a 293

PIK-293 is a PI3K inhibitor, for PI3Kδ( IC50=0.24 μM), and less potent for PI3Kα/β/ γ.

(S)-BAY-293 is a potent pan-KRAS inhibitor for the study of primary non-small lung and pancreatic cancers.

BAY-293 is a potent, cell-active SOS1 inhibitor that disrupts the KRAS-SOS1 interaction (IC50: 21 nM).

293P-1 is a hepatocyte-specific homing peptide characterized by the sequence SNNNVRPIHIWP [1].

GNE-293 is a potent and selective PI3Kδ inhibitor.

IBC 293 is selective for GPR109B over niacin receptor GPR109A. IBC 293 is a highly selective agonist for GPR109B, a human orphan G-protein-coupled receptor expressed in adipocytes.

DB293 is an inhibitor of PIT-1 and BRN-3 transcription factors. DB293 binds as head-to-tail stacked dimers in the minor groove of 5'-ATGA sequence, thereby leading to an increase in the size of minor groove.

V-9302 (V9302) is a competitive antagonist of transmembrane glutamine flux that selectively and potently targets the amino acid transporter ASCT2 (IC50: 9.6 uM).

AVE1231 is a TASK-1 channel blocker that inhibits TASK-1 and can be used in the study of atrial fibrillation.

AHR antagonist 4 is a potent aryl hydrocarbon receptor (AHR) antagonist(example 293; IC50: 82.2 nM).It has anti-cancer effects.

SNX7886 is a potent PROTAC (proteolysis-targeting chimera) that effectively degrades CDK8 and CDK19, achieving 90% degradation of CDK8 and 80% degradation of CDK19 in 293 cells [1].

JHU37152 (JHU 37152) is a Designer Receptors Exclusively Activated by Designer Drug (DREADD) agonist with Ki of 1.8 nM and 8.7 nM for human muscarinic acetylcholine M3 receptors (hM3Dq) and hM4Di in vitro, respectively. And EC50 values are 5 nM and 0.5 nM for hM3Dq and hM4Di in fluorescent and BRET-based assays in HEK-293 cells, respectively.

PMX-205 is a cyclic hexapeptide that acts as a potent antagonist of C5a receptor (C5aR; IC50= 31 nM).1It is orally active and blocks inflammatory signaling and symptoms in animal models of colitis and allergic asthma.2,3PMX-205 is also brain penetrant and reduces neuroinflammation and neurodegeneration in an animal model of Alzheimer's disease.4 1.March, D.R., Proctor, L.M., Stoermer, M.J., et al.Potent cyclic antagonists of the complement C5a receptor on human polymorphonuclear leukocytes. Relationships between structures and activityMol. Pharmacol.65(4)868-879(2004) 2.Jain, U., Woodruff, T.M., and Stadnyk, A.W.The C5a receptor antagonist PMX205 ameliorates experimentally induced colitis associated with increased IL-4 and IL-10Br. J. Pharmacol.168(2)488-501(2013) 3.Staab, E.B., Sanderson, S.D., Wells, S.M., et al.Treatment with the C5a receptor/CD88 antagonist PMX205 reduces inflammation in a murine model of allergic asthmaInt. Immunopharmacol.21(2)293-300(2014) 4.Fonseca, M.I., Ager, R.R., Chu, S.-H., et al.Treatment with a C5aR antagonist decreases pathology and enhances behavioral performance in murine models of Alzheimer's diseaseJ. Immunol.183(2)1375-1383(2009)

JHU37160 (JHU 37160) is a Designer Receptors Exclusively Activated by Designer Drug (DREADD) agonist with Ki of 1.9 nM and 3.6 nM for human muscarinic acetylcholine M3 receptors (hM3Dq) and hM4Di in vitro, respectively. And EC50 values are 18.5 nM and 0.2 nM for hM3Dq and hM4Di in fluorescent and BRET-based assays in HEK-293 cells, respectively.

STAT6-IN-2(R)-84 is a STAT6 inhibitor that inhibits eotaxin-3 secretion, induces STAT6 reporter luciferase activity in 293-EBNA cells, and inhibits tyrosine phosphorylation of STAT6.

ARN-6039 is an orally available inverse agonist of RORγ for Autoimmune Neuroinflammatory Demyelinating Disease. The activity of ARN-6039 against RORγ was demonstrated in a RORγ-activated IL-17A Prom/LUCPorter assay in HEK 293 cells (360 nM) and in IL-17 r

Palmatine hydroxide is an orally active, irreversible inhibitor of indoleamine 2,3-dioxygenase 1 (IDO-1), demonstrating IC50 values of 3 μM for HEK 293-hIDO-1 and 157μM for rhIDO-1. Additionally, it uncompetitively inhibits the West Nile virus (WNV) NS2B-NS3 protease with an IC50 of 96 μM. This compound exhibits a range of biological activities, including anti-cancer, anti-oxidation, anti-inflammatory, neuroprotective, antibacterial, and antiviral effects.

KPC-2-IN-1, a boronic acid derivative, serves as an effective KPC-2 inhibitor with a K i of 0.032 μM, augmenting cefotaxime's efficacy against KPC-2 expressing E. coli. It demonstrates good tolerance in human HEK-293 cells, rendering it valuable for researching E. coli's resistance to β-lactam antibiotics [1] [2].

NPS-2143 hydrochloride (NPS-2143 HCL) is a selective potent calcium ion-sensing receptor antagonist.

GNE-0946 is a potent and selective agonist of RORγ (EC50: 4 nM for HEK-293 cell).

Praliciguat (IW-1973) stimulates sGC in HEK-293 cells (EC50: 197 nM). Praliciguat is an effective and orally active soluble guanylate cyclase stimulator. It also enhances NO signaling and acts as a vasodilator.

GNE-6468 is a potent and selective agonist of RORγ(RORc) (EC50: 13 nM for HEK-293 cell).

Antimalarial agent 12 is an effective antimalarial agent that inhibits the growth of Plasmodium falciparum strains Dd2 and 3D7 with EC50 values of 155 nM and 136 nM, respectively. antimalarial agent 12 has a MIC >250,000 nM against E. coli and also acts on Antimalarial agent 12 has a MIC of >250,000 nM against E. coli and also works on HEK-293 and hPHep cell lines with CC50 values of 10,000-50,000 nM.

Etrolizumab (rhuMAb Beta7), a gut-selective anti-β7 integrin monoclonal antibody, targets the β7 subunit of α4β7 and αEβ7 integrins specifically, demonstrating affinity with K i values of 18 nM for Human α4β7 and 1800 pM for Human αEβ7-293. It is utilized in the research of inflammatory bowel disease (IBD) [1] [2].

Z-Ala-Ala-Asn-AMC, also known as Cbz-Ala-Ala-Asn-AMC, serves as a substrate for legumain. The overexpression of legumain in 293 HEK-Leg cells results in efficient cleavage of Cbz-Ala-Ala-Asn-AMC.

Alniditan is a receptors agonist of 5-HT1B/1D in HEK 293 cells (IC50: 1.7 and 1.3 nM). For 5-HT1B/1D receptors, the pKi values are 8.96 and 9.40, respectively.

Apelin-36(human) TFA, an endogenous agonist of the orphan G protein-coupled receptor APJ, exhibits a potent EC50 of 20 nM and high affinity (pIC5 50 = 8.61) for human APJ receptors in HEK 293 cells. It is involved in significant cardiovascular and metabolic activities. Furthermore, Apelin-36(human) TFA can inhibit the entry of certain HIV-1 and HIV-2 strains into NP2/CD4 cells expressing the APJ receptor. [1] [2] [3] [4]

Apelin-17(human, bovine) TFA is an endogenous agonist of the orphan G protein-coupled receptor APJ. This compound demonstrates affinity for human APJ receptors on HEK 293 cells, evidenced by a pIC50 value of 9.02. Additionally, Apelin-17(human, bovine) TFA has been shown to block the entry of certain HIV-1 and HIV-2 strains into NP2/CD4 cells that express the APJ receptor [1] [2] [3].

Pexmetinib (ARRY-614) (ARRY-614) is a potent, orally bioavailable, dual p38 MAPK/Tie-2 inhibitor with IC50 of 4 nM/18 nM in a HEK-293 cell line. Phase 1.

P-gp inhibitor 5 is a potent inhibitor of P-glycoprotein (P-gp), inhibiting P-gp by a factor of 2.5 and 3.0 at 1.25 μM and 2.5 μM, respectively. p-gp inhibitor 5 exhibits anti-proliferative effects on some cancer cells. P-gp inhibitor 5 was able to restore cellular sensitivity to Vincristine and Paclitaxel, thereby reversing the multidrug resistant (MDR) phenotype of ABCB1/Flp-InTM-293 and KBvin.

Amitifadine hydrochloride (EB-1010 hydrochloride) is a triple reuptake inhibitor (TRI) or serotonin-norepinephrine-dopamine reuptake inhibitor (SNDRI).

Milpocitide, a (293-333)-peptide fragment of the human low-density lipoprotein receptor (LDLR), specifically corresponds to the EGF-like domain 1 [1].

PF-04449613 is a phosphodiesterase 9A (PDE9A) inhibitor (IC50= 22 nM).1It is selective for PDE9A over PDE1C (IC50= >1,000 nM), as well as over a variety of other PDEs, inhibiting PDE2-8, -10, and -11 activity by less than 30% in a panel of enzymes, ion channels, and transporters at 1 μM but does inhibit the human dopamine transporter (DAT; Ki= 293 nM). PF-04449613 (0.1-100 mg/kg, s.c.) increases cerebrospinal fluid (CSF) levels of cyclic GMP (cGMP) in rats. Subcutaneous administration of PF-04449613 (10 mg/kg) increases the rate of dendritic spine formation and elimination in mouse primary motor cortex pyramidal neuronsin vivo.2It increases the average running speed of mice in an accelerating rotarod task, indicating improved motor learning, at the same dose. 1.Claffey, M.M., Helal, C.J., Verhoest, P.R., et al.Application of structure-based drug design and parallel chemistry to identify selective, brain penetrant, in vivo active phosphodiesterase 9A inhibitorsJ. Med. Chem.55(21)9055-9068(2012) 2.Lai, B., Li, M., Hu, A., et al.The phosphodiesterase 9 inhibitor PF-04449613 promotes dendritic spine formation and performance improvement after motor learningDev. Neurobiol.78(9)859-872(2018)

Mpro inhibitor N3 hemihydrate is a potent antagonist of the SARS-CoV-2 main protease (Mpro), demonstrating an EC50 of 16.77 μM against SARS-CoV-2. It exhibits specific inhibition of Mpro in a range of coronaviruses, including SARS-CoV and MERS-CoV. Furthermore, it effectively inhibits HCoV-229E, FIPV, and MHV-A59, with IC50 values of 4.0 μM, 8.8 μM, and 2.7 μM, respectively[1][2].

V-9302 hydrochloride is a potent and selective competitive antagonist that inhibits transmembrane glutamine flux by specifically targeting the amino acid transporter ASCT2 (SLC1A5), and not ASCT1. In HEK-293 cells, V-9302 hydrochloride effectively inhibits ASCT2-mediated glutamine uptake with an IC50 value of 9.6 μM.

Dooku1 is an analog of Yoda1 and a selective antagonist of endogenous Piezo1 channels. Dooku1 inhibits Ca2+ entry induced by 2μMYoda1 with IC50 values of 1.3μM (in HEK 293 cells) and 1.5μM (in HUVEC). Dooku1 inhibits Yoda1-induced aortic relaxation.

Nrf2 activator-2 (referred to as compound O15), an Osthole derivative, is a highly potent Nrf2 agonist exhibiting an EC 50 of 2.9 μM in 293 T cells. By effectively disrupting the binding between Keap1 and Nrf2, Nrf2 activator-2 activates the Nrf2 pathway. Furthermore, this compound significantly reduces the ubiquitination of Nrf2 in cells, indicating its potential in regulating Nrf2 activity [1].

NPS-2143 (SB 262470A) is a novel potent and selective antagonist of Ca(2+) receptor.

AMP-579 is an adenosine A1 receptor agonist. AMP-579 also acts as a A2b-adenosine receptor agonist in human 293 cells and rabbit hearts.

1. Palmatine (Burasaine) is an inhibitor of dopamine generation. 2. Palmatine could potentially be developed for the treatment of flavivirus infections. 3. Palmatine has been used in the treatment of jaundice, dysentery, hypertension, inflammation, and liver-related diseases.

Palmatine chloride an isoquinoline alkaloid, is an important medicinal herbal extract with diverse pharmacological and biological properties.