NRPa-308 is a neuropilin-1 (NRP-1) antagonist, inhibits the VEGF-A165/NRP-1 binding with IC50 of 42 uM, exerts in vitro anti-angiogenic activity.

ζ-Stat trisodium (NSC37044 trisodium) is a specific and atypical PKC-ζ inhibitor, with an IC50 of 5 μM. ζ-Stat trisodium can reduce melanoma cell lines proliferation and induce apoptosis, and has antitumor activity in vitro.

SAR439883 (SAR 439883) is a novel potent, selective, orally active PKR inhibitor with IC50 of 0.68/0.69 uM against hPKR/mPKR, respectively.

PZ09 (PKC-zeta inhibitor 9, PKC-ζ inhibitor PZ9) is a potent, isoform selective PKC-zeta (PKC-ζ) inhibitor with IC50 of 5.18 nM, displays excellent selectivity (>200-fold) over other PKC isoforms with exception of PKC-i (10-fold). PZ09 also shows high selectivity for CDK-2 (>200-fold), as well as a broader range of other kinases (<50% inhibition at 10 uM). PZ09 is a small-molecule inhibitor, the first tool to successfully interrogate aPKC signaling in cells.

AZD8797 is an allosteric non-competitive modulator of the human CX3CR1 receptor; antagonizes CX3CL1 with IC50 values of 6 and 300 nM in B-lymphocyte cell line and human whole blood, respectively.

5'-Cytidylic acid is a nucleotide that is used as a monomer in RNA.

Misetionamide is an orally oxathiazin-like compound. Misetionamide is a glyceraldehyde-3-phosphate dehydrogenase (GAPDH) inhibitor with antineoplastic activity. Misetionamide can be used for the research of cancer.

Adrenochrome is a chemical compound produced by the oxidation of adrenaline (epinephrine). The derivative carbazochrome is a hemostatic medication.

A serine protease inhibitor that inhibits the esterolytic activity of factor D (IC50=96 nM) and C1s (IC50=1.6 nM).

AM-9022 (AM9022) is a potent, selective and orally active mitotic kinesin KIF18A inhibitor with IC50 of 47 nM in kinesin-8 microtubule (MT)-ATPase motor assays.

Cotransin CT8 (CT-08) is a substrate-selective co-translational translocation inhibitor, binds the Sec61 translocon to inhibit cotranslational translocation of a subset of secreted and type I transmembrane proteins.

JR1-157 is a potent selective sigma 2 receptor (σ2R) ligand with Ki value of 47 nM, >10-fold selectivity over σ1R.

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.

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

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.

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).

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.

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

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).