NCI-006 is a potent new inhibitor of lactate dehydrogenase (LDH) that disrupts tumor growth in mice. LDH inhibition slows tumor growth but rapidly redirects pyruvate to support mitochondrial metabolism. Inhibiting both mitochondrial complex 1 and LDH suppresses metabolic plasticity of glycolytic tumors in vivo, significantly prolonging tumor growth inhibition.

BI-4924 (BI 4924) is a potent, selective NADH/NAD+-competitive PHGDH inhibitor with IC50 of 2 nM.BI-4924 splays high selectivity against the majority of other dehydrogenase targets.

TAS-119 is a potent, selective and orally active Aurora A inhibitor with an IC50 of 1.0 nM. TAS-119 shows high selectivity for Aurora A over other protein kinases, including Aurora B (IC50 of 95 nM). TAS-119 has potent antitumor activites.

KW-2478 is a nonansamycin HSP90 inhibitor with IC50 of 3.8 nM. Phase 1/2

ACT-541468 is a dual orexin receptor antagonist.

Sodium channel blocker. Suppresses tetrodotoxin (TTX)-resistant Na+ currents approximately twice as selectively as TTX-sensitive currents. Antinociceptive; displays analgesic effects in animal models of inflammatory and neuropathic pain.

EB-42486 is a novel, potent, and highly selective G2019S-LRRK2 inhibitor (IC50 < 0.2 nM).

ISO-1 is a macrophage migration inhibitory factor (MIF) antagonist with an IC50 of 7 μM.

Elosulfase alfa (BMN 110) is a recombinant form of human N-acetylgalactosamine-6-sulfatase (GALNS). Elosulfase alfa is used as an enzyme replacement therapy for mucopolysaccharidosis IVA (MPS IVA), also known as Morquio A syndrome.

Lumogallion is a highly sensitive fluorescent reagent for the detection of aluminum, gallium and other metals. Lumogallion has an excitation wavelength of 490 nm and an emission spectrum in the range of 520 nm to 650 nm, with a peak near 580 nm.

Palmitoyloleoylphosphatidylglycerol is an anionic surfactant lipid. Palmitoyloleoylphosphatidylglycerol suppresses Der p 2-stimulated inflammatory responses in lung epithelial cells and macrophages.

Diphenyl-1-pyrenylphosphine (DPPP) is a fluoregenic peroxide reactive probe. Diphenyl-1-pyrenylphosphine exhibits a unique phototriggered aggregation-induced emission (AIE)/aggregation-induced quenching (ACQ) transition with a remarkable third-order nonlinear optical signal change.

MSC-4106 is an orally active and potent inhibitor of YAP/TAZ-TEAD. MSC-4106 inhibits TEAD1 or TEAD3 auto-palmitoylation and shows inhibitory effect on NCI-H226 tumor xenograft model.

Febuxostat (TEI 6720) sodium is a potent, selective and non-purine xanthine oxidase (XO) inhibitor with a Ki value of 0.6 nM. Febuxostat sodium has the potential for the research of hyperuricemia and gout.

Flazin is a non-enzymatic protein glycation inhibitor, also inhibits peroxynitrite (ONOO-), with an IC50 value of 85.31 μM for bovine serum albumin (BSA) glycation and an EC50 value of 71.99 μM for ONOO-. Flazin can be used for researching diabetes and neuronal disorders. Flazin also can used as a lipid droplet (LD) regulator against lipid disorders, and a xanthine oxidase (XOD) inhibitor.

HA-100 is an inhibitor of cGMP-dependent protein kinase (PKG), cAMP-dependent protein kinase (PKA), protein kinase C (PKC) and MLC-kinase.

Dioleoylphosphatidylglycerol (DOPG) is a naturally occurring phospholipid that can be produced by the combined action of aquaporin 3 (AQP3) and phospholipase D2 (PLD2). Dioleoylphosphatidylglycerol inhibits macrophage inflammatory mediator production in response to heat shock protein B4 (HSPB4) activation of toll-like receptor 2 (TLR2) .

TM-1 is a potent inhibitor of pyruvate dehydrogenase kinase (PDHK1). TM-1 inhibits PDHK1 and PDHK2 with IC50s of 2.97 μM and 5.2 μM, respectively. TM-1 blocks pyruvate dehydrogenase complex (PDHC) phosphorylation, and inhibits cell proliferation.

HOE961, the diacetate ester prodrug of S2242, is active against respiratory cowpox virus infections, is orally active in infection models. Anti-orthopoxvirus activity.

TP0556351 is a potent and selective matrix metalloproteinase-2 (MMP2) inhibitor with an IC50 value of 0.2 nM. TP0556351 reduces the amount of collagen in the lungs of a Bleomycin-induced pulmonary fibrosis mouse model. TP0556351 can be used for researching idiopathic pulmonary fibrosis (IPF).

JZP-361 is a potent and reversible inhibitor of human recombinant MAGL (hMAGL, IC50=46 nM), and has almost 150-fold higher selectivity over human recombinant fatty acid amide hydrolase (hFAAH, IC50=7.24 μM) and 35-fold higher selectivity over human α/β-hydrolase-6 (hABHD6, IC50=1.79 μM). JZP-361 represents a dual-acting pharmacological tool possessing both MAGL inhibitory and antihistaminergic activities.

(S,R,S)-AHPC-O-PEG1-propargyl (Compound 10b) is an E3 ligand for the synthesis of PROTAC.

Raltegravir (MK 0518) sodium is a potent and orally active integrase (IN) inhibitor, used to treat HIV infection.

Tazemetostat (EPZ-6438) hydrochloride is a potent, selective and orally active EZH2 inhibitor with IC50 values of 11 and 16 nM for EZH2 peptide and nucleosome, respectively. Tazemetostat hydrochloride can be used for cancer research.

(S)-MRTX-1719 (example 16-7) is the S-enantiomer of MRTX-1719. (S)-MRTX-1719 is a PRMT5/MTA complex inhibitor, with an IC50 of 7070 nM.

EML425 is a potent and selective CREB binding protein (CBP)/p300 inhibitor with IC50s of 2.9 and 1.1 μM, respectively.

WAY-303290 (GluR6 antagonist-1) is a benzothiophene derivative acting as an ionotropic glutamate receptor 6 (GluR6) antagonist, which can be used for researching acute and chronic neurological disorders.

KR-39038 is an orally active and potent GRK5 (G protein-coupled receptor kinase 5) inhibitor, with an IC50 of 0.02 μM. KR-39038 significantly inhibits angiotensin II-induced cellular hypertrophy through suppression of HDAC5 pathway in neonatal cardiomyocytes. KR-39038 shows profound anti-hypertrophic effects and improved cardiac function. KR-39038 can be used for heart failure research.

Aminobenzenesulfonic auristatin E TFA is a drug-linker conjugate for ADC with potent antitumor activity by using Auristatin E (a cytotoxic tubulin modifier), linked via the ADC linker Aminobenzenesulfonic.