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SERT inhibitor 69419 inhibits serotonin reuptake.

SERT-IN-2, a potent SERT inhibitor (IC 50 = 0.58 nM), exhibits promising efficacy as an anti-depressant. It demonstrates a favorable bioavailability of 83.28% in rats and has the ability to cross the blood-brain barrier.

RAGE/SERT-IN-1 is a potent, orally active inhibitor of advanced glycation end products (RAGE) and serotonin transporter (SERT), with IC50 values of 8.26 μM and 31.09 nM, respectively. It demonstrates a significant neuroprotective effect against Aβ25-35-induced neuronal damage and alleviates depressive behavior in mice. RAGE/SERT-IN-1 is useful for research on the comorbidity of Alzheimer's disease and depression [1].

CFI-400945 is an potent, selective and orally active inhibitor of polo-like kinase 4(PLK4; Ki value of 0.26 nM).

Onvansertib (NMS-1286937), an oral, specific Polo-like Kinase 1 (PLK1) inhibitor, is with IC50 of 2 nM. The specificity of NMS-P937 forPLK1 is 5000-fold higher over PLK2/PLK3.

Camonsertib (RP-3500) is a selective, orally active ATR kinase inhibitor (ATRi) with an IC50: 1.00 nM in biochemical assays and exhibits potent antitumour effects. Camonsertib is 30 times more selective for ATR than mTOR (IC50: 120 nM) and is a more active inhibitor of ATM, DNA-PK and PI3Kα kinases. PK and PI3Kα kinases.

Ipatasertib (GDC-0068) (GDC-0068), a highly specific pan-Akt inhibitor, targets Akt1/2/3 with IC50 of 5 nM/18 nM/8 nM, respectively.

Galunisertib (LY2157299) is an orally available inhibitor of TGFβRI kinase (IC50: 56 nM) with potential antineoplastic activity.

Uprosertib (GSK2141795) (GSK2141795) is a selective, ATP-competitive, and orally bioavailable Akt inhibitor with IC50 of 180 nM, 328 nM, and 38 nM for Akt 1, 2 and 3, respectively. Phase 2.

Capivasertib (AZD5363) is a broad-spectrum AKT inhibitor with inhibitory activity against Akt1, Akt2, and Akt3 (IC50=3/7/7 nM) with oral activity. Capivasertib has antitumor activity for the treatment of breast cancer.

Berzosertib (VE-822) has been used in trials studying the treatment of Ovarian Neoplasms, Ovarian Serous Tumor, Adult Solid Neoplasm, Advanced Solid Tumor, and Advanced Solid Neoplasm, among others.

Oditrasertib (DNL-788) is a potent RIPKl inhibitor with an IC50 value of less than 100 nM.Oditrasertib can be used for the study of immune and neurological disorders such as multiple sclerosis and Alzheimer's disease.

Delcasertib acetate is a selective δ protein kinase C (δPKC) inhibitor for the study of acute myocardial infarction and pain.

Delcasertib (KAI-9803) is a potent and selective inhibitor of δ-protein kinase C (δPKC).

(1S,4R)-N-DesmethylSertralineHydrochloride is a Serotonin transporter and Norepinephrine transporter inhibitor with IC50 of 19 nM and 35 nM, respectively.

Cenisertib is A potent ATP-competitive multi-kinase inhibitor, showing inhibitory effects on the activity of Aurora-kinase-A/B, ABL1, AKT, STAT5, FLT3, as well as kinase inhibitors of FER and its homolog. Cenisertib inhibits the growth of tumor mast cells (MCS) by inhibiting the activity of several different molecular targets. Cenisertib also inhibits tumor growth in pancreatic, breast, colon, ovarian and lung cancer and leukemia in xenograft models.

ATR inhibitor 2 is an orally active, ATP-competitive, and selective ATR inhibitor (Ki <150 pM) with antitumor activity. ATR inhibitor 2 potently inhibits ATR-driven phosphorylated checkpoint kinase-1 (Chk1) phosphorylation (IC50: 8 nM).

Zabedosertib (BAY 1834845) is an inhibitor of IRAK4 with immunomodulatory potential. Zabedosertib protects against acute respiratory distress syndrome, a new study suggests.

Ipatasertib dihydrochloride (GDC-0068 dihydrochloride) is a highly selective and ATP-competitive inhibitor of pan-Akt (IC50s: 5, 18 and 8 nM for Akt1, Akt2 and Akt3, respectively).

Plogosertib (CYC140) is an orally active, selective, potent, and ATP-competitive PLK1 inhibitor with an IC50 value of 3 nM.Plogosertib exhibits antiproliferative and anticancer activity and can be used for the study of solid and hematologic tumors. and hematologic tumors.

Sertraline hydrochloride (Sertraline HCl) is a selective serotonin uptake inhibitor that is used in the treatment of depression.

Miransertib (ARQ-092) is an orally bioavailable, selective, and potent allosteric Akt inhibitor.

Rabusertib (IC-83) is an inhibitor of the cell cycle checkpoint kinase 1 (chk1) with potential chemopotentiating activity. Rabusertib has been used in trials studying the treatment of Cancer, Solid Tumors, Advanced Cancer, Pancreatic Neoplasms, and Non-Small Cell Lung Cancer.

Silmitasertib (CX-4945) is a potent, orally bioavailable inhibitor of casein kinase 2 (CK2; Ki: 0.38 nM).

Danusertib (PHA-739358) is a small-molecule 3-aminopyrazole derivative with potential antineoplastic activity. Danusertib binds to and inhibits the Aurora kinases, which may result in cell growth arrest and apoptosis in tumor cells in which Aurora kinases are overexpressed.

Alisertib (MLN 8237) is a specific Aurora A inhibitor (IC50: 1.2 nM). The selectivity of Alisertib(MLN 8237) is >200-fold higher for Aurora A than Aurora B.

Barasertib-HQPA (AZD2811) is a highly selective Aurora B inhibitor (IC50: 0.37 nM) and demonstrates ~3,700-fold greater selectivity than Aurora A.

Tomivosertib (eFT508) is a potent, highly selective MNK1 and MNK2 inhibitor with IC50 value of 1-2 nM.

Afuresertib (GSK2110183) is an orally bioavailable inhibitor of the serine/threonine protein kinase Akt (protein kinase B) with potential antineoplastic activity.

Tozasertib (MK-0457) is a pan-Aurora kinase inhibitor (Kis: 0.6/18/4.6 nM for Aurora A/Aurora B/Aurora C). It shows selectivity against more than 190 different kinases.

Selonsertib (GS-4997) is an orally bioavailable inhibitor of apoptosis signal-regulating kinase 1 (ASK1), with potential anti-inflammatory, antineoplastic and anti-fibrotic activities.

Vactosertib (EW-7197) is an orally bioavailable inhibitor of the serine/threonine kinase, transforming growth factor (TGF)-beta receptor type 1 (TGFBR1), also known as activin receptor-like kinase 5 (ALK5), with potential antineoplastic activity.

Ceralasertib (AZD6738) is an orally active, and selective ATR kinase inhibitor with IC50 of 1 nM.

Adavosertib (MK-1775) is a small molecule inhibitor of the checkpoint kinase WEE1 (IC50: 5.2 nM). It hinders the G2 DNA damage checkpoint.

Volasertib (BI 6727) (BI-6727) is a potent inhibitor of PLK1 (IC50: 0.87 nM), inducing mitotic arrest and apoptosis. It also inhibits PLK2/PLK3 (IC50s: 5/56 nM).

MPP+ iodide, the metabolite of a neurotoxin MPTP, causes symptom of Parkinson's disease (PD) in animal models by selectively destroying dopaminergic neurons in substantia nigra. MPP+ induces dopamine transporter (DAT) externalization in dopaminergic (DA)

Dapoxetine hydrochloride (LY-210448 hydrochloride) is a selectivity short-acting serotonin reuptake inhibitor, used for the therapy of premature ejaculation.

Vilazodone (SB659746A) is a selective serotonin (5-HT) reuptake inhibitor (SSRI) and a 5-HT-1A receptor partial agonist, with antidepressant and anti-anxiety activities. Vilazodone inhibits the reuptake of serotonin from the synaptic cleft while stimulating the release of 5-HT into the synaptic cleft. This increases the concentration of 5-HT in the synaptic cleft and potentiates serotonergic neurotransmission in the central nervous system.

Fluoxetine hydrochloride (Lilly110140) is the first highly specific serotonin uptake inhibitor. It is used as an antidepressant and often has a more acceptable side-effects profile than traditional antidepressants.

Ipatasertib-NH2 (GDC-0068-NH2;RG7440-NH2) is a ligand for target protein AKT for PROTAC, binds to lenalidomide, a ligand of ubiquitin E3 ligase cereblon (CRBN), via a ten-hydrocarbon linker to form INY-03-041 to degrade AKT[1].

Desertomycin A is fungal metabolite and the major component of the desertomycin antibiotic complex that has been found in S. flavofungini.

Vevorisertib (ARQ 751) is a highly effective oral compound that selectively inhibits pan-AKT serine/threonine kinases such as AKT1 (with an IC50 value of 0.55 nM), AKT2 (with an IC50 value of 0.81 nM), and AKT3 (with an IC50 value of 1.31 nM). This compound, either as a standalone treatment option or in combination with other anti-cancer agents, is ideally suited for conducting research on solid tumors characterized by PIK3CA/AKT/PTEN mutations[4].

Ipatasertib-NH2 dihydrochloride is a ligand for the target protein AKT in PROTAC INY-03-041. INY-03-041 consists of Ipatasertib-NH2, a ten-hydrocarbon linker, and the CRBN ligand Lenalidomide, which acts as an E3 ubiquitin ligase.

Tilpisertib is a serine/threonine kinase inhibitor (WO2017007689).

Nitroxazepine (CIBA 2330Go) is a serotonin-norepinephrine reuptake inhibitor, and treatment depression. Nitroxazepine is a tricyclic antidepressant (TCA) for the research of depression

Azaphen (Pipofezin hydrochloride) is the reuptake of serotonin inhibitor.with antidepressant action and has sedative effects, suggesting antihistamine activity.

Edecesertib (GS-5718) is a selective, orally active IRAK-4 inhibitor that exhibits anti-inflammatory activity. edecessertib can be used to study rheumatoid arthritis (RA) and lupus erythematosus (LE).

CFI-402257 hydrochloride, a highly selective and orally bioavailable inhibitor targeting TTK/Mps1, demonstrates an in vitro IC50 value of 1.7 nM against TTK. This compound exhibits anti-cancer activity [1].

Tozasertib lactate is a potent and selective small-molecule inhibitor of the Aurora kinases which suppresses tumor growth by inducing apoptosis in tumor cells in which Aurora kinases are overexpressed.

Amcasertib (BBI503) is an orally administered investigational agent designed to inhibit cancer stem cell pathways via targeting stemness kinases.