CB 3705 is a dihydrofolate reductase (DHFR) and thymidylate synthetase (TS) inhibitor. CB 3705 inhibits L1210 cells and mutant L1210 cell line (L1210:C15) with ID50s of 4.77 μM and 408 μM, respectively.

EMD527040 (hydrochloride) is a highly potent and selective αvβ6 antagonist with anti-fibrotic activity. EMD527040 (hydrochloride) is used in the research of liver cancer and liver fibrosis.

DS21412020 is a fluoroquinolone antibacterial agent. DS21412020 inhibits bacterial DNA gyrase (GyrA) and topoisomerase IV, leading to DNA breaks. DS21412020 exhibits significant activity against Gram-positive bacteria such as Staphylococcus aureus (MIC = 0.006 μg/mL), Streptococcus pneumoniae (MIC = 0.05 μg/mL), and Methicillin)-resistant Staphylococcus aureus (MIC = 0.2 μg/mL), and Gram-negative bacteria such as Escherichia coli (MIC = 0.006 μg/mL) and Pseudomonas aeruginosa (MIC = 0.78 μg/mL). DS21412020 significantly reduces bacterial load in mouse pneumonia and MRSA infection models. DS21412020 can be used in the development of next-generation quinolone antibiotics.

APL-5125 (Compound 61f) is a potent, selective and orally active ATP-competitive CK2α inhibitor with an IC50 of 0.348 nM and a Ki of 0.095 nM. APL-5125 binds to CK2α in a bivalent manner, simultaneously interacting with the ATP-binding site and the αD pocket. APL-5125 exhibits antitumor activity and can be used for the research of cancer, such as colon cancer.

GA-0056 is an angiotensin II receptor blocker. GA-0056 can be used in the research of heart disease.

UK-356202 is a urokinase-type plasminogen activator (uPA) with a Ki value of 0.037 μM. UK-356202 can be used in research related to the topical treatment of chronic ulcerous wounds.

ABT-255 hydrochloride is an orally active anti-bacterial agent. ABT-255 hydrochloride exhibits potent in vitro potency (MIC = 0.016-0.031 μg/mL) against drug-susceptible and Rifampin- or Ethambutol-resistant Mycobacterium tuberculosis. ABT-255 hydrochloride shows efficacy against S. aureus, S. pneumoniae and E. coli and reduces viable counts of drug-resistant Mycobacterium tuberculosis in CF-1 mice. ABT-255 hydrochloride can be used for the study of pulmonary tuberculosis.

MRS4917 is an orally active, potent selective P2Y14 receptor (hP2Y14R) antagonist (IC50 = 2.88 nM, Ki = 1.67 nM) that shows >18,000 fold selectivity against P2Y6R (IC50 = 54 μM). MRS4917 demonstrates oral efficacy in reversing established mechanoallodynia in the chronic constriction injury (CCI) mouse model, while having no effect on thermoregulation. MRS4917 can be used for neurological diseases research.

AJI-9561 is a benzoxazole derivative produced by Streptomyces sp. AJI-9561 exhibits cytotoxicity and antibacterial activity. AJI-9561 inhibits the proliferation of Jurkat T cells and mouse P388 leukemia cells, with its IC50 being 0.88 and 1.63 μM respectively. AJI-9561 can be used for research on anti-cancer and antibacterial properties.

FR-158999 is a potent orally active fibrinogen inhibitor. FR-158999 exhibits potent anti-platelet activities with a pIC50 of 7.50. FR-158999 can be used for antithrombotic research.

BMS-180431 is an inhibitor of HMG-CoA reductase (IC50: 43 nM).

ZD 2486 is a glycoprotein IIb/IIIa (GP IIb/IIIa) antagonist. ZD 2486 inhibits platelet aggregation by blocking the binding of fibrinogen to the GP IIb/IIIa receptor on platelets. ZD 2486 can be used for the study of conditions related to unwanted platelet aggregation, such as acute coronary syndrome, unstable angina pectoris, acute myocardial infarction, and complications from cardiovascular interventional procedures[1]

HCV-371 is a highly selective, potent, and low cytotoxicity HCV NSSB (EC50 = 4.8-6.1 μM) polymerase allosteric inhibitor. HCV-371 can be used for research on hepatitis C virus infection.

(R,R)-dWIZ-1 TFA is the the (R,R)-enantiomer of dWIZ-1. dWIZ-1 is a potent WIZ molecular glue degrader. dWIZ-1 has the potential for the research of sickle cell disease (SCD).

Perfluoroenanthic acid (Perfluoroheptanoic acid) is a type of perfluoroalkyl substance (PFAS) that can negatively impact the development of seminiferous tubules and m6A RNA methylation in the testes of offspring mice when exposed during pregnancy, consequently disrupting spermatogenesis and leading to reproductive toxicity. Perfluoroenanthic acid alters the morphology of dendritic spines and synaptic formation in primary cortical neuron cultures, enhancing neuronal activity and synaptic transmission, and increasing the expression of excitatory synapse-related proteins Synaptophysin and PSD95.

ONO-2570366 (Compound 11a) is an antagonist of the cysteinyl leukotriene receptors CysLT1R and CysLT2R (IC50 = 14 nM). ONO-2570366 inhibits the binding of LTD4

J-104132 (L-753037) is a potent, orally active, selective and competitive ETA/ETB receptor antagonist with Ki of 0.034 nM for ETA and 0.104 nM for ETB receptors. J-104132 inhibits Endothelin-1 (ET-1)-induced signaling and vascular contractions in vitro. J-104132 alleviates hypertension, vascular remodeling, and diabetic endothelial dysfunction in vivo by dual ETA/ETB blockade. J-104132 can be used for research on diabetic vascular complications[1][3].

BQ-610 is a selective antagonist of the endothelin A receptor (ETA receptor). BQ-610 specifically blocks the ETA receptor, competitively inhibiting the binding of endothelin-1 (ET-1) (a vasoconstrictive peptide) to the receptor, thereby blocking the effects of ET-1 such as vascular smooth muscle contraction, cell mitosis, and inhibition of hormone secretion. BQ-610 significantly alleviates cerebral vasospasm in rabbits. BQ-610 blocks the bronchial epithelial and pulmonary vascular cell proliferation caused by cigarette smoke in rat models. BQ-610 can delay the natural luteal regression in the cow's uterus. BQ-610 can be used for research on vasospasm, abnormal cell proliferation, and reproductive endocrine disorders.

NGD 94-1 (dimaleate) is a potent and selective dopamine D4 receptor antagonist. NGD 94-1 (dimaleate) shows high affinity for the cloned human D4.2 receptor (Ki = 3.6 nM). NGD 94-1 (dimaleate) modulates the cognitive functions of the frontostriatal system and regulates dopaminergic transmission in Phencyclidine (PCP)-induced monkeys. NGD 94-1 (dimaleate) can be used for neurological disease research[1][2].

BMS-505130 (fumarate) is a potent, selective and orally active serotonin transport inhibitor with a Ki for binding to the serotonin transporter of 0.18 nM (Ki for norepinephrine and dopamine transporters of 4.6 and 2.1 μM, respectively). BMS-505130 (fumarate) can be used for the research of neurological disease, such as depression.

UNC7437 is a inositol phosphate multikinase (IPMK) inhibitor, with an IC50 value of 26.2 nM. UNC7437 exhibits anti-proliferative activity against glioblastoma cells. UNC7437 decreases the accumulation of InsP4, InsP5, and InsP6 in cells. UNC7437 can be used for the study of TEN-negative glioblastoma models.

BRL-26830A is a β-adrenergic receptor agonist. In obese mouse models, BRL-26830A reduces body weight and increases metabolic rate. BRL-26830A stimulates insulin release and significantly reduces blood glucose levels in ICR mouse models. BRL-26830A can be used to study endocrine and metabolic diseases such as obesity and diabetes.

KW-5092 (fumarete) is a gastrokinetic agent. KW-5092 (fumarete) can increase intraluminal 5-HT release via the stimulation of cholinergic neurons .

9-cis-UAB30 is a rexinoid agonist. 9-cis-UAB30 significantly decreases the proliferation, viability, and motility of both patient-derived xenografts (PDXs). 9-cis-UAB30 induced cell-cycle arrest as demonstrated by the significant increase in the percentage of cells in G1 and a decrease in the percentage of cells in S phase by downregulating SKP2 and/or 20S proteasome activity, which leads to increased p27kip1 protein stability. 9-cis-UAB30 downregulates the abundance of stem cell marker mRNAs (Oct4, Nanog, Sox2, nestin) and upregulates the abundance of differentiation marker mRNAs (β3-tubulin, NSE, HOXC9, GAP43). 9-cis-UAB30 has no adverse effects on the central nervous system and cardiovascular system at the tested dose. 9-cis-UAB30 can be used for the study of neuroblastoma, cutaneous T-cell lymphomas, and breast cancer.

BCN-HS-PEG2-VA-PABC is a ADC linker that can be used in the synthesis of PL1601.

Bay-y-1015 is an orally active quinoline-based 5-lipoxygenase inhibitor. Bay-y-1015 inhibits LTB4 and LTC4 synthesis. Bay-y-1015 can be used in the research of inflammatory diseases.

PD-254552 is a MEK inhibitor. PD-254552 exhibits hepatotoxicity and gastrointestinal toxicity in mice.

PySAHA is a multifunctional HDAC inhibitor. PySAHA can degrade intracellular HDAC via a hydrophobic tagging mechanism. PySAHA also possesses photodynamic therapeutic activity and can generate reactive oxygen species under light irradiation. PySAHA can inhibit the proliferation, migration and induce cell apoptosis of breast cancer cells. PySAHA has antitumor activity and can be used in breast cancer research.

WMJ-J-09 is an HDAC inhibitor with IC50 values of 7.5 nM (HDAC1), 21.3 nM (HDAC2), 18.4 nM (HDAC3), 90.9 nM (HDAC8), 3.9 nM (HDAC6) and 8715.7 nM (HDAC4). WMJ-J-09 blocks the cell cycle and induces apoptosis in cancer cells. WMJ-J-09 induces cancer cell death through the LKB1-AMPK-p38MAPK-p63-survivin signaling cascade.WMJ-J-09 inhibits HDAC enzyme activity, leading to acetylation of key proteins and thereby regulating cancer cell death. WMJ-J-09 can be used in HCT116 cells and FaDu cells research[1][2].

MPT0G413 (Compound 6) is a potent, selective, orally active and brain-penetrant HDAC6 inhibitor with an IC50 of 3.92 nM. MPT0G413 decreases not only the level of phosphorylation of tau proteins but also the aggregation of tau proteins. MPT0G413 can ameliorate the impaired learning and memory. MPT0G413 can be used for the research of neurological disease, such as Alzheimer's disease.