Belzutifan (PT2977, MK-6482) is a potent and selective small-molecule inhibitor of HIF2α with SPA IC50 of 9 nM, EC50 of 11 nM (HIF-2α luciferase assay). PT2977 demonstrated high potency with EC50 of 17 nM in the VEGFA secretion assay in 786-O cells. PT2977 (0.3, 1, and 3 mg/kg, oral) potently and dose-dependently reduced mRNA levels of human cyclin D1, a target gene regulated by HIF-2α, exhibited excellent antitumor activity in the 786-O mouse xenograft model In phase 1 clinical, PT2977 decreased in the HIF-2α target erythropoietin (EPO) following once daily oral administration of PT2977 at the dose levels of 20, 40, 80, 120, 160, and 240 mg in patients with solid tumors, also showed encouraging outcomes in patients with advanced renal cell carcinoma in an expansion cohort of 55 patients with ccRCC treated at 120 mg q.d.

ML213 is a novel potent, selective KCNQ2 (Kv7.2) and KCNQ4 (Kv7.4) activator with EC50 of 230 and 510 nM, respectively. ML213 displays >80-fold selectivity over other related potassium channels (KCNQ1/3/5). ML213 causes significant hyperpolarization in mesenteric artery smooth muscle cells, shows potent vasorelaxant effects in different blood vessels.

Hi 76-0079 (NNC0076-0079) is a specfic, small molecule inhibitor of hormone-sensitive lipase (HSL) with IC50 of 0.11 uM. Hi 76-0079 does not affect ATGL or other lipases (IC50>50 uM). Hi 76-0079 inhibits lipolysis in vivo.

Enpatoran (M5049) hydrochloride is a potent, orally active, and dual TLR7/8 inhibitor with IC50s of 11.1 nM and 24.1 nM, respectively, in HEK293 cells.

1-Thioglycerol(Mercaptopropanedioltech) is an inhibitor of glycerol kinase activity. It stimulates the synthesis of porphyrin in aerobically growing Escherichia coli.

3,4-Dichlorophenyl isocyanate(1,2-Dichloro-4-isothiocyanatobenzene) is a chemical compound used as a chemical intermediate and in organic synthesis.

Glutaraldehyde(Glutaric dialdehyde, Pentane-1,5-dial) is an effective biochemical reagent used as a protein crosslinker, enzyme immobilization microscopy, histochemistry, and cytochemistry.

BW 755C is a 5-lipoxygenase (5-LO) inhibitor with an IC50 of 5 μM. BW 755C also inhibits cyclooxygenase (COX) with IC50s of 0.65 and 1.2 μg/mL against COX-1 and COX-2, respectively.

Vidofludimus (4sc-101; SC12267) hemicalcium is an orally active inhibitor for dihydroorotate dehydrogenase (DHODH) and also is a novel modulator for farnesoid X receptor (FXR). Vidofludimus hemicalcium, as an immunomodulatory agent, can be used for the research of autoimmune disorders such as inflammatory bowel disease (IBD). Vidofludimus hemicalcium also can be used for the research of fatty liver by targeting FXR.

BMS-433771 dihydrochloride hydrate is a potent orally active inhibitor of respiratory syncytial virus (RSV). BMS-433771 dihydrochloride hydrate is active against both A and B groups of RSV, with an average EC50 of 20 nM. BMS-433771 dihydrochloride hydrate can be used for the research of respiratory tract disease.

Varlitinib (ASLAN001) tosylate is a potent, reversible, small molecule pan-EGFR inhibitor with IC50s of 7, 2, 4 nM for HER1, HER2 and HER4, respectively.

FR 113680 is a tripeptide substance P antagonist that interacts selectively with the NK1 neurokinin receptor.

Fradafiban (BIBU-52) hydrochloride is a nonpeptide platelet glycoprotein IIb/IIIa antagonist, which binds to the human platelet GP IIb/IIIa complex with a Kd value of 148 nM.

STING agonist-22 (CF501) is a potent non-nucleotide STING agonist. STING agonist-22 is a adjuvant by activating STING to induce the type I interferon (IFN-I) response and proinflammatory cytokine production. STING agonist-22 can be used as an adjuvant to boost the original protein vaccine, producing potent, broad, and long-term immune protection. STING agonist-22 can be used for SARS-CoV-2 variants and sarbecovirus diseases research.

EBL-3183, an indole-2-carboxylate, is a potent metallo-β-lactamase (MBL) inhibitor. EBL-3183 is reversibly binding, non-covalent, competitive NDM-1 inhibitor with a pIC50 of 7.7.

S-Allylmercapturic acid is a biomarker of food intake (BFIs) for garlic consumption.

N4-Benzoyl-3’-O-methylcytidine is a cytidine analog. Cytidine analogs have a mechanism of inhibiting DNA methyltransferases (such as Zebularine, HY-13420), and have potential anti-metabolic and anti-tumor activities.

Fmoc-DON-Boc (Compound 8b) is an Fmoc-protected compound that can be used for the synthesis of proagent of 6-diazo-5-oxo-L-norleucine (DON; HY-108357). DON is a glutamine antagonist.

2’-O-Methyl-N1-methyladenosine is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc.

3’-Deoxy-methyl-2-thiouridine is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc.

5-Bromo-2′-deoxy-2′-fluorouridine (Example 1), a 5-halo analog, is potential as an antiviral agent.

Sitagliptin fenilalanil is a dipeptidyl aminopeptidase 4 (DPP-4) inhibitor.

Culmerciclib maleate is a cyclin dependent kinase (CDK) inhibitor, and has antineoplastic activity.

RDR 02308 is a TLR4-MyD88 binding inhibitor that inhibits full-length β-lactamase.

FM04 is a potent P-glycoprotein (P-gp) inhibitor (EC50=83 nM). FM04 inhibits P-gp in 2 mechanism: (1)FM04 binds to Q1193, followed by interacting with the functionally critical residues H1195 and T1226; or (2)FM04 binds to I1115 (a functionally critical residue itself), disrupting the R262-Q1081-Q1118 interaction pocket and uncoupling ICL2-NBD2 interaction and thereby inhibiting P-gp.

Thiotraniliprole (HY366) is an ortho formamidobenzamide insecticide that can be used for the synthesis of insecticidal combinations. Thiotraniliprole has potential applications in the prevention of lepidoptera pests, coleoptera pests, ants, and termites.

Didocosahexaenoin, an omega-3 derivative, is a diglyceride of DHA and can be synthesised from DHA triglycerides. Didocosahexaenoin causes significant loss of mitochondrial membrane potential and induces ROS production. Didocosahexaenoin induces apoptosis. Didocosahexaenoin induces stronger cytotoxicity than DHA in human prostate carcinoma cells.

PF-07059013 is an orally active and potent noncovalent modulator of sickled hemoglobin (HbS). PF-07059013 specifically binds to Hb with nanomolar affinity and displays strong partitioning into red blood cells (RBCs). PF-07059013 can be used for sickle cell disease (SCD) research.

BAY-297 is a potent and selective PIP4K2A inhibitor. BAY-297 can serve as valuable chemical probes to study PIP4K2A signaling and its involvement in pathophysiological conditions such as cancer.

IACS-15414 (IACS 15414) is a potent, selective, orally bioavailable SHP2 inhibitor with IC50 of 122 nM; IACS-15414 potently suppressed the mitogen-activated protein kinase (MAPK) pathway signaling and tumor growth in RTK-activated and KRASmut xenograft models in vivo. IACS-15414 potently suppressed the mitogen-activated protein kinase (MAPK) pathway signaling and tumor growth. IACS-15414 had excellent PK properties across species but a narrow hERG window.