Triethylene glycol monododecyl ether is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Ajugasterone C is an ecdysteroid isolated from Leuzea carthamoides. Ajugasterone C shows significant inhibitory effect at 100 mg/kg dose on rat paw oedema development due to Carrageenan-induced inflammation in Sprague Dawley rats[1][2].
Kp7-6, a Fas mimetic peptide, is a Fas/FasL antagonist. Kp7-6 protects cells from Fas-mediated apoptosis, and protects mice from Fas-mediated hepatic injury[1][2].
Eprodisate is a new compound designed to interfere with interactions between amyloidogenic proteins and glycosaminoglycans and thereby inhibit polymerization of amyloid fibrils and deposition of the fibrils in tissues[1]. Eprodisate slow the progression of AA amyloidosis-related renal disease and has possible applicability to other types of amyloidosis[2].
Naptumomab, a tumor targeting superantigen (TTS), is a fusion protein containing. Naptumomab stimulates the immune system to identify and kill tumour cells. Naptumomab can be used for the research of refractory solid tumors such as renal cell carcinoma[1][2].
N-(Boc-PEG1)-N-bis(PEG2-propargyl) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
COX-2-IN-27 is a potent and selective COX-2 inhibitor with IC50 values of 13.22, 0.045, 1.67 µM for COX-1, COX-2, 15-LOX, respectively. COX-2-IN-27 shows anti-inflammatory activity[1].
Furprofen is an non-steroidal anti-inflammatory drug (NSAID) with analgesic properties[1]. Furprofen acts via the inhibition of prostaglandin (PGE) synthesis. Furprofen can be treated orally for the relief of pain[2][3].
Safranal is an orally active main component of Saffron (Crocus sativus) and is responsible for the unique aroma of this spice. Safranal has neuroprotective and anti-inflammatory effects and has the potential for Parkinson’s disease research[1].
Salazopyridazine is an antibacterial agent. Salazopyridazine shows activities against ulcerative colitis. Salazopyridazine can be used for the research of rheumatic diseases[1][2].
Tokinolide B is isolated from the rhizomes of Ligusticum porter[1].
Didanosine(Videx) is a reverse transcriptase inhibitor with an IC50 of 0.49 μM.Target: NRTIs; HIVDidanosine is a dideoxynucleoside compound in which the 3'-hydroxy group on the sugar moiety has been replaced by a hydrogen. This modification prevents the formation of phosphodiester linkages which are needed for the completion of nucleic acid chains. Didanosine is a potent inhibitor of HIV replication, acting as a chain-terminator of viral DNA by binding to reverse transcriptase. Didanosine demonstrated linear pharmacokinetic behavior over the dose ranges of 0.4 to 16.5 mg/kg intravenously and 0.8 to 10.2 mg/kg orally. Bioavailability of didanosine when administered as a solution with an antacid was approximately 43% for doses from 0.8 to 10.2 mg/kg in patients with AIDS and advanced AIDS-related complex. Bioavailability of didanosine from the citrate-phosphate-buffered solution, the formulation currently used in phase II and expanded access studies, was comparable to the formulation used in the phase I trials [1]. ddI might be responsible for fulminant hepatitis in all three AIDS patients. This toxic effect may be added to the list of potential adverse events occurring during ddI therapy [2].
Tafenoquine Succinate (WR 238605 Succinate) is an 8-aminoquinoline. Tafenoquine is an anti-malarial prophylactic agent[1].
Enzastaurin is a potent and selective PKCβ inhibitor with an IC50 of 6 nM, showing 6- to 20-fold selectivity over PKCα, PKCγ and PKCε.
Antibacterial agent 47, an antibacterial agent, significantly lowers MIC value of antibacterial agent Ceftazidime[1].
Cdc7-IN-15 (Example 108) is a cdc7 kinase inhibitor. Cdc7-IN-15 can be used for cancer research[1].
Trifluoperazine Dihydrochloride is a potent dopamine D2 receptor inhibitor used as an antipsychotic and an antiemetic.Target: Dopamine D2 ReceptorTrifluoperazine Dihydrochloride is a potent dopamine D2 receptor inhibitor used as an antipsychotic and an antiemetic. Trifluoperazine inhibited in a dose-dependent manner the stimulation of glycogenolysis, gluconeogenesis, and ureogenesis due to alpha 1-adrenergic stimulation in rat hepatocytes. Trifluoperazine is much more potent at alpha 1- than at alpha 2-adrenergic receptors [1]. Trifluoperazine was not clearly different in terms of 'no substantial improvement' (n=1016, 27 RCTs, RR 1.06 CI 0.98 to 1.14) or leaving the study early (n=930, 22 RCTs, RR 1.15 CI 0.83 to 1.58). Almost identical numbers of people reported at least one adverse event (60%) in each group (n=585, 14 RCTs, RR 0.99 CI 0.87 to 1.13), although trifluoperazine was more likely to cause extrapyramidal adverse effects overall when compared to low potency antipsychotics such as chlorpromazine (n=130, 3 RCTs, RR 1.66 CI 1.03 to 2.67, NNH 6 CI 3 to 121). One small study (n=38) found no clear differences between trifluoperazine and the atypical drug, sulpiride [2].
3,4-Dimethoxyphenol is a plant-derived phenylpropanoid compound and can use as a whitening agent in cosmetics. 3,4-Dimethoxyphenol has tyrosinase-inhibiting activity[1]. 3,4-Dimethoxyphenol has potent antioxidant effect isolated from the bacterial fermentation broth[2].
Bibapcitide, a 26 amino acid, inhibits thrombosis[1].
HPK1-IN-25 (example 94) is a hematopoietic progenitor kinase 1 (HPK1) inhibitor with a enzymatic activity IC50 of 129 nM. HPK1-IN-25 has the potential for cancer research[1].
Biotin-PEG3-C3-NH2 is a PEG-based PROTAC linker, with NH2 functional group, that can be used in the synthesis of PROTACs[1].
NHS-5(6)Carboxyrhodamine is a dye used for fluorescence labeling applications, where accurate dye/protein ratios can be obtained under native conditions[1].
SN 6 is a selective Na+/Ca2+ exchanger (NCX) inhibitor, and inhibits 45Ca2+ uptake by NCX1, NCX2, and NCX3, with IC50s of 2.9, 16, and 8.6 μM, respectively.
Fmoc-Thr-OBu-t is a threonine derivative[1].
Benzethonium chloride inhibit human recombinant α7 and α4β2 neuronal nicotinic acetylcholine receptors in Xenopus oocytes.
Polyphyllin I is a bioactive constituent extracted from Paris polyphylla, has strong anti-tumor activity. Polyphyllin I is an activator of the JNK signaling pathway and is an inhibitor of PDK1/Akt/mTOR signaling. Polyphyllin I induces autophagy, G2/M phase arrest and apoptosis[1][2][3].
CID 2745687 acts as a specific, reversible and competitive GPR35 antagonist with a Ki of 12.8 nM[1].
Lys-Arg-Thr-Leu-Arg-Arg (KRTLRR) is a hexapeptide. Lys-Arg-Thr-Leu-Arg-Arg is a substrate of protein kinase C from EGF receptor. Lys-Arg-Thr-Leu-Arg-Arg can be used to determine the activity of protein kinase C[1].
1-Isopropyltryptophan (1-IsoPT) is a IDO1 inhibitor. 1-Isopropyltryptophan decreases the expression of IFN-γ stimulated ID0-1 and ID0-2 mRNA[1].
Thiorphan methoxyacetophenone derivative-d7 is the deuterium labeled Thiorphan methoxyacetophenone derivative[1].