Boc-Ser(Tos)-OMe is a serine derivative[1].
Fosteabine is an oral and prodrug analogue of cytarabine which is resistant to deoxycytidine deaminase.
2,5-Dioxopyrrolidin-1-yl acrylate (N-Succinimidyl acrylate) is a protein crosslinker. 2,5-Dioxopyrrolidin-1-yl acrylate can react with a monoclonal anti-horseradish peroxidase IgG antibody (anti-HRP) to modify lysine residues[1].
Methyl α-D-galactopyranoside monohydrate is an alpha-D-galactoside having a methyl substituent at the anomeric position. Methyl α-D-galactopyranoside inhibits debaryomyces hansenii UFV-1 extracellular and intracellular α-galactosidases with Ki values of 0.82 and 1.12 mM, respectively[1].
(R)-2-Amino-2-(4-fluorophenyl)acetic acid hydrochloride is a Glycine (HY-Y0966) derivative[1].
Erythromycin dihyrate dihydrate is a macrolide antibiotic produced by actinomycete Streptomyces erythreus with a broad spectrum of antimicrobial activity. Erythromycin dihyrate acts by binding to bacterial 50S ribosomal subunits and inhibits RNA-dependent protein synthesis by blockage of transpeptidation and/or translocation reactions, without affecting synthesis of nucleic acid[1].
Cabazitaxel is a semi-synthetic derivative of the natural taxoid 10-deacetylbaccatin III with potential antineoplastic activity.
PF-04856264 is a potent and selective Nav1.7 inhibitor, with IC50s of 28, 131, 19, and 42 nM for human, mouse, cynomolgus monkey and dog Nav1.7, respectively. PF-04856264 has low potency against the rat Nav1.7 channel. PF-04856264 shows analgesic effect[1][2].
GNE-049 is a highly potent and selective CBP inhibitor with an IC50 of 1.1 nM in TR-FRET assay. GNE-049 also inhibits BRET and BRD4(1) with IC50s of 12 nM and 4200 nΜ, respectively.
Endokinin C is a peptide component of endokinin. Endokinin C works as a neurotransmitter or modulator in the pain system. Pretreatment with endokinin C prevents induction of scratching behavior and thermal hyperalgesia of endokinin A/B in mice[1].
Enterostatin, human, mouse, rat is a pentapeptide that reduces fat intake.
Risarestat (CT-112), an aldose reductase inhibitor, is developed for the treatment of diabetic complications.
Lovastatin-d3 is deuterium labeled Lovastatin. Lovastatin is a cell-permeable HMG-CoA reductase inhibitor used to lower cholesterol.
Clofibrate is an agonist of PPAR, with EC50s of 50 μM, ∼500 μM for murine PPARα and PPARγ, and 55 μM, ∼500 μM for human PPARα and PPARγ, respectively.
NVP-TAE 226 is a dual tyrosine kinase inhibitor of FAK (IC50=5.5 nM) and IGF-IR (mean IC50=0.14 μM).
Gitoxigenin is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
NVP-BBD130 is a potent, stable, ATP-competitive and orally active dual PI3K and mTOR inhibitor[1].
Metolazone(Zaroxolyn) is primarily used to treat congestive heart failure and high blood pressure.Target: OthersMetolazone is a thiazide-like diuretic marketed under the brand names Zytanix from Zydus Cadila, Zaroxolyn, and Mykrox. It is primarily used to treat congestive heart failure and high blood pressure. Metolazone indirectly decreases the amount of water reabsorbed into the bloodstream by the kidney, so that blood volume decreases and urine volume increases. This lowers blood pressure and prevents excess fluid accumulation in heart failure. Metolazone is sometimes used together with loop diuretics such as furosemide or bumetanide, but these highly effective combinations can lead to dehydration and electrolyte abnormalities.Metolazone and the other thiazide diuretics inhibit the function of the sodium-chloride symporter, preventing sodium and chloride, and therefore water too, from leaving the lumen to enter the tubule cell. As a result, water remains in the lumen and is excreted as urine, instead of being reabsorbed into the bloodstream. Since most of the sodium in the lumen has already been reabsorbed by the time the filtrate reaches the distal convoluted tubule, thiazide diuretics have limited effects on water balance and on electrolyte levels. Nevertheless, they can be associated with low sodium levels, volume depletion, and low blood pressure, among other adverse effects.
SLU-PP-915 is an agonist of ERR. SLU-PP-915 has an EC50 value of approximately 400 nM for ERRα, ERRβ, and ERRγ. SLU-PP-915 has potential application in maintaining oxidative metabolism and heart failure[1][2][3].
IDRA 21 is a positive and orally active modulator of the AMPA receptor. IDRA 21 facilitates excitatory neurotransmission via GluR1/2 receptors. IDRA 21 has the potential for the research of cognitive/memory disorders, including those associated with aging[1].
5′-Amino-5′-deoxythymidine 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].
PSI-6206 13CD3 is the deuterium labeled PSI-6206. PSI-6206 is the deaminated derivative of PSI-6130, which is a potent and selective inhibitor of HCV NS5B polymerase. PSI-6206 low potently inhibits HCV replicon with EC90 of >100 μM.
(S)-methyl 2-((S)-4-methyl-2-((S)-2-(2-morpholinoacetamido)-4-phenylbutanamido)pentanamido)-3-phenylpropanoate is a phenylalanine derivative[1].
Pomalidomide-5-O-CH3 is the Pomalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein. Pomalidomide-5-O-CH3 can be connected to the ligand for protein by a linker to form PROTAC[1].
Cimiracemoside D is a natural product found in Actaea racemosa with unknown details.
Cevipabulin(TTI-237) is a novel, potent, synthetic small molecule, inhibits binding of vinblastine at the Vinca alkaloid site of the αβ-tubulin heterodimer.IC50 value: Target: Antimicrotubule agentin vitro: TTI-237 inhibited the binding of [(3)H]vinblastine to tubulin, but it caused a marked increase in turbidity development that more closely resembled the effect observed with docetaxel than that observed with vincristine. When applied to cultured human tumor cells at concentrations near its IC(50) value for cytotoxicity (34 nmol/L), TTI-237 induced multiple spindle poles and multinuclear cells, as did paclitaxel, but not vincristine or colchicine. Flow cytometry experiments revealed that, at low concentrations (20-40 nmol/L), TTI-237 produced sub-G(1) nuclei and, at concentrations above 50 nmol/L, it caused a strong G(2)-M block. The compound was a weak substrate of multidrug resistance 1 (multidrug resistance transporter or P-glycoprotein). In a cell line expressing a high level of P-glycoprotein, the IC(50) of TTI-237 increased 25-fold whereas those of paclitaxel and vincristine increased 806-fold and 925-fold, respectively. TTI-237 was not recognized by the MRP or MXR transporters [1]. TTI-237 inhibited the exchange of [(3)H]GTP at the exchangeable nucleotide site of the tubulin heterodimer, and was similar to vincristine in its effects on the phosphorylation of eight intracellular proteins in HeLa cells [3].in vivo: TTI-237 was active in vivo in several nude mouse xenograft models of human cancer, including LoVo human colon carcinoma and U87-MG human glioblastoma, when dosed i.v. or p.o [1].
Thyminose-13C-1 is the 13C labeled Thyminose. Thyminose is an endogenous metabolite[1].
DL-Asarinin (compound 88) is a natural product that can be found in waste leaves of Cinnamomum camphora[1].
Drahebenineis animidazole alkaloidthatcan be found in Dracocephalum heterophyllum[1].
Zonisamide-d4 (AD 810-d4) is the deuterium labeled Zonisamide. Zonisamide (AD 810) is an inhibitor of zinc enzyme carbonic anhydrase (CA), with Kis of 35.2 nM and 20.6 nM for human mitochondrial isozyme hCA II and hCA V, respectively. Zonisamide has antiepileptic activity. Zonisamide can be used for the rsearch for epilepsy, seizures and Parkinson's disease[1][2].