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Novel inhibitors

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Cat. No. Product Name Field of Application Chemical Structure
DC81281 Phosphonoformyl-CMP
Phosphonoformyl-CMP (CMP-5'-Phosphonoformic acid) is a nucleoside metabolite.
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DC81280 Phe-PEG1-Dasa
Phe-PEG1-Dasa is a BCR-ABL PROTAC degrader, with its DC50 being 1.56 nM. Phe-PEG1-Dasa uses a single amino acid (Phe) as the E3 ligand and employs the N-end rule pathway to induce the degradation of the target protein, significantly reducing the molecular size, thus being called a mini-PROTAC. Phe-PEG1-Dasa significantly inhibits the proliferation of K562 cells. Phe-PEG1-Dasa can be used for the study of leukemia. (Pink: Bcr-Abl ligand ; Blue: Ligands for E3 Ligase ligand ; Black: linker).
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DC81279 Phenylaminojuglone AJ-2
Phenylaminojuglone AJ-2 is a nitric oxide synthase inhibitor that interacts with soluble guanylate cyclase, β-adrenergic receptor, CaV1.2 calcium channel, KV channel and KCa channel. Phenylaminojuglone AJ-2 blocks extracellular Ca2+ influx, regulates the activity of the NO−sGC−cGMP signaling pathway, and inhibits pharmacologic and electromechanical contractions of smooth muscle. Phenylaminojuglone AJ-2 is applicable to studies related to intestinal spasm.
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DC81278 Phenylalanylphenylalanylamide
Phenylalanylphenylalanylamide (H-Phe-Phe-NH₂) is a ligand for the substance P 1–7 (SP1-7) binding site with a Ki value of 1.5 nM. Phenylalanylphenylalanylamide exerts significant anti-allodynic and anti-hyperalgesic effects in animal models of neuropathic pain following central administratio. Phenylalanylphenylalanylamide shows no distinct effect after peripheral (intraperitoneal) administration. Phenylalanylphenylalanylamide can be used for research on pain-related diseases.
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DC81277 Phenamacide hydrochloride
Phenamacide hydrochloride is an anti-spasmodic agent that can be used for the study of urinary incontinence.
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DC81276 PHD-1-IN-4
PHD-1-IN-4 is a brain-penetrant PHD-1 inhibitor with an IC50 of 0.074 μM.
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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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DC81274 PGK1-IN-2
PGK1-IN-2 (Compound 60) is a PGK1 inhibitor with an IC50 of 8.24 μM. PGK1-IN-2 demonstrates a significant ability to inhibit the proliferation of osteosarcoma cells. PGK1-IN-2 interferes with the glycolytic pathway of tumor cells by inhibiting PGK1. PGK1-IN-2 inhibits cell migration and invasion, and induces cell S phase and G2-M phase cycle arrest. PGK1-IN-2 may kill cells by inducing cuproptosis. PGK1-IN-2 shows a significant anti-tumor effect in the MNNG-HOS osteosarcoma xenograft mouse model. PGK1-IN-2 can be used for the study of osteosarcoma.
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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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DC81267 Penisimplicissin
Penisimplicissin is a funicone-like compound and antiviral agent. Penisimplicissin reduces the expression of AhR and viral nucleocapsid protein. Penisimplicissin improves the cell viability and morphological characteristics of CCoV-infected cells. Penisimplicissin inhibits CCoV infection. Penisimplicissin can be used in studies related to canine coronavirus infection.
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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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DC81264 PDL1 degrader-3
PDL1 degrader-3 (comppund e24) is a CSN5-binding antitumor immunomodulator with a human CSN5 Kd of 4.53 μM. PDL1 degrader-3 inhibits CSN5 enzymatic activity, increases PD-L1 ubiquitination, and induces PD-L1 degradation via the ubiquitin-proteasome pathway, reducing PD-L1 expression on tumor cell membranes. PDL1 degrader-3 blocks PD-1/PD-L1 interaction, activates the tumor immune microenvironment, enhances tumor-infiltrating T-cell immunity, and inhibits activation of immunosuppressive MDSCs and Tregs. PDL1 degrader-3 exerts antitumor effects in mouse tumor models. PDL1 degrader-3 can be used for the research of colorectal cancer, lung cancer.
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DC81263 PDI-IN-5
PDI-IN-5 (compound 30z) is an allosteric-covalent inhibitor targeting protein disulfide isomerase (PDI) with a 2-chloro-pyrrolopyrimidin-4-one scaffold, with an IC50 of 0.4 μM. PDI-IN-5 exhibits selectivity for ERp57 and GPX4, and inhibits glioblastoma. PDI-IN-5 can be used in glioblastoma-related research.
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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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DC81261 PDE4-IN-33
PDE4-IN-33 is a phosphodiesterase 4 (PDE4) inhibitor. PDE4-IN-33 reduces uric acid levels. PDE4-IN-33 PDE4-IN-33 can be used for the research of hyperuricemia and gout.
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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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DC81257 PDE3/4-IN-4
PDE3/4-IN-4 is an orally active PDE3A and PDE4B inhibitor with IC50 values of 10 nM and 9.4 nM, respectively. PDE3/4-IN-4 shows selective activity relative to most other PDE family members. PDE3/4-IN-4 modulates the cAMP/PKA/CREB signaling pathway. PDE3/4-IN-4 inhibits pro-inflammatory factor IL-6. PDE3/4-IN-4 reduces expression of inflammatory markers in liver tissue. PDE3/4-IN-4 attenuates liver fibrosis. PDE3/4-IN-4 limits liver damage in cholestatic and sepsis-induced liver disease mice models. PDE3/4-IN-4 can be used for the research of liver injury, cholestatic liver diseases, sepsis-induced liver injury.
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DC81256 PDE1-IN-12
PDE1-IN-12 (P78, the first compound in 12) is a PDE1 inhibitor. PDE1-IN-12 inhibits PDEl-mediated suppression of the dopamine D1 receptor intracellular pathway and can be used for narcolepsy.
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DC81255 PDE1-IN-11
PDE1-IN-11 (Compound 5cc) is an orally active and highly selective PDE1A1 inhibitor. PDE1-IN-11 increases intracellular cAMP and cGMP levels, activating the PKA-CREB and NO-cGMP-PKG signaling pathways, promoting osteoblast differentiation and bone formation, while suppressing osteoclastogenesis and bone resorption. PDE1-IN-11 is promising for research of postmenopausal osteoporosis (PMO) and other bone metabolism disorders.
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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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