TD-6301 is a bladder-selective M2/4 muscarinic receptor antagonist. TD-6301 binds to and blocks M2/4 muscarinic receptors with high selectivity, especially human M2 receptors with strong affinity (Ki = 0.36 nM). TD-6301 inhibits volume-induced bladder contractions (ID50 = 0.075 mg/kg). TD-6301 can be used in the research of overactive bladder.

BC264 is a highly potent and selective CCK-B agonist that crosses the blood-brain barrier. BC264 increases dopamine in the nucleus accumbens and facilitates motivation and attention in rats.

Mal-G(PEG8-Me)-AAN-NH2 is a linker of the drug conjugate QHL-1618. QHL-1618 has anti-tumor activity.

Ledasorexton (Example 1 ) is an orally active OX2R agonist (EC50: 0.99 nM). Ledasorexton has awakening effect.

BP 554 is a selective 5-HT1A receptor agonist and Piperazine derivative. BP 554 leads to hypothermia.

Guanidino ethyl disulfide (GED) (Compound 23) is a NO Synthase (NOS) inhibitor with EC50s of 110, 630 and 180  μM for iNOS, eNOS and bNOS, respectivly. Guanidino ethyl disulfide effectively inhibits nitrite production in J774.2 macrophages. Guanidino ethyl disulfide can be used for circulatory shock, inflammation and neurological diseases research.

S-0636 is a novel glutamyl cyclase (QC) inhibitor characterized by high selectivity, low cytotoxicity, and difficulty in inducing drug resistance. S-0636 can effectively inhibit the virulence factors of P. gingivalis. S-0636 can be used for research on bacterial infections.

DX-9065a (free base) is a selective, nonpeptidic, and orally active factor Xa (FXa) inhibitor with a Ki of 41 nM for human FXa. DX-9065a (free base) has low activity against other serine proteases. DX-9065a (free base) has strong anticoagulant actions.

NAPAP is a thrombin inhibitor. It has potent antithrombin activity (Ki: 2.1 nM). NAPAP selectively inhibits thrombin via a rapid binding mechanism, and has weaker inhibitory effects on trypsin, factor Xa, and plasmin. NAPAP can be used in the study of thrombotic diseases (e.g., venous thrombosis, myocardial infarction).

SRI 31215 is a Matriptase/Hepsin/hepatocyte growth factor activator (HGFA) triplex inhibitor and mimics the activity of HAI-1/2 (endogenous inhibitors of HGF activation). SRI 31215 has potent inhibitory activity against matriptase, hepsin and HGFA with IC50 values of 0.69 μM, 0.65 μM and 0.30 μM, respectively. SRI 31215 can be used for the research of cancer.

APC8696 is a reversible uPA inhibitor, with a Ki of 8 nM.

Exatecan-3-amine is an effective exatecan derivative. Exatecan-3-amine can be connected to monoclonal antibodies via linkers to form antibody-drug conjugate (ADC) molecules. Exatecan-3-amine is often combined with CLDN6 mAb to form ADC drugs for the study of tumors with high expression of CLDN6.

PENAO TFA is the trifluoroacetic acid of PENAO. PENAO is a potent tumour cell mitochondrial toxin. PENAO inactivates tumor cell mitochondria by targeting inner-membrane adenine nucleotide transferase.

NBTI 5463 is a bacterial type II topoisomerases (topoisomerase II) inhibitor with antibacterial activity. NBTI 5463 inhibits GyrA and TopoIV in Pseudomonas aeruginosa and Escherichia coli. NBTI 5463 binds to topoisomerase II to prevent DNA cleavage and religation, inhibiting bacterial DNA replication and transcription. NBTI 5463 is promising for research of Gram-negative bacterial infection.

Neomycin C hexaacetate, a tetracyclic antibacterial agent, is a major active isomeric components of the Neomycin complex. Neomycin, is a 2-DOS-containing aminoglycoside, consisting of Neomycin A, Neomycin B, and Neomycin C.

Lyso-monosialoganglioside GM2 (LysoGM2) ammonium is a lysosphingolipid and protein kinase C inhibitor (IC50: 50 μM). Lyso-monosialoganglioside GM2 ammonium can inhibit the binding of protein kinase C to Phorbol 12,13-dibutyrate. Lyso-monosialoganglioside GM2 ammonium is a specific biomarker for GM2 gangliosidosis. Lyso-monosialoganglioside GM2 ammonium can be used in the research of sphingolipidoses.

ZJS178 is a novel inhibitor of myosin I. ZJS178 is a fungicide that has inhibitory activity against Fusarium graminearum and can reduce DON toxin synthesis. ZJS178 can be used for research on plant diseases such as wheat scab.

BMS-182264 is a highly selective ATP-sensitive potassium channel agonist. BMS-182264 promotes potassium efflux and membrane hyperpolarization to induce smooth muscle relaxation and vasodilation. BMS-182264 is promising for research of cardiovascular diseases such as hypertension and myocardial ischemia.

KI 1769 is a potassium channel opener. KI 1769 can exhibit vasodilating effect. KI 1769 prolongs the micturition interval and reduces the resistance to fluid infusion through the urethral lumen. KI 1769 can be used for the research of cardiovascular disease.

ICP-103 (Compound 3K) is a highly selective protein kinase C (PKC) inhibitor with an IC50 of 30 nM. ICP-103 is promising for research of cancers.

Z56 is a Ras protein inhibitor. Z56 can be used for the research of cancer, such as pancreatic cancer.

Tanerasertib (Compound 456) is an AKT1 inhibitor with an IC50 of less than 15 nM against AKT1 E17K. Tanerasertib can be used in the study of cancer.

MCL1020 is a CHK1 inhibitor with an IC50 of 1.61 μM. MCL1020 properly occupies the ATP pocket by interacting with a diverse range of the sites of CHK1 kinase. MCL1020 can be used for the study of hematologic malignancies.

SKS-927 is a Src kinase inhibitor, with an IC50 value of 3.9 nM. SKS-927 inhibits the proliferation of Src-transformed rat fibroblasta, with an IC50 value of 73 nM. SKS-927 exhibits an IC50 value of 720 nM against EGFR. SKS-927 can be used for the study of cancer and osteoporosis.

EMD 86006 is a candidate for selective serotonin inhibitors. EMD 86006 has the potential for research on depressive disorders.

CGP-79807 is a purine-based CDK inhibitor. CGP-79807 can block the cell cycle by inhibiting CDK activity to suppress the proliferation of tumor cells. CGP-79807 can be used in the study of cancer.

NPH16 is an orally active PD-1/PD-L1 inhibitor with an IC50 of 24.4 nM. NPH16 can promote HepG2 cell apoptosis. NPH16 shows excellent in vivo antitumor efficacy and favorable pharmacokinetic properties. NPH16 can be used for the study of liver cancer.

c-Met ligand-Linker Conjugate 2 is a synthesized target protein ligand-linker conjugate that can be used for synthesis of PROTACs, such as PROTAC c-Met degrader-6. PROTAC c-Met degrader-6 is a c-Met PROTAC degrader with anti-tumor activity[1].

TR-213 is a potent molecular glue degrader that targets Cyclin K (CDK). TR-213 induces 91% and 56% decrease in CDK12 and Cyclin at 1 μM. TR-213 can inhibit RNA polymerase II activity and regulates alternative polyadenylation (APA) activity. TR-213 can be used for the research of cancer.

SGC-CK1γ-1 is a potent and selective probe for the CK1γ subfamily. SGC-CK1γ-1 can inhibit LRP6 phosphorylation levels. SGC-CK1γ-1 can selectively inhibit the CK1γ kinases in living cells and inhibit both WNT signaling and human cytomegalovirus (CMV) replication. SGC-CK1γ-1 can be used for the research of infection.