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Trametinib
JTP-74057, GSK1120212
T2125871700-17-3
Trametinib (GSK1120212) is a MEK inhibitor that inhibits MEK1 and MEK2 (IC50=0.7 0.9 nM) with ATP non-competitive and oral activity. Trametinib activates autophagy and induces apoptosis.
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TargetMol | Inhibitor Hot
Gut restricted-7
GR-7
T115152553218-46-3In house
Gut restricted-7 (GR-7) is a covalent and orally active pan-bile salt hydrolase (BSH) inhibitor that reduces gut bacterial BSHs and decreases deconjugated bile acid levels in the feces of mice.
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TargetMol | Inhibitor Hot
Y-27632 dihydrochloride
Y-27632 2HCl
T1725129830-38-2
Y-27632 dihydrochloride (Y-27632 2HCl) is an orally potent, ATP-competitive inhibitor of ROCK-I and ROCK-II. Y-27632 dihydrochloride also inhibits isolation-induced apoptosis in mouse prostate stem or progenitor cells.
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Fedratinib
TG-101348, SAR 302503
T1995936091-26-8
Fedratinib (TG-101348) (TG101348) is an ATP-competitive inhibitor of JAK2 (IC50: 3 nM) with significantly less potent activity against JAK3.
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Venetoclax
GDC-0199, ABT-199, ABT199, ABT 199
T21191257044-40-8
Venetoclax (ABT-199) is a Bcl-2 inhibitor (Ki<0.01 nM) with potent, selective, and orally active properties. Venetoclax has a 3-order-of-magnitude lower affinity for Bcl-xL and Bcl-W (Kis=48 245 nM). Venetoclax induces autophagy and apoptosis.
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Olaparib
KU0059436, AZD2281
T3015763113-22-0
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.
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BAY-876
T37131799753-84-6In house
BAY-876 is an orally active, selective inhibitor of glucose transporter 1 (GLUT1, IC50= 2 nM), exhibiting over 130-fold greater selectivity for GLUT1 than GLUT2, GLUT3, and GLUT4. It also inhibits glycolytic metabolism and ovarian cancer growth.
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PLX5622
PLX-5622
T71001303420-67-8
PLX5622 is a highly selective, brain-penetrant, and orally active CSF1R inhibitor.
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Pantoprazole Sodium Hydrate
SKF96022 sodium hydrate, SKF96022 (sodium hydrate), BY1023 (sodium hydrate)
T0161164579-32-2
Pantoprazole Sodium Hydrate (BY1023 (sodium hydrate)) is a proton pump inhibitor drug, used for short-term treatment of erosion and ulceration of the esophagus caused by gastroesophageal reflux disease.
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TargetMol | Inhibitor Sale
L-DOPA
Levodopa, 3,4-Dihydroxyphenylalanine
T084859-92-7
L-DOPA (Levodopa) is an amino acid precursor of dopamine with antiparkinsonian properties. It is a prodrug converted to dopamine by DOPA decarboxylase and can cross the blood-brain barrier. In the brain, levodopa is decarboxylated to dopamine, stimulating dopaminergic receptors and compensating for depleted endogenous dopamine in Parkinson's disease. To ensure adequate concentrations reach the central nervous system, levodopa is administered with carbidopa, a decarboxylase inhibitor that does not cross the blood-brain barrier, reducing peripheral decarboxylation and increasing CNS dopamine delivery.
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Nicotinamide riboside
T137951341-23-7
Nicotinamide riboside increases NAD[+] levels and activates SIRT1 and SIRT3, culminating in enhanced oxidative metabolism and protection against high fat diet-induced metabolic abnormalities.
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Dasatinib
BMS-354825
T1448302962-49-8
Dasatinib (BMS-354825) is an orally active, ATP-competitive tyrosine kinase inhibitor that targets Src and Bcr-Abl (Ki=16 30 pM), with antitumor activity, used in the treatment of leukemia and lymphoma.
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Dasatinib monohydrate
BMS-354825 Monohydrate
T1448L863127-77-9
Dasatinib monohydrate (BMS-354825 Monohydrate) is an orally bioavailable synthetic small molecule-inhibitor of SRC-family protein-tyrosine kinases. Dasatinib monohydrate binds to and inhibits the growth-promoting activities of these kinases. Apparently, because of its less stringent binding affinity for the BCR-ABL kinase, Dasatinib monohydrate has been shown to overcome the resistance to imatinib of chronic myeloid leukemia (CML) cells harboring BCR-ABL kinase domain point mutations.
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3-(3,4-Dimethoxyphenyl)propanoic acid
3,4-Dimethoxyhydrocinnamic acid
T16922107-70-2
3-(3,4-Dimethoxyphenyl)propanoic acid (3,4-Dimethoxyhydrocinnamic acid) is an orally active short-chain fatty acid (SCFAs) that promotes γ-globin gene expression and erythropoiesis in vivo, making it useful in treating beta hemoglobinopathies and other anemias.
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Obeticholic Acid
INT-747, 6-Ethylchenodeoxycholic acid, 6-ECDCA
T1789459789-99-2
Obeticholic Acid (6-ECDCA, INT-747) is a high-affinity, semisynthetic, bile acid-derived FXR agonist with an EC50 of 99 nM and is able to upregulate IκB-α, KLF-2, and KLF-4 expression. Obeticholic Acid (6-ECDCA, INT-747) also shows potential for treating hepatic steatosis, inflammation, and fibrosis while increasing insulin sensitivity.
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Ponatinib
AP24534
T2372943319-70-8
Ponatinib (AP24534) is an orally available, multitargeted kinase inhibitor with IC50 values of 0.37 nM (Abl), 1.1 nM (PDGFRα), 1.5 nM (VEGFR2), 2.2 nM (FGFR1), and 5.4 nM (Src).
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Niraparib
MK-4827
T32311038915-60-4
Niraparib (MK-4827) is a PARP inhibitor that selectively targets PARP1 and PARP2 (IC50=3.8 2.1 nM), exhibiting antitumor activity, inhibiting DNA damage repair, and inducing apoptosis.
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Ranitidine
Ranitidin, HSDB 3925
T361066357-35-5
Ranitidine (HSDB 3925) is a non-imidazole blocker of those histamine receptors that mediate gastric secretion (H2 receptors). It is used to treat gastrointestinal ulcers.
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N,N'-Dimethylthiourea
DMTU
T40615534-13-4
N,N'-Dimethylthiourea (DMTU) (DMTU), isolated from Allii Sativi Bulbus, is an orally active scavenger of hydroxyl radical ( OH) and blocks OH production by activated neutrophils in vitro. N,N'-Dimethylthiourea protects against water-immersion restraint stress (WIRS)-induced gastric mucosal lesions in rats by exerting its antioxidant action including OH scavenging and anti-inflammatory action [1][2] .
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Nicotinamide riboside chloride
T622023111-00-4
Nicotinamide riboside chloride, also known as NR and SRT647, is a pyridine-nucleoside form of vitamin B3 that functions as a precursor to nicotinamide adenine dinucleotide or NAD+.
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Cysteamine hydrochloride
β-Mercaptoethylamine Hydrochloride, Thioethanolamine Hydrochloride, Cysteamine HCl, Bekaptan, 2-Mercaptoethylamine Hydrochloride, 2-Aminoethanethiol Hydrochloride
T6460156-57-0
Cysteamine hydrochloride (Thioethanolamine Hydrochloride) is an agent for the treatment of nephropathic cystinosis and an antioxidant.
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Troxipide
Aplace
T671030751-05-4
Troxipide (Aplace), a new-type systemic non-antisecretory gastric cytoprotective agent, which is mucus-secreting, anti-ulcer, and anti-inflammatory properties irrespective of pH of stomach or duodenum.
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Niraparib tosylate monohyrate
T94971613220-15-7
Niraparib, also know as MK-4827, is an inhibitor of poly (ADP-ribose) polymerase (PARP) with potential antineoplastic activity. MK4827 inhibits PARP activity, enhancing the accumulation of DNA strand breaks and promoting genomic instability and apoptosis. The PARP family of proteins detect and repair single strand DNA breaks by the base-excision repair (BER) pathway.
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Emedastine
LY188695, Emadine
T397987233-61-2
Emedastine (LY188695) is a second generation, selective histamine H1 receptor antagonist with anti-allergic activity. Emedastine reversibly and competitively blocks histamine by binding to H1 receptors, thus blocking its downstream activity. As a result this agent interferes with mediator release from mast cells either by inhibiting calcium ion influx across mast cell basophil plasma membrane or by inhibiting intracellular calcium ion release within the cells. In addition, emedastine may also inhibit the late-phase allergic reaction mediated through leukotrienes or prostaglandins, or by producing an anti-platelet activating factor effect. Upon ocular administration, emedastine causes a dose-dependent inhibition of histamine-stimulated vascular permeability in the conjunctiva. Emedastine does not affect adrenergic, dopamine, or serotonin receptors.
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