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Inhibitors & Agonists

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Cat. No. Product Name Field of Application Chemical Structure
DC81306 PMEG
PMEG is a nuclear DNA polymerases α, δ, and ε inhibitor that causes DNA chain termination, inhibits DNA synthesis, induces cytotoxicity in dividing cells. PMEG is an acyclic nucleotide phosphonate that forms an active phosphorylated metabolite, PMEG diphosphate, within cells. PMEG has activity against leukemia and melanoma in rodent models. PMEG has poor cell permeability; its prodrug is Rabacfosadine (GS-9219). PMEG shows antiviral activity against against various DNA virus infections including murine cytomegalovirus (MCMV) and human cytomegalovirus (HCMV). PMEG can be used for the research of non-hodgkin's lymphoma[1][2].
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DC81305 PLX-4104
PLX-4104 is an orally active BRD4 molecular glue degrader with a DC50 of 2 nM. PLX-4104 selectively promotes BRD4 degradation via DCAF11 recruitment, triggering ubiquitination and proteasomal breakdown. PLX-4104 inhibits cancer cell proliferation. PLX-4104 induces complete regression of AML xenograft tumors. PLX-4104 can be used for the research of acute myeloid leukemia.
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DC81304 Plenolin
Plenolin is an anticancer agent. Plenolin exhibits inhibitory activity against human epidermoid carcinoma cells. Plenolin shows in vivo antitumor activity against ascites carcinosarcoma and lymphocytic leukemia in rodent models. Plenolin can be used for research related to ascites tumors and leukemia.
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DC81303 PLAGL2-IN-1
PLAGL2-IN-1 is a inhibitor of pleiomorphic adenoma-like protein 2 (PLAGL2) with a Kd of 2.23 µM. PLAGL2-IN-1 suppresses PLAGL2 transcriptional activity, induces G0/G1 cell cycle arrest, and apoptosis, thereby inhibiting hepatocellular carcinoma (HCC) cell proliferation. PLAGL2-IN-1 disrupts extracellular matrix organization and suppresses the PI3K-AKT pathway by reducing AKT phosphorylation. PLAGL2-IN-1 inhibits tumor growth in an HCCLM3 xenograft mouse model. PLAGL2-IN-1 can be used for the research of HCC.
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DC81302 PKMYT1-IN-12
PKMYT1-IN-12 (Compound 4) is a selective inhibitor of PKMYT1, with an IC₅₀ of 2.6 nM. PKMYT1-IN-12 can effectively inhibit the phosphorylation of CDK1, with an IC₅₀ of 44 nM. PKMYT1-IN-12 is a target protein ligand that can be used for the synthesis of PROTAC D16-M1P2.
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DC81301 PKMYT1-IN-11
PKMYT1-IN-11 (Example 1) is a PKMYT1 inhibitor with an IC50 of 4.49 nM. PKMYT1-IN-11 inhibits the proliferation of HCC1569 cells. When combined with Gemcitabine, PKMYT1-IN-11 shows a significant anti-tumor effect in the OVCAR3 xenograft mouse model. PKMYT1-IN-11 can be used for the study of various cancers such as breast cancer and ovarian cancer.
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DC81300 PKM2 agonist-1
PKM2 agonist-1 (Compound D16) is a highly effective, allosteric PKM2 agonist with an AC50 value of 77 nM. PKM2 agonist-1 inhibits Ang II-induced smooth muscle cell phenotypic switching. PKM2 agonist-1 effectively prevents aortic dissection and results in reduced mortality.
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DC81297 Pitavastatin magnesium
Pitavastatin magnesium is an orally active HMG-CoA Reductase inhibitor. Pitavastatin magnesium lowers total cholesterol and low-density lipoprotein cholesterol in a hyperlipidemic rat model. Pitavastatin magnesium can be used in research on cardiovascular and cerebrovascular diseases such as hyperlipidemia.
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DC81296 Piroctone
Piroctone is a potent hydroxypyridone antimicrobial agent that shows remarkable activity against fungi including Candida species. Piroctone inhibits hyphal induction of Candida albicans. Piroctone can efficiently chelate intracellular iron to induce relevant cytotoxicity in neuroblastoma cells. Piroctone can be used for antimicrobial and neuroblastoma research.
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DC81294 Piperidine-CO-C8-COOH
Piperidine-CO-C8-COOH is a PROTAC linker. Piperidine-CO-C8-COOH can be used to synthesize PROTAC BRD4 Degrader-42.
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DC81293 PIN1 degrader-3
PIN1 degrader-3 is a Pin1 (peptidyl-prolyl isomerase protein) (IC50 = 4.65 nM) degrader. PIN1 degrader-3 bound covalently to Pin1. PIN1 degrader-3-induced Pin1 degradation reduced cell viability, with EC50 values after 72 h of 8.4 μM in MIA PaCa-2 cells and 5.3 μM in KPC cell lines.PIN1 degrader-3 can destabilize Pin1 in vitro, causing its degradation in cells. PIN1 degrader-3 can be used for the study of pancreatic cancer.
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DC81291 PIM-IN-3
PIM-IN-3 (Compound 50) is an orally active new anti-intestinal worm drug. PIM-IN-3 exhibits strong inhibitory activity in vitro, especially for whipworms (IC50 = 6.6 µM). PIM-IN-3 has low cytotoxicity. PIM-IN-3 can be used in the research of gastrointestinal nematode diseases.
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DC81289 PI3Kδ-IN-27
PI3Kδ-IN-27 is an PI3Kδ inhibitor with an IC50 of 355.3 nM. PI3Kδ-IN-27 exhibits anti-SARS-CoV-2 activity. PI3Kδ-IN-27 can be used for the research of infection, such as COVID-19.
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DC81288 PI3Kα-IN-31
PI3Kα-IN-31 is an orally active and selective PI3Kα inhibitor. PI3Kα-IN-31 shows potent preference for mutant PI3Kα over wild-type PI3Kα. PI3Kα-IN-31 exerts antiproliferative effects in PI3Kα-mutant cancer cells. PI3Kα-IN-31 suppresses tumor growth in xenograft models. PI3Kα-IN-31 can be used for the research of breast cancer.
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DC81287 PI3Kα-IN-28
PI3Kα-IN-28 (Compound 23) is an efficient dual targeted PI3K/BRD4 inhibitor. PI3Kα-IN-28 can inhibit the proliferation of various cells, such as KYSE180 and KYSE450 cells. PI3Kα-IN-28 can concentration dependently inhibit migration and colony formation, induce G0/G1 phase arrest, significantly inhibit DNA synthesis, and significantly increase the proportion of senescent cells. PI3Kα-IN-28 can inhibit the expression of p-AKT and c-Myc and activate the AMPK-p27 pathway. PI3Kα-IN-28 can be used for research on cancers such as esophageal cancer.
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DC81286 PI3Kα-IN-27
PI3Kα-IN-27 (Compound 50b) is an orally active PI3K-α inhibitor, with an IC50 of 40 nM. PI3Kα-IN-27 effectively inhibits PAK3, p110α, phospho-mTOR and phospho-ERK1/2. PI3Kα-IN-27 induces early Apoptosis. PI3Kα-IN-27 shows anticancer activity against pancreatic cancer, lung cancer, breast cancer.
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DC81285 PI3K/PIKK-IN-2
PI3K/PIKK-IN-2 (compound 2) is an inhibitor of PI3K/PIKK. PI3K/PIKK-IN-2 can be used in preparing antibody-drug conjugates (ADCs).
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DC81283 PI3K/AKT-IN-5
PI3K/AKT-IN-5 (Compound 3h) is a PI3K/AKT inhibitor. PI3K/AKT-IN-5 exhibits outstanding broad-spectrum anti-cancer activity, especially being sensitive to colorectal cancer. PI3K/AKT-IN-5 significantly reduces cell colony formation, induces G2/M phase cell cycle arrest and cell apoptosis. PI3K/AKT-IN-5 can be used for research on colorectal cancer.
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DC81282 PI3K/AKT/ERK/CREB activator 1
PI3K/AKT/ERK/CREB activator 1 is an orally active PI3K/AKT/ERK/CREB pathway activator. PI3K/AKT/ERK/CREB activator 1 maintains neuronal survival and function, promotes neuronal proliferation, restores the viability of damaged neurons, and facilitates synapse formation. PI3K/AKT/ERK/CREB activator 1 alleviates neuroinflammation by reducing the levels of pro-inflammatory cytokines, preserves synaptic ultrastructure and restores spatial memory in Alzheimer's disease models. PI3K/AKT/ERK/CREB activator 1 can be used in research related to Alzheimer's disease.
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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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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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