ec-1

CVT-2738 (RS-94287) is a metabolite of Ranolazine. Ranolazine is a partial fatty acid oxidation (pFOX) inhibitor and anti-anginal drug.

Decanenitrile is a biochemical.

1. Crassicauline A (Crassicauline I) and Yunaconitine possesses feeding deterrent activity against T. castaneum adults, with EC(5) values of 1134.5 and 653.4 ppm, respectively.

Viloxazine (Viloxazin) (Viloxazin) is a dual-action compound that functions as a norepinephrine reuptake inhibitor and exhibits potent agonistic activity towards 5-HT 2C receptors while acting as an antagonist for 5-HT 2B receptors, with respective potency values of EC 50 = 32 μM and IC 50 = 27 μM. Its primary mechanism of action involves the modulation of serotonergic and noradrenergic pathways. Viloxazine is commonly employed in depression research [1] [2].

Sp-cAMPS sodium salt is an analog of cAMP that is a potent activator of cAMP-dependent PKA I and PKA II. Sp-cAMPS sodium salt is also a potent, competitive phosphodiesterase (PDE3A) inhibitor with a K i of 47.6 μM. Sp-cAMPS sodium salt binds the PDE10 GAF domain with an EC 50 of 40 μM [1] [2] [3].

(Rac)-EC5026 ((Rac)-BPN-19186) is a potent piperidine inhibitor of soluble epoxide hydrolase (sEH) with Ki of 0.06 nM. (Rac)-EC5026 can be used for the research of Parkinson's disease and dementia with Lewy Bodies (DLB) [1].

GW3965 is a potent, selective agonist of liver X receptor (LXR) with EC 50 s of 190 nM and 30 nM for hLXRα and hLXRβ, respectively [1] [2] [3].

Afatinib Dimaleate (BIBW 2992MA2) is an orally bioavailable anilino-quinazoline derivative and inhibitor of the receptor tyrosine kinase (RTK) epidermal growth factor receptor (ErbB; EGFR) family, with antineoplastic activity.

Afatinib (BIBW 2992) is an irreversible inhibitor of EGFR family (EGFR-wt, EGFR-L858R, EGFR-L858R/T790M and HER2 with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM , respectively).

Glutathione reductase (EC 1.6.4.2) is an enzyme that ensures the availability of reduced glutathione [1].

Adrenomedullin (rat), a potent vasodilator peptide, is secreted by both endothelial cells (EC) and vascular smooth muscle cells (VSMC) [1].

Pyrimorph is a fungicide with high activity against the plant pathogen Phytophthora capsici. Pyrimorph inhibited different stages in the life cycle of P. capsici including mycelial growth, sporangium production, zoospore release, and cystospore germination with EC(50) values of 1.84, 0.17, 4.92, and 0.09 microg mL(-1), respectively.

7,8-Didehydrocimigenol can be used for the treatment of cardiovascular disorders such as atherosclerosis. It upregulates PPAR-γ in EC inhibits NF-kB activity of TNF-α-activated EC which leads to selective inhibition of VCAM-1 expression.

Moronic acid shows oral therapeutic efficacy in HSV-infected mice and possessed novel anti-HSV activity. It also shows significant anti-HIV activity (EC(50) 186) and was modified to develop more potent anti-AIDS agents. Moronic acid is a new structural lead for anti-EBV drug development, can substantially reduce the numbers of EBV particles produced by the cells after lytic induction. Morolic and moronic acids have shown sustained antidiabetic and antihyperglycemic action possibly mediated by an insulin sensitization with consequent changes of glucose, cholesterol and triglycerides, in part mediated by inhibition of 11β-HSD 1 as indicated by in vitro.

ACBI2, an orally active and highly potent VHL PROTAC (EC 50: 7 nM), selectively degrades SMARCA2, demonstrating a DC 50 value of 1 nM in RKO cells. This compound holds potential for lung cancer research [1].

LeuRS-IN-1 hydrochloride is a potent and orally active inhibitor of M. tuberculosis leucyl-tRNA synthetase (M.tb LeuRS). It has IC 50 and Kd values of 0.06 μM and 0.075 μM, respectively, for M.tb LeuRS. Additionally, LeuRS-IN-1 hydrochloride inhibits human cytoplasmic LeuRS with an IC 50 of 38.8 μM and HepG2 protein synthesis with an EC 50 of 19.6 μM.

SAH-SOS1A TFA is a peptide-based SOS1/KRAS protein interaction inhibitor. SAH-SOS1A TFA binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity ( EC 50 =106-175 nM). SAH-SOS1A TFA directly and independently blocks nucleotide association. SAH-SOS1A TFA impairs KRAS-driven cancer cell viability and exerts its effects by on-mechanism blockade of the ERK-MAPK phosphosignaling cascade downstream of KRAS [1] .

Sp-cAMPS triethylamine, a cAMP analog, serves as a potent activator of cAMP-dependent PKA I and II and acts as a competitive inhibitor of phosphodiesterase (PDE3A) with a K i of 47.6 µM. Additionally, it binds the PDE10 GAF domain with an EC 50 of 40 μM [1] [2] [3].

THI0019 is a highly potent agonist of the integrin α4β1 (VLA-4) receptor, with an EC 50 range of 1-2 μM. It effectively promotes the adhesion of stem/progenitor cells. Furthermore, THI0019 successfully modulates adhesion processes mediated by α4β7, α5β1, and αLβ2 integrins.

Acetylcholinesterase (ACHE; EC 3.1.1.7) is a cholinergic enzyme mainly found in neuromuscular junctions and cholinergic type chemical synapses, and is often used in biochemical research. Acetylcholinesterase catalyzes the breakdown or hydrolysis of acetylcholine and some other choline esters that act as neurotransmitters into acetate and choline. Acetylcholinesterase's main role is to terminate neuronal transmission and signaling between synapses to prevent ACh spread and activation of nearby receptors [1] .

Stem bromelain (EC 3.4.22.32), a cysteine proteinase from pineapple (Ananas comosus) stem, is a significant type of bromelain known for its fibrinolytic, antiedematous, antithrombotic, and anti-inflammatory properties. It also demonstrates in vivo antitumoral, antileukemic, and antimetastatic activities [1] [2].

LeuRS-IN-1 is a highly potent and orally active inhibitor of the leucyl-tRNA synthetase enzyme derived from Mycobacterium tuberculosis (M.tb LeuRS). It exhibits significant inhibitory activity against M.tb LeuRS with IC 50 and Kd values of 0.06 μM and 0.075 μM, respectively. Additionally, LeuRS-IN-1 effectively inhibits human cytoplasmic LeuRS with an IC 50 value of 38.8 μM and suppresses protein synthesis in HepG2 cells with an EC 50 value of 19.6 μM.

BIM-23027 is a selective sst 2 receptor agonist (EC 50 = 0.32 nM) with effects analogous to the cyclic tetradecapeptide somatostatin (SRIF). It promotes dopamine release through a Glu-dependent mechanism [1] [2].

Compound 2, or 15α-Hydroxy-20-oxo-6,7-seco-ent-kaur-16-en-1,7α(6,11α)-diolide, is an ent-kaurene diterpenoid extracted from Rubescens rubescens. This compound exhibits cytotoxic activity against various cell lines, including EC-1, U87, A549, MCF-7, and HeLa, with IC50 values of 37.69 μM, 79.362 μM, 80.07 μM, 197.35 μM, and 462.13 μM, respectively, as well as 180.09 μM against another unspecified line [1].

Carboxypeptidase A (EC 3.4.2.1), a zinc-containing metalloprotease, catalyzes the hydrolysis of peptide bonds near the C-terminal end of polypeptides and is frequently utilized in biochemical research. As a prototypical enzyme for metalloproteases, it is essential in biological systems [1].

MCH (human, mouse, rat) TFA is a potent peptide agonist for MCH receptors, demonstrating strong affinity with binding IC 50 values of 0.3 nM for MCH1R and 1.5 nM for MCH2R. It is notably effective against MCH-2R in a CHO cell line, as evidenced by the mobilization of intracellular calcium measured with FLIPR, revealing functional activation EC 50 values of 3.9 nM for MCH-1R and 0.1 nM for MCH-2R [1].

FSL-1 TFA, a toll-like receptor 2/6 (TLR2/6) agonist derived from bacteria, bolsters resistance against experimental HSV-2 infection[1] and stimulates MMP-9 production via the TLR2 and NF-κB/AP-1 signaling pathways in monocytic THP-1 cells[2].

ASN04421891 is a potent GPR17 receptor modulator, with an EC 50 of 3.67 nM in [35S]GTPγS binding assay. ASN04421891 is promising to be used for neurodegenerative diseases research[1].

MitTx, a complex consisting of MitTx-α and MitTx-β, serves as an ASIC1 channel activator, demonstrating EC50 values of 9.4 nM and 23 nM for the ASIC1a and ASIC1b isoforms, respectively. It exhibits high selectivity for ASIC1 isoforms at neutral pH, while under acidic conditions, it substantially potentiates proton-evoked activation of the ASIC2a channel [1].

LSN2814617 is an orally active, potent, brain-penetrant, and selective mGlu 5 (metabotropic glutamate 5) positive allosteric modulator (PAM), with EC 50 values of 52 nM (Human mGlu5) and 42 nM (rat mGlu5). In vivo EEG studies demonstrated that LSN2463359 has marked wake-promoting properties but little in the way of rebound hypersomnolence. LSN2814617 can be used for schizophrenia research [1].

PCSK9 modulator-3 (Compound 13) is a potent PCSK9 modulator with an EC 50 value of 2.46 nM that has the potential in the hyperlipidemia research. PCSK9 is a recently proved target for lowering low-density lipoprotein cholesterol (LDL-C) [1].

HIF-2α-IN-7 is a hypoxia inducible factor 2α (HIF-2α) inhibitor. HIF-2α-IN-7 can inhibit HIF-2α with an EC 50 value of 6 nM. HIF-2α-IN-7 can be used for the research of various types of diseases including cancer , liver disease, inflammatory disease, pulmonary diseases and iron load disorders .

RSV-IN-7 (example 253) is a RSV inhibitor ( EC 50 : < 0.4 μΜ) .

DENV-IN-9 is a DENV2 inhibitor with an EC 50 of 0.88 μM .

(S,S)-BMS-984923 is a less active (S,S)-enantiomer of BMS-984923. (S,S)-BMS-984923 shows an EC 50 >1μM for mGluR5 receptor [1] . BMS-984923 is a potent mGluR5 silent allosteric modulator [2] .

BigLEN(rat) is a potent GPR171 agonist with an EC 50 of 1.6 nM [1] .

α-Helical CRF(9-41) TFA acts as a competitive antagonist for the CRF2 receptor, possessing a binding constant (K B) of approximately 100 nM. Additionally, it serves as a partial agonist for the CRF1 receptor, exhibiting a half-maximal effective concentration (EC 50) of 140 nM [1] [2].

α-Galactosidase (EC 3.2.1.22), a glycoside hydrolase enzyme, is prevalent across animals, plants, and microorganisms, and is often utilized in biochemical research. It facilitates the hydrolysis of α-1,6-linked terminal galactose residues in substrates such as galactooligosaccharides, galactomannans, and galactolipids. This includes catalyzing key catabolic processes involved in the cleavage of glycoproteins, glycolipids, and polysaccharides [1].

[Lys4] Sarafotoxin S6c, an analogue of sarafotoxin, serves as a potent, partial agonist of the endothelin receptor, inducing contraction in pig coronary artery with an effective concentration (EC 50) of 1.5 nM [1].

Viral 2C protein inhibitor 1 (compound 6aw) is a potent and broad-spectrum enterovirus antiviral agent that inhibits viral 2C protein. Viral 2C protein inhibitor 1 has relatively low cytotoxicity and high selectivity index that inhibits multiple strains of EV-D68, EV-A71 and CVB3 with EC 50 s of 0.1~3.6 μM [1].

mGlu4 receptor agonist 1 (compound 62) is a highly effective positive allosteric modulator of mGlu4 receptors, displaying an EC 50 of 308 nM. Additionally, it exhibits noteworthy anxiolytic and antipsychotic properties [1].

PIM-IN-1 is a pan-PIM kinase inhibitor (KG-1, EC 50 = 61 nM; pS6, EC 50 = 71 nM).

RAD51-IN-8, a new RAD51 binder, is a RAD51-BRCA2 inhibitor that inhibits the RAD51 BRCA2 protein protein interaction in the micromolar range. RAD51-IN-8 also is a protein protein interaction (PPI) inhibitor. RAD51-IN-8 has inhibitory activity for H4A4 with an EC 50 value of 19 μM [1].

L-796568, is a β3 adrenergic receptor agonist. L-796568 is a potent full beta(3) agonist (EC(50) = 3.6 nM, 94% activation) with >600-fold selectivity over the human beta(1) and beta(2) receptors, which also displays good oral bioavailability in several

Vin-C01 can be used for the research of type 2 diabetes mellitus that is a potent protective agent of pancreatic β-cells (EC 50 = 0.22 μM). Vin-C01 effectively protects β-cells from apoptosis induced by STZ and promotes β-cell survival [1].

YAP/TAZ inhibitor-2 is a potent and orally active TEAD-YAP/TAZ inhibitor with an EC 50 value of 3 nM. YAP/TAZ inhibitor-2 shows anti-proliferative and antitumor activity [1].

mGluR2 modulator 4 (compound 47) is a highly potent positive allosteric modulator of mGluR2, exhibiting an EC 50 value of 0.8 μM. It holds the potential for investigating antipsychotic properties [1].

Utrophin Modulator 1 (UM1) is a highly effective agent that upregulates utrophin protein levels, displaying an EC 50 of 0.11 μM. Its application in the investigation of Duchenne Muscular Dystrophy (DMD) has been well-established [1].

Influenza virus-IN-2 (compound 19) has anti-influenza A virus activities that is a potent inhibitor of influenza virus with an CC 50 of 150.85 μM and EC 50 of 2.58 μM. Influenza virus-IN-2 concentration-dependently inhibits the PAN endonuclease with EC 50 of 489.39 nM [1].

HIV-1 Inhibitor-57 (Compound 12g) is an antiviral agent that potently inhibits both wild-type and five common NNRTI-resistant strains of HIV-1, exhibiting EC50 values between 0.024 and 0.0010 μM. It achieves this efficacy by forming supplementary interactions with residues surrounding the binding site in the HIV-1 reverse transcriptase (RT) [1].