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PROTAC AR Degrader-4 comprises a IAP ligand binding group, a linker and an Androgen Receptor (AR) binding group. PROTAC AR Degrader-4 is an AR degrader. Degradation inducers based on cIAP1 are called specific and non-genetic IAP-dependent protein erasers (SNIPERs).In Vitro: Specific and Nongenetic IAPs-dependent Protein Erasers (SNIPERs) are bifunctional compounds which are designed by conjugating […]
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PROTAC AR-V7 degrader-1 (Compound 6) is a potent, orally?bioavailable and selective AR-V7 degrader with the DC50?of 0.32?μM by recruiting VHL E3?ligase?to Androgen receptor?(AR) DNA binding?domain (DBD) binder. PROTAC AR-V7 degrader-1 exhibits activity against 22Rv1 cell-line expressing AR-V7 with the EC50 of 0.88 μM.
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PROTAC Bcl-xL degrader-2 is a potent Bcl-xL (Bcl-2 family member) degrader based on von Hippel-Lindau ligand, with an IC50 of 0.6 nM.In Vitro: PROTAC Bcl-xL degrader-2 (PROTAC 6; 0.1 nM-10 μM; 24 hours) treatment decreases the level of Bcl-xL protein in THP-1 cells.PROTAC Bcl-xL degrader-2 (PROTAC 6) inhibits caspase 3/7 activity in MOLT-4 cells with […]
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PROTAC Bcl2 degrader-1 (Compound C5) is a PROTAC based on Cereblon ligand, which potently and selectively induces the degradation of Bcl-2 (IC50, 4.94 μM; DC50, 3.0 μM) and Mcl-1 (IC50, 11.81 μM) by introducing the E3 ligase cereblon (CRBN)-binding ligand pomalidomide to Mcl-1/Bcl-2 dual inhibitor Nap-1.IC50 & Target: IC50: 4.94 μM (Bcl-2), 11.81 μM (Mcl-1)DC50: […]
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PROTAC BET-binding moiety 1 is a key intermediate for the synthesis of high-affinity BET inhibitors.In Vitro: The bromodomain and extra-terminal (BET) family proteins, consisting of BRD2, BRD3, BRD4, and testis-specific BRDT members, are epigenetic “readers” and play a key role in the regulation of gene transcription. BET proteins are considered to be attractive therapeutic targets […]
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PROTAC BRAF-V600E degrader-1 is a potent PROTAC BRAF-V600E degrader with Kd value of 2.4 nM and 2 nM for BRAF and BRAF-V600E, respectively. PROTAC BRAF-V600E degrader-1 degrades BRAF-V600E via the ubiquitin-proteasome system (UPS). PROTAC BRAF-V600E degrader-1 can inhibit melanoma cell growth.In Vitro: PROTAC BRAF-V600E degrader-1 (compound 23) (1 nM-10 μM; 72 h) inhibits the cell […]
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PROTAC BRD4 degrader for PAC-1 (compound 5), a PROTAC-linker Conjugate for PAC, comprises the chimeric BET degrader GNE-987 and disulfide-containing linker.
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PROTAC BRD4 Degrader-11 (compound 9a) is a PROTAC connected by ligands for von Hippel-Lindau and BRD4. PROTAC BRD4 Degrader-11 can be conjugated with STEAP1 and CLL1 antibodies to degrade the BRD4 protein in PC3 prostate cancer cells, with a DC50 of 0.23 nM and 0.38 nM, respectively.
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PROTAC BRD4 ligand-1 is a potent BET inhibitor and a ligand for target BRD4 protein for PROTACT GNE-987 (HY-129937A).
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PROTAC CBP/P300 Degrader-1 is a potent PROTAC CBP/P300 degrader. PROTAC CBP/P300 Degrader-1 potently inhibited cell viability of multiple cancer cell lines.In Vitro: PROTAC CBP/P300 Degrader-1 shows LNCaP prostate cancer cell viability inhibition (IC50=0.4 nM). PROTAC CBP/P300 Degrader-1 (10 nM) induces degradation of P300 (≥ 80%).PROTAC CBP/P300 Degrader-1 potently inhibited cell viability of multiple cancel cell […]
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PROTAC CRBN Degrader-1 comprises a cereblon (CRBN) ligand binding group, a linker and an von Hippel-Landau (VHL) binding group. PROTAC CRBN Degrader-1 is an cereblon (CRBN) degrader.
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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.IC50 & Target: pKD: 9.02 (EED)pIC50: 8.17 (PRC2)In Vitro: PROTAC EED degrader-1 (Compound PROTAC 2) binds to EED with a pKD of 9.02±0.09 and inhibits […]
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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.IC50 & Target: pKD: 9.27 (EED)pIC50: 8.11 (PRC2)In Vitro: PROTAC EED degrader-2 (Compound PROTAC 1) binds to EED with a pKD of 9.27±0.05 and inhibits […]
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PROTAC ER Degrader-4 is a von Hippel-Lindau-based PROATC estrogen receptor (ER) degrader, binding to ER with an IC50 of 0.8 nM. PROTAC ER Degrader-4 induces ER degradation in MCF-7 cells with an IC50 of 0.3 nM.In Vitro: PROTAC ER Degrader-4 shows equal to 100% ER degradation at 0.3 μM in the MCF-7 ER degradation cellular […]
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PROTAC ERRα Degrader-3 is a potent and selective ERRα degrader based on von Hippel-Lindau ligand. PROTAC ERRα Degrader-3 is capable of specifically degrading ERRα protein by >80% at a concentration of 30 nM. PROTAC ERRα Degrader-3 is inactive against ERRβ and ERRγ proteins.In Vitro: PROTAC ERRα Degrader-3 (compound 6c; 0.3 nM-10 μM; 4 hours) dose-dependently […]
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PROTAC EZH2 Degrader-1 (Compound 150d), a potent PROTAC EZH2 Degrader, exerts inhibitory effect on EZH2 methyltransferase activity with the IC50 of 2.7 nM. EZH2 plays an important role in many tumorigenesis and development processes.IC50 & Target: IC50: 2.7 nM (EZH2)
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PROTAC FKBP Degrader-3 is a PROTAC that comprises a FKBP ligand binding group, a linker and an von Hippel-Lindau binding group. PROTAC FKBP Degrader-3 is a potent FKBP degrader.IC50 & Target: FKBPIn Vitro: PROTAC treatment time courses demonstrated a notable increase in polyubiquitination of EGFP-FKBP in response to treatment with 250 nM of PROTAC FKBP […]
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PROTAC FLT-3 degrader 1 is a von Hippel-Lindau-based PROTAC FLT-3 internal tandem duplication (ITD) degrader with an IC50 0.6 nM. Anti-proliferative activity; apoptosis induction.IC50 & Target: IC50: 0.6 nM (FLT-3 ITD)
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PROTAC IRAK4 degrader-1 is a Cereblon-based PROTAC interleukin-1 receptor-associated kinase 4 (IRAK4) degrader extracted from patent US20190192668A1 Compound I-210, makes 20-50%, and >50% IRAK4 degradation at 0.01, 0.1, and 1 μM in OCI-LY-10 cells, respectively.
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PROTAC IRAK4 ligand-1 is a synthetic ligand for interleukin-1 receptor-associated kinase 4 (IRAK4). PROTAC IRAK4 ligand-1 can be used in the synthesis of PROTAC IRAK4 degrader-1 (HY-129966).
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PROTAC K-Ras Degrader-1 (Compound 518) is a PROTAC. PROTAC K-Ras Degrader-1 can effectively degrades K-Ras based on Cereblon E3 ligand, exhibits ≥70% degradation efficacy in SW1573 cells.IC50 & Target:PROTAC, K-RasIn Vitro:PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target […]
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PROTAC KRAS G12C degrader-1 is a Cereblon-based KRASG12C PROTAC degrader. PROTAC KRAS G12C degrader-1 induces CRBN/ KRASG12C dimerization and degrades GFP- KRASG12C in reporter cells.In Vitro:PROTAC KRAS G12C degrader-1 (Compound 10) engages CRBN in cells, bound KRASG12C in vitro, induces CRBN/KRASG12C dimerization, and degrades GFP-KRASG12C in reporter cells in a CRBN-dependent manner.
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PROTAC Mcl1 degrader-1 (compound C3), a proteolysis targeting chimera (PROTAC) based on Cereblon ligand, is a potently and selectively Mcl-1 (Bcl-2 family member) inhibitor with an IC50 of 0.78 μM. PROTAC Mcl1 degrader-1 inhibits Bcl-2 with an IC50 of 0.54 μM.In Vitro:PROTAC Mcl1 degrader-1 (compound C3) induces the ubiquitination and proteasomal degradation of Mcl-1 by […]
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PROTAC PD-1/PD-L1 degrader-1, a PD-1/PD-L1 PROTAC based on Cereblon E3 ligand, inhibits PD-1/PD-L1 interaction with an IC50 of 39.2 nM. PROTAC PD-1/PD-L1 degrader-1 significantly restores the immunity repressed in a co-culture model of Hep3B/OS-8/hPD-L1 and CD3 T cells. PROTAC PD-1/PD-L1 degrader-1 moderately reduces the protein levels of PD-L1 in a lysosome-dependent manner.In Vitro: PROTAC PD-1/PD-L1 […]
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PROTAC SGK3 degrader-1 (SGK3-PROTAC1), is a potent SKG3 degrader based on von Hippel-Lindau ligand. PROTAC SGK3 degrader-1 (0.3 μM) induces 50% degradation of endogenous SGK3 within 2 hours, with maximal 80% degradation observed within 8 hours, accompanied by a loss of phosphorylation of NDRG1 (an SGK3 substrate).
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PROTAC-O4I2 is a PROTAC targets splicing factor 3B1 (SF3B1). PROTAC-O4I2 induces FLAG-SF3B1 degradation with an IC50 value of 0.244 μM in K562 cells. PROTAC-O4I2 also induces cellular apoptosis in K562 WT cells.In Vitro: PROTAC-O4I2 introduces Thalidomide to ubiquitin E3 ligase cereblon (CRBN), which selectively degrades SF3B1 and inhibits tumor growth in cells.PROTAC-O4I2 degrades and inhibits […]
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Protease-Activated Receptor-1, PAR-1 Agonist is a selective proteinase-activated receptor1 (PAR-1) agonist peptide. Protease-Activated Receptor-1, PAR-1 Agonist corresponds to PAR1 tethered ligand and which can selectively mimic theactions of thrombin via this receptor[2].IC50 & Target: PAR-1In Vitro: Protease-Activated Receptor-1, PAR-1 Agonist induces activation of protein kinase C isoenzymes alpha and epsilon in human HT-29 colon carcinoma […]
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Protease-Activated Receptor-3 (PAR-3) (1-6), human TFA is a proteinase-activated receptor (PAR-3) agonist peptide.IC50 & Target: PAR-3
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Protein deglycase DJ-1 against-1, a DJ-1-binding compound, dependently targets DJ1. Protein deglycase DJ-1 against-1 penetrates through the blood brain barrier (BBB). Protein deglycase DJ-1 against-1 is used as a neuroprotective agent and has the potential for Parkinson’s disease research.In Vivo: Protein deglycase DJ-1 against-1 (compound-23; 1 mg/kg; IP; pretreatment one hour; daily; for 4 days) […]
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Przewalskinic acid A is a phenolic acid found in the Salvia przewalskii Maxim herb. Phenolic acids show potent antioxidant activities and potential effects in protecting against brain and heart damage caused by ischemia reperfusion.
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Przewaquinone A, a lipophilic diterpene quinone present only in Salvia przewalskii, induces a potent inhibitory action on vascular contraction.
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Psammaplin A, a marine metabolite, is a potent inhibitor of HDAC and DNA methyltransferases. Psammaplin A ia a highly potent and selective DAC1 inhibitor with an IC50 of 0.9 nM. Psammaplin A possess the antimicrobial effect on the Gram-positive bacteria and inhibits DNA synthesis and DNA gyrase activity. Antitumor Activity[2].IC50 & Target:IC50: 0.9 nM (DAC1)
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PSB-603 is a potent and highly selective A2B adenosine receptor antagonist exhibiting a Ki value of 0.553 nM and virtually no affinity for the human and rat A1 and A2A and the human A3 receptors up to a concentration of 10 μM.In Vitro: PSB-603 is a potent and selective adenosine A2B receptor antagonist exhibiting a […]
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PSB36 is a potent and selective antagonist of adenosine A1 receptor, with Kis 0.12 nM, 187 nM, 552 nM, 2300 nM, and 6500 nM for rA1, hA2B, rA2A, hA3 and rA3 receptors respectively. PSB36 can be used for the research of hyperalgesia[2].
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Pseudocoptisine (Isocoptisine) chloride is a quaternary alkaloid with benzylisoquinoline skeleton, was isolated from Corydalis Tuber. Pseudocoptisine chloride inhibits acetylcholinesterase (AChE) activity with an IC50 of 12.8 μM. Anti-inflammatory and anti-amnestic effects[2].In Vitro: Pseudocoptisine (0, 60, 90 μM; 1 hour) dose-dependently inhibited LPS-induced NO production in RAW264.7 cells[2].Pseudocoptisine (30-90 μM; 1 hour; RAW264.7 cells) significantly reduces […]
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PSI-6206-13C,d3 (RO-2433-13C,d3) is the deuterium labeled PSI-6206. PSI-6206 is the deaminated derivative of PSI-6130, which is a potent and selective inhibitor of HCV NS5B polymerase. PSI-6206 low potently inhibits HCV replicon with EC90 of >100 μM.
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Psychosine (Galactosylsphingosine), a substrate of the galactocerebrosidase (GALC) enzyme, is a potential biomarker for Krabbe disease. Psychosine is a highly cytotoxic lipid, capable of inducing cell death in a wide variety of cell types including, most relevantly to globoid cell leukodystrophy (GLD), oligodendrocytes. Psychosine causes cell death at least in part via apoptosis. Psychosine also […]
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Pt(II) Octaethylporphine ketone is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
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PT2399 is a potent and selective HIF-2α antagonist, which directly binds to HIF-2α PAS B domain with an IC50 of 6 nM. PT2399 displays potent antitumor activity in vivo[2].IC50 & Target: IC50: 6 nM (HIF-2α)In Vitro: PT2399 (compound 10f) inhibits HIF-2α with an IC50 of 6 nM. PT2399 can bind directly to the HIF-2α PAS […]
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Pterosin B, a indanone found in bracken fern (Pteridium aquilinum), is an inhibitor of salt-inducible kinase 3 (Sik3) signaling. Pterosin B prevents chondrocyte hypertrophy and osteoarthritis in mice by inhibiting Sik3[2].
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