Tyrosinase-IN-1 (compound 90) is a potent inhibitor of tyrosinase. Tyrosinase is a copper-containing metalloenzyme that is responsible for the rate-limiting catalytic step in the melanin biosynthesis and enzymatic browning. Tyrosinase-IN-1 has the potential for the research of skin whitening agents and food preservatives[1].
Dmt-2'fluoro-da(bz) amidite, an uniformly modified 2'-deoxy-2'-fluoro phosphorothioate oligonucleotide, is a nuclease-resistant antisense compound with high affinity and specificity for RNA targets. Dmt-2'fluoro-da(bz) amidite is also an intermediate for 5’-DMT-3’-phosphoramidite synthesis[1].
Chlorotetracycline (7-Chlorotetracycline) is a specific and potent calcium ionophore antibiotic, inhibits binding of aminoacyl-tRNA to ribosomes.
SR121566A is a novel non-peptide Glycoprotein IIb/IIIa (GP IIb-IIIa) antagonist, which can inhibit ADP-, arachidonic acid- and collagen-induced human platelet aggregation with IC50s of 46±7.5, 56±6 and 42±3 nM, respectively.
TCO-PEG4-DBCO is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
ddATP (2',3'-Dideoxyadenosine 5'-triphosphate) trisodium, an active metabolite of 2',3'-dideoxyinosine, is a chain-elongating inhibitor of DNA polymerase. ddATP trisodium can be used for Sanger method for DNA sequencing and research of virus infection[1][2][4].
Thiorphan is a selective NEP (neprilysin) inhibitor with an IC50 of 6.9 nM[1].
(Rac)-Etodolac-d3 ((Rac)-AY-24236-d3) is a labelled racemic Etodolac. Etodolac (AY-24236) is a non-steroidal anti-inflammatory compound that is a non-selective inhibitor of COX (IC50=53.5 nM)
Amiloride hydrochloride dihydrate is an inhibitor of both Epithelial sodium channel (ENaC) and urokinase-type plasminogen activator receptor (uTPA).
E3330 (APX-3330) is a direct, orally active AP endonuclease 1 (APE1; also known as REF-1) inhibitor, which suppresses NF-κB DNA-binding activity. E3330 (APX-3330) blocks TNF-α-induced activation of IL-8 production in liver cancer cell lines. E3330 (APX-3330) shows anticancer properties, such as inhibition of cancer cell growth and migration[1-4].
J1038 is a novel Inhibitor of Histone Deacetylase 8 (HDAC8).
Propargyl-PEG1-Boc is an alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTACs[1].
AChE-IN-3 shows moderate inhibitory activity against AChE and strong NO inhibitory activity with an EC50 of 0.57 μM.
DHODH-IN-13 (Compound 7a) is a hydroxyfurazan analog of A771726. DHODH-IN-13 is a dihydroorotate dehydrogenase (DHODH) inhibitor with an IC50 of 4.3 μM for rat liver DHODH. DHODH-IN-13 can be used for rheumatoid arthritis[1].
Cathepsin K inhibitor 5 is a potent Cathepsin K inhibitor[1].
AD57 is an orally active multikinase inhibitor, inhibits RET, BRAF, S6K and Src, with greatly reduces mTOR activity[1].
Citral is a monoterpene found in Cymbopogon citratus essential oil, with antihyperalgesic, anti-nociceptive and anti-inflammatory effects[1].
(D-Arg1,D-Pro2,D-Phe7,D-His9)-Substance P is a selective NK1 receptor antagonist[1].
LY 254155, an antifolate, inhibits hGARFT and binds to mFBP with Kis of 2.1±0.2 and 1.7±0.1 nM, respectively.
Cyclophosphamide is a synthetic alkylating agent chemically related to the nitrogen mustards with antineoplastic and immunosuppressive activities.
Gosogliptin is a potent and selective inhibitor of dipeptidyl peptidase-IV (DPP-IV).
Giloralimab (ABBV-927) is a potent antiCD40 agonistic monoclonal antibody. Giloralimab has the potential for the research of cancer[1][2].
Oxeglitazar is an orally active compound that can be used for the research of type II diabetes[1].
N'-Boc-N-(Gly-Oleoyl)-Lys is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Karavilagenin D, a cucurbitane-type triterpene isolated from Japanese bitter melon leaves, is a potential tumor-promoting inhibitor[1].
Levofloxacin, a synthetic fluoroquinolone, is an antibacterial agent that inhibits the supercoiling activity of bacterial DNA gyrase, halting DNA replication.Target: AntibacterialLevofloxacin reduced bacterial load compared with placebo by 4.9-fold (95% confidence interval, 1.4-25.7; P=0.02) at day 7 but had no effect at any point on any marker of neutrophilic airway inflammation. In patients with a baseline bacterial load of more than 10(6) cfu/mL, levofloxacin treatment was associated with a 26.5% (95% confidence interval, 1.8%-51.3%; P=0.04) greater reduction in the percentage neutrophil count compared with placebo at day 7 [1]. Levofloxacin was found to significantly improve the clinical and microbiological parameters in CP individuals [2]. A 30-day course of levofloxacin does not significantly improve BK viral load reduction or allograft function when used in addition to overall reduction of immunosuppression [3].
DIM-C-pPhOH is a nuclear receptor 4A1 (NR4A1) antagonist. DIM-C-pPhOH inhibits cancer cell growth and mTOR signaling, induce apoptosis and cellular stress. DIM-C-pPhOH reduces cell proliferation with IC50 values of 13.6 μM and 13.0 μM for ACHN cells and 786-O cells, respectively[1].
Prednisone (Adasone) is a synthetic corticosteroid agent that is particularly effective as an immunosuppressant compound.Target: OthersPrednisone is a synthetic corticosteroid drug that is particularly effective as an immunosuppressant drug. It is used to treat certain inflammatory diseases (such as moderate allergic reactions) and (at higher doses) some types of cancer, but has significant adverse effects. Because it suppresses the immune system, it leaves patients more susceptible to infections.Prednisone can also be used in the treatment of decompensated heart failure to potentiate renal responsiveness to diuretics, especially in heart failure patients with refractory diuretic resistance with large dose of loop diuretics. The mechanism is prednisone, as a glucocorticoid, can improve renal responsiveness to atrial natriuretic peptide by increasing the density of natriuretic peptide receptor type A in the renal inner medullary collecting duct, inducing a potent diuresis.
EGFR-IN-21 is a potent EGFR inhibtior with an IC50 of 0.38 nM. EGFR-IN-21 has antitumor activity[1].
BACE1-IN-12 (compound 7g) is a potent and BBB-penetrated BACE1 inhibitor, with an IC50 of 8.9 µM. BACE1-IN-12 shows selective BuChE (butyrylcholinesterase) inhibitory activity with an IC50 of 3.2 µM. BACE1-IN-12 shows effective antioxidant effect with an IC50 of 10.2 μM (DPPH). BACE1-IN-12 might be served as a potential anti-Alzheimer agent[1].