TMX-4140 is a selective PIP4K2C inhibitor with a KD of 7.2 nM for PIP4K2C over PIP4K2B. TMX-4140 can be used for synthesis of PROTAC TMX-4153.

MSC778 is an effective and orally active flap endonuclease 1 (FEN1) inhibitor with an IC50 of 3 nM and a KD of 2.9 nM. MSC778 exhibits 145-fold, 516-fold, and 65-fold selectivity over EXO1, GEN1, and XPG, respectively. MSC778 selectively kills BRCA2-deficient cells and potentiates the activity of Niraparib to induce tumor stasis in a BRCA2 KO DLD-1 mouse xenograft. MSC778 can be used in the research of colorectal cancer.

CGP-59326 (TRX-13) is a highly potent and selective epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor. CGP-59326 blocks the EGFR signaling pathwa, demonstrating highly selective inhibition of EGFR-dependent tumor cells. CGP-59326 is promising for research of cancers.

PD-166285 is a PKMYT1 inhibitor, with an IC50 value of 17 nM. PD166285 shows strong antiproliferative effects against CCNE1-amplified OVCAR3 cells (IC50 = 0.14 μM) and HCC1569 cells (IC50 = 0.21 μM). PD166285 induces apoptosis and arrests CCNE1-amplified HCC1569 cells at the G1/S phase of the cell cycle. PD166285 can be used for the research of PKMYT1-targeted therapies for CCNE1-amplified cancers.

(R)-KRAS G12D inhibitor 28 hydrochloride dehydrate is the hydrochloride dehydrate of (R)-KRAS G12D inhibitor 28. KRAS G12D inhibitor 28 (Compound 1) is a KRAS G12D inhibitor. KRAS G12D inhibitor 28 (Compound 1) can be used in the cancer research.

CGS 22652 is a potent thromboxane A2 receptor antagonist. CGS 22652 has selective thromboxane A2 synthase inhibitory properties. CGS 22652 can be used in the research of coronary artery thrombosis.

ADD-17014 is a L-Glu antagonist. ADD-17014 impairs presynaptic excitatory amino acid L-Glu neurotransmission. ADD-17014 is a prodrug of its β-amino alcohol metabolite, and the metabolite acts as a NMDA receptor antagonist by binding to the MK-801 site located inside the NMDA receptor or ion channel. ADD-17014 has an anticonvulsant and anti-ischemic activity. ADD-17014 can be used for neurodegenerative diseases like Parkinson’s disease, Alzheimer’s disease and stroke research.

MK-5596 is an efficient, selective and orally active CB1R (IC50 = 1.0 nM, EC50 = 5.8 nM) inverse agonist. MK-5596 has weak hERG inhibitory activity. MK-5596 has strong weight loss and appetite suppression effects. MK-5596 has a certain inhibitory effect on CYP enzymes (CYP3A4: IC50 = 3.3 μM, CYP2C8: IC50 = 11 μM, CYP2C9: IC50 = 18 μM, CYP2D6: IC50 = 6 μM). MK-5596 can be used for research on conditions such as obesity.

GR 175737 is a partial histamine H3 receptor agonist, with an EC50 of 7.8 nM. GR 175737 can be used in the research of inflammatory diseases.

FCN-338 (LOXO-338) is an orally active and selective Bcl-2 inhibitor with an IC50 of 4.5 nM for Bcl-2/BAK interaction. FCN-338 potently inhibits tumor growth in follicular lymphoma (FL), acute myeloid leukemia (AML), and acute lymphoblastic leukemia (ALL) xenograft mice model without significant weight loss. FCN-338 has a broad-spectrum anti-cancer activity, such as FL, CLL/SLL, AML, and ALL.

AM-36 is a neuroprotective agent with combined antioxidant and sodium channel blocking actions. AM-36 can inhibit cell apoptosis and ROS prodiction. AM-36 can reduce neuronal damage and DA release after middle cerebral artery occlusion in rats. AM-36 can be used for the researches of inflammation and neurological disease, such as stroke.

VSP-77 is an orally active PPARγ agonist. VSP-77 selectively upregulates the expression of insulin sensitivity-related genes (Glut4 and Adiponectin) by inhibiting CDK5-mediated phosphorylation of PPARγ at Ser-273. VSP-77 significantly improves glucose tolerance, reduces fasting blood glucose and insulin levels in high-fat diet (HFD)-induced diabetic mouse models. VSP-77 can be used for the study of diabetes.

ZG-2492 is an orally active LDHA inhibitor with an IC50 of 156 nM. ZG-2492 can reduce lactate production and induce cell cycle arrest and apoptosis in pancreatic cancer cells . ZG-2492 has antitumor activity and can be used in the research of tumors such as pancreatic cancer.

KRAS IN-44 (Compound S2C2M2) is a PDE6D degrader. KRAS IN-44 inhibits PDE6D-dependent KRAS trafficking and KRAS downstream signaling pathways. KRAS IN-44 down-regulates EGF-induced the phosphorylation of PI3K, AKT, and mTOR. KRAS IN-44 increases Apoptosis. KRAS IN-44 has antitumor activity against hepatoblastoma.

DOV-102,677 is an orally sctive triple monoamine neurotransmitter reuptake inhibitor that simultaneously inhibits the dopamine (DAT) (IC50 = 129 nM; Ki = 222 nM), norepinephrine (NET) (IC50 = 103 nM; Ki = 1030 nM), and serotonin (SERT) (IC50 = 133 nM; Ki = 740 nM) transporters. DOV-102,677 demonstrated significant antidepressant-like activity and sensory-motor gating regulatory effects in mouse experiments. DOV-102,677 can be used for research on depression.

ODS-2004436 is a small molecule radiotracer that uses positron emission tomography (PET) imaging to measure the activity of the epidermal growth factor receptor (EGFR) in tumors. ODS-2004436 labeled with the radioactive isotope fluorine-18 shows significantly higher uptake in the xenograft models of lung cancer with EGFR mutations compared to the wild-type models, and could be used to distinguish the mutation status. ODS-2004436 can be used to identify EGFR-positive tumors and predict their response to certain reagent treatments, especially for non-small cell lung cancer (NSCLC).

VVD-849 is a RAS ligand. VVD-849 binds covalently to cysteine 242 in the RAS binding domain of PI3K p110α and promotes RAS/PI3K interaction. VVD-849 partially inhibits pAKT(S473) in HER2 over-expressing tumors. VVD-849 can be used cancers like breast cancer research.

SDZ 208-912 is a dual-action 5-HT1A/2 receptor agonist and dopamine D1 receptor antagonist. SDZ 208-912 exhibits partial dopamine agonism and atypical neurosedative effects in rodent models. SDZ 208-912 can be used in research on neurological disorders such as schizophrenia.

Lergotrile is a potent and orally active dopamine agonist and a prolactin secretion inhibitor. Lergotrile inhibits prolactin release from pituitaries by activating an adenohypophyseal dopamine receptor. Lergotrile has the potential for the research of Parkinson's disease.

PKRA83 (PKRA7) hydrochloride is a potent, blood-brain-penetrating PK2 antagonist that competes for PK2 binding to its receptors, PKR1 and PKR2. PKRA83 hydrochloride potently inhibits PK2 receptors with IC50 values of 5.0 nM and 8.2 nM for PKR1 and PKR2, respectively. PKRA83 hydrochloride exhibits anticancer, antiarthritis, and antiangiogenic activities.

SD 8381 is a potent and selective COX-2 inhibitor. SD 8381 shows IC50 values of 0.0098 μM for hCOX-2 and 0.69 μM for hCOX-1.

Repunapanor (compound 123) is a potent Na+/H+ exchanger 3 (NHE-3) inhibitor.

FTO ligand-1 is a FTO ligand for FTO PROTAC degrader FP54. FTO ligand-1 can inhibit cell proliferation and block the FP54-induced FTO degradation. FTO ligand-1 can be used for research of cancer, such as acute myeloid leukemia (AML).

Tilivapram (AVE8112) is an orally active PDE4 inhibitor. Tilivapram can regulate neurophysiological activities and improve cognitive and memory impairments. Tilivapram can be used in the research of various neuropsychiatric disorders such as schizophrenia and Parkinson's disease.

TK-684 is a potent and selective allosteric SHP2 inhibitor with IC50 values of 2.1, ＞1000 nM for SHP2WT, SHP22PTP, respectively. TK-684 inhibits cell proliferation and induces apoptosis. TK-684 decreases the protein expression of p-AKT, p-ERK.

KB-15 is a STAT3 inhibitor. KB-15 exhibits potent anti-proliferative activity against AGS gastric cancer cells (IC50 = 0.29 μM) and BGC-823 gastric cancer cells (IC50 = 0.65 μM). KB-15 exerts anti-tumor effects by inhibiting STAT3 phosphorylation, downregulating HO-1 expression, and promoting intracellular ROS accumulation. KB-15 induces G0/G1 phase cell cycle arrest and apoptosis, as well as suppresses colony formation and migration of gastric cancer cells. KB-15 demonstrates excellent anti-tumor efficacy in BGC-823 subcutaneous xenograft model. KB-15 can be used for the study of gastric cancer.

CS47 is a reversible Thioredoxin reductase 1 (TrxR1) inhibitor. CS47 activates stress-responsive GSH and iron regulatory programs, depleting GSH and promoting HO-1 overexpression and intracellular iron overload by ROS accumulation, and finally inducing ferroptosis in KRAS-independent lung cancers. CS47 has an anticancer activity with low cytotoxicity toward normal lung fibroblasts.

F 2833 is a lipid-lowering agent. F 2833 can reduce the levels of cholesterol, triglycerides, and plasma phospholipids. F 2833 can be used for research on diseases such as hyperlipidemia.

TK-685 is an orally active, selective, and allosteric SHP2 inhibitor with an IC50 of 2.1 nM. TK-685 inhibits esophageal cancer cell proliferation and induced apoptosis by targeting SHP2-mediated AKT and ERK signaling pathways.

Raxlaprazine etomoxil is a small molecule compound with dopamine D2 and D3 receptor modulating activity, which has potential application value in research related to mental illnesses. Raxlaprazine etomoxil exhibits high affinity for human recombinant D2L receptors, with an inhibition constant (Ki) of 1.95 nM. Raxlaprazine etomoxil effectively inhibits forskolin-stimulated cAMP accumulation, with an half maximal effective concentration (EC50) of 3.72 nM in functional activity experiments.