Bicuculline methobromide is a selective GABAA receptor antagonist with an IC50 value of 3 μM. Bicuculline methobromide induces clonic tonic convulsions in mammals and can also be used to block Ca2+ activated potassium channels. Bicuculline methobromide can be used in studies of epilepsy and other related psychiatric disorders[1][2].
Iodoacetyl-PEG4-NHS ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
5-Hydroxyseselin is a natural product isolated from Metrodorea flavida[1].
Trijuganone B (Tetrahydro tanshinone I) can be extracted from from the roots of Salvia miltiorrhiza f. alba. Trijuganone B inhibits the proliferation of leukemia cells[1][2].
WSD-0922 is a potent, selective, orally active, and BBB penetrable EGFR/EGFRVIII inhibitor. WSD-0922 is against EGFRm+ (EGFRvIII/Del19/L858R) with an IC50 of <10 nM. WSD0922 shows good safety profile and preclinical anti-tumor efficacy[1].
RSS0680 (Example 22) is a bifunctional compound targeted protein degradation of kinases. RSS0680 degrades AAK1, CDK1, CDK16, CDK2, CDK4, CDK6, EIF2AK4, GAK, LATSl, LIMK2, MAPK6, MAPKAPK5, MARK2, MARK4, MKNK2, NEK9, RPS6KB1, SIK2, SNRK, STK17A, STK17B, STK35, and WEEl. RSS0680 can be used for research of disease or disorder mediated by aberrant kinase activity[1].
Cbl-b-IN-1 (example 519) is a Cbl-b inhibitor, extracted from patent WO2019148005A1, with an IC50 <100 nM[1].
4-Methylumbelliferyl phosphate (4-MUP) disodium, an anionic organophosphate, is a acid and alkaline phosphatase fluorogenic substrate. 4-Methylumbelliferyl phosphate disodium is also a nerve agent simulant[1][2][3].
Himastatin is a antitumor antibiotic produced by a strain of S. hygroscopicus sp. Himastatin is a dimeric cyclohexadepsipeptide containing piperazic acid and a unique central aromatic core[1].
DDR1-IN-5 is a selective Discoidin Domain Receptor family, member 1 (DDR1) inhibitor with an IC50 of 7.36 nM. DDR1-IN-5 inhibits auto-phosphorylation DDR1b (Y513) with an IC50 of 4.1 nM. DDR1-IN-5 has anti-cancer activity[1].
Abiraterone metabolite 1 is a 5β-reduced metabolite of abiraterone. Abiraterone, a steroidal drug, inhibits CYP17A1, blocks androgen synthesis and prolongs survival in prostate cancer.
(tert-Butoxycarbonyl)-D-histidine is a histidine derivative[1].
BChE/HDAC6-IN-2 (compound 29a) is a dual inhibitor of BChE and HDAC6 with IC50s of 1.8 nM and 71.0 nM, respectively. BChE/HDAC6-IN-2 has prominently neuroprotective effects and reactive oxygen species (ROS) scavenging activity. BChE/HDAC6-IN-2 is also an effective chelator of metal ion (Fe2+ and Cu2+). BChE/HDAC6-IN-2 inhibits phosphorylation of tau, and exhibits moderate immunomodulatory effect.
Clomethiazole hydrochloride is a sedative and anticonvulsant. Clomethiazole hydrochloride is neuroprotective and prevents the degeneration of serotonergic nerve terminals induced by 3,4-methylenedioxymethamphetamine (MDMA)[1][2].
N,N-dimethyl-4-(phenyldiazenyl)aniline-d5 is the deuterium labeled N,N-dimethyl-4-(phenyldiazenyl)aniline[1].
Transcainide (R 54718) is an orally active antiarrhythmic agent[1].
Nazartinib S-enantiomer (EGF816 S-enantiomer) is the less active S-enantiomer of Nazartinib. Nazartinib (EGF816) is an EGFR inhibitor.
Trifluoperazine N-Glucuronide (UGT1A4), as one of the human UGT1A isoforms, is expressed in the liver. Trifluoperazine N-Glucuronide catalyzes the imipramine and trifluoperazine Nglucuronide formation[1].
CPI-613 is a lipoic acid analog that inhibits pyruvate dehydrogenase (PDH) and α-ketoglutarate dehydrogenase, disrupts mitochondrial metabolism and shows strong antitumor activity.
4-Feruloylquinic acid may be a potential biomarker for food products[1].
IRAK4-IN-21 (compound 17) is an orally active, potent and selective IRAK4 inhibitor with IC50 values of 5 and 56 nM for IRAK4 and TAK1, respectively. IRAK4-IN-21 effectively inhibits IL-23 production (IC50=0.17 µM) and can be used in studies of autoimmune diseases such as plaque psoriasis and psoriatic arthritis[1].
Dehydronitrosonisoldipine is a calcium channel antagonist.
GLPG0492 is a novel selective androgen receptor modulator; exhibited anabolic activity on muscle, strongly dissociated from the androgenic activity on prostate after oral dosing.IC50 value:Target: AR modulatorGLPG0492 has very good pharmacokinetic properties, including bioavailability in rat (F > 50%), and is currently under evaluation in phase I clinical trials [1]. GLPG0492 is a new non-steroidal selective androgen receptor modulator that is currently under development for musculo-skeletal diseases such as sarcopenia and cachexia. In acute exhaustion tests, a surrogate of the 6-min walking test used in DMD patients, GLPG0492 preserved running performance, whereas vehicle- or comparator-treated animals showed a significant increase in fatigue (30-50%) [2]. GLPG0492 treatment partially prevents immobilization-induced muscle atrophy with a trend to promote muscle fiber hypertrophy in a dose-dependent manner. Interestingly, GLPG0492 was found as efficacious as TP at reducing muscle loss while sparing reproductive tissues. Furthermore, gene expression studies performed on tibialis samples revealed that both GLPG0492 and TP were slowing down muscle loss by negatively interfering with major signaling pathways controlling muscle mass homeostasis [3].
NCGC00262650 is a potent apical membrane antigen 1-rhoptry neck protein 2 (AMA1-RON2) interaction inhibitor. NCGC00262650 can block entry of merozoites into red blood cells[1].
Semustine is a DNA alkylator, binds to DNA, and acts as a cancer chemotherapeutic agent[1].
AR-M 1000390 hydrochloride is an exceptionally selective, potent δ opioid receptor agonist with an EC50 of 7.2±0.9 nM for δ agonist potency.
(R)-2-formamido-4-methylpentanoic acid is a leucine derivative[1].
Ethosuximide-d3 is the deuterium labeled Ethosuximide. Ethosuximide, a widely prescribed anti-epileptic drug, improves the phenotypes of multiple neurodegenerative disease models and blocks the low voltage activated T-type calcium channel[1][2].
Efmitermant alfa (ACE-083) is a locally acting, follistatin-based fusion protein. Efmitermant alfa also is a muscle-promoting agent. Efmitermant alfa can be used for the research of muscle disorders[1][2].
Novel Inhibitor of Bacterial Cytokinesis, inhibiting FtsZ