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.

BAY 2416964 is a small molecule inhibitor that selectively targets aromatic receptor (AhR) with an IC50 of 341 nM and is commonly used in cancer immunotherapy research.

Erdafitinib (JNJ-42756493), a quinoxaline derivative, targets FGFR1 2 3 4.

Niraparib (MK-4827) is a PARP inhibitor that selectively targets PARP1 and PARP2 (IC50=3.8 2.1 nM), exhibiting antitumor activity, inhibiting DNA damage repair, and inducing apoptosis.

(+)-JQ-1 (JQ1) is a specific, reversible BET bromine domain inhibitor that targets BRD4 (1 2) with IC50 values of 77 33 nM. (+)-JQ-1 induces cell autophagy and inhibits cell proliferation.

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]

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.

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.

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).

JAK3i is a selective covalent inhibitor of JAK3 kinase. JAK3i reveals two distinct temporal waves of STAT5 phosphorylation and more potently targets the second wave, which is required for cell cycle progression and T cell proliferation.

BFC1108 targets Bcl-2 and converts it to a pro-apoptotic protein, inhibits the growth of triple-negative breast cancer xenografts with high Bcl-2 expression, inhibits breast cancer lung metastasis, and induces apoptosis of Bcl-2-expressing cancer cells.

(+)-JNJ-A07 is a pan-serotypic dengue virus inhibitor that targets NS3-NS4B interaction with high potency. (+)-JNJ-A07 has antiviral activity and can be used to study dengue virus infections.

UNC1062 is a highly selective tyrosine kinase inhibitor that specifically targets MERTK. This compound effectively suppresses MERTK-mediated downstream signaling, induces apoptosis in cell cultures, reduces colony formation in soft agar, and inhibits invasion of melanoma cells. Notably, UNC1062 demonstrates potent inhibition of MERTK kinase activity, with an IC50 of 1.1 nM and a Morrison Ki of 0.33 nM. It also displays specificity within the TAM family, exhibiting IC50 values of 60 nM for TYRO3 and 85 nM for AXL [1].

PGD2-IN-1 (PGD2-inhibitor) is an effective DP receptor antagonist (IC50:0.3 nM), a compound that can inhibit prostaglandin D2 (PGD2) signaling. PGD2-IN-1 specifically targets and regulates the activity of PGD2 receptors or enzymes involved IN PGD2 synthesis or metabolism.

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.

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.

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.

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.

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.

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.

MV151 is a fluorescent broad-spectrum proteasome inhibitor for labeling proteasomes in vitro and in vivo. MV151 specifically targets all active subunits of the proteasome and immunoproteasome in living cells, allowing for rapid and sensitive in-gel detection. The inhibition profile of a panel of commonly used proteasome inhibitors could be readily determined by MV151 labeling. Administration of MV151 to mice allowed for in vivo labeling of proteasomes, which correlated with inhibition of proteasomal degradation in the affected tissues. This probe can be used for many applications ranging from clinical profiling of proteasome activity, to biochemical analysis of subunit specificity of inhibitors, and to cell biological analysis of the proteasome function and dynamics in living cells.

Astrophloxine is a fluorescent imaging probe that targets antiparallel dimers and can be used to detect aggregated Aβ in brain tissue and cerebrospinal fluid samples from Alzheimer's disease (AD) mice.

Bosutinib (SKI-606) is a synthetic quinolone derivative and dual kinase inhibitor that targets both Abl (IC50: 1 nM) and Src (IC50: 1.2 nM) kinases.

Ethyl gallate (gallic acid ethyl ester) obviously decreases cell proliferation in MDA-MB-231 and MCF-7 cells in a dose- and time-dependent manner, exhibits cytotoxicity in a dose-dependent manner. Ethyl gallate can inhibit the abilities of invasion of breast cancer in vitro by inhibiting the mRNA levels of MMP-9 MMP-2, phosphorylation of Akt and protein expression of NF-κB and inhibits hydrogen peroxide signaling, may represent an alternative class of vasopressors for use in septic shock. Also, Ethyl gallate suppresses proliferation and invasion in human breast cancer cells by modulating the PI3K Akt pathway, which may contribute to inhibiting their downstream targets such as NF-κB p-65, Bcl-2 Bax, and mRNA levels of MMP-2 and MMP-9 in breast cancer cells, could be used as potential antioxidants with safe therapeutic application in cancer chemotherapy.

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.

Nitroxynil (4-Hydroxy-3-iodo-5-nitrobenzonitrile) is an anthelmintic compound that effectively targets parasites in both adult and immature stages. It is extensively employed in investigations pertaining to Fasciola hepatica infection.

Procaine (Vitamin H3) is a local anesthetic of the ester type that has a slow onset and a short duration of action. It is mainly used for infiltration anesthesia, peripheral nerve block, and spinal block.

Bedaquiline fumarate (TMC207), a diarylquinoline antibiotic that targets ATP synthase, is effective for the treatment of Mycobacterium tuberculosis infections. It blocks the proton pump for ATP synthase of mycobacteria. It is the first member of a new class of drugs called diarylquinolines.

Rac-Belinostat (PX-105684) is a novel hydroxamic acid-type histone deacetylase (HDAC) inhibitor with antineoplastic activity. Belinostat targets HDAC enzymes, thereby inhibiting tumor cell proliferation, inducing apoptosis, promoting cellular differentiation, and inhibiting angiogenesis. This agent may sensitize drug-resistant tumor cells to other antineoplastic agents, possibly through a mechanism involving the down-regulation of thymidylate synthase.

Tanshinone IIA (Tanshinone B) is a diterpene quinone natural product that targets the protein kinase domain of VEGF VEGFR2. Tanshinone IIA inhibits angiogenesis and exhibits anti-inflammatory, antioxidant, and therapeutic activities against coronary heart disease.

Methyl 2-(3-oxo-2-(pent-2-en-1-yl)cyclopentyl)acetate ((±)-Jasmonic Acid methyl ester) induces the synthesis of proteinase inhibitors in plant leaves, suppresses proliferation, and induces apoptosis in cancer cells. It inhibits hexokinase bound to mitochondria, disrupting mitochondrial hexokinase activity to selectively target and kill cancer cells. Derivatives of Methyl 2-(3-oxo-2-(pent-2-en-1-yl)cyclopentyl)acetate also exhibit potential as anti-inflammatory agents, and the compound has been primarily detected in urine.

2'-O-Methyl-5-iodouridine (5-Iodo-2'-O-methyluridine) is a purine nucleoside analog that targets malignant tumors of the inert lymphatic system and possesses a broad spectrum of antitumor activity. The anticancer mechanism of 2'-O-Methyl-5-iodouridine is dependent on the inhibition of DNA synthesis and induction of apoptosis.

Procaine hydrochloride (Novocaine HCl) is the hydrochloride salt form of procaine, a benzoic acid derivative with local anesthetic and antiarrhythmic properties. Procaine binds to and inhibits voltage-gated sodiumchannels, thereby inhibiting the ionic flux required for the initiation and conduction of impulses. In addition, this agent increases electrical excitation threshold, reduces rate of rise of action potential and slows nerve impulse propagation thereby causing loss of sensation.

Diazinon (Dimpylate) is a thiophosphoric acid ester, functioning as a nonsystemic organophosphate insecticide that effectively targets and controls a variety of pests including cockroaches, silverfish, ants, and fleas.

Acetylspiramycin (Spiramycin B) targets 50S ribosome to inhibit protein synthesis.

Levocetirizine Dihydrochloride (Xyzal Dihydrochloride) is a third-generation peripheral H1-receptor antagonist. Acting as an antihistaminic agent, it specifically targets the histamine H1-receptor. Levocetirizine Dihydrochloride is the R-enantiomer of Cetirizine, which gives it a higher affinity for the H1-receptor than the S-enantiomer. Due to this enhanced affinity, Levocetirizine Dihydrochloride is effective in treating allergic rhinitis and chronic idiopathic urticaria.

Ataluren (PTC124) is a novel, orally administered drug that targets nonsense mutations. Ataluren is approved for use by the European Medicines Agency to treat Duchenne Muscular Dystrophy in patients aged 5 years and older who are able to walk.

Agmatine sulfate (Agmatine sulfate salt) is a bioactive metabolite of the arginine amino acid. It exerts modulatory action at multiple molecular targets, such as neurotransmitter systems, ion channels and nitric oxide synthesis. It is an endogenous agonist at imidazoline receptor and a NO synthase inhibitor.

Cloquintocet-mexyl, a herbicide, targets and controls coarse annual grasses within the Poaceae family.

Glycocholic acid (Glycocholate) is a bile acid with anticancer activity. Glycocholic acid targets against pump resistance-related and non-pump resistance-related pathways.

2,2-BIS(2-HYDROXY-5-BIPHENYLYL)PROPANE is targets the thyroid stimulating hormone receptor (human)

Dmt-2'fluoro-da(bz) amidite is a 2'-deoxy-2'-fluoro-phosphorothioate oligonucleotide with high affinity and specificity for RNA targets and serves as an intermediate in the synthesis of 5'-DMT-3'-phosphoramidite, an antisense compound resistant to nuclease.

N-Nitroso-N-methylurea is a nitrosourea compound with alkylating, carcinogenic and mutagenic properties. It targets a variety of animal organs, causes various cancers and degenerative diseases, and can be used in diazomethane synthesis.

Dasatinib (BMS-354825) is an orally active, ATP-competitive tyrosine kinase inhibitor that targets Src and Bcr-Abl (Ki=16 30 pM), with antitumor activity, used in the treatment of leukemia and lymphoma.

3- Phenyl- N- [1- (phenylmethyl) - 4- piperidinyl] -tricyclo[3.3.1.13, 7] decane- 1- carboxamide with antiviral activity against Ebola virus that targets the surface-exposed glycoprotein and inhibits viral entry into host cells. In vitro studies in Vero cells revealed the compound inhibits the viral replication with EC50 of 0.38 μM.

carfenazine targets the Dopamine receptor and is used for schizophrenia research.

Glu-urea-Lys is a molecular scaffold that targets PSMA and can be used as a prostate cancer imaging agent to study prostate-specific membrane antigens.