mice

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).

PACMA 31 is an irreversible and covalent inhibitor of protein disulfide isomerase (PDI) with an IC50 of 10 μM. PACMA 31 significantly suppresses ovarian tumor growth and exhibits tumor targeting ability.

RGX-202 (β-GPA) is a creatine analog that alters skeletal muscle energy expenditure. It reduces cellular ATP, creatine, and phosphocreatine levels and stimulates AMP-activated protein kinase (AMPK), activating PPARγ coactivator 1α (PGC-1α).

MYCMI-6 (NSC-354961) is a potent and selective inhibitor of endogenous MYC:MAX protein interactions,reduces proliferation and induces massive apoptosis in tumor tissue from a MYC-driven xenograft tumor model without severe side effects.

Estrogen receptor modulator 1 causes regression of Tamoxifen-resistant, hormone-independent xenograft tumors. Estrogen receptor modulator 1 is an orally active and selective estrogen receptor modulator (SERM) (pIC50: 0.46).

CCG-1423, a selective RhoA pathway inhibitor, suppresses SRF-mediated transcription.

YK 4-279, an inhibitor of RNA Helicase A (RHA), binds to the oncogenic transciption factor EWS-FLI1.

Fanotaprim is a dihydrofolate reductase (DHFR) inhibitor, suppressing the growth of T. gondii strains with a TgDHFR IC50 of 1.57 ± 0.11 nM, a hDHFR IC50 of 308 ± 71 nM, and a hDHFR to TgDHFR selectivity ratio of 196.

PMEDAP is a potent inhibitor of Moloney murine sarcoma virus (MSV)-induced tumor formation and mortality, as well as a human immunodeficiency virus (HIV) replication inhibitor with anti-murine cytomegalovirus (MCMV) activity.

CP-724714 (CP724714) is an effective and selective HER2/ErbB2 inhibitor (IC50: 10 nM), >640-fold selectivity against EGFR, Abl, InsR, PDGFR, IRG-1R, Src, VEGFR2, c-Met etc.

GSK-J4 Hydrochloride (GSK J4 HCl) is a cell permeable, potent and selective histone demethylase(JMJD3 )inhibitor. is an ethyl ester derivative of the GSK-J1 with an IC50 value greater than 50 μM in vitro.

GSK4112 (SR6452) is a Rev-erbα agonist with an EC50 of 0.4 μM and serves as a small molecule chemical probe for studying the cell biology of the nuclear heme receptor Rev-erbα.

Fatostatin hydrobromide (Fatostatin A HBr) ia an inhibitor of sterol regulatory element binding protein (SREBP). It impairs the activation of SREBP-1 and SREBP-2.

S29434 (NMDPEF) is a potent, competitive inhibitor of quinone reductase 2 (QR2), with an IC50 range of 5-16 nM.

NIBR189 is a potent and selective antagonist of EBI2 (GPR183) receptor (IC50 of 11 and 15 nM for human and mouse EBI2 receptors, respectively)

PD146176 (NSC-168807) is an inhibitor of 15-Lipoxygenase (15-LO) , it inhibits rabbit reticulocyte 15-LO with Ki of 197 nM and IC50 of 0.54 μM. PD146176 reverses cognitive impairment, brain amyloidosis, and tau pathology by stimulating autophagy in aged triple transgenic mice.

Tuxobertinib (BDTX-189) is a potent and selective inhibitor of allosteric EGFR and HER2 oncogenic mutations, with KDs of 0.2, 0.76, 13, and 1.2 nM for EGFR, HER2, BLK, and RIPK2, respectively, and exhibits anticancer activity.

Fatostatin is a specific inhibitor of SREBP activation, it impairs the activation of SREBP-1 and SREBP-2. Fatostatin binds to SCAP (SREBP cleavage-activating protein), and inhibits the ER-Golgi translocation of SREBPs.

CHR-6494 TFA is a potent haspin inhibitor with an IC50 of 2 nM, inhibiting histone H3T3 phosphorylation. It induces apoptosis in cancer cells, including melanoma and breast cancer, and is useful for cancer research.

Kaempferol 3-O-β-D-glucuronide (Kaempferol-3-beta-O-glucuronide) exhibits antioxidant activity. Flavonoid glucuronides can be deconjugated by microsomal α²-glucuronidase from various human cells.

Ketoprofen (RP-19583) is a propionic acid derivative and nonsteroidal anti-inflammatory drug (NSAID) with anti-inflammatory, analgesic, and antipyretic effects. It inhibits cyclo-oxygenase I and II, decreasing the formation of prostaglandin and thromboxane precursors. This reduction in prostaglandin synthesis, mediated by prostaglandin synthase, is responsible for its therapeutic effects. Additionally, Ketoprofen decreases thromboxane A2 formation via thromboxane synthase, inhibiting platelet aggregation.

Doxylamine Succinate is a pyridine derivate histamine H1 antagonist with pronounced sedative properties. Doxylamine succinate (Decapryn) competitively blocks the histamine H1 receptor and limits the typical allergic and anaphylactic responses, including bronchoconstriction, vasodilation, increased capillary permeability, and spasmodic contraction of the gastrointestinal smooth muscle, caused by actions of histamine on bronchial and gastrointestinal smooth muscles, and on capillaries. This drug also prevents histamine-induced pain and itching of the skin and mucous membranes.

Capmatinib 2HCl (INC-280 2HCl) is a novel, ATP-competitive inhibitor of c-MET kinase with an IC50 with 0.13 nM.Capmatinib 2HCl exhibits picomolar enzymatic potency and is highly specific for c-MET with more than 10, 000-fold selectivity over a large panel of human kinases. This inhibitor potently blocks c-MET phosphorylation and activation of its key downstream effectors in c-MET-dependent tumor cell lines. As a result, Capmatinib 2HCl potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis in vitro.

methyl isoeugenol (MIE) is a natural food flavour that constitutes 93.7% of an essential oil from Pimenta pseudocaryophyllus leaf. The leaf extracts of this species are used as a calming agent. As a ubiquitous food additive, the application of MIE for tre