small molecule

Pexidartinib (PLX-3397) is a capsule formulation containing a small-molecule receptor tyrosine kinase (RTK) inhibitor of KIT, CSF1R and FLT3 with potential antineoplastic activity.

Duvelisib (INK1197) is an orally bioavailable, highly selective and potent small molecule inhibitor of the delta and gamma isoforms of phosphoinositide-3 kinase (PI3K) with potential immunomodulating and antineoplastic activities.

Avacopan (CCX168) is an orally administered small-molecule C5aR ( IC50 : 0.1 nM.)antagonist that blocks the effects of C5a and prevents the development of GN induced by anti-myeloperoxidase antibodies in a murine model of AAV.

(E)-Daporinad (FK866) is a small molecule inhibitor of nicotinamide phosphoribosyltransferase (NMPRTase), with potential antineoplastic and antiangiogenic activities.

Olaparib (KU0059436) is a small molecule inhibitor of PARP1/PARP2 (IC50=5/1 nM), with weak inhibitory activity against PARP tankyrase-1 (IC50=1.5 μM), and is selective and orally active. Olaparib exhibits autophagy and mitochondrial autophagy activation activity.

Selinexor (KPT-330) is a small molecule inhibitor of CRM1 with selective and oral activity. Selinexor blocks the cell cycle, induces apoptosis, and has antitumor activity for the treatment of multiple myeloma.

CSRM617 hydrochloride is a selective small-molecule inhibitor of the transcription factor ONECUT2 ( OC2, a master regulator of androgen receptor) with a K d of 7.43 uM in SPR assays, directly binds to OC2-HOX domain. CSRM617 hydrochloride induces apoptosis through the appearance of cleaved Caspase-3 and PARP. CSRM617 hydrochloride is well tolerated in the mouse model of prostate cancer [1]

VX-702 is a highly specific p38α MAPK inhibitor, 14-fold higher selectivity for the p38α than p38β. VX-702 is a small molecule investigational oral anti-cytokine therapy for treatment of inflammatory diseases, specifically rheumatoid arthritis (RA).

MW01-2-151SRM is a novel small molecule inhibitor of microglia activation that crosses the blood-brain barrier, has anti-neuroinflammatory effects, attenuates the up-regulation of glial cytokines in models of neuroinflammation, and can be used in studies of traumatic brain injury, Alzheimer's disease, and alginate toxicity.

(E)-3-(4-Methoxyphenyl)acrylic acid is a small molecule compound isolated from the rhizome of Etlingera pavieana (Pierre ex Gagnep.) R. M. Sm. It is a novel α-glucosidase inhibitor. (E)-3-(4-Methoxyphenyl)acrylic acid has hepatoprotective activity, antiamnesic activity, enhances cognitive effects, and can be used to lower blood pressure sugar.

Methotrexate Diglutamate Small molecule compound present in the liver that acts as a partially purified human dihydrofolate reductase inhibitor.

Pazopanib (GW786034), a small molecule inhibitor, inhibits multiple protein tyrosine kinases with potential antineoplastic activity. Pazopanib selectively inhibits VEGFR-1, -2 and -3, c-kit and PDGF-R, which may result in inhibition of angiogenesis in tumors in which these receptors are upregulated.

BMS-906024 (Osugacestat) is an orally available and selective inhibitor of γ-secretase, a small molecule Notch inhibitor.BMS-906024 has broad-spectrum antitumour activity against a variety of human cancer xenografts.BMS-906024 prevents the activation of all four Notch receptors, and is active against Notch1, -2, -3 and -4 receptors. BMS-906024 prevents the activation of all four Notch receptors, with IC50s of 1.6, 0.7, 3.4 and 2.9 nM for Notch1, -2, -3 and -4 receptors, respectively.

Chromium(III) acetate （Chromium acetate） is a small molecule ionic crosslinker that is used as a feedstock for the synthesis of other compounds.

JG-2016, as a small molecule histone acetyltransferase 1 (HAT1) inhibitor, inhibits the growth of human cancer cell lines, inhibits enzyme activity in cellulose, and interferes with tumor growth.

TCH-165 is a small molecule modulator of proteasome assembly, resulting in an increase in 20S levels. The increase in the level of free 20S corresponds to enhanced proteolysis of IDPs.

VRT-532 (CFpot-532) is an effective modulator of CFTR and is commonly used in studies of cystic fibrosis (CF) caused by CFTR defects. Arylsulfatase B (ARSB), which is necessary to reduce the accumulation of sulphate glycosaminosaccharide (gag) in cystic fibrosis, and modification of CFTR by small molecule modulator VRT-532 can increase ARSB and reduce the accumulation of 4-chondroitin sulfate.

Ammonium chloride acts as a small molecule autophagy inhibitor.Ammonium chloride is a pH-regulating, heteropolar compound that can cause intracellular alkalosis and metabolic acidosis, thereby affecting enzyme activity and influencing processes in biological systems.Ammonium chloride has potential antimicrobial activity. Ammonium Chloride has potential antimicrobial activity and prevents training-induced improvement in mitochondrial respiratory function in male rat flounder muscle.

GSK3a-IN-38 is a novel small molecule compound that has inhibitory effects on GSK-3a.

Panomifene TFA（GYKl13504 TFA） is a small molecule antagonist of ERs with anticancer activity that can be used to study breast cancer and musculoskeletal diseases.

Faxeladol, a potent adrenergic absorption inhibitor and serotonin reuptake inhibitor, is a small-molecule Opioid receptor agonist that can be used to study neurological disorders.

Epetirimod (S-30563) is a small molecule immunomodulator with antitumor and anti-infective activity for the study of papillomavirus infections.

KX2-361 is a orally bioavailable small molecule dual Src/tubulin inhibitor that provides long term survival in a murine model of glioblastoma

Anatibant 2HCl is a small molecule bradykinin B2 receptor antagonist for the treatment of neurological disorders and may be used in the study of brain injury.

ROS inducer 1 is a small molecule compound with bactericidal activity that inhibits the production of ROS in Xanthomonas axonopodis pv. citri (Xac), Xanthomonas oryzae pv. oryzae (Xoo) and Pseudomonas syringae pv. actinidiae (Psa). ROS inducer 1 induces ROS production in Xanthomonas cells and can be used to study bacterial infections in crops.

NUCC-390, a novel small-molecule CXCR4 receptor agonist, selectively induces CXCR4 receptor internalization while acting antagonistically to AMD3100. This compound facilitates nerve functional recovery following neurodegeneration in vivo.

1,1'-(Heptane-1,7-diyl)diguanidine dihydrochloride is a potent and selective small molecule inhibitor of glycogen synthase kinase-3 (GSK-3). It is used in studies of stem cell differentiation, tumors and neurodegenerative diseases.

FL104 is a potent agonist of small-molecule urotensin II receptor, pEC50= 7.11.

PF-3758309 hydrochloride (PF-03758309 hydrochloride) , is a PAK4 inhibitor, is also a n orally bioavailable small-molecule inhibitor of p21-activated kinase 4 (PAK4) with potential antineoplastic activity. PF-3758309 hydrochloride binds to PAK4, inhibiting PAK4 activity and cancer cell growth. PAK4, a serine/threonine kinase belonging to the p21-activated kinase (PAK) family, is often upregulated in a variety of cancer cell types and plays an important role in cancer cell motility, proliferation, and survival.

(2E,4E,6Z)-Methyl deca-2,4,6-trienoate (Methyl (2E,4E,6Z)-decatrienoate) is a small molecule compound from the bed bug Thyanta pallidovirens. (Methyl (2E,4E,6Z)-decatrienoate), a small molecular compound from Thyanta pallidovirens, is a sexually attractive pheromone that is thermally unstable.

BMS202 hydrochloride (1675203-84-5(free base)) (PD-1/PD-L1 inhibitor 2 hydrochloride) is a small-molecule PD-1/PD-L1 interaction inhibitor (IC50: 18 nM). Biophysical studies demonstrate that BMS202 binds directly to PD-L1. Binding of BMS202 promotes PD-L1 dimerisation and blocks the PD-L1/ PD1 interaction.

Patamostat HCl is a highly potent and selective small molecule protease (protease) inhibitor that inhibits trypsin, fibrinolytic enzymes, and thrombin with IC50 values of 39 nM, 950 nM, and 1.9 μM, respectively.Patamostat HCl is used in the study of acute pancreatitis.

VB 201 is an oxidized phospholipid small molecule with anti-inflammatory activity that inhibits CD14 and Toll-like receptor 2-dependent innate cell activation and limits atherosclerosis, and can be used to study atherosclerosis.

Anisperimus HCl (LF 150195 HCl) is a small molecule immunizing agent for the study of autoimmune diseases.

2,5-Dihydroxybiphenyl (TFIIH Modulator12), a small molecule destabilization inducer, induces the dimerization of trichothiodystrophy group A protein to modulate TFIIH transcriptional activity.

AMG-0347 (UNII-CD7L9290QR) is a small molecule inhibitor targeting TRPA1(transient receptor potential ankyrin 1) ion channels, a receptor found in sensory neurons and involved in the detection of pain and environmental stimuli. AMG-0347 acts by blocking the function of TRPA1 and has analgesic effects.

Iroxanadine (BRX-005) is a Novel small molecule MAPK p38 inhibitor that induces phosphorylation of p38 SAPK and induces concentration-dependent relaxation in guinea pig pulmonary artery preparations precontracted with phenylephrine.CAS 번호13480-84-5

HDAC6 degrader 9c is a small molecule histone deacetylase 6 (HDAC6) degrader that can be used to study cancer or other diseases.

Alethine (β-Alethine) is a small molecule compound with antitumour activity and is used to treat tumours and infections. The alethine-induced up-regulation of TNFα increases the cytotoxicity of T cells.

Pomisartan (BIBR-363) is a small molecule angiotensin type 1 receptor (AT1R) antagonist that is used in the treatment of cardiovascular disease, studying heart failure and hypertensio

BPR1J-097, a new-type small molecule FLT-3 inhibitor(IC50=11±7 nM), is with great anti-tumor activities in vivo.

BMS-488043 is a novel and unique oral small molecule HIV fusion inhibitor that inhibits the attachment of Human Immunodeficiency Virus type 1 (HIV-1) to CD4(+) lymphocytes.BMS-488043 is used for the treatment of immune disorders, infections, and genitourinary disorders, and can be used in the study of HIV infect

Aplindore Fumarate (DAB-452) is a small molecule dopamine D2 receptor partial agonist.Aplindore Fumarate exhibits high affinity for dopamine D2 and D3 receptors, and low affinity for dopamine D4, 5-hydroxytryptophan (5-HT2), and α1-adrenergic receptors.Aplindore Fumarate is used in the study of Parkinson's disease and schizophrenia. Fumarate can be used to study Parkinson's and schizophrenia.

Tienoxolol FA is a small molecule beta-adrenergic receptor antagonist used in the treatment of cardiovascular disease and in the study of hypertension and cardiac machine ischemia.

Ezatiostat TFA (TLK199) is a liposomal small-molecule glutathione analog inhibitor of glutathione S-transferase (GST) P1-1 with hematopoiesis-stimulating activity.

FiVe1 is a vimentin binding small molecule that promotes the disintegration and phosphorylation of vimentin in the metaphase, leading to mitotic disasters, polynuclearization, and loss of cancer cell dryness. FiVe1 selectively and irreversibly inhibit the growth of mesenchymal transformed breast cancer cells (FOXC2-HMLER cell, IC50=234nM) and soft tissue sarcomas of different histological subtypes.

Mtb-IN-2 is a small molecule compound of Mycobacterium tuberculosis (Mtb) with antimicrobial activity and low toxicity that interferes with methionine metabolism processes and can be used to study tuberculosis.

(1S,2R)-2-PCCA is a novel and potent small molecule GPR88 receptor agonist with an EC50 value of 3 nM in the non-cellular system and 603 nM in the cellular system.

AW68 is a potential small molecule BRD4 inhibitor that prevents and treats BRD4-related diseases and can be used in cancer research.

2-Quinolinecarboxaldehyde (Quinoline-2-carbaldehyde) is a small rigid molecule that is a compound in the Henry reaction and subsequent elimination. 2-Quinolinecarboxaldehyde inhibits AChE with an IC50 of 13.48 μM.