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PKD

" in MedChemExpress (MCE) Product Catalog:

52

Inhibitors & Agonists

1

Screening Libraries

3

Peptides

2

Natural
Products

1

Recombinant Proteins

1

Isotope-Labeled Compounds

3

Antibodies

10

Oligonucleotides

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-131962A

    PDK-1 Metabolic Disease Cancer
    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 dihydrochloride
  • HY-131962

    PKD Metabolic Disease Cancer
    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 .
    PKD-IN-1
  • HY-RS00002

    Small Interfering RNA (siRNA) PKD Others

    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 Mouse Pre-designed siRNA Set A
    Pkd1 Mouse Pre-designed siRNA Set A
  • HY-RS00003

    Small Interfering RNA (siRNA) PKD Others

    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 Human Pre-designed siRNA Set A
    PKD1 Human Pre-designed siRNA Set A
  • HY-RS00004

    Small Interfering RNA (siRNA) PKD Others

    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.

    Pkd1 Rat Pre-designed siRNA Set A
    Pkd1 Rat Pre-designed siRNA Set A
  • HY-RS10591

    Small Interfering RNA (siRNA) Others

    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 Human Pre-designed siRNA Set A
    PKD2 Human Pre-designed siRNA Set A
  • HY-RS10592

    Small Interfering RNA (siRNA) Others

    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 Mouse Pre-designed siRNA Set A
    Pkd2 Mouse Pre-designed siRNA Set A
  • HY-RS10593

    Small Interfering RNA (siRNA) Others

    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.

    Pkd2 Rat Pre-designed siRNA Set A
    Pkd2 Rat Pre-designed siRNA Set A
  • HY-RS00005

    Small Interfering RNA (siRNA) Others

    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.

    PKD1L1 Human Pre-designed siRNA Set A
    PKD1L1 Human Pre-designed siRNA Set A
  • HY-RS00006

    Small Interfering RNA (siRNA) Others

    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.

    PKD1L2 Human Pre-designed siRNA Set A
    PKD1L2 Human Pre-designed siRNA Set A
  • HY-RS00007

    Small Interfering RNA (siRNA) Others

    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.

    PKD1L3 Human Pre-designed siRNA Set A
    PKD1L3 Human Pre-designed siRNA Set A
  • HY-RS10594

    Small Interfering RNA (siRNA) Others

    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.

    PKD2L1 Human Pre-designed siRNA Set A
    PKD2L1 Human Pre-designed siRNA Set A
  • HY-128142

    PKD PKC Cardiovascular Disease
    PKC/PKD-IN-1 (Compound 13C) is an orally active dual protein kinase C/D (PKC/PKD) inhibitor with an IC50 value of 0.6 nM for PKD1. PKC/PKD-IN-1 can attenuate high-salt diet-induced cardiac hypertrophy and can be used in the study of heart failure .
    PKC/PKD-IN-1
  • HY-12239
    CID755673
    5+ Cited Publications

    PKD Cancer
    CID755673 is a potent PKD inhibitor with IC50s of 182 nM, 280 nM and 227 nM for PKD1, PKD2 and PKD3, respectively.
    CID755673
  • HY-13454

    PKD Cancer
    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.
    CID 2011756
  • HY-118052

    PKD Cardiovascular Disease
    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 .
    BPKDi
  • HY-15528

    PKD Cancer
    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.
    kb NB 142-70
  • HY-112547

    CRT0066051

    PKD Others
    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 .
    CRT5
  • HY-151374

    PKD Cancer
    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 .
    3-IN-PP1
  • HY-15698A
    CRT0066101 dihydrochloride
    2 Publications Verification

    PKD Pim Apoptosis Inflammation/Immunology Cancer
    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 exhibits anti-inflammatory activity in mice LPS (HY-D1056)-induced lung injury models, and has anticancer effects .
    CRT0066101 dihydrochloride
  • HY-15698
    CRT0066101
    2 Publications Verification

    PKD Pim Apoptosis Inflammation/Immunology Cancer
    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 exhibits anti-inflammatory activity in mice LPS (HY-D1056)-induced lung injury models, and has anticancer effects .
    CRT0066101
  • HY-15698B

    PKD Pim Apoptosis Inflammation/Immunology Cancer
    CRT0066101 trihydrochloride is the trihydrochloride salt form of CRT0066101 (HY-15698). CRT0066101 trihydrochloride is an orally active PKD inhibitor with IC50 values of 1 nM, 2.5 nM and 2 nM for PKD1, PKD2, and PKD3, respectively. CRT0066101 trihydrochloride is also an inhibitor for PIM2 with an IC50 of ~135.7 nM. CRT0066101 trihydrochloride exhibits anti-inflammatory activity in mice LPS (HY-D1056)-induced lung injury models, and has anticancer effects .
    CRT0066101 trihydrochloride
  • HY-151372

    PKD 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 .
    Protein kinase D inhibitor 1
  • HY-103199

    SDZ21009

    5-HT Receptor Neurological Disease
    Carpindolol (SDZ21009) is a 5-HT1B receptor antagonist (pKd of 8.53 and pKB of 8.0) and a 5-HT1D receptor agonist (pEC50 of 5.91 and pKd of 6.37) .
    Carpindolol
  • HY-16698

    Others Cancer
    kb-NB77-78 is an analogue of CID797718, but shows no PKD inhibitory activity .
    kb-NB77-78
  • HY-138563

    Epigenetic Reader Domain Cancer
    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) .
    GSK973
  • HY-103197

    RX821002 hydrochloride

    Adrenergic Receptor Neurological Disease
    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) .
    2-Methoxyidazoxan monohydrochloride
  • HY-14557
    Pimavanserin
    Maximum Cited Publications
    12 Publications Verification

    ACP-103

    5-HT Receptor Neurological Disease
    Pimavanserin is a selective inverse agonist of the 5-HT2A receptor with pIC50 and pKd of 8.73 and 9.3, respectively.
    Pimavanserin
  • HY-N2057

    Aquaporin Metabolic Disease
    Steviol is a major metabolite of the sweetening compound stevioside. Steviol slows renal cyst growth by reducing AQP2 expression and promoting AQP2 degradation .
    Steviol
  • HY-N2057R

    Aquaporin Metabolic Disease
    Steviol (Standard) is the analytical standard of Steviol. This product is intended for research and analytical applications. Steviol is a major metabolite of the sweetening compound stevioside. Steviol slows renal cyst growth by reducing AQP2 expression and promoting AQP2 degradation .
    Steviol (Standard)
  • HY-P1233

    Motilin Receptor Metabolic Disease
    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
  • HY-114204

    Epigenetic Reader Domain Cancer
    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 .
    GSK8814
  • HY-P1233A

    Motilin Receptor Metabolic Disease
    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 .
    ANQ-11125 TFA
  • HY-135392

    AC-279

    Drug Metabolite Neurological Disease
    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.
    N-Desmethyl Pimavanserin
  • HY-117051

    Others Cancer
    STA-2842 is a small molecule agent that inhibits heat shock protein 90 (HSP90) to treat autosomal dominant polycystic kidney disease (ADPKD). The disease is caused by inherited mutations in the PKD1 or PKD2 genes that aberrantly activate multiple signaling proteins and pathways that regulate cell proliferation. Through network construction, we found that many HSP90 client proteins associated with ADPKD are regulated by HSP90. STA-2842 induced degradation of these clients in Pkd1?/? primary kidney cells and in vivo. In experiments using conditional Cre-mediated in vivo knockout of Pkd1 in mice, we found that weekly administration of STA-2842 for 10 weeks significantly reduced initial renal cyst formation and kidney growth in mice and slowed disease progression in mice with pre-existing cysts. These improved disease phenotypes were accompanied by improvements in renal function markers and reductions in the expression and activity of HSP90 clients and their effectors, with the extent of this inhibition correlating with the extent of cyst expansion in individual animals. Pharmacokinetic analysis showed that HSP90 was overexpressed in cystic kidney tissue and HSP90 inhibitors were selectively retained in cystic tissue, which is similar to the situation in solid tumors. These results provide a preliminary basis for evaluating HSP90 inhibitors as therapeutic agents for ADPKD.
    STA-2842
  • HY-B1281
    Mepyramine maleate
    2 Publications Verification

    Pyrilamine maleate

    Histamine Receptor Neurological Disease Endocrinology
    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.
    Mepyramine maleate
  • HY-14557R

    5-HT Receptor Neurological Disease
    Pimavanserin (Standard) is the analytical standard of Pimavanserin. This product is intended for research and analytical applications. Pimavanserin is a selective inverse agonist of the 5-HT2A receptor with pIC50 and pKd of 8.73 and 9.3, respectively.
    Pimavanserin (Standard)
  • HY-130614

    PROTACs Histone Methyltransferase Cancer
    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-1
  • HY-130615

    PROTACs Histone Methyltransferase Cancer
    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 .
    PROTAC EED degrader-2
  • HY-12689
    Mitapivat
    1 Publications Verification

    AG-348

    Pyruvate Kinase Metabolic Disease
    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 .
    Mitapivat
  • HY-12689A

    AG-348 hemisulfate sesquihydrate

    Pyruvate Kinase Metabolic Disease
    Mitapivat hemisulfate sesquihydrate (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 .
    Mitapivat hemisulfate sesquihydrate
  • HY-12689B

    AG-348 hemisulfate

    Pyruvate Kinase Metabolic Disease
    Mitapivat hemisulfate is an orally active pyruvate kinase allosteric activator. Mitapivat hemisulfate 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 hemisulfate can be used in study of PK deficiency .
    Mitapivat hemisulfate
  • HY-B1281R

    Histamine Receptor Neurological Disease Endocrinology
    Mepyramine maleate (Standard) is the analytical standard of Mepyramine maleate. This product is intended for research and analytical applications. 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.
    Mepyramine maleate (Standard)
  • HY-106258

    OHM 11638; BAX-ACC 1638; MOT 288

    Motilin Receptor Metabolic Disease
    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 .
    Atilmotin
  • HY-144425

    NEKs Inflammation/Immunology
    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 .
    BSc5367
  • HY-135392S

    AC-279-d9 hydrochloride

    Isotope-Labeled Compounds Neurological Disease
    N-Desmethyl Pimavanserin-d9 hydrochloride (AC-279-d9 hydrochloride) is the deuterium labeled N-Desmethyl Pimavanserin (HY-135392). 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 .
    N-Desmethyl Pimavanserin-d9 hydrochloride
  • HY-19490

    AQW-051

    nAChR Neurological Disease
    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 .
    VQW-765
  • HY-12709A

    Adrenergic Receptor Cardiovascular Disease Inflammation/Immunology
    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 .
    ARC 239 dihydrochloride
  • HY-130816

    VH032-O-Ph-PEG1-NH2

    E3 Ligase Ligand-Linker Conjugates Cancer
    (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 .
    (S,R,S)-AHPC-O-Ph-PEG1-NH2
  • HY-101009

    Metitepine maleate; Ro-8-6837 maleate

    5-HT Receptor Neurological Disease
    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 maleate

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