Oridonin, a diterpenoid isolated from Rabdosia rubescens, acts as an inhibitor of AKT, with IC50s of 8.4 and 8.9 μM for AKT1 and AKT2; Oridonin possesses anti-tumor, anti-bacterial and anti-inflammatory effects.
Alisol A 23-acetate is a natural product that can be isolated from Rhizoma Alismatis[1].
Estramustine is an antineoplastic agent. Estramustine depolymerizes microtnbules by binding to tubulin 1, exhibits antimitotic activity with an IC50 value of ~16 μM for mitosis of DU 145 cells. Estramustine blocks cells at mitosis in prostate tumor xenografts[1].
NADP disodium salt is a participant coenzyme in aerobic and anaerobic oxidations.
Boc-N-Me-DL-Val-OH is a valine derivative[1].
Suptavumab (REGN2222) is a human monoclonal antibody. Suptavumab can bind and block a conserved epitope on RSV A and B subtypes. Suptavumab can be used for the research of RSV infection[1][2].
Tat-NR2BAA is the control peptide of Tat-NR2B9c (HY-P0117), inactive. The sequence of Tat-NR2BAA is similar to Tat-NR2B9c, but it has a double-point mutation in the COOH terminal tSXV motif, making it incapable of binding PSD-95. Tat-NR2B9c is a membrane-permeant peptide and disrupts PSD-95/NMDAR binding, correlate with uncoupling NR2B- and/or NR2A-type NMDARs from PSD-95[1][2].
Methyl diethyldithiocarbamate-d3 is the deuterium labeled Methyl diethyldithiocarbamate[1].
2'-Hydroxy-1'-acetonaphthone is a Schiff base used as pharmaceutical intermediates[1].
Nevanimibe hydrochloride (PD-132301 hydrochloride; ATR101 hydrochloride) is a selective and potent acyl-coenzyme A:cholesterol O-acyltransferase 1 (ACAT1) inhibitor with an EC50 of 9 nM. Nevanimibe hydrochloride (PD-132301 hydrochloride; ATR101 hydrochloride) inhibits ACAT2 with an EC50 of 368 nM[1].
Vicenin 3 is an angiotensin-converting enzyme (ACE) inhibitor (IC50=46.91 μM) from the aerial parts of Desmodium styracifolium[1].
Cephaeline is a phenolic alkaloid in Indian Ipecac roots. Cephaeline exhibits potent inhibition of both Zika virus (ZIKV) and Ebola virus (EBOV) infections[1][2].
PB2 is a tris(2-carboxyethyl)phosphine (TCEP) analogue increasing retinal ganglion (RGCs) cells survival after axotomy in vitro at nanomolar and picomolar concentrations. PB2 is substantially more permeable than TCEP. PB2, as a reducing agent, is highly neuroprotective for RGCs[1].
Levoglucosenone is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
Methyl 2-(((benzyloxy)carbonyl)amino)acrylate is an alanine derivative[1].
Peptide F, bovine is a proenkephalin peptide F from in bovine brain and adrenal medulla. Enkephalinergic system involves in pain transmission[1].
3-Oxobetulin, an antifungal agent, shows antifungal activities against white rot fungus L. betulina and the brown rot fungus L. sulphureus[1].
Gadobutrol (Gd-DO3A-butrol; ZK 135079) is a nonionic, paramagnetic contrast agent developed for tissue contrast enhancement in magnetic resonance imaging (MRI).IC50 value:Target: The major chemical differences among these Gd chelates or Gd-based contrast agents (GBCAs) are the presence or absence of overall charge, ionic or nonionic, and their ligand frameworks (linear or macrocyclic). Gd-DO3A-butrol has a macrocyclic framework and is neutral. The DO3A-butrol ligand was developed based on the belief that high overall hydrophilicity of an agent is generally associated with very low protein binding and good biological tolerance. The Gd(III) in Gd-DO3A-butrol has a coordination number of 9. Gd-DO3A-butrol is a water-soluble, highly hydrophilic compound with a partition coefficient between n-butanol and buffer at pH 7.6 of ~ 0.006. Gd-DO3A-butrol is not commercially available in the United States, but it is commercially available in Canada at a concentration of 1.0 mmol/ml (604.72 mg/ml) for contrast enhancement during cranial and spinal imaging with MRI and MR angiography.
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].
RS-1 is a RAD51 activator, and also increases CRISPR/Cas9-mediated knock-in efficiencies.
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].
Kuwanon K is a natural product that can be isolated from Morus Lhou[1].
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].
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.
NCI172112 is a classical bifunctional alkylating agent synthesized in an effort to develop antitumor agents effective against CNS tumors.
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].
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.