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Biovision | Guanfacine hydrochloride | B2990

Guanfacine is an α2-adrenergic receptor (α2-AR) agonist with anti-hypertensive activity. It shows Ki values of 93, 1,380, and 3,890 nM for α2A-, α2B-, and α2C-ARs, respectively, in a radioligand...

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Biovision | Poly(I:C) | B2989

Poly(I:C) is a double-stranded homopolymer of polyinosinic acid and polycytidylic acid. Transfection of Poly(I:C) (1 μg/ml) into NIT 1 cells has been used as a model of intracellular double-stranded...

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Biovision | 27-Hydroxycholesterol | B2988

27-Hydroxycholesterol is a hydroxylation product of cholesterol which is produced by the activity of the enzyme sterol 27-hydroxylase. It activates LXRα and LXRβ in vitro with EC₅₀ values of 85 and...

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Biovision | Desipramine hydrochloride | B2987

Desipramine HCl is a tricyclic antidepressant that is a selective inhibitor of norepinephrine transporter with Ki values of 4 nM, 61 nM and 78.72 μM for Norepinephrine Transporter (NET), Serotonin...

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Biovision | LDN-193189 dihydrochloride | B2986

LDN-193189 inhibits transcriptional activity of the (Bone Morphogenetic Protein) BMP type I receptors known as activin receptor-like kinases (ALKs). It inhibits ALK2 and ALK3 with IC₅₀ values of 5 nM...

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Biovision | Tasimelteon | B2985

Tasimelteon is a potent Dual Melatonin Receptor Agonist (DMRA). It is used to treat non-24-hour sleep-wake disorder. The Ki values for binding affinity at melatonin receptors MT1 and MT2 receptor are...

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Biovision | Ripasudil hydrochloride dihydrate | B2984

Ripasudil (K-115) is a potent inhibitor of Rho kinase (ROCK), with IC₅₀ values of 19 and 51 nM for ROCK-2 and ROCK-1, respectively. Ripasudil (10 μM) induces cytoskeletal changes, including...

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Biovision | Vigabatrin | B2983

Vigabatrin (VGB) is a structural analogue of gamma-aminobutyric acid (GABA) that irreversibly inhibits GABA-transaminase (GABA-T). It inhibits the catabolism of GABA by GABA transaminase and...

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Biovision | Cystamine dihydrochloride | B2982

Cystamine is an organic disulfide that inhibits transglutaminase (TGM2) with 44% inhibition observed at a concentration of 2.5 mM. It shows neuroprotective activity in a mouse model of Huntington’s...

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Biovision | NQTrp | B2981

NQTrp is an inhibitor of amyloid β (Aβ) oligomerization and fibrillization, with an IC₅₀ of 50 nM for formation of fibrils from Aβ1-42. It reduces the cytotoxic effect of Aβ oligomers in rat PC12...

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Biovision | AC-186 | B2980

AC-186 is a potent and selective estrogen receptor β (ERβ) agonist. It shows EC₅₀ values of 6 and 5000 nM for ERβ and ERα respectively in functional assays. Decrease in the sex steroids is associated...

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Biovision | TGN-020 | B2979

TGN-020 is an inhibitor of aquaporin 4 (AQP4), the most abundant water channel in brain. It inhibits AQP4 inhibitor with an IC₅₀ of 3 μM in vitro. Pretreatment with the AQP4 inhibitor TGN-020...

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Biovision | AMTB hydrochloride | B2978

AMTB is an antagonist of transient receptor potential melastatin 8 (TRPM8). It inhibits icilin-induced calcium influx with a pIC₅₀ of 6.23. Intravenous administration of AMTB (3 mg/kg) decreases the...

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Biovision | TCS 5861528 | B2977

TCS 5861528 is a selective transient receptor potential ankyrin 1 (TRPA1) blocker that antagonizes TRPA1-mediated calcium influx induced by allyl isothiocyanate and 4-hydroxy nonenal with IC₅₀ values...

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Biovision | ASP7663 | B2976

ASP7663 is a selective transient receptor potential ankyrin 1 (TRPA1) activator. It activates human, rat and mouse TRPA1 receptors with EC₅₀ values of 510 nM, 540 nM and 500 nM, respectively. It...

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Biovision | R-59-022 | B2975

R-59-022 is an inhibitor of Diacylglycerol (DAG) kinase with an IC₅₀ of 2.8 µM. The inhibition of Diacylglycerol kinase results in increased DAG-dependent protein kinase C (PKC) activity and...

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Biovision | JNJ-17203212 | B2974

JNJ-17203212 is a reversible and potent antagonist of transient receptor potential vanilloid 1 (TRPV1) with pKi values of 6.5, 7.1 and 7.3 at rat, guinea pig and human TRPV1 respectively. It Inhibits...

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Biovision | A-839977 | B2973

A-839977 is a potent antagonist of the purinergic receptor P2X subtype 7 (P2X7). A-839977 potently blocks BzATP-induced calcium influx at recombinant human, rat and mouse P2X7 receptors with IC₅₀...

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Biovision | JNJ-47965567 | B2972

JNJ-47965567 is a potent and selective antagonist of the purinergic receptor P2X subtype 7 (P2X7), a ligand-gated ion channel. Activation of P2X receptors by BzATP induces calcium flux. JNJ-47965567...

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Biovision | CA-074 | B2971

CA-074 is an epoxysuccinyl peptide inhibitor of cathepsin B. It selectively inhibits cathepsin B with an IC₅₀ of 2.24 nM over other cysteine proteinases such as cathepsins L and H, and calpains. It...

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Biovision | 666-15 | B2970

666-15 is a potent and selective inhibitor of cyclic adenosine monophosphate response element binding protein (CREB)-mediated gene transcription with an IC₅₀ of 81 nM. The IC₅₀ values for inhibiting...

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Biovision | COG133 | B2969

COG 133 is a fragment of Apolipoprotein E (APOE) that mimics the anti-inflammatory and neuroprotective effects of the intact apoE protein. It functions through the low-density lipoprotein...

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Biovision | Probucol | B2968

Probucol is a potent antioxidant that inhibits the oxidation of cholesterol in LDL which prevents the formation of macrophage-derived foam cells that lead to atherosclerotic vascular lesions. The use...

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Biovision | Gramicidin A | B2967

Gramicidin A is a peptide component of gramicidin, an antibiotic mixture originally isolated from Bacillus brevis. Gramicidin A is a linear channel-forming ionophore pentadecapeptide that forms a...

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Biovision | Anidulafungin | B2966

Anidulafungin is an echinocandin antifungal drug. It inhibits (1→3)-β-D-glucan synthase which is required for synthesis of the fungal cell wall. It shows potent in vitro activity against Aspergillus...

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Biovision | PLX5622 (free base) | B2965

PLX5622 is an inhibitor of colony-stimulating factor 1 receptor (CSF1R) tyrosine kinase with a Ki of 5.9 nM. It causes sustained and specific elimination of microglia. As a result of microglial...

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Biovision | Astragalin | B2964

Astragalin is a flavonoid isolated from leaves of persimmon, green tea seeds, wine and American pokeweed. It shows anti-inflammatory and anti-oxidant activity. It dose-dependently (20-80 µg/ml)...

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Biovision | Benserazide hydrochloride | B2963

Benserazide is an inhibitor of aromatic L-amino acid decarboxylase (AADC), an enzyme that has dopamine decarboxylase activity. It blocks the conversion of L-DOPA to dopamine by AADC in the peripheral...

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Biovision | CAY10505 | B2962

CAY10505 is a potent inhibitor of phosphoinositide 3-kinase (PI3K), selectively inhibiting the γ isoform with an IC₅₀ of 30 nM. It inhibits the α, β, and δ isoforms of PI3K with IC₅₀ values of 0.94,...

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Biovision | Boceprevir | B2961

Boceprevir is a protease inhibitor that binds to the catalytic site (Ser139) of hepatitis C virus (HCV) nonstructural protein 3/4A (NS3/4A), a serine protease that is essential for viral replication,...

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Biovision | Allicin | B2960

Allicin is a natural product isolated from garlic (Allium sativum) that exhibits many biological effects including antioxidative, anticancer, antimicrobial, and antifungal activities. Allicin (5-10...

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Biovision | Thiamet G | B2959

Thiamet G is a potent and selective inhibitor of O-GlcNAcase with a Ki value of 21 nM. It increases cellular O-GlcNAc-modified protein levels with an EC₅₀ of 30 nM and blocks phosphorylation of tau...

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Biovision | Importazole | B2958

Importazole is a 2,4-diaminoquinazoline that inhibits the function of transport receptor importin-β, likely by altering its interaction with RanGTP. Importazole prevents nuclear import of GFP-tagged...

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Biovision | Daltroban | B2957

Daltroban is an antagonist of thromboxane A2 receptor. Daltroban (20 mg/kg per h i.v.) protects the myocardium from ischaemic injury by preventing ischaemia-induced leukocytosis in cats. Infusion (1...

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Biovision | Aphidicolin | B2956

Aphidicolin is a natural tetracyclic diterpene antibiotic which shows antiviral activity against herpes simplex. In eukaryotic cells, it is a cell-permeable, reversible inhibitor of DNA replication,...

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Biovision | Flubendazole | B2955

Flubendazole is a benzimidazole carbamate anthelmintic agent. It eliminates larvae in a mouse model of A. cantonensis infection and exhibits a mean larval reduction of 100% in a T. spiralis infection...

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Biovision | Valbenazine | B2954

Valbenazine is an inhibitor of vesicular monoamine transporter 2 (VMAT2). VMAT2 plays an important role in the packaging of monoamines into presynaptic vesicles. Valbenazine shows Ki values of 110...

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Biovision | Wogonoside | B2953

Wogonoside is a flavonoid with antioxidant, anti-cancer and anti-angiogenic activity. Wogonoside inhibits the growth of U937 and HL-60 cells cells. It arrests the cell cycle at the G0/G1 phase and...

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Biovision | GSK 1016790A | B2952

GSK1016790A is a transient receptor potential vanilloid 4 (TRPV4) agonist that elicits calcium influx in HEK cells expressing mouse or human transient TRPV4 with EC₅₀ values of 18 and 2.1 nM,...

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Biovision | Tryptanthrin | B2951

Tryptanthrin is an alkaloid isolated from various plants and shows antimicrobial activity. It inhibits both 5-lipoxygenase and cyclooxygenase-2 with IC₅₀ values of 600 nM and 64 nM, respectively. It...

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Biovision | ONC212 | B2950

ONC212 is a fluorinated imipridone analogue of ONC201. It is an activator of GPCR GPR132 and Gαq signaling, which functions as a tumor suppressor. It induces apoptosis in HPAF-II and AsPC1 cell lines...

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Biovision | Valnemulin hydrochloride | B2949

Valnemulin is a pleuromutilin antibiotic that inhibits protein synthesis by binding to the 50S ribosomal subunit of bacteria. It is used to treat swine diseases including Brachyspira hyodysenteriae...

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Biovision | Destruxin B | B2948

Destruxin A is a cyclic hexadepsipeptide metabolite from the fungus Metarhizium anisopliae. It shows insecticidal and anti-cancer properties. It induces a concentration-dependent antiproliferative...

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Biovision | Destruxin A | B2947

Destruxin A is a cyclic hexadepsipeptide metabolite from the fungus Metarhizium anisopliae. Destruxins show insecticidal, anti-viral, and phytotoxic properties. Destruxin A suppresses the Drosophila...

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Biovision | Sanguinarine | B2946

Sanguinarine is a benzylisoquinoline alkaloid that inhibits PP2C and shows selectivity for PP2C over PP1, PP2A, and PP2B in vitro. It inhibits MKP-1 with an IC₅₀ of 10 μM and shows selectivity for...

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Biovision | Demethoxycurcumin | B2945

Demethoxycurcumin is a curcumin derivative with anti-inflammatory and anti-proliferative properties. It suppresses tumor necrosis factor (TNF)-induced nuclear factor-kappaB (NF-kappaB) activation in...

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Biovision | Bisdemethoxycurcumin | B2944

Bisdemethoxycurcumin is a curcumin analogue with anti-inflammatory and anti-proliferative properties. It suppresses tumor necrosis factor (TNF)-induced nuclear factor-kappaB (NF-kappaB) activation in...

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Biovision | GNE-9605 | B2943

GNE-9605 is a selective, brain-penetrable Leucine-rich repeat kinase 2 (LRRK2) inhibitor with an IC₅₀ of 19 nM. Mutations in LRRK2 are associated with Parkinson's disease. GNE-9065 inhibits LRRK2...

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Biovision | GNE-0877 | B2942

GNE-0877 is a selective, brain-penetrable Leucine-rich repeat kinase 2 (LRRK2) inhibitor with a Ki of 0.7 nM. Mutations in LRRK2 are associated with Parkinson's disease. GNE-0877 inhibits LRRK2...

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Biovision | CZC-25146 | B2941

CZC-25146 is a potent inhibitor of Leucine-rich repeat kinase 2 (LRRK2) with an IC₅₀ of 4.76 nM. Mutations in LRRK2 are associated with Parkinson's disease. CZC-25146 attenuates LRRK2 G2019S mutant...

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Biovision | LRRK2-IN-1 | B2940

LRRK2-IN-1 is a potent inhibitor of Leucine-rich repeat kinase 2 (LRRK2). Mutations in LRRK2 are associated with Parkinson's disease. LRRK2-IN-1 inhibits wild-type and G2019S mutant LRRK2 with IC₅₀...

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Biovision | IQA | B2939

IQA is an indoloquinazoline derivative that acts as a selective and reversible casein kinase (CK2) inhibitor with an IC₅₀ of 390 nM with 100 µM ATP. It inhibits CK2 in an ATP- and GTP-competitive...

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