PDE5-IN-9 (Compound 59) is a PDE5 inhibitor (IC50: 11.2 μM). PDE5-IN-9 shows interaction with Gln 817, Tyr 612, and Ala 767 amino acid residues. PDE5-IN-9 can be used for research of cardiovascular disease[1].
Danofloxacin-d3 is deuterium labeled Danofloxacin. Danofloxacin is a third generation fluoroquinolone and orally active antimicrobial agent. Danofloxacin shows a broad spectrum of activity against most Gram-negative and Gram-positive bacteria, mycoplasma and chlamydia species, and plays an antimicrobial role by inhibition of bacterial DNA-gyrase[1][2].
Prodigiosin (Prodigiosine) is a secondary metabolite of Symbiotic bacteria, with anti-fungal and anti-cancer activity[1][2].
TBI-223 is an orally bioavailable oxazolidinone antibiotic and an antimicrobial. TBI-223 shows activity against Mycobacterium tuberculosis (Mtb)[1][2].
Hydroxytanshinone IIA is a hydroxylated metabolite of Tanshinone IIA. Tanshinone IIA may suppress angiogenesis by targeting the protein kinase domains of VEGF/VEGFR2[1].
Dacinostat is a potent HDAC inhibitor, with an IC50 of 32 nM; Dacinostat also inhibits HDAC1 with an IC50 of 9 nM, and used in cancer research.
Perospirone (SM-9018 free base) is an orally active antagonist of 5-HT2A receptor (Ki=0.6 nM) and dopamine D2 receptor (Ki=1.4 nM), and also a partial agonist of 5-HT1A receptor (Ki=2.9 nM). Perospirone is an atypical antipsychotic drug and has the potential for schizophrenic disease[1][2].
Avasopasem manganese (GC4419; M-40419) is a potent superoxide dismutase mimetic that rapidly and specifically converts O2*- to hydrogen peroxide (H2O2), arresting the initiation of this cascade. Avasopasem manganese can be used for the research of severe oral mucositis (SOM) and cancer[1].
N-Me-Val-Leu-anilide is a biologically active peptide.
Ald-CH2-PEG5-azide is a non-cleavable 5 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
3β-Ursodeoxycholic acid (Isoursodeoxycholic acid) is a bile acid. 3β-Ursodeoxycholic acid (Isoursodeoxycholic acid) shows good tolerance and well intestinal absorption by oral adminstation. 3β-Ursodeoxycholic acid (Isoursodeoxycholic acid) can be isomerized by intestinal and hepatic enzymes to yield UDCA[1].
(2R)-2-Amino-3-(methylsulfinyl)propanoic acid is a cysteine derivative[1].
Semaxinib (SU5416) is a potent and selective inhibitor of the vascular endothelial growth factor receptor (Flk-1/KDR) with an IC50 of 1.23 μM.
pNP-ADPr is a colorimetric substrate that used for the first continuous Poly(ADP-ribose) glycohydrolase (PARG) and ADP-ribosyl hydrolase 3 (ARH3) activity assays. pNP-ADPr can be used for the research of poly(ADP-ribose)polymerase (PARP) enzymes[1][2].
Niflumic Acid-d5 is the deuterium labeled Niflumic acid. Niflumic acid, a Ca2+-activated Cl- channel blocker, is an analgesic and anti-inflammatory agent used in the treatment of rheumatoid arthritis[1][2].
MART-1 (27-35) (human) is an immunogenic epitope recognized by HLA-A2-restricted melanoma-specific tumor-infiltrating lymphocytes (TIL)[1].
LY315920 (Varespladib) is a potent and selective human non-pancreatic secretory phospholipase A2 (sPLA) inhibitor with IC50 of 7 nM.IC50 value: 7 nMTarget: sPLA2in vitro: LY315920 exhibits the significant inhibitory effect on sPLA2 activity in serum from various species including rat, rabbit, guinea pig and human with IC50 of 8.1 nM, 5.0 nM, 3.2 nM and 6.2 nM, respectively. [2] In BAL cells challenged with human sPLA2, LY315920 at doses ranging from 0.1 μM–3 μM reduces the formation of thromboxane mediated by human sPLA2 in a concentration-dependent manner with an IC50 of approximately 0.8 μM. [2] In human conjunctival epithelial cell line (HCjE), LY315920 (10 μM) significantly inhibits all-trans-retinoic acid (RA) -induced membrane-associated mucin MUC16 expression by 100% at 24 hours and 99% at 48 hours. [3]in vivo: Ex vivo, LY315920 at doses ranging from 3 mg/kg to 30 mg/kg via i.v. inhibits human sPLA2-induced release of thromboxane from guinea pig BAL cells with ED50 of 16.1 mg/kg. [2] In Transgenic Mice Expressing Human sPLA2, both oral and i.v. administration of LY315920 (0.3 mg/kg–3 mg/kg) abolishes serum sPLA2 activity in a dose and time dependent manner. [2]
Panepoxydone is an inhibitor of NF-κB activation. Panepoxydone interferes with the NF-κB mediated signal transduction by inhibiting the phosphorylation of IκB. Panepoxydone exhibits antitumor, anti-inflammatory, antimalarial and anti-parasitic activity[1][2].
(S)-2-Amino-3-(3-nitrophenyl)propanoic acid is a phenylalanine derivative[1].
Boc-NH-PEG9-azide is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Adenosine 5'-monophosphate disodium is an orally active purine nucleotide, and participates in ATP metabolism. Adenosine 5'-monophosphate disodium is also a ligand for adenosine 2B receptor. Adenosine 5'-monophosphate disodium can activate AMPK in skeletal muscle, and ameliorates insulin resistance and impaired glucose metabolism. Adenosine 5'-monophosphate disodium can be used for research of diabetes[1][2][3].
Etofenamate-d4 is the deuterium labeled Etofenamate. Etofenamate, a non-steroid anti-inflammatory drug (NSAID) and a non-selective COX inhibitor, possesses analgesic, anti-rheumatic, antipyretic and anti-inflammatory properties. Etofenamate is used in the research for osteoarthritis, arthritis and other inflammatory diseases[1][2][3].
Z-DEVD-FMK is a specific and irreversible caspase-3 inhibitor with IC50 of 18 μM.
BAY-3827 is a potent and selective AMPK inhibitor with IC50 values of 1.4 nM at low (10 µM ATP concentration) and 15 nM at high (2 mM ATP concentration). BAY-3827 shows over 500-fold selectivity for most of the 331 kinases. BAY-3827 prevents phosphorylation of acetyl-CoA carboxylase 1 and shows strongest anti-proliferative activity in androgen-dependent prostate cancer cell lines[1].
Moth Cytochrome C (MCC) (88-103), derived from the carboxyl terminus of moth cytochrome c, induces positive selection of TCR transgenic thymocytes[1].
Amentoflavone is a natural biflavone compound with many biological properties, including anti-inflammatory, antioxidative, and neuroprotective effects.IC50 value:Target:In vitro: In irradiated v79 cells, Pretreatment with amentoflavone 24 hours prior to 8 Gy 60Co γ-ray irradiation significantly inhibited apoptosis, promoted the G2 phase, decreased the concentration of ROS and mitochondrial mass [2]. Amentoflavone dose-dependently inhibited the viability of SW480 cells, and a high concentration of amentoflavone (150 μmol/L) obviously induced apoptosis of the cells [3]. In vivo: In epilepsy models, amentoflavone effectively prevented pilocarpine-induced epilepsy in a mouse kindling model, suppressed nuclear factor-κB activation and expression, inhibited excessive discharge of hippocampal neurons resulting in a reduction in epileptic seizures, shortened attack time, and diminished loss and apoptosis of hippocampal neurons [1].
BDP FL-PEG4-TCO is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Senexin C is a novel potent, selective and orally bioavailable CDK8/19 inhibitor with Kd of 1.4 and 2.9 nM for CDK8/CycC and CDK19/CycC, respectively.Senexin C inhibits CDK8/CycC with IC50 of 3.6 nM, shows high selectivity against other HDAC isoforms.Senexin C is more metabolically stable and provides a more sustained inhibition of CDK8/19-dependent cellular gene expression when compared with the prototype inhibitor Senexin B.Senexin C inhibits MV4-11 leukemia growth in a systemic in vivo model with good tolerability.
Bendazac is an oxyacetic acid with anti-inflammatory, antinecrotic, choleretic and antilipidaemic properties. Bendazac acts by preventing protein denaturation and delays the cataractogenic process[1][2].
Brilliant blue R250 (Brilliant Blue R), an anionic dye, is the most popular stain to detect proteins resolved in SDS-PAGE gels[1].