MYCMI-7 is a small molecule MYC-binding compound (Kd=4 uM) that inhibits MYC-MAX interaction.MYCMI-7 efficiently and selectively inhibits MYC:MAX and MYCN:MAX interactions in cells, binds directly to recombinant MYC, and reduces MYC-driven transcription.MYCMI-7 induces degradation of MYC and MYCN proteins.MYCMI-7 potently induces growth arrest/apoptosis in tumor cells in a MYC/MYCN-dependent manner and downregulates the MYC pathway on a global level.MYCMI-7 downregulates MYC/MYCN, inhibits tumor growth, and prolongs survival through apoptosis in mouse tumor models of MYC-driven AML, breast cancer, and MYCN-amplified neuroblastoma.

A potent, selective and competitive corticotropin-releasing factor CRF2 receptor antagonist with Ki of 1.4 nM, 100-fold selectiivity over CRF1.

Nattokinase, Natto fermentation is a potent fibrinolytic enzyme. Nattokinase can break down blood clots by directly hydrolyzing fibrin and plasmin substrate. Nattokinase can be used for the research of cardiovascular diseases.

NNC63-0532 is a potent and selective non-peptide agonist of the NOP receptors.

Delta-Valerobetaine (hydrobromide) is a precursor of trimethylamine N-oxide (TMAO).

Nigratine (6E11) is a highly specific, non-ATP competitive inhibitor of RIPK1 kinase (IC50=1.6 uM), inhibits necroptosis and ferroptosis.Nigratine inhibits necroptotic cell-death induced by TNF-α in Jurkat-Fadd def cells with IC50 of 4.6 uM.Nigratine is significantly more potent than the specific RIPK1 necroptosis inhibitor, Nec-1s.Nigratine (50 uM) strongly inhibits the ferroptotic cell death induced by excess of glutamate, erastin, and RSL3, in both murine HT22 and human SH-SY5Y cell lines, protects SH-SY5Y human neuroblastoma cell line from cell death triggered by both class I and II-inducers of ferroptosis.Nigratine protects porcine kidney epithelial LLC-PK1 cell line from lipid peroxidation and cell death triggered by RSL3.Nigratine protects human bronchial organoids from necroptosis and ferroptosis.

AZ'9567 is a potent inhibitor of MAT2A with pIC50 of 8.2. in vitro with excellent preclinical pharmacokinetic properties. AZ'9567 shows robust antitumor response in the MTAP KO HCT116 model.

TRIM24 inhibitor X is a potent TRIM24 bromodomain inhibitor for synthesis dTRIM24..

Z-Asp-CH2-DCB is an irreversible broad spectrum caspase inhibitor. Z-Asp-CH2-DCB also inhibits proteases with caspase-like activity. Z-D-CH2-DCB blocks the production of IL-1β, TNF-α, IL-6, and IFN-γ in staphylococcal enterotoxin B (SEB)-stimulated peripheral blood mononuclear cells (PBMC), and reduces SEB-1-stimulated T-cell proliferation in a dose-dependent manner. Z-Asp-CH2-DCB prevents SU5416-induced septal cell apoptosis and emphysema development.

A small molecule inhibitor (IC50=0.3 uM) of DEAD-box polypeptide 3 (DDX3), a human host factor required for the replication of several DNA and RNA viruses.

CLC-2-IN-AK42 (CLC-2 inhibitor AK42, AK42) is a potent, specific small-molecule inhibitor of voltage-gated chloride channel CLC-2 with IC50 of 17 nM (human CLC-2).AK42 displays unprecedented selectivity (>1,000-fold) over CLC-1, the closest CLC-2 homolog, and no off-target engagement a diverse panel of 61 CNS receptors, channels, and transporters expressed in brain tissue.AK-42 binds to an extracellular vestibule above the channel pore. AK-42 is almost three orders-of-magnitude more potent than MCFA, demonstrates high potency (IC50=14 nM for rat CLC-2) in manual patch-clamp experiments on CHO cells transiently transfected with rat CLC-2.AK-42 inhibits hyperpolarization-activated current in hippocampal cells, attenuates steady-state currents and eliminated relaxation currents in recorded neurons.AK-42 is a powerful tool for investigating CLC-2 neurophysiology.

Potent and selective inhibitor of diacylglycerol acyltransferase 2 (DGAT2)

PSB-CB-27 is a potent, selective antagonist of GPR18 with IC50 of 650 nM, shows no inhibition on GPR55 and low affinity for CB1/CB2 receptors.

Tinlarebant (LBS-008) is an orally active non-retinoid RBP4 (retinol-binding protein 4) antagonist. Tinlarebant can be used for the research of the Stargardt disease.

ALK-001 is a vitamin A analog potentially for the treatment of Stargardt’s disease.

Encequidar (HM30181) is a potent selective inhibitor of MDR1 (ABCB1, P-gp) with IC50 of 0.63 nM.Encequidar (HM30181) effectively blocked transepithelial transport of paclitaxel in MDCK monolayers.Encequidar (HM30181) does not inhibit MRP1 (ABCC1), MRP2 (ABCC2), and MRP3 (ABCC3), and partially inhibited BCRP (ABCG2) only at very high concentrations.Oral co-administration of paclitaxel and HM30181 showed a tumor-inhibitory strength equal or superior to that of intravenous paclitaxel in the xenograft model in nude mice.

SS-1-148 is a potent, selective inhibitor of human ornithine δ-aminotransferase (hOAT) with Ki of 60 uM, shows excellent selectivity over other related aminotransferases (e.g., GABA-AT).

IDH1 Inhibitor 8 (91) is isocitrate dehydrogenase 1 (IDH1) inhibitor. IDH1 Inhibitor 8 can be used for the research of cancer.

E1231 (E-1231) is a small molecule SIRT1 activator with EC50 of 0.83 uM, interactes with recombinant human SIRT1 protein and deacetylated liver X receptor-alpha (LXRα).

AdipoRon hydrochloride is an orally active and specific AdipoR agonist, binding to AdipoR1 and AdipoR2, with Kds of 1.8 and 3.1 μM, respectively.

AdipoRon is a novel small-molecule AdipoR agonist; binds to both AdipoR1(Kd= 1.8 uM) and AdipoR2(Kd=3.1 uM).

7,12-Dimethylbenz[a]anthracene (DMBA) is an immunosuppressor as well as a potent organ-specific carcinogen.

Turbinaric acid is a moderately cytotoxic secosqualene carboxylic acid that is isolated from the brown alga Turbinaria ornata.

Eplerenone, also known as Inspra and CGP-30083, is a selective aldosterone receptor antagonist used to treat hypertension and congestive heart failure. Eplerenone provides marked protection against vascular injury in the kidney and heart.

AMG-073 HCl (Cinacalcet HCl) represents a new class of compounds for the treatment of hyperparathyroidism.

Cinacalcet(AMG-073) is an orally active, second-generation calcimimetic compound; AMG 073 represents a new class of compounds for the treatment of hyperparathyroidism.

Macrocyclic peptide D4-2 is a macrocyclic peptide consisting of 15 amino acids that binds to the ectodomain of mouse SIRPα (Kd=10 nM, IgV-B6 SIRPα) and efficiently blocks CD47-SIRPα interaction in an allosteric manner (IC50=0.18 uM).

Darizmetinib (HRX-0215, HRX0215) is a potent, selective inhibitor of MKK4 (MAP2K4/SEK1), shows potential for promoting liver regeneration or reducing or preventing hepatocyte death.

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