Jun15799 is an Enterovirus (EVs) 2C protein (EVs 2C) inhibitor with Kis of 0.8, 21.1 and 3.0 μM for EV-D68, EV-A71 and CVB3, respectively. Jun15799 has a significant antiviral activity against EV-D68 US/MO/14-18947, EV-A71 Tainan/4643/1998 and CVB3 Nancy cells (EC50s of 0.3, 11.4 and 0.3 μM, respectively). Jun15799 can be used for viral infections research, such as meningitis, hand, foot and mouth disease (HFMD) and viral myocarditis.

G923-0271 is a TDP-43 protein inhibitor. G923-0271 can be used for the research of neurological disease, such as Alzheimer's Disease.

MBL-II-141 is potent ABCG2 inhibitor with an IC50 of 0.11 μM. MBL-II-141 inhibits the transport function of ABCG2 in a non-competitive manner, preventing ABCG2 from pumping substrates (such as Irinotecan) out of the cells, thereby increasing the accumulation of drugs within the cells. MBL-II-141 has no effect on ABCB1 (P-gp) and ABCC1 (MRP1) and has extremely low cytotoxicity (IG50 > 100 μM). MBL-II-141 can be used for the study of multidrug resistance (MDR) cancers.

Y-20811 (sodium) is a selective and orally active thromboxane synthetase inhibitor. Y-20811 (sodium) can irreversibly inhibit thromboxane (TX) A2 synthesis. Y-20811 (sodium) can be used for the research of cardiovascular disease, such as thrombosis.

DPC423 free base is a selective and orally active factor Xa inhibitor with a Kis of 0.15 (human) and 0.3 (rabbit) nM. DPC423 free base exhibits Kis of 60, 61 and 6000 nM against human trypsin, plasma kallikrein and thrombin. DPC423 free base blocks the formation of prothrombinase complex, reduces thrombin production, inhibits fibrin formation and platelet activation. DPC423 free base has demonstrated antithrombotic effects in animal models, and when used in combination with Aspirin, it shows a strong synergistic effect. DPC423 free base can be used for the study of anticoagulation of arterial thrombosis.

SL-870495 is a calcium antagonist targeting L-type calcium channels. SL-870495 is promising for research of cardiovascular diseases such as hypertension and angina pectoris.

SLV-317 (free base) is an antagonist of the neurokinin-1 receptor with oral activity. SLV-317 (free base) can effective antagonist of substance P-induced effects.

CDD-1132 (Compound 8) is a potent inhibitor of BRDT-BD2. CDD-1132 has an IC50 of 13 nM against BRDT-BD2. CDD-1132 can be studied in research on nonhormonal contraceptive agent.

Jun15716 is an Enterovirus (EVs) 2C protein (EVs 2C) inhibitor with Kis of 15.9, 44.2 and 17.8 μM for EV-D68, EV-A71 and CVB3, respectively. Jun15716 has a potent antiviral activity against EV-D68 US/MO/14-18947 and CVB3 Nancy cells (EC50s of 1.0 and 0.7 μM, respectively). Jun15716 can be used for viral infections research, such as meningitis, hand, foot and mouth disease (HFMD) and viral myocarditis.

FL-166 is a SARS coronavirus main protease (Mpro) inhibitor (Ki: 40 nM). FL-166 exerts its inhibitory effect by targeting a cluster of serine residues near the active site of the protease. FL-166 can be used in the study of SARS-CoV.

KL1333 hydrochloride is an orally active NAD+ modulator that reacts with NAD(P)H:quinone oxidoreductase 1 (NQO1) as a substrate, leading to increased intracellular NAD+ levels through NADH oxidation. Elevated NAD+ levels trigger activation of SIRT1 and AMPK, and subsequently activate PGC-1α. KL1333 hydrochloride improves energy metabolism and mitochondrial dysfunction in mitochondrial encephalomyopathy, lactic acidosis, and stroke-like episodes (MELAS) fibroblasts. KL1333 hydrochloride protects against cisplatin-induced ototoxicity in mouse cochlear cultures.

KF-20444 is an orally active ALK inhibitor with blood-brain barrier penetration. KF-20444 exhibits strong inhibitory activity against ALK fusion proteins (EML4-ALK) and ALK resistance mutations (including L1196M, G1202R, and F1174L). KF-20444 effectively suppresses the phosphorylation of ALK in ALK-driven cancer cell lines, thereby inhibiting cancer cell proliferation and inducing apoptosis. KF-20444 demonstrates anti-tumor efficacy in mouse models bearing ALK-positive non-small cell lung cancer (NSCLC) or neuroblastoma. KF-20444 can be used for the study of ALK-driven malignancies.

KC-764 is an orally active, reversible cyclooxygenase inhibitor with relative selectivity for platelet cyclooxygenase. KC-764 inhibits platelet thromboxane A2 (TXA2) production and platelet aggregation, with IC50s of 0.23 μM and 26 nM, respectively. KC-764 can be used for the research on antiplatelet and recurrence prevention in ischemic stroke.

MG-3C is a potent matrix metalloproteinase 9 (MMP-9) inhibitor. MG-3C can selectively kill non-small-cell lung cancer (NSCLC) cells harboring the EGFR T790M mutation. MG-3C blocks the EGFR/STAT3 signaling pathway, inducing G2/M phase arrest, growth inhibition, and apoptosis of cancer cells. MG-3C is promising for research of lung cancer.

UC-84 (NSC-615985) is a non-nucleoside reverse transcriptase inhibitor (NNRTI) with anti-HIV activity.

BMS 183920 is a diacidic and potent angiotensin II receptor antagonist, with a Ki value of 2.9 nM in the rat adrenal cortex binding assay and a KB value of 0.061 nM in the rabbit aorta functional assay. BMS 183920 can be used for research of antihypertensive.

Y-20024 (hydrochloride) is an orally active D2 receptor antagonist with blood-brain barrier permeability. Y-20024 can inhibit Apomorphine-induced ADHD in mice. Y-20024 can inhibit Apomorphine-induced vomiting in dogs. Y-20024 has prolactin-promoting activity. Y-20024 can be used in research on neurological disorders such as ADHD and vomiting.

RPX 7546 is a potent inhibitor of metallo-𝛽-lactamases (MBLs) with IC50 values of 1.4 and 48 μM for IMP-1 and IMP-78, respectively. RPX 7546 has antibacterial activity.

BRI-12349 (Compound 50) is a dual antagonist of CysLT1R/CysLT2R with Ki values of 1.03 and 6.46 μM. BRI-12349 can inhibit the generation of IP1 induced by LTD4 (the main ligand of CysLTs). BRI-12349 can be used for the research of immunology and inflammation, such as asthma.

MLS6357 is a D3 dopamine receptor (D3R)-selective positive allosteric modulator (PAM)-antagonist. MLS6357 exhibits antagonist activity in the D3R-mediated and the BRET-based β-arrestin recruitment assay with IC50s of 13 and 14 μM, and no activity for other DAR subtypes (D1R/D2R/D4R/D5R) (IC50 > 100 μM). MLS6357 is also an antagonist in the D3R-mediated Go-BRET assay with an IC50 of 17 μM. MLS6357 can be used for the study of neuropsychiatric disorders, including substance use disorder.

sGC stimulator 1 is a carbonyl sulfide (COS)/H2S-donor hybrid soluble guanylyl cyclase (sGC) stimulator (EC50 = 496 nM). sGC stimulator 1 exhibits a well-characterized H2S-releasing property. sGC stimulator 1 reduces fibrosis in TGF-β1-treated cardiac fibroblasts by increasing cGMP and H2S levels. sGC stimulator 1 can exert anti-fibrotic effects by activating sGC and increasing H2S. sGC stimulator 1 can be used for the study of heart failure (HF).

AG-12275 is a cyclin-dependent kinase (CDK) inhibitor. AG-12275 can be used for the research of cancer.

Ifebemtinib (tosylate) (BI-853520 (tosylate); IN-10018 (tosylate)) is a highly selective PTK2 kinase inhibitor. Ifebemtinib (tosylate) demonstrates anti-tumor activity. Ifebemtinib (tosylate) inhibits FAK autophosphorylation in prostate carcinoma cells. Ifebemtinib (tosylate) can inhibit spheroid formation and orthotopic tumor growth in vivo. Ifebemtinib (tosylate) can be studied in anticancer research such as solid tumors, breast cancer, and malignant pleural mesothelioma.

KP 736 (sodium) is a broad-spectrum antibacterial agent. KP 736 (sodium) exhibits excellent broad-spectrum anti Gram negative bacterial activity in vitro, especially effective against Pseudomonas aeruginosa and multiple drug-resistant bacteria. KP 736 (sodium) can be used for research on bacterial infections.

ZK-813039 is a potent and orally active factor Xa inhibitor. ZK-813039 can prolong prothrombin time. ZK-813039 can be used for the research of cardiovascular disease.

MDI-117740 is a dual LIMK1/2 inhibitor. MDI-117740 shows effective cellular target engagement with LIMK1 (pIC50 = 6.73) and LIMK2 (pIC50 = 7.18) in HEK293 cells. MDI-117740 exerts significant anti-migratory activity in MDA-MB-231 cells. MDI-117740 can be used for the study of diseases associated with LIMK dysregulation, such as cancers and neurodegenerative disorders.

PSB-1737 is a human-selective GPR17 agonist with an EC50 for human GPR17 of 27 nM, and its activity on murine GPR17 is relatively weak (EC50 > 10 μM). PSB-1737 shows no significant inhibition at the glycine binding site of NMDA receptors, and has no significant agonistic or antagonistic activity on P2Y receptor subtypes. PSB-1737 can be used in demyelinating diseases (such as multiple sclerosis) or inflammatory-related anemia.

Illudinine, a sesquiterpenoid alkaloid, is a monoamine oxidase B (MAO-B) inhibitor with an IC50 of 18.3 μM. Illudinine can be used for research on neurological diseases.

(Rac)-MK 0686 is the racemate of MK 0686. MK 0686 is a bradykinin B1 receptor antagonist.

LIBX-A402 (Compound 15b) is a selective ACSL4inhibitor with an IC50 of 0.33  μM. LIBX-A402 significantly protects MDA-MB-231 and LUHMES cells from ferroptosis. LIBX-A402 can be used for cancer, ischemia-reperfusion injury and neurodegenerative diseases like Parkinson’s disease research.