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PKD-IN-1 dihydrochloride (compound 32), an aminoethylamino-aryl (AEAA) compound, acts as PKD-1 inhibitor. PKD-IN-1 can be used for protein kinase D (PKD)-mediated diseases research .
PKD-IN-1 (compound 32), an aminoethylamino-aryl (AEAA) compound, acts as PKD-1 inhibitor. PKD-IN-1 can be used for protein kinase D (PKD)-mediated diseases research .
Pkd1 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Pkd1 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
PKD1 Human Pre-designed siRNA Set A contains three designed siRNAs for PKD1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
Pkd1 Rat Pre-designed siRNA Set A contains three designed siRNAs for Pkd1 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
PKD2 Human Pre-designed siRNA Set A contains three designed siRNAs for PKD2 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
Pkd2 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Pkd2 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
Pkd2 Rat Pre-designed siRNA Set A contains three designed siRNAs for Pkd2 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
PKD1L1 Human Pre-designed siRNA Set A contains three designed siRNAs for PKD1L1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
PKD1L2 Human Pre-designed siRNA Set A contains three designed siRNAs for PKD1L2 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
PKD1L3 Human Pre-designed siRNA Set A contains three designed siRNAs for PKD1L3 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
PKD2L1 Human Pre-designed siRNA Set A contains three designed siRNAs for PKD2L1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
CID 2011756 is an ATP competitive PKD inhibitor, with an IC50 of 3.2 µM for PKD1 in cell free assay, and also shows cellular pan-PKD inhibitory activity against PKD2 and PKD3 (IC50, 0.6 and 0.7 µM, respectively). CID 2011756 also has antitumor activity.
BPKDi is a potent bipyridyl PKD inhibitor with IC50s of 1 nM, 9 nM and 1 nM for PKD1, PKD2 and PKD3, respectively. BPKDi blocks signal-dependent phosphorylation and nuclear export of class IIa HDACs in cardiomyocytes .
kb NB 142-70 is a potent PKD inhibitor, with IC50s of 28.3, 58.7 and 53.2 nM for PKD1, PKD2, and PKD3, respectively. kb NB 142-70 also has antitumor activity.
CRT0066101 dihydrochloride is a potent and orally active PKD inhibitor with IC50 values of 1 nM, 2.5 nM and 2 nM for PKD1, PKD2, and PKD3, respectively . CRT0066101 dihydrochloride is also a potent PIM2 inhibitor with an IC50 of ~135.7 nM. CRT0066101 dihydrochloride has anticancer effects .
CRT0066101 is a potent and orally active PKD inhibitor with IC50 values of 1 nM, 2.5 nM and 2 nM for PKD1, PKD2, and PKD3, respectively . CRT0066101 is also a potent PIM2 inhibitor with an IC50 of ~135.7 nM. CRT0066101 has anticancer effects .
CRT5, a pyrazine benzamide, is a potent and selective inhibitor for all three isoforms of PKD in endothelial cells treated with VEGF (IC50s = 1, 2, and 1.5 nM for PKD1, PKD2, and PKD3, respectively). CRT5 decreases VEGF-induced endothelial migration, proliferation and tubulogenesis .
3-IN-PP1 is a protein kinase D (PKD) inhibitor. 3-IN-PP1 has potent pan-PKD inhibitory activity for PKD1, PKD2 and PKD3 with IC50 values of 108, 94 and 108 nM, respectively. 3-IN-PP1 also is a broad spectrum anticancer agent and has inhibition of several tumor cells growth. 3-IN-PP1 can be used for the research of cancer .
Protein kinase D inhibitor 1 (compound 17m) is a pan-PKD inhibitor, with IC50 values ranging from 17 to 35 nM. Protein kinase D inhibitor 1 inhibits PKD-dependent cortactin phosphorylation .
GSK973 is a highly selective, orally bioavailable inhibitor of the BD2s (second bromodomains) of the BET family, with a pIC50 of 7.8 and a pKd of 8.7 for BRD4 BD2. GSK973 displays a 1600-fold selectivity for BRD4 BD2 over BRD4 BD1. GSK973 shows good potency against BRD2 BD2, BRD3 BD2, and BRDT BD2 (pIC50=7.4~7.8; pKd=8.3~8.5) .
2-Methoxyidazoxan monohydrochloride (RX821002 hydrochloride) is a highly selective alpha 2-adrenoceptor antagonist with little or no imidazoline antagonist effect. RX 821002 has markedly higher affinity for (guinea-pig) alpha 2D-adrenoceptors (pKd 9.7) than for (rabbit) alpha 2A-adrenoceptors (pKd 8.2) .
ANQ-11125 is a potent and selective antagonist of motilin, with the pKd of 8.24. ANQ-11125 blocks motilide-induced contractions in vitro in the rabbit .
GSK8814 is a potent, selective, and ATAD2/2B bromodomain chemical probe and inhibitor, with a binding constant pKd=8.1 and a pKi=8.9 in BROMOscan. GSK8814 binds to ATAD2 and BRD4 BD1 with pIC50s of 7.3 and 4.6, respectively. GSK8814 shows 500-fold selectivity for ATAD2 over BRD4 BD1 .
ANQ-11125 TFA is a potent and selective antagonist of motilin, with the pKd of 8.24. ANQ-11125 TFA blocks motilide-induced contractions in vitro in the rabbit .
N-Desmethyl Pimavanserin is the active metabolite of Pimavanserin. Pimavanserin is a selective inverse agonist of the 5-HT2A receptor with pIC50 and pKd of 8.73 and 9.3, respectively.
Mitapivat (AG-348) is an orally active pyruvate kinase allosteric activator. Mitapivat increases enzymatic activity, protein stability, and ATP levels over a broad range of PKLR genotypes, shows the potential to restore the activity of PK (pyruvate kinase)-deficient glycolytic pathways. Mitapivat can be used in study of PK deficiency .
Mepyramine maleate, a first generation antihistamine, is an antagonist of histamine H1 receptor, with Kds of 0.8 nM, 5200 nM and >3000 nM for H1, H2, and H3 receptor, respectively, and a pKd of 9.4 for H1 receptor.
PROTAC EED degrader-1 is a von Hippel-Lindau-based PROTAC targeting EED with a pKD of 9.02. PROTAC EED degrader-1 is a polycomb repressive complex 2 (PRC2) inhibitor (pIC50=8.17) targeting the EED subunit .
PROTAC EED degrader-2 is a von Hippel-Lindau-based PROTAC targeting EED with a pKD of 9.27. PROTAC EED degrader-2 is a polycomb repressive complex 2 (PRC2) inhibitor (pIC50=8.11) targeting the EED subunit .
OHM 11638 (Atilmotin), an analogue of the (1-14) fragment of porcine motilin, is a motilin receptor agonist with a pKd of 8.94 for the motilin receptor. OHM 11638 affects esophageal, lower esophageal sphincter (LES), and gastric motility. OHM 11638 increases LES and gastric pressures, OHM 11638 can be used as prokinetic agents .
BSc5367 is a potent Nek1 inhibitor with an IC50 of 11.5 nM. NIMA-related protein kinase Nek1 is crucially involved in cell cycle regulation, DNA repair and microtubule regulation and dysfunctions of Nek1 play key roles in amyotrophic lateral sclerosis (ALS), polycystic kidney disease (PKD) and several types of radiotherapy resistant cancer .
VQW-765 (AQW-051) is a selective and orally active alpha-7 nicotinic acetylcholine receptor (α7-nAChR) agonist with a pKD value of 7.56 to recombinantly expressed human α7-nAChR. VQW-765 shows anxiolytic-like effect in vivo. VQW-765 can be used for the research of anxiety disorder and acute performance anxiety .
ARC 239 dihydrochloride is a selective α2B/2C adrenoceptor antagonist (pKd values are 5.95, 7.41 and 7.56 at α2A, α2B, and α2C receptors respectively). ARC 239 dihydrochloride binds to CHO cell membranes expressing human recombinant a2A-, a2B- or a2C-adrenoceptor subtypes with pKis of 5.6, 8.4, and 7.08, respectively .
(S,R,S)-AHPC-O-Ph-PEG1-NH2 (VH032-O-Ph-PEG1-NH2) is E3 ligase ligand-linker conjugate and incorporates a VHL ligand for the E3 ubiquitin ligase, and a PROTAC linker. (S,R,S)-AHPC-O-Ph-PEG1-NH2 is used in PROTAC EED degrader-1 (HY-130614). PROTAC EED degrader-1 is a PROTAC targeting EED with a pKD of 9.02 .
Methiothepin maleate is a potent and non-selective 5-HT2 receptor antagonist, with pKds of 7.10 (5-HT1A), 7.28 (5HT1B), 7.56 (5HT1C), 6.99 (5HT1D), 7.0 (5-HT5A), 7.8 (5-HT5B), 8.74 (5-HT6), and 8.99 (5-HT7), and pKis of 8.50 (5HT2A), 8.68 (5HT2B), and 8.35 (5HT2C).
Methiothepin (Metitepine) mesylate is a potent and non-selective 5-HT2 receptor antagonist, with pKds of 7.10 (5-HT1A), 7.28 (5HT1B), 7.56 (5HT1C), 6.99 (5HT1D), 7.0 (5-HT5A), 7.8 (5-HT5B), 8.74 (5-HT6), and 8.99 (5-HT7), and pKis of 8.50 (5HT2A), 8.68 (5HT2B), and 8.35 (5HT2C).
Apoptosis is an ordered and orchestrated cellular process that occurs in physiological and pathological conditions, which is also called programmed cell death (PCD). Apoptosis plays a crucial role in developing and maintaining the health of the body by eliminating old cells, unhealthy cells and unnecessary cells. Too little or too much apoptosis contribute to many diseases. When apoptosis does not work correctly, cells that should be eliminated may persist and become immortal, for example, in cancer and leukemia. When apoptosis works overly well, it kills too many cells and inflicts grave tissue damage. This is the case in strokes and neurodegenerative disorders such as Alzheimer's, Huntington's, and Parkinson's disease.
MCE designs a unique collection of 2238 apoptosis-related compounds mainly focusing on the key targets in the apoptosis signaling pathway and can be used in the research of apoptosis signal pathway and related diseases.
ANQ-11125 is a potent and selective antagonist of motilin, with the pKd of 8.24. ANQ-11125 blocks motilide-induced contractions in vitro in the rabbit .
ANQ-11125 TFA is a potent and selective antagonist of motilin, with the pKd of 8.24. ANQ-11125 TFA blocks motilide-induced contractions in vitro in the rabbit .
OHM 11638 (Atilmotin), an analogue of the (1-14) fragment of porcine motilin, is a motilin receptor agonist with a pKd of 8.94 for the motilin receptor. OHM 11638 affects esophageal, lower esophageal sphincter (LES), and gastric motility. OHM 11638 increases LES and gastric pressures, OHM 11638 can be used as prokinetic agents .
Protein kinase D2 (PRKD2) is a serine/threonine protein kinase that mediates various cellular processes downstream of PKC. It affects cell proliferation through MAPK1/3 (ERK1/2) signaling, activates NF-kappa-B under oxidative stress, inhibits HDAC7 transcriptional repression, and regulates T cell antigen receptor (TCR) signaling, cytokine production, Golgi trafficking, angiogenesis, particle release, and cell adhesion. Protein Kinase D2/PRKD2 Protein, Human (sf9, His-GST) is the recombinant human-derived protein Kinase D2/PRKD2 protein, expressed by Sf9 insect cells , with N-His, N-GST labeled tag. The total length of Protein Kinase D2/PRKD2 Protein, Human (sf9, His-GST) is 878 a.a., with molecular weight of ~120 kDa.