Blasticidin S hydrochloride is a nucleoside antibiotic isolated from Streptomyces griseochromogenes. Blasticidin S is a potent inhibitor of protein synthesis in both prokaryotic and eukaryotic cells[1].
Papain inhibitor (Glycylglycyl-L-tyrosyl-L-arginine) acts as an effective competitive inhibitor to papain, with a Ki of 9 μM at pH 6.2[1].
Ciraparantag TFA is a thrombin and factor Xa inhibitor. Ciraparantag TFA is a broad-spectrum reversal agent for anticoagulants, including low-molecular-weight heparin, unfractionated heparin, and certain direct oral anticoagulants. It is reported to antagonize the effects of all coagulants except VKAs and agratroban[1][2][3][4].
Altretamine is an alkylating antineoplastic agent.
((4-Chloro-3-(trifluoromethyl)phenyl)sulfonyl)proline is a proline derivative, contains both an amino group and a carboxyl group in its molecule.
Tacrine hydrochloride hydrate is an inhibitor of both acetyl (AChE) and butyryl-cholinestrase (BChE) with IC50s of 31 nM and 25.6 nM, respectively.
CW-069 is an allosteric inhibitor of HSET with an IC50 of 75 μM.
XMD8-92 is a highly selective ERK5/BMK1 inhibitor with dissociation constant (Kd) value of 80 nM.
Phorbol 12-tiglate is a derivative of Phorbol (HY-N2147). Phorbol, a hydrolyzed product of Croton oil, promotes tumor development by activating protein kinase C. Phorbol and its derivatives can be used to construct carcinogenic models in biomedical research[1].
The product is the analog of the NSC601980, NSC601980 shows antitumor activity in the yeast screening experiment, which can inhibit cell proliferation in the COLO 205 and HT29 with Log GI 50 of -6.6 and -6.9 respectively.
2-Methoxy-6-pentadecyl-1,4-benzoquinone (1c) is a pentadecyl derivative that can be isolated from seed oils of different iris plants such as I. pseudacorus, I. missouriensis and I. sibirica[1].
Mezlocillin sodium is a broad-spectrum penicillin antibiotic. It is active against both Gram-negative and some Gram-positive bacteria.Target: AntibacterialMezlocillin sodium is penicillin antibiotic, prescribed for certain types of bacterial infections.
Stains-All is a cationic carbocyanine dye.
Hypoxanthine-13C2,15N is a 15N-labeled and 13C-labled DL-Cystine[1].
GSK-7975A is a potent and orally available CRAC channel inhibitor.
Ethyl pyruvate is a simple derivative of the endogenous metabolite, pyruvic acid. Ethyl pyruvate is an anti-inflammatory agent[1].
Prexasertib dimesylate (LY2606368 dimesylate) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib dimesylate inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib dimesylate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib dimesylate shows potent anti-tumor activity[1][2].
Chlordantoin is an antifungal drug which can be used to treat vaginal candidiasis.
Felbamate hydrate (FBM) is a potent nonsedative anticonvulsant whose clinical effect may be related to the inhibition of N-methyl-D-aspartate (NMDA) .Target: NMDA ReceptorFelbamate (marketed under the brand name Felbatol by MedPointe) is an anti-epileptic drug used in the treatment of epilepsy. It is used to treat partial seizures (with and without generalization) in adults and partial and generalized seizures associated with Lennox-Gastaut syndrome in children. However, an increased risk of potentially fatal aplastic anemia and/or liver failure limit the drugs usage to severe refractory epilepsy.Felbamate has been proposed to a unique dual mechanism of action as a positive modulator of GABAA receptors and as a blocker of NMDA receptors, particularly isoforms containing the NR2B subunit. Although it is clear that felbamate does cause pharmacological inhibition of NMDA receptor of relevance of NMDA receptor blockade as a strategy for the treatment of human epilepsy has been questioned. Therefore, the importance of the effects of felbamate on NMDA receptors to its therapeutic action in epilepsy is uncertain.
Cefoperazone sodium salt is a cephalosporin antibiotic for inhibition of rMrp2-mediated [3H]E217βG uptake with IC50 of 199 μM.Target: AntibacterialCefoperazone is a sterile, semisynthetic, broad-spectrum, parenteral cephalosporin antibiotic for intravenous or intramuscular administration. After intravenous administration of 2 g of Cefoperazone, levels in serum rang from 202μg/mL to 375 μg/mL depending on the period of drug administration. After intramuscular injection of 2 g of Cefoperazone, the mean peak serum level is 111 μg/mL at 1.5 hours. At 12 hours after dosing, mean serum levels are still 2 to 4 μg/mL. Cefoperazone is 90% bound to serum proteins.
NMDA receptor modulator 5 (Compound 195) is a potent NMDA receptor modulator. NMDA receptor modulator 5 can be used for neurological disorder research[1].
Rhein is a lipophilic anthraquinone extensively found in medicinal herbs, and has many pharmacological effects, including epatoprotective, nephroprotective, anti-inflammatory, antioxidant, anticancer, and antimicrobial activities. IC50 value:Target:In vitro: Rhein (0.1 and 1 mg/mL) evidently suppressed cell proliferation and mitogen-activated protein (MAP) kinase activation in human colon adenocarcinoma cells (Caco-2) but significantly lessened H2O2-induced DNA damage and the elevated MDA and ROS levels induced by H2O2/Fe2+ at the concentrations of 0.1–10 mg/mL [1].In vivo: Oral administration of rhein (150 mg/kg/d) evidently ameliorated renal interstitial fibrotic lesions and attenuated the expression of α-SMA and deposition of fibronectin (FN) in mice with renal interstitial fibrosis induced by unilateral ureteral obstruction. Rhein also suppressed TGF-β1 and its type I receptor expression in obstructed kidneys [1]. The biochemical parameters results of IgAN model rats showed that rhein-prevented and rhein-treated both improved the biochemical parameters and relieved renal pathological injury. The expressions of renal tissue TLR4, TGF-β1, but not TLR9 were significantly elevated in IgAN model rats (P < 0.05). Rhein-prevented and rhein-treated both inhibited TLR4 and TGF-β1 expressions [2].
Pifithrin-α, p-Nitro, Cyclic (PFN-α) is cell-permeable and active-form p53 inhibitor. Pifithrin-α, p-Nitro, Cyclic is one order magnitude more active than Pifithrin-α in protecting cortical neurons exposed to Etoposide (ED50=30 nM). Pifithrin-α, p-Nitro, Cyclic behaves as a p53 posttranscriptional activity inhibitor. Pifithrin-α, p-Nitro, Cyclic do not prevent p53 phosphorylation on the S15 residue[1][2].
THPN is a potent Nur77 agonist. THPN specifically binds the LBD of Nur77 (TR3) but not that of retinoic acid receptor α and PPARγ with a Kd of 270 nM. THPN leads to Nur77 translocation to the mitochondria to induce autophagic cell death in melanoma[1][2].
BRD3308 is a potent, selective HDAC3 inhibitor with IC50 of 54 nM, displays >20-fold selectivity over HDAC1 and HDAC2, >500-fold selectivity over other HDAC isoforms; attenuates PE-mediated phosphorylation of ERK, but not JNK; also activates HIV-1 transcription in the 2D10 cell line, induces outgrowth of HIV-1 from resting CD4+ T cells isolated from antiretroviral-treated, aviremic HIV+ patients ex vivo and disrupts HIV-1 latency; suppresses pancreatic β-cell apoptosis induced by inflammatory cytokines or glucolipotoxic stress, and increases functional insulin release.
Millewanin G is a prenylated isoflavonoid with antiestrogenic activity (IC50=29 μM). Millewanin G can be isolated from the leaves of M. pachycarpa cultivated in Japan[1].
ChemR23-IN-2 is a potent and orally efficacious ChemR23 inhibitor with an IC50 value of 3.2 nM.
Thalrugosaminine is a benzylisoquinoline alkaloid isolated from the roots of Thalictrum minus. Thalrugosaminine shows good antibacterial activity with MIC values of 64-128 µg/ml[1].
Eflepedocokin alfa is a recombinant fusion protein with potential cell protective activity. Eflepedocokin alfa consists of human IL-22 fused to human IgG2-Fc domain. Eflepedocokin alfa leads to the activation of IL-22/IL-22R-mediated signal transduction pathways as well as STAT3. Eflepedocokin alfa plays a role in immune response and bacterial infection, enhancing intestinal barrier function, intestinal immunity, and tissue repair[1].
Minerval (2-Hydroxyoleic acid) is a synthetic oleic acid (OA) derivative that binds to the plasma membrane and alters lipid organization. Minerval has anti-tumor effect[1].