2-Amino-6-meThythio-9-(β-D-ribofuranosyl)-9H-purine 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[1].
Brazilin is a red dye precursor obtained from the heartwood of several species of tropical hardwoods. Brazilin inhibits the cells proliferation, promotes apoptosis, and induces autophagy through the AMPK/mTOR pathway. Brazilin shows chondroprotective and anti-inflammatory activities[1][2][3].
RS-1 is a RAD51 activator, and also increases CRISPR/Cas9-mediated knock-in efficiencies.
Tetrahydrocoptisine is an alkaloid compound originally isolated from Corydalis tubers that exhibits anti-inflammatory and anti-parasitic activities.IC50 value:Target:in vitro: THC significantly inhibited LPS-induced TNF-α, interleukin-6(IL-6) and nitric oxide (NO) production. THC inhibited the production of TNF-α and IL-6 by down-regulating LPS-induced IL-6 and TNF-α mRNA expression [1].in vivo: Pretreatment with THC (i.p.) inhibited the paw and ear edema in the carrageenan-induced paw edema assay and xylene-induced ear edema assay, respectively. In the lipopolysaccharide (LPS)-induced systemic inflammation model, THC significantly inhibited serum tumor necrosis factor-alpha (TNF-α) release in mice [1]. Pretreatment of THC at doses of 10 and 20mg/kg bodyweight significantly attenuated the gastric lesions as compared to the ethanol group [2].
Kuwanon K is a natural product that can be isolated from Morus Lhou[1].
NCI172112 is a classical bifunctional alkylating agent synthesized in an effort to develop antitumor agents effective against CNS tumors.
Drisapersen, a antisense oligonucleotide, induces exon 51 skipping during dystrophin pre-mRNA splicing and allows synthesis of partially functional dystrophin in Duchenne muscular dystrophy (DMD) patients with amenable mutations.
2,6-Dichloroquinone-4-chloroimide is a spray reagent for organic compounds. 2,6-Dichloroquinone-4-chloroimide can be used in thin-layer chromatograms. 2,6-Dichloroquinone-4-chloroimide can be used as an optical sensor for rapid detection of permethrin in treated wood[1][2].
E-6123 is a platelet-activating factor (PAF) receptor antagonist.
α-Eleostearic acid (cis-Eleostearic acid), a conjugated linolenic acid, is an apoptosis inducer. α-Eleostearic acid is also a ferroptosis inducer. α-Eleostearic acid exhibits antioxidant and antitumor activity[1][2][3].
Mitoguazone (Methylglyoxal-bis(guanylhydrazone)) is a synthetic polycarbonyl derivative with potent antineoplastic activity. Mitoguazone is a brain-penetrant and competitive S-adenosyl-methionine decarboxylase (SAMDC) inhibitor that disrupts polyamine biosynthesis. Mitoguazone induces cell apoptosis. Mitoguazone inhibits HIV DNA integration into the cellular DNA in both monocytes and macrophages. Mitoguazone has the potential for acute leukemia, Hodgkin's and non-Hodgkin's lymphoma treatment[1][2][3][4].
M2698 (MSC2363318A) is an orally active, ATP competitive, selective p70S6K and Akt dual-inhibitor with IC50s of 1 nM for p70S6K, Akt1 and Akt3. M2698 can cross the blood-brain barrier and has anti-cancer activity[1].
Mal-PEG2-NH-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
HPGDS inhibitor 1 is a novel and selective Hematopoietic Prostaglandin D Synthase (HPGDS) inhibitor with an IC50 Value of 0.7 nM.IC50 Value: 0.7 nM [1]Target: HPGDSHPGDS inhibitor 1 was elected for further profiling based on its enzyme and cell potency. The compound illustrated equal potency against purified HPGDS from human , rat, dog, and sheep (IC50, 0.5-2.3 nM). HPGDS inhibitor 1 was profiled in a panel of cellular assays to screen for activity against several relevant human enzyme targets. Those assay indicated that HPGDS inhibitor 1 does not inhibit human L- PGDS, m-PGDS, COX-1, COX-2 or 5 LOX (IC50 values > 10000 nM).HPGDS inhibitor 1 had a solubility of 1.5 ug/ml (3.9 uM) at pH 6.5. The compound had excellent PK characteristics when dosed in rats at 1 mpk with 76% bioavailavility. Rats dosed orally with 1 and 10 mpk HPGDS inhibitor 1 were sacrificed at various times, and plasma concentrations of HPGDS inhibitor 1 and spleen PGD2 concentrations were measured. Oral administration of HPGDS inhibitor 1 blocked PGD2 production in the rat spleen; inhibition of PGD2 was inversely correlated with the plasma concentration of HPGDS inhibitor 1 in a time and dose-dependent manner. Spleen PGD2 levels fall as HPGDS inhibitor 1 plasma levels increase over time; PGD2 levels return to baseline levels as HPGDS inhibitor 1 plasma levels decline.
pTH (44-68) (human) is apTH ((Human parathyroid hormone) fragment.
Myrciaphenone A is an acetophenone glucoside[1].
Ganoderone A is a triterpene compound that can be isolated from the fruiting body of Ganoderma pfeifferi and Ganoderma calidophilum. Ganoderone A has antiviral activity against HSV with IC50 value of 0.3 µg/mL. Ganoderone A has potential applications in viral infections and tumors[1][2][3].
E7766 disodium is a macrocycle-bridged STING agonist with a Kd of 40 nM. E7766 disodium shows potent pan-genotypic and antitumor activities[1].
5-Hydroxymethyl-2’-β-C-methyluridine is a thymidine analogue. Analogs of this series have insertional activity towards replicated DNA. They can be used to label cells and track DNA synthesis[1].
Ascr#5 is a highly conserved ascaroside isolated from Caenorhabditis elegans.
W-7 hydrochloride is a selective calmodulin antagonist. W-7 hydrochloride inhibits the Ca2+-calmodulin-dependent phosphodiesterase and myosin light chain kinase with IC50 values of 28 μM and 51 µM, respectively[1][2]. W-7 hydrochloride induces apoptosis and has antitumor activity[3].
pTH (7-84) (human) is a biologically active peptide.
MARK-IN-4 is a potent microtubule affinity regulating kinase (MARK) inhibitor with an IC50 of 1 nM. Inhibition of microtubule affinity regulating kinase (MARK) represents a potentially attractive means of arresting neurofibrillary tangle pathology in Alzheimer's disease[1].
Dexloxiglumide is a selective cholecystokinin type A (CCKA) receptor antagonist[1]. Dexloxiglumide, the active enantiomer of Loxiglumide, inhibits smooth muscle cell contractions induced by cholecystokinin-octapeptide (CCK-8)[2].
S16961 is a nicotinic receptor agonist.
Pantothenate kinase-IN-2 is a potent Pantothenate kinase 1/3 (PanK1/3) inhibitor with an IC50 of 0.14 μM and 0.36 μM. Pantothenate kinase-IN-2 is a promising agent for PKAN (PanK-associated neurodegeneration) and diabetes research[1].
STING agonist-33 (example 1) is an agonist of STING (stimulator of interferon genes) based on 4-ethyl-2-methylthiazole-5-carboxylic acid[1].
N-(3-Nitro-2-pyridinesulfenyl)-O-t-butyl-L-tyrosine is a tyrosine derivative[1].
Fmoc-Phe(F5)-OH is a phenylalanine derivative[1].
CDK4/6-IN-16 (example 195) is a potent CDK4 and CDK6 inhibitor, with an IC50 of 0.013 μM for CDK4. CDK4/6-IN-16 can be used for the research of CDK4-mediated disorders, such as cancer[1].