targets

Sorafenib (Bay 43-9006) is a multikinase inhibitor that targets Raf-1, B-Raf, VEGFR2, VEGFR3, VEGFR4, PDGFRβ, FLT3, c-Kit, and others (IC50=6 22 90 15 20 20 57 58 nM) with oral activity. It exhibits antitumor properties and can induce autophagy, apoptosis, and agonistic iron death.

Resveratrol (SRT 501) is a polyphenolic natural product, a plant antitoxin with antioxidant and chemopreventive activities. Resveratrol has a wide range of targets including COX, SIRT, LOC, etc. Resveratrol induces autophagy and apoptosis.

SQ109 (NSC-722041) is an effective inhibitor of the trypomastigote form of the parasite (IC50 = 50 nM). SQ109 is an antitubercular agent and targets MmpL3.

Alpelisib (BYL-719) is a PI3Kα inhibitor (IC50=5 nM) with selective, potent, and oral activity, inhibiting PI3Kβ γ δ with low activity (IC50=250 290 1200 nM). Alpelisib demonstrates antitumor activity and specifically targets PIK3CA mutant tumors.

AU-15330 is a proteolytic targeting chimera (PROTAC) that simultaneously targets SMARCA4, SMARCA2, and PBRM1 for degradation and exhibits cytotoxicity in H3.3K27M cells but not in H3 wild-type cells. [2]

Go 6983, a pan-PKC inhibitor, targets PKCα, PKCβ, PKCγ, PKCδ, and PKCζ, with IC50 values of 7 nM, 7 nM, 6 nM, 10 nM, and 60 nM, respectively.

Voxelotor (GBT 440) is a novel hemoglobin S (HbS) polymerization inhibitor primarily used for the treatment of sickle cell disease (SCD) and a cytochrome P450 3A4 inhibitor. Voxelotor targets and covalently binds to the N-terminal valine of the HbS alpha chain, thereby stabilizing sickle cell hemoglobin (HbS).

Aducanumab (BIIB037), A selective human immunoglobulin gamma-1 (IgG1) monoclonal antibody, targets the clustered form of amyloid beta (Aβ). Aducanumab shows brain permeability and may be used to treat Alzheimer's disease (AD).

Adalimumab (anti-TNF-alpha) is the first fully human recombinant IgG1 monoclonal antibody that specifically targets human TNF-alpha.

Atezolizumab is an antibody inhibitor, a humanized monoclonal antibody, IgG1, which targets PD-L1 and blocks the interaction of PD-L1 with PD-1. Atezolizumab has antitumor activity and promotes T-cells to attack tumor cells.

A2AR-agonist-1 (N-(2-(1H-Indol-3-yl)ethyl)adenosine) is a potent A2AR and ENT1 agonist (Ki: 4.39 and 3.47 for A2AR and ENT1. It targets the Adenosine A2A Receptor and Adenosine Transporter for Neuroprotection.

β-NF-JQ1 is a PROTAC that recruits aryl hydrocarbon receptor E3 (AhR E3) ligase to target proteins. Using β-NF as an AhR ligand, it targets bromodomain (BRD)-containing proteins and induces AhR and BRD protein interactions. β-NF-JQ1 exhibits potent anticancer activity associated with protein knockdown activity.

IPN60090 is a novel, potent, orally bioavailable, renal-type glutaminase (GLS1)-specific inhibitor with an IC50 value of 31 nM for GLS1. IPN60090 has potential anticancer and immunostimulant immunomodulatory activity, selectively targets, binds, and inhibits human glutaminase, and can be used to study GLS1-mediated diseases.

HLY78 (4-Ethyl-5-methyl-5,6-dihydro-[1,3]dioxolo[4,5-j]phenanthridine) targets the DIX domain of Axin, is an activator of the Wnt β-catenin signaling pathway and can enhance Axin-LRP6 binding to promote Wnt signaling.

Masupirdine free base (SUVN-502 free base) is an orally available 5-HT6 receptor antagonist that crosses the blood-brain barrier, with a Ki value of 2.04 nM for the human 5-HT6 receptor. It is potent and selective, inhibiting multiple targets, and can be used in the study of neurological disorders such as Alzheimer's disease.

MBC-11 is a first-in-class conjugate of the bone-targeting bisphosphonate etidronate covalently linked to the antimetabolite cytarabine (araC), with potential to treat tumor-induced bone disease (TIBD).

SAR7334 hydrochloride, a potent and specific inhibitor of TRPC6 (IC50 of 7.9 nM), effectively targets and inhibits the TRPC6 channel.

3CAI is a potent and specific AKT1 and AKT2 inhibitor, demonstrating significant inhibition of AKT in an in vitro kinase assay. It suppressed the expression of AKT direct downstream targets (such as mTOR and GSK3β) and induced growth inhibition and apoptosis in colon cancer cells.

AY 9944 is a specific cholesterol biosynthesis inhibitor that targets the 7-dehydrocholesterol Δ7-reductase (DHCR7) enzyme (IC50=13 nM). At high doses, AY 9944 also inhibits sterol Δ7-Δ8 isomerase in cultured embryos, leading to the accumulation of cholest-8-en-3β-ol[1][2][3]. Additionally, AY 9944 causes hypocholesterolemia and accumulation of 7DHC.

Debio 0932 (CUDC-305) is a heat shock protein 90 (Hsp90) inhibitor that targets the n-terminal atp-binding pocket to promote apoptosis, and has the advantage of being orally available and able to cross the blood-brain barrier (BBB) for the treatment of cancers such as non-small-cell lung cancer (NSCLC) and neuroblastoma.

K777 is a potent, orally active, and irreversible inhibitor of cysteine protease, functioning as a potent CYP3A4 inhibitor (IC50 = 60 nM) and a selective CCR4 antagonist, which inhibits chemotaxis. K777 irreversibly inhibits Cruzain, the major cysteine protease of Trypanosoma cruzi, and cathepsins B and L, targeting cathepsin-mediated cell entry and exhibiting broad-spectrum antiviral activity. It inhibits EBOV and SARS-CoV pseudovirus entry with IC50 values of 0.87 nM and 0.68 nM, respectively.

YKL-06-062 is a second-generation salt-inducible kinase (SIK) inhibitor that targets SIK1, SIK2, and SIK3, with IC50 values of 2.12 nM, 1.40 nM, and 2.86 nM, respectively.

ASM-024, a potent nicotinic receptor agonist, is a small molecule synthetic piperazine compound that promotes different targets and signaling pathways of β2-adrenergic receptors mediating smooth muscle relaxation, and is a potential compound for the treatment of asthma and chronic obstructive bronchitis with anti-inflammatory activity.

Glutathione arsenoxide hydrochloride (Glutathione arsenoxide hydrochloride(1271726-51-2 Free base)) is a potentially active anti-cancer molecule and inhibitor of tumour metabolism. glutathione arsenoxide hydrochloride targets the mitochondrial inner membrane adenine nucleotidyl transferase (ANT), which inhibits cell proliferation and promotes apoptosis. Glutathione arsenoxide hydrochloride can be used to recognize cell surface proteins such as protein disulfide isomerases.