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WDR5-0102 is an inhibitor targeting WDR5-MLL1 interface (Kdis=7 μM, Kd=4 μM). WDR5-0102 suppresses MLL1 HMT activity, but not human H3K4 methyltransferase SETD7 and six other HMTs: G9a, EHMT1, SUV39H2, SETD8, PRMT3, and PRMT5[2].
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WDR5-IN-4 TFA is an inhibitor of the WIN site of chromatin-associated WD repeat-containing protein 5 (WDR5), with a Kd of 0.1 nM. WDR5-IN-4 TFA displaces WDR5 from chromatin and decreases the expression of associated genes, causing translational inhibition, nucleolar stress. Anti-cancer activity.
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WEE1-IN-4 is a potent checkpoint Wee1 kinase inhibitor with an IC50 of 0.011 μM.IC50 & Target:IC50: 0.011 μM (Wee1 kinase)pIC50: 7.96
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WEHI-9625 is a tricyclic sulfone, first-in-class inhibitor of apoptosis with an EC50 of 69 nM. WEHI-9625 binds to VDAC2 and promotes its ability to inhibit apoptosis driven by mouse BAK. WEHI-9625 is completely inactive against both human BAK and the closely related apoptosis effector BAX.In Vitro: WEHI-9625 (0-10 μM; Mcl1?/?Bax?/? MEFs cells) treatment could prevent […]
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WF-47-JS03 is a potent and selective RET kinase inhibitor with IC50s of 1.7 nM and 5.3 nM for KIF5B-RET transfected Ba/F3 cells and CCDC6-RET transfected LC-2/ad lung cancer cells, respectively. WF-47-JS03 demonstrates >500-fold selectivity against kinase insert domain receptor (KDR). Effective brain penetration.In Vitro: WF-47-JS03 inhibits Tel-KDR transfected Ba/F3 cells and Ba/F3 wild-type cell lines […]
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WH-10417-099 is a degrader that could collectively induce degradation of the largest number of unique kinases (>125 unique kinases).
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Wilforgine is a bioactive sesquiterpene alkaloid in Tripterygium wilfordii Hook. F. Wilforgine can induce microstructural and ultrastructural changes in the muscles of Mythimna separata larvae, and the sites of action are proposed to be calcium receptors or channels in the muscular system[2].
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Withanolide B is an active component of W. somnifera Dunal. Withanolide B promotes osteogenic differentiation of hBMSCs via ERK1/2 and Wnt/β-catenin signaling pathways. Withanolide B exhibits neuroprotective, anti-arthritic, anti-aging and anti-cancer effects[2].In Vitro: Withanolide B (1-100 nM; 3-5 days) significantly increases the expression of COL1A1 and RUNX2 genes and proteins in hBMSCs.Withanolide B (1-100 nM; […]
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WL12 is a specifically targeting programmed death ligand 1 (PD-L1) binding peptide. WL12 can be radiolabeled by different radionuclides, generating radiotracers, which can assess the tumor PD-L1 expression.IC50 & Target: PD-L1
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WNK1-IN-1 is a selective inhibitor of WNK1 with an IC50 value of 1.6 μM. WNK1-IN-1 inhibits OSR1 phosphorylation with an IC50 value of 4.3 μM. WNK1-IN-1 can be used for the research of blood pressure regulation and cancer.IC50 & Target:IC50: 1.6 μM (WNK1), 4.3 μM (OSR1 phosphorylation)In Vitro: WNK1-IN-1 (0-1000 μM; 30 min) shows high […]
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Wnt pathway activator 1 is a potent Wnt activator extracted from patent WO2012024404A1, compound 1, has an EC50s of 28-29 nM.IC50 & Target: IC50: 28-29 nM (Wnt)
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Wnt/β-catenin agonist 3 hydrochloride is a Wnt/β-catenin signalling pathway agonist. Wnt/β-catenin agonist 3 (compound 98) can be used for the research of osteoporosis.In Vitro: Wnt/β-catenin agonist 3 hydrochloride (compound 98; 24 h; HEK293 and SW480 cells) has 54% cell activity at 120 μM concentration compared with the positive control group LiCl (20mM).Wnt/β-catenin agonist 3 hydrochloride […]
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Wnt/β-catenin agonist 4 (Derivative 83) is an agonist of Wnt that activates Wnt/β-catenin signal transmission.IC50 & Target:WntIn Vitro:Wnt/β-catenin agonist 4 (Derivative 83) (120 μM; 24 h) shows 1049% β-catenin activity in HEK293 and SW480 cells.Wnt/β-catenin agonist 4 (11 μM; 4 days) shows 2848% ALP activity on differentiation of ST2 cell line into osteoblasts.
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WRVYEKC(dnp)ALK tetraTFA contains tryptophan that can be liberated from the dinitrophenol (DNP) quencher by aminopeptidase activity. WRVYEKC(dnp)ALK tetraTFA can be used as a hydrolysis reaction decapeptide substrate.
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WSF1-IN-1 (compound 136), an orally active WSF1 inhibitor, can be used in the study for WSF1 (Wolfram syndrome) related tumors, with IC50 values of 0.33 μM and >27 μM in HepG2 parental and HepG2 WFS1 KO cell lines, respectively.In Vitro: WSF1-IN-1 (compound 136) exhibits IC50 values of >27 μM and 0.03 μM for Hek293 empty […]
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WWL123 is a potent and selective ABHD6 inhibitor with an IC50 of 430 nM[2]. WWL123 crosses the blood-brain-barrier and inhibits ABHD6 in brain parenchyma. ABHD6 blockade by WWL123 exerts an antiepileptic effect in Pentylenetetrazole (PTZ)-induced epileptiform seizures and spontaneous seizures in R6/2 mice.
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WYC-210, a Tazarotene derivative, is a retinoid compound with lower anticancer activity.In Vitro:WYC-210 (10 μM; 5 days) inhibits cell growth of B16-F1 TRC cells with an inhibition rate of 18.1%.
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WYE-687 dihydrochloride is an ATP-competitive mTOR inhibitor with an IC50 of 7 nM. WYE-687 dihydrochloride concurrently inhibits activation of mTORC1 and mTORC2[2]. WYE-687 also inhibits PI3Kα and PI3Kγ with IC50s of 81 nM and 3.11 μM, respectively.
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X-Gluc cyclohexanamine is a dye reagent for the detection of β-glucuronidase (GUS), an enzyme produced by E. coli. X-Gluc cyclohexanamine can be used to detect E. coli contamination in food, water and the urinary tract (GUS as a specific detection indicator). X-Gluc cyclohexanamine is also widely used in molecular biology experiments to label and detect […]
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X5050 is a REST inhibitor, with an EC50 of 2.1 μM.In Vitro: X5050 (100 μM, 1 day) induces a dosedependent decrease in the REST isoform in protein level.In Vivo: X5050 (2 x 2μl of 20 mM) is active in HD pathological context.
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X77 is a potent non-covalent inhibitor of the main protease of SARS-CoV-2 (SARS-CoV-2 Mpro). X77 binds to SARS-CoV-2 Mpro with a Kd value of 0.057 μM[2].IC50 & Target: Kd: 0.057 μM (SARS-CoV-2 Mpro)[2]In Vitro: X77 can bind to SARS-CoV-2 Mpro (PDB code: 6W63). SARS-CoV-2 Mpro (PDB code: 6W63) is the main protease of SARS-CoV-2 and […]
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Xamoterol hemifumarate is a selective and potent agonist of beta1-adrenergic receptor. Xamoterol hemifumarate has the potential for the research of arrhythmogenesis. Xamoterol hemifumarate has the potential for the investigating the relationship between β1-adrenergic stimulation and IKr.
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Xanthine amine congener (XAC) hydrochloride is a non-selective adenosine receptor antagonist. Xanthine amine congener hydrochloride induces convulsions in mice.
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Xanthohumol D, isolated from hops, is an inhibitor of quinone reductase-2 (QR-2) with the IC50 value of 110 μM, and binds to the active site of QR-2. Xanthohumol D shows antiproliferative activity on human cancer cell lines in vitro[2].IC50 & Target:IC50: 110 μM (Quinone reductase-2)
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Xanthopterin hydrate, an unconjugated pteridine compound, is the main component of the yellow granule in the Oriental hornet bear wings, produces a characteristic excitation/emission maximum at 386/456 nm[2]. Xanthopterin hydrate(XPT) causes renal growth and hypertrophy in rat.Xanthopterin hydrate inhibits RNA synthesis.In Vitro: Xanthopterin (7.8-250 mM; 24 hours) show a significant reduction in mitochondrial activity with […]
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Xanthopurpurin, an anthraquinone glycoside, isolated from the roots of Rubia akane, shows mainly strong inhibition of collagen-induced platelet aggregation.
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XE 991 dihydrochloride, a Kv7 (KCNQ) channels blocker, potently inhibits Kv7.1 (KCNQ1), Kv7.2 (KCNQ2), Kv7.2 + Kv7.3 (KCNQ3) channel, and M-current with IC50s of 0.75 μM, 0.71 μM, 0.6 μM, and 0.98 μM, respectively.IC50 & Target: IC50: 0.75 μM ( Kv7.1 channel), 0.71 μM (Kv7.2 channel), 0.6 μM (Kv7.2 + Kv7.3 channel), 0.98 μM (M-current)In […]
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Xevinapant (AT-406) hydrochloride is a potent and orally bioavailable Smac mimetic and an antagonist of the inhibitor of apoptosis proteins (IAPs). Xevinapant hydrochloride binds to XIAP, cIAP1, and cIAP2 proteins with Kis of 66.4, 1.9, and 5.1 nM, respectively. Xevinapant hydrochloride effectively antagonizes XIAP BIR3 protein in a cell-free functional assay, induces rapid degradation of […]
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XJB-5-131 is a mitochondria-targeted ROS and electron scavenger. XJB-5-131 is a bi-functional antioxidant that comprises a radical scavenger. XJB-5-131 is a?synthetic antioxidant that targets mitochondria[2].?XJB-5-131 is an effective ionizing irradiation protector and mitigator of cord blood mononuclear cells (CB MNCs).In Vitro: XJB-5-131 also ameliorates hemorrhagic shock (HS)-induced activation of the pro-apoptotic enzymes, caspases 3 and […]
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XL177A is a highly potent and selective irreversible USP7 inhibitor with an IC50 of 0.34?nM. XL177A elicits cancer cell killing through a p53-dependent mechanism.In Vitro: XL177A is a potent USP7 inhibitor and p53 stabilizer in cyto. XL177A suppresses cancer cell growth predominantly through a p53-dependent mechanism. XL177A labels the catalytic cysteine, C223, of USP7 with […]
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XMD-17-51 TFA is a pyrimido-diazepinone compound that is able to modulate protein kinases.In Vitro:XMD-17-51 TFA is a pyrimido-diazepinone compound that is able to modulate protein kinases, including MPS1 (TTK), ERK5 (BMK1, MAPK7), polo kinase 1, 2, 3, or 4, Ack1, Ack2, Abl, DCAMKL1, ABL1, Abl mutants, DCAMKL2, ARK5, BRK, MKNK2, FGFR4, TNK1, PLK, ULK2, PLK, […]
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XP-524 is a potent BET and EP300 inhibitor. XP-524 shows great tumoricidal activity in vivo. XP-524 prevents KRAS-induced, neoplastic transformation in vivo and extends survival in two transgenic mouse models of aggressive PDAC. XP-524 also enhances the presentation of self-peptide and tumor recruitment of cytotoxic T lymphocytes. XP-524 has the potential for the research of […]
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XP-59 is a potent inhibitor of the SARS-CoV Mpro, with a Ki of 0.1 μM.IC50 & Target: Ki: 0.1 nM (SARS-CoV Mpro).In Vitro: The SARS-CoV main proteinase (Mpro) plays a central role in the formation of the viral replicase/transcriptase complex and is thus an ideal target for the development of suitable drugs.
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XPC-6444 is a highly potent, isoform-selective, and CNS-penetrant NaV1.6 inhibitor (IC50=41 nM for hNaV1.6). XPC-6444 also displays potent block of NaV1.2 (IC50=125 nM). XPC-6444 shows anticonvulsant activity.IC50 & Target: IC50: 41 nM (hNaV1.6), 125 nM (hNaV1.2)In Vitro: XPC-6444 shows high selectivity over NaV1.1 and NaV1.5.In Vivo: XPC-6444 exhibits good metabolic stability in human liver microsomes […]
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XST-14 is a potent, competitive and highly selective ULK1 inhibitor with an IC50 of 26.6 nM. XST-14 induces autophagy inhibition by reducing the phosphorylation of the ULK1 downstream substrate. XST-14 induces apoptosis in hepatocellular carcinoma (HCC) cells and has antitumor effects.In Vitro: XST-14 inhibits ULK1 (IC50=13.6 nM), MAP2K1/MEK1 (IC50=721.8 nM), MAPK14/p38 alpha (IC50=283.9 nM), TGFBR2 […]
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XY028-133 (example 14) is a PROTAC-based CDK4/6 degrader with anti-tumor activity, which consists of ligands for von Hippel-Lindau and CDK.In Vitro: XY028-133 (1 and 3 μM, 24 h) significantly decreases CDK4/6, Cyclin A, PLK1 and pRb protein levels in A375 cells.
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XY101 is a potent, selective, metabolically stable and orally available RORγ inverse agonist with an IC50 of 30 nM and a Kd of 380 nM.IC50 & Target: IC50: 30 nM (RORγ)Kd: 380 nM (RORγ)In Vitro: XY101 potently inhibits cell growth, colony formation, and the expression of androgen receptor (AR), AR-V7 and prostate-specific antigen (PSA).In Vivo: […]
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