K2V-9 is an AChE and MAO-B inhibitor with IC50 values of 1.72 μM and 0.950 μM against AChE and MAO-B, respectively. K2V-9 inhibits amyloid β self-aggregation and reduces ROS. K2V-9 has neuroprotective effects.

RDS-04-010 is an atypical dopamine transporter (DAT) inhibitor. RDS-04-010 has the effect of inhibiting cocaine intake and seeking behavior. RDS-04-010 exerts its modulatory effect mainly by binding to the inward conformation of DAT, thereby reducing the reinforcing effect of cocaine. RDS-04-010 can be used in the study of cocaine use disorder (CUD).

Pan-KRAS ligand 3 is a pan-KRAS inhibitor. Pan-KRAS ligand 3 can be used for synthesis of PROTAC pan-KRAS degrader-1.

Naperiglipron (LY3549492) (Example 2) is a Glucagon-like peptide 1 receptor (GLP-1R) agonist with an EC50 of 1.14 nM for hGLP-1R. Naperiglipron significantly decreases the level of blood glucose in GLP-1R knock-in mouse models. Naperiglipron inhibits PDE10A1 enzyme activity (IC50: 7.43 μM) with a weak hERG inhibitory activity. Naperiglipron can be used for type II diabetes mellitus (T2DM) and obesity research.

MK-5108-NH-PEG2-alkyne is a Aurora kinase A (AURKA) inhibitor. MK-5108-NH-PEG2-alkyne can be used for synthesis of PROTAC AURKA degrader 1.

Photosensitizer-7 is a endoplasmic reticulum (ER)-targeted photosensitizer (PS) (λab = 610 nm, λem = 622 nm). Photosensitizer-7shows an IC50 of 4.006 μM in HeLa cells and 3.28 μM in MCF-7 cells under light irradiation. Photosensitizer-7 exhibits dose-dependent cellular uptake and predominant colocalization with ER. Photosensitizer-7 induces dose-dependent intracellular ROS generation, reduces mitochondrial membrane potential, and increases apoptosis upon light irradiation in cells. Photosensitizer-7 significantly inhibits tumor growth in MCF-7 tumor-bearing mice. Photosensitizer-7 can be used for the study of photodynamic anticancer applications.

endo-S-cGAFMP (Compound 3) is a STING agonist. endo-S-cGAFMP induces the production of interferon regulatory factors and proinflammatory cytokines by activating the cGAS-STING pathway, thereby enhancing innate and adaptive immune responses. endo-S-cGAFMP has potent immunostimulatory capacity in THP1 monocytes and RAW macrophages (EC50 values of 2.45 μM and 5.54 μM, respectively). endo-S-cGAFMP has significant antitumor activity. endo-S-cGAFMP can be used as a potential cancer immunotherapeutic agent, especially for studies of systemic administration.

A-228839 is a potent farnesyltransferase inhibitor. A-228839 inhibits lymphocyte activation and cytokine production.

DL-017 is a Quinazoline derivative. DL-017 shows inhibitory constants of approximately 0.90 nM for α1-adrenergic receptors and 404 nM for Na+ channels. DL-017 exerts antihypertensive effect.

T-01-C7-amide is an E3 ligase ligand-linker conjugate. T-01-C7-amide can be used in the synthesis of PROTAC BRD4 Degrader-36.

TRK-530 sodium is an orally active bisphosphonate. TRK-530 sodium inhibits CINC-1. TRK-530 sodium inhibits dental calculus formation. TRK-530 sodium also inhibits paw edema, joint destruction and osteomyelitis.

CP-5068is a cell wall inhibitor that can be used for the study of infectious diseases.

Alanycarb (OK-135) is a broad-spectrum oxime carbamate insecticide with contact and oral toxicity. Alanycarb is effective against a wide variety of insect pests and is a pro-insecticide. The principal active molecule produced by the biological modification of Alanycarb within target organisms is methomyl.

Cystemustine is a DNA inhibitor (a chloroethyl nitrosourea, CENU). Cystemustine can cause DNA cross-linking, thereby inhibiting the proliferation of tumor cells. Cystemustine can also exert cytotoxic effects by interfering with the cell cycle, inducing cell re-differentiation, and altering phospholipid metabolism. Cystemustine exhibits high anti-tumor activity and a relatively short plasma half-life in mice. Cystemustine can be used for the study of various malignant tumors, including melanoma, glioma, renal cancer, head and neck cancer, and colorectal cancer, etc.

T 162559 is a potent and selective inhibitor of the Na+/H+ exchanger isoform NHE1 with IC50 values of 0.96 nM. T 162559 does not affect Na+/HCO3- cotransport and Na+/Ca2+ exchange. T 162559 can be used for the research of cardiovascular disease.

(R)-Pirlindole mesylate is selective and reversible a Monoamine oxidase A (MAO-A) inhibitor with an IC50 of 0.43  μM for MAO-A over MAO-B. (R)-Pirlindole mesylate has an antidepressant activity. (R)-Pirlindole mesylate significantly decreases immobility time of the forced swim test and inhibits Reserpine-induced palpebral ptosis in behavioural mice models. (R)-Pirlindole mesylate can be used for depression research.

RG7109 is an inhibitor of HCV NS5B polymerase. RG7109 has EC50 values of 1.1 nM and 1.0 nM for HCV GT-1a H77 and GT-1b Con1, respectively. RG7109 exhibits favorable pharmacokinetic properties and can be used in anti-HCV research.

BMS-210285 is a highly selective agonist for the β3 receptor. BMS-210285 can be studied for obesity and type 2 diabetes research.

Apicidin C (Compound 5a) is a cyclic tetrapeptide. Apicidin C has an antiprotozoal and antimalarial activity against Eimeria tenella (IC50: 6 nM) by reversibly inhibiting HDAC acyivity. Apicidin C can be used for malaria infections research.

4-(3-Tosyl-2-(tosylmethyl)propanoyl)benzoic acid-glu(PEG24-Me)-val-cit-NH-benzyloxyformic acid-MMAE is a drug-linker conjugate for ADC. 4-(3-Tosyl-2-(tosylmethyl)propanoyl)benzoic acid-glu(PEG24-Me)-val-cit-NH-benzyloxyformic acid-MMAE contains a linker and bioactive small molecule toxins MMAE. 4-(3-Tosyl-2-(tosylmethyl)propanoyl)benzoic acid-glu(PEG24-Me)-val-cit-NH-benzyloxyformic acid-MMAE can conjugate with NN2101 (anti c-Kit) for synthesizing NN3201. NN3201 rapidly internalizes and inhibits SCF-driven signaling, thereby delivering its payload to induce cell cycle arrest and apoptosis. NN3201 exhibits significant c-Kit-dependent anti-tumor efficacies in various tumor models, such as small cell lung cancer (SCLC) and gastrointestinal stromal tumor (GIST).

SHY-855 is a pan RAS inhibitor. SHY-855 effectively prevents the binding of K-Ras proteins and other members of the Ras superfamily of small GTPases with IC50 values of 0.3-5 μM. SHY-855 effectively inhibits the phosphorylation of MEK, ERK1/2, and AKT downstream of K-Ras. SHY-855 inhibits the formation of the Ras-GTP activity complex. SHY-855 can be used to the studies of pancreatic cancer and non-small cell lung cancer.

CB2R ligand-1 (Compound L14) is a selective Cannabinoid type 2 receptor (CB2R) ligand with a with Ki of 0.16  nM for CB2R over CB1R. CB2R ligand-1 as be used as a tracer for positron emission tomography (PET) imaging of neurodegenerative diseases, inflammation and cancer.

Rodin-B is a selective histone deacetylase (HDAC)-co-repressor of repressor element-1 silencing transcription factor (CoREST) complex inhibitor with an IC50 value of 0.50 μM for the CoREST complex, 0.27 μM for HDAC1, and 0.28 μM for HDAC2. Rodin-B increases the acetylation level of histone H3K9, upregulates the expression of neuron-related genes, thereby promoting the increase in dendritic spine density, the colocalization of synaptic proteins (SV2A and PSD95), and the improvement of hippocampal long-term potentiation (LTP), exerting synaptic protection and repair activity. Rodin-B is promising for research of neurodegenerative diseases related to synaptic dysfunction, especially Alzheimer’s disease.

BMS-577098 is an orally active and ATP-competitive insulin-like growth factor-1 receptor (IGF-1R) inhibitor with an IC50 of 0.016 μM. BMS-577098 shows anti-tumor effect.

UK-315716 is an NMDA receptor antagonist. UK-315716 has a synergistic neuroprotective effect. UK-315716 can be used for research on neurological diseases such as stroke and headache.

FCE-25199 is a novel oral penem antibiotic. FCE-25199 has antibacterial activity against various Gram positive and Gram negative bacteria. FCE-25199 is commonly used in the study of bacterial infections.

SIB 1663 is a conformationally restricted analog of nicotine. SIB-1663 selectively activatedα2β4 and α4β4 human recombinant neuronal nAChRs. SIB 1663 can increase DA and NE release. SIB 1663 can be used for the research of neurological disease.

CP-100356 is an orally active dual MDR1 (P-gp)/BCRP inhibitor, with an IC50s of 0.5 and 1.5 µM for inhibiting MDR1-mediated Calcein-AM transport and BCRP-mediated Prazosin transport, respectively. CP-100356 is also a weak inhibitor of OATP1B1 (IC50 = ∼66 µM). CP-100356 is devoid of inhibition against MRP2 and major human P450 enzymes (IC50 > 15 µM).

UVI3502 is a cannabinoid receptor 1 (CB1) antagonist with an IC50 value of 4641 nM for CB1 and approximately 16200 nM for CB2. UVI3502 blocks Gi/o protein coupling induced by the agonist CP55,940. UVI3502 is promising for research of endocannabinoid system-related diseases in the central nervous system (such as cognitive impairment and neurodegenerative diseases).

G9D-4 (TFA) is a potent PROTAC degrader of G9a, with the DC50 value of 0.1 μM in PANC-1 cells and do not directly perturb GLP protein, with the DC50 of ＞10 μM. G9D-4 (TFA) plays an important role in pancreatic cancer research.