) of 9.02[1].

3-IN-PP1, a potent protein kinase D (PKD) inhibitor, exhibits pan-PKD inhibitory activity with IC50 values of 108 nM for PKD1, 94 nM for PKD2, and 108 nM for PKD3. Additionally, it serves as a broad-spectrum anticancer agent by inhibiting the growth of various tumor cells. 3-IN-PP1 is utilized in cancer research [1].