Tocainide hydrochloride is an orally activesodium channel blocker, it blocks the sodium channels in the pain-producing foci in the nerve membranes. Tocainide hydrochloride is a primary amine analog of lidocaine, can be used for the treatment of tinnitus.

SB02024 is a novel highly potent, selective, ATP competitive, orally active inhibitor of vacuolar protein sorting 34 (Vps34) with Kd of 1 nM, >1000 times selective towards other PI3K isoenzymes; SB02024 is also highly selective at 1 uM in the DiscoveRx ScanMax panel of 468 kinases; reduces the number of GFP-2xFYVE puncta with IC50 of 14 nM, induces a dose-dependent increase in levels of NCOA4 and p62; blocks autophagy in vitro and reduces xenograft growth of two breast cancer cell lines, MDA-MB-231 and MCF-7; also significantly potentiates cytotoxicity of Sunitinib and Erlotinib in MCF-7 and MDA-MB-231 in vitro.

Cyclizine is a piperazine first-generation antagonist of histamine 1 receptor.

MRS 1845 is a potent calcium channel protein inhibitor and inhibits capacitative Ca2+ influx in HL-60 cells (IC50 = 1.7 mM).

Guanabenz (WY 8678) is an α2 adrenergic receptor agonist that is used as an antihypertensive agent, also has been proposed to exert protective effects against misfolding by interfering with eIF2α-P dephosphorylation through selective disruption of a PP1-P

PI103 is a potent inhibitor with low IC50 values against recombinant PI3K isoforms p110alpha (IC50= 2 nM), p110beta (IC50= 3 nM), p110delta (IC50= 3 nM), and p110gamma (IC50= 15 nM), less potent to mTOR/DNA-PK with IC50 of 30 nM/23 nM.

J14 is a reversible sulfiredoxin inhibitor with an IC50 of 8.1 μM. J14 induces oxidative stress (intracellular ROS accumulation) by inhibiting sulfiredoxin, leading to cytotoxicity and cancer cell death.

The product is discontinued. DDD107498, also known as DDD 498, is a multiple-stage antimalarial agent that inhibits protein synthesis. DDD107498 demonstrates potential to address a variety of clinical needs, including single-dose treatment, transmission blocking and chemoprotection. DDD107498 was developed from a screening programme against blood-stage malaria parasites; its molecular target has been identified as translation elongation factor 2 (eEF2), which is responsible for the GTP-dependent translocation of the ribosome along messenger RNA, and is essential for protein synthesis. This discovery of eEF2 as a viable antimalarial drug target opens up new possibilities for drug discovery.

This product is discontinued. LTX-315 (Oncopore) is a synthetic 9-mer anticancer peptide that preferentially permeabilizes mitochondrial membranes, thereby causing partially BAX/BAK1-regulated, caspase-independent necrosis.

PT2977 (MK-6482) is an orally active and selective HIF-2α inhibitor with an IC50 of 9 nM. PT2977, as a second-generation HIF-2α inhibitor, increases potency and improves pharmacokinetic profile. PT2977 is a potential treatment for clear cell renal cell carcinoma (ccRCC)[1].

Tigecycline hydrate is a broad spectrum glycylcycline antibiotic. Tigecycline hydrate is bacteriostatic, that inhibits protein synthesis by binding to the 30S ribosomal subunit of bacteria and thereby blocking entry of Aminoacyl-tRNA into the A site of the ribosome during prokaryotic translation. Tigecycline hydrate is active against resistant strains of Gram-positive and Gram-negative bacteria.

PY-60 is a novel activator of YAP-dependent gene expression.It targets ANXA2 in the Hippo pathway. PY-60 targets ANXA2 to activate YAP[1]. PY-60, a thiazole-substituted derivative, dose-dependently induces luciferase activity in 293A-TEAD-LUC cells in the presence or absence of serum when cells were plated at high cell density (EC50= 1.5 and 1.6 µM, respectively). PY-60 treatment also dose-dependently promoted the association of YAP and TEAD proteins in cells and induced the nuclear localization of YAP in response to increased cell density. PY-60 robustly increases the levels of YAP-controlled transcripts (that is, ANRKD1, CYR61 and CTGF) in 293A cells and other human cell lines (that is, MCF10A, HEK293T, H69 and HaCaT), but did not augment the levels of YAP itself (YAP1)[1]. PY-60 activates a proproliferative, YAP-dependent transcriptional program in the adult animal capable of remodeling the epidermis through proliferation[1]. PY-60 liberates the ANXA2-YAP complex from the cell membrane and competes for ANXA2 binding of phosphoinositides[1]. PY-60 (10 uM; applied topically to the dorsal skin of wild-type adult C57BL/6 mice over the course of 10 days) promotes a dramatic expansion of keratinocytes and K14-positive precursors, as assessed by hematoxylin and eosin and anti-K14 histological staining at the study end. PY-60 results in an approximate doubling of epidermal thickness, a result derived from an increased number of keratinocytes per unit length of skin[1].

CG347B is a biochemical.

VV116, also known as JT001, is an oral drug candidate of nucleoside analog against SARS-CoV-2. VV116 is a deuterated, tri-isobutyrate ester prodrug of the RDV parent nucleoside, and is rapidly metabolized into the parent nucleoside (116-N1) in the body. 116-N1 is intracellularly converted to the nucleoside triphosphate active form, which would interfere with the function of RNA-dependent RNA polymerase of SARS-CoV-2, thus exerting antiviral effects (Fig. 1). VV116 showed potent activity against a panel of SARS-CoV-2 variants (alpha, beta, delta, and omicron) and excellent therapeutic efficacy in the mice model.

NNC 55-0396, Mibefradil derivative, is a highly selective T-type calcium channel blocker; displays IC50 values of 6.8 and > 100 μM for inhibition of Cav3.1 T-type channels and HVA currents respectively in INS-1 cells. IC50 value: 6.8 nMTarget: Cav3.1 T-type channelNNC 55-0396 can be an essential tool in preventing human ovarian cancer cell proliferation as a result of its ability to inhibit the function of T-type Ca2+ channels. It is believed that NNC 55-0396 may functions by dissolving in or passing through the plasma membrane of cells.

RO-3 is a potent, CNS-penetrant, and orally active P2X3 and P2X2/3 antagonist with pIC50s of 5.9 and 7.0 for human homomultimeric P2X3 and heteromultimeric P2X2/3 receptors, respectively. RO-3 shows selectivity for P2X3 and P2X2/3 over all other functional homomultimeric P2X receptors (IC50 >10 μM at P2X1,2,4,5,7)[1].

RO 46-8443 is the first non-peptide endothelin ETB receptor selective antagonist. RO 46-8443 displays up to 2000-fold selectivity for ETB receptors both in terms of binding inhibitory potency and functional inhibition. The observed parallel rightward shift of concentration-response curves with different antagonist concentrations is consistent with a competitive binding mode. Since R0 46-8443 selectively inhibits ETB receptor mediated responses, it is a valuable tool for clarifying the role of ETB receptors in pathology.

SB-649868 is a potent and selective orally active orexin (OX) 1 and OX2 receptor antagonist (pKi =9.4 and 9.5 at the OX1 and OX2 receptor, respectively).

OTS193320 (OTS-193320) is a potent inhibitor of protein methyltransferase SUV39H2 with IC50 of 22.2 nM.

BMX-IN-1 is a selective, irreversible inhibitor of bone marrow tyrosine kinase on chromosome X (BMX) that targets Cys496 in the BMX ATP binding domain with an IC50 of 8 nM, also targets the related Bruton’s tyrosine kinase (BTK) with an IC50 value of 10.4 nM, but is more than 47-656-fold less potent against Blk, JAK3, EGFR, Itk, or Tec activity.

SR-11237 is a selective pan retinoid X receptor (RXR) agonist with no retinoid A receptor (RAR) activity. .

Yakuchinone A, a natural product isolated from Alpinia oxyphylla Miquel (Zingiberaceae), has strong inhibitory effects on the synthesis of prostaglandins (PGs) and leukotrienes (LTs).

Humanin (human) (1-24-Protein humanin (human)), a small mitochondrial-derived cytoprotective polypeptide encoded by mtDNA, exhibits protective effects in several cell types against cellular stress conditions and apoptosis through regulating various signaling mechanisms, such as JAK/STAT pathway and interaction of BCL-2 family of protein.

IHMT-TRK-284 (Compound 34) is a potent, orally active type II TRK kinase inhibitor with IC50 values of 10.5, 0.7, and 2.6 nM to TRKA, B, and C respectively. IHMT-TRK-284 displays great selectivity profile in the kinome and good in vivo antitumor efficacies.

Chol-CTPP is a ligand with dual targeting effect on blood-brain barrier (BBB) and glioma cells. Lip-CTPP can be gained by Chol-CTPP and another mitochondria targeting ligand (Chol-TPP). Lip-CTPP is a promising potential carrier to exert the anti-glioma effect of doxorubicin (DOX) and lonidamine (LND) collaboratively. Lip-CTPP elevates the inhibition rate of tumor cell proliferation, migration and invasion, promote apoptosis and necrosis, and interfere with mitochondrial function.

Antiproliferative against-4 (comp 4) shows the highest potency for MCF-7 cells (IC50 = 0.19 nM).

LY393558 is a potent and orally active inhibitor of the 5-HT transporter and an antagonist of 5-HT1B and 5-HT1D receptors. LY393558 increase the extracellular levels of 5-HT in mice model frontal cortex. LY393558 can be used for researching depression.

Letosteine is an orally active, potent and safe expectorant. Letosteine dissolves bronchial mucus and reduces respiratory inflammation symptoms, and restores gas exchanges and natural defense mechanisms in the lung. Letosteine can be used for acute or chronic respiratory diseases (such as bronchopneumopathies) research.

Fluocortin butyl ester is a developed corticosteroid compound with no detectable systemic corticosteroid activity when it is used topically. Fluocortin butyl ester appears to be an effective well-tolerated topical steroid useful in the research of perennial rhinitis.

SAH-13C5 (SAH (S-Adenosylhomocysteine)-13C5) is the 13C-labeled SAH. SAH (S-Adenosylhomocysteine) is an amino acid derivative and a modulartor in several metabolic pathways. It is an intermediate in the synthesis of cysteine and adenosine. SAH is an inhibitor for METTL3-METTL14 heterodimer complex (METTL3-14) with an IC50 of 0.9 µM.