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Inhibitors & Agonists

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Cat. No. Product Name Field of Application Chemical Structure
DC81275 PHD-1-IN-2
PHD-1-IN-2 is an orally active inhibitor of hypoxia-inducible factor prolyl hydroxylase domain 1 (PHD-1) with an IC50 of 0.07 μM. PHD-1-IN-2 acts as a substrate of MDR1 in MDR1-MDCK cell monolayer assays. PHD-1-IN-2 can be used in the research of ischemia, inflammatory responses and neurodegenerative diseases, such as inflammatory bowel disease and ischemia-reperfusion injury.
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DC81273 PFKFB4-IN-1
PFKFB4-IN-1 is a potent and selective ATP-competitive PFKFB4 inhibitor (IC50 = 4.50 μM) that reduces intracellular PFKFB4 protein levels. PFKFB4-IN-1 exhibits >12-fold selectivity over PFKFB1/4 and PFKFB3/4. PFKFB4-IN-1 inhibits cancer cell proliferation, induces apoptosis, and inhibits cell migration. PFKFB4-IN-1 inhibits tumor growth in the MDA-MB-231 xenograft mouse model. PFKFB4-IN-1 can be used for breast, lung and liver cancer research.
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DC81272 PF-5236216
PF-5236216 is a brain-penetrant CK1δ/CK1ε inhibitor with IC50 values of 8 and 36 nM. PF-5236216 inhibits CK1δ and CK1ε-mediated PER3 nuclear translocation. PF-5236216 forms an H-bond with the backbone NH of Leu85, hydrophobic stacking with Met82, and a water-mediated H-bond with Lys38 of CK1δ. PF-5236216 can be used as a tool ligand for CNS PET studies.
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DC81271 PF-07245303
PF-07245303 is a ITK/TRK inhibitor. PF-07245303 reduces the production of inflammatory cytokines such as IL-4 and IFNγ, and inhibits the phosphorylation of PLCγ1. PF-07245303 inhibits nerve growth factor-induced basophil activation and the phosphorylation of TRKA. PF-07245303 reduces oxazolone-induced ear swelling in mouse ear tissues. PF-07245303 is applicable to research related to atopic dermatitis.
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DC81270 PF-03246799 monohydrochloride
PF-03246799 monohydrochloride is a potent and selective 5-HT2C receptor agonist with an EC50 of 190 nM and a Ki of 160 nM. PF-03246799 monohydrochloride shows selectivity for 5-HT2C over 5-HT2A and 5-HT2B receptors. PF-03246799 monohydrochloride has the potential for stress urinary incontinence (SUI) research.
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DC81269 Perrimustine
Perrimustine is a cysteamine (CysA) derivative with potent antitumor activity. Perrimustine exhibits significant effect on B16 melanoma and metastasized melanoma cells by causing DNA damage. Perrimustine exhibits antitumor effects in mice bearing various cancers, including lung carcinoma, leukemia, lymphoma, melanoma, colon carcinoma, and glioma. Perrimustine can be used for cancer research, such as melanoma and leukemia.
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DC81268 Periplocoside O
Periplocoside O is a natural steroid.
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DC81266 Pegcantratinib
Pegcantratinib (CT327) is a potent and selective TRKA antagonist with activity against TRKB and TRKC. Pegcantratinib can be used for research of CYLD cutaneous syndrome (CCS) and inflammatory dermatoses, such as psoriasis and concomitant pruritus.
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DC81265 PD-L1-IN-8
PD-L1-IN-8 is a PD-L1 inhibitor (IC50 = 0.89 nM). PD-L1-IN-8 shows low CYP inhibition and minimal hERG activity. PD-L1-IN-8 can be used for the study of colon cancer.
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DC81262 PDE5/CA-IN-1
PDE5/CA-IN-1 is a dual PDE5 and carbonic anhydrase (CA) inhibitor, with IC50 values of 0.41, 38.4, and 9.1 nM against PDE5, hCA II, and hCA VA, respectively. PDE5/CA-IN-1 inhibits multiple hCA subtypes associated with Alzheimer's disease. As a cytoprotective agent and oxidative stress alleviator, PDE5/CA-IN-1 reduces oxidative stress, and prevents recognition memory and working memory impairments. PDE5/CA-IN-1 is available for the research of Alzheimer's disease.
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DC81260 PDE4-IN-32
PDE4-IN-32 (Compound B05) is a selective, blood-brain barrier permeable PDE4B and PDE4D inhibitor with IC50 values of 13.7 nM and 23.8 nM, respectively. PDE4-IN-32 promotes the recovery of motor and cognitive function in MCAO/R mouse models. PDE4-IN-32 reduces cerebral edema. PDE4-IN-32 can be used for the research of ischemic stroke.
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DC81259 PDE4B/D-IN-5
PDE4B/D-IN-5 (Compound P32) is a peripherally restricted, oral active inhibitor of PDE4B and PDE4D with extremely low blood-brain barrier penetration, with IC50 values of 3.4 nM and 2.2 nM, respectively. PDE4B-IN-8 inhibits the production of TNF-α. PDE4B/D-IN-5 significantly reduces the Bax/Bcl2 ratio, and alleviates oxidative stress by decreasing MPO activity and NO levels. PDE4B/D-IN-5 exhibits anti-inflammatory, antioxidant, and anti-apoptotic activities. PDE4B/D-IN-5 can be used for the research of acute lung injury.
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DC81258 PDE4/5-IN-1
PDE4/5-IN-1 is a selective phosphodiesterase 4/5 (PDE4/5) dual inhibitor. PDE4/5-IN-1 functionally inhibits PDE5, PDE4B2, and PDE4D2 activity. PDE4/5-IN-1 relaxes isolated rat prostate tissue, enhances nitric oxide-induced relaxation in isolated rat prostate tissue, and reduces alpha-1 adrenoceptor-mediated contractile responses in isolated rat prostate tissue. PDE4/5-IN-1 inhibits proliferation of human hyperplastic prostate cells. PDE4/5-IN-1 can be used for the research of benign prostatic hyperplasia.
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DC81254 PDE10A-IN-1
PDE10A-IN-1 is a phosphodiesterase 10A (PDE10A) inhibitor with an IC50 of 250 nM and the ability to cross the blood-brain barrier. PDE10A-IN-1 can be used in research on neurological disorders such as schizophrenia.
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DC81253 PD-143188
PD-143188 (CI 1007) is a selective agonist targeting dopamine (DA) receptors, with Ki values of 25.5 nM and 16.6 nM for human D2 and D3 receptors, respectively and lower affinity for D4.2 receptors (Ki=90.9 nM). PD-143188 inhibits DA release, synthesis and metabolism, while reducing cellular cyclic AMP levels, exerting antipsychotic activity. PD-143188 is promising for research of psychopharmacology.
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DC81252 PD-1/PD-L1-IN-61
PD-1/PD-L1-IN-61 is a PD-1/PD-L1 interaction inhibitor with a human IC50 of 5.3 nM. PD-1/PD-L1-IN-61 embeds into the hydrophobic pocket at the PD-L1 dimer interface, stabilizing binding through hydrogen bonds and π-π stacking with PD-L1 residues. PD-1/PD-L1-IN-61 acts as an immune activator, enhances immune-killing activity of peripheral blood mononuclear cells against cancer cells, restores T-cell immune function, and promotes IFN-γ secretion. PD-1/PD-L1-IN-61 can be used for the research of triple-negative breast cancer.
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DC81251 PD-1/PD-L1-IN-60
PD-1/PD-L1-IN-60 is the counterpart of the small-molecule immuno-probe [18F] LG‑8, and the two together enable integrated immuno-diagnosis and therapy. PD-1/PD-L1-IN-60 exhibits potent anti-tumor activity in mouse models of melanoma and lung cancer with high PD‑L1 uptake. PD-1/PD-L1-IN-60 can be used for relevant research on melanoma and lung cancer.
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DC81250 PD 168368 derivative-1
PD 168368 derivative-1 (Compound 16) is a derivative of PD 168368, with Ki values of 0.46 and 3.7 nM for the subtypes of bombesin receptor (BB₁ and BB₂). PD 168368 derivative-1 can be used for the study of various diseases, such as cancer, depression, and eating disorders.
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DC81249 PC6-VC-PAB-MMAE
PC6-VC-PAB-MMAE is a Drug-Linker Conjugates for ADC. PC6-VC-PAB-MMAE consists of the ADC Cytotoxin MMAE and a linker. PC6-VC-PAB-MMAE can be used for synthesis of ADCs.
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DC81248 PB2-IN-3
PB2-IN-3 (Compound 11) is a PB2 inhibitor. PB2-IN-3 exhibits antiviral activity against Influenza A H1N1 and H3N2 strains. PB2-IN-3 can be used in studies related to influenza A virus infection.
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DC81245 Parsalmide
Parsalmide is an orally active non-steroidal anti-inflammatory drug and gastroprotective agent, with an IC50 of 9.92 μM against COX-1 and 155 μM against COX-2. Parsalmide prevents gastric injury and reduces edema. Parsalmide can be used in the research of arthritis.
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DC81243 PARP1-IN-55
PARP1-IN-55 is a potent and selective PARP1 inhibitor with an IC50 value of 0.019 μM. PARP1-IN-55 exhibits anti-proliferative selective activity against MCF-7 breast cancer cells (IC50 = 3.6 μM). PARP1-IN-55 inhibits the PARP1-mediated DNA damage repair pathway, induces ROS accumulation, disrupts mitochondrial membrane potential, induced apoptosis and suppresses cancer cell migration, invasion, and colony formation. PARP1-IN-55 can be used for the study of breast cancer.
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DC81241 PARP1-IN-51
PARP1-IN-51 (P55 the second compound in the fifth row) is a PARP1 inhibitor. PARP1-IN-51 can be used for the research of cancer, such as breast cancer.
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DC81240 PARP1-IN-50
PARP1-IN-50 is a selective and orally active PARP-1 inhibitor with an IC50 of 64.98 nM. PARP1-IN-50 can inhibit PAR formation and induce DNA double strand breaks, thereby causing DNA damage. PARP1-IN-50 can induce G2/M phase arrest and cancer cells apoptosis. PARP1-IN-50 demonstrates significant antiproliferative activity against various cancer cells. PARP1-IN-50 can be used for the research of cancer, such as breast cancer.
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DC81239 PARP1-IN-48
PARP1-IN-48 (Compound 61) is a highly selective PARP1 (PARP1 IC50 = 3 nM, PARP2 IC50 = 170 nM) inhibitor. PARP1-IN-48 can be used for research on cancer, viral infections, and metabolic conditions.
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DC81238 PARP1-IN-47
PARP1-IN-47 (Compound 35) is a highly selective PARP1 inhibitor (IC50 <100 nM). PARP1-IN-47 blocks poly(ADP-ribosyl)ation and disrupts DNA damage repair pathways to induce tumor cell apoptosis. PARP1-IN-47 is promising for research of solid tumors and hematological malignancies.
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DC81236 PARP1/NAMPT-IN-1
PARP1/NAMPT-IN-1 is a potent and dual PARP1 and NAMPT inhibitor with IC50 values of 1.2 nM and 6.7 nM, respectively. PARP1/NAMPT-IN-1 can disrupt the homologous recombination repair (HRR) pathway, leading to the accumulation of DNA double-strand breaks (DSBs), inducing cell cycle arrest and apoptosis, and also has antimigratory effects. PARP1/NAMPT-IN-1 exhibits excellent antitumor effects in a breast cancer xenograft model. PARP1/NAMPT-IN-1 can be used for the study of triple-negative breast cancer (TNBC).
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DC81235 PARP1/ERK IN-1
PARP1/ERK IN-1 is a dual PARP1/ERK inhibitor, with a PARP1 IC50 of 0.9 nM and an ERK2 IC50 of 1.8 nM. PARP1/ERK IN-1 inhibits proliferation and migration of various cancer cell lines, and induces apoptosis and DNA damage. PARP1/ERK IN-1 suppresses tumor growth in mouse models of colorectal cancer, and reduces the expression of Ki‑67, BRCA1 and Rad51. PARP1/ERK IN-1 can be used in the research of colorectal cancer, triple-negative breast cancer and pancreatic cancer.
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DC81234 PARP1/c-Met-IN-3
PARP1/c-Met-IN-3 (Compound L19) is a selective c-Met and PARP1 inhibitor, with an IC50 of 5.4 nM against c-Met and an IC50 of 3.7 nM against PARP1. PARP1/c-Met-IN-3 inhibits PARP2 enzymatic activity with an IC50 of 4.52 nM, and shows no specificity for PARP1 and PARP2. PARP1/c-Met-IN-3 induces cell cycle arrest and apoptosis. PARP1/c-Met-IN-3 exhibits anti-tumor activity against triple-negative breast cancer.
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DC81233 Pantothenate kinase-IN-3
Pantothenate kinase-IN-3 is a PANK3-selective binder and CoA biosynthesis activator with a human PANK3 Ki of 9.1 nM, human PANK3 Ka of 1.8 nM, human PANK1β Ki of 113 nM, human PANK1β Ka of 23.4 nM, and oral effectiveness.Pantothenate kinase-IN-3 binds PANK3 via a water-mediated interaction between its sulfonamide NH and Gly193, elevates cellular, hepatic, and forebrain CoA levels, and shows improved metabolic stability in mouse and human microsomes.Pantothenate kinase-IN-3 has solubility properties favorable at pH 7.Pantothenate kinase-IN-3 can be used for the research of hepatic metabolic CoA deficiencies (acidemias).
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