D5261 is a potent, type III allosteric tropomyosin-related kinase A (TrkA) inhibitor[1].
Germanicol is a selective antineoplastic agent against human colon cancer cell lines HCT-116 and HT29 . Germanicol induces apoptosis via chromatin condensation and DNA damage[1].
Pam3CSK4 is a toll-like receptor 1/2 (TLR1/2) agonist with an EC50 of 0.47 ng/mL for human TLR1/2[1].
FlAsH-EDT2 is a protein labeling reagent. FlAsH-EDT2 also is a membrane-permeant fluorogenic biarsenicals. FlAsH-EDT2 binds to CCXXCC motifs and non-specifically to endogenous cysteine-rich proteins. FlAsH-EDT2 can be useful only for labeling those recombinant proteins that express at a very high level[1][2].
CCCI-01 is a centrosome clustering inhibitor. CCCI-01 has selective effects on cancer. CCCI-01 can be used for the research of non-cross-resistant anti-cancer agents with blocking centrosome clustering[1].
ATM Inhibitor-5 [formula (1)] is a potent inhibitor of serine/threonine protein kinase ATM (extracted from patent WO2022058351A1)[1].
Cyclophostin is an acetylcholinesterase (AChE) inhibitor with IC50 values of 45, 0.76 and 1.3 nM for humans and two different insects, respectively[1].
Protopine hydrochloride, an isoquinoline alkaloid, is a specific reversible and competitive inhibitor of acetylcholinesterase. Protopine hydrochloride exhibits anti-inflammation, anti-microbial, anti-angiogenic and anti-tumour activity[1][2].
5'-ODMT cEt G Phosphoramidite Amidite is a potent nucleic acid analog. 5'-ODMT cEt G Phosphoramidite Amidite shows excellent safety and antisense activity[1][2].
Thymus Factor is a key factor responsible for the maturation of humoral immunological faculty[1].
NH2-PEG5-OH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1]. NH2-PEG5-OH is also a non-cleavable 5 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[2].
Protogracillin is a steroidal saponin isolated from Dioscorea zingiberensis Wright (DZW). Steroidal saponins from DZW rhizomes have the potential to reduce the risk of cardiovascular diseases by anti-thrombotic action[1].
Manzamine A hydrochloride, an orally active beta-carboline alkaloid, inhibits specifically GSK-3β and CDK-5 with IC50s of 10.2 and 1.5μM, respectively. Manzamine A hydrochloride targets vacuolar ATPases and inhibits autophagy in pancreatic cancer cells. Manzamine A hydrochloride has antimalarial and anticancer activities. Manzamine A hydrochloride also shows potent activity against HSV-1[1][2][3][4].
PF-3845 is a selective fatty acid amide hydrolase (FAAH) inhibitor (Ki = 0.23 μM); showing negligible activity against FAAH2.IC50 value: 0.23 uMTarget: FAAHPF-3845 selectively inhibits FAAH by carbamylating FAAH's serine nucleophile [1]. PF-3845 treated mice (10 mg/kg, i.p.) shows rapid and complete inactivation of FAAH in the brain, as judged by competitive activity-based protein profiling (ABPP) with the serine hydrolase-directed probe fluorophosphonate (FP)-rhodamine. PF-3845 shows a long duration of action up to 24 hour. PF-3845-treated mice also shows dramatic (>10-fold) elevation in brain levels of AEA and other NAEs (N-pamitoyl ethanolamine [PEA] and N-oleoyl ethanolamine [OEA]). FAAH is AEA-degrading enzyme fatty acid amide hydrolase. PF-3845 (1–30 mg/kg, oral administration [p.o.]) causes a dose dependent inhibition of mechanical allodynia with a minimum effective dose (MED) of 3 mg/kg (rats are analyzed at 4 hour post dosing with PF-3845). At higher doses (10 and 30 mg/kg), PF-3845 inhibits pain responses to an equivalent, if not greater, degree than the nonsteroidal anti-inflammatory drug naproxen (10mg/kg, p.o.) [1]. PF-3845 (10 mg/kg, i.p.) significantly reverses LPS-induced tactile allodynia, but doesn't modify paw withdrawal thresholds in the saline-injected paw [2].
Fmoc-Tle-OH is a leucine derivative[1].
Nω-(4-Methoxy-2,3,6-trimethylbenzenesulfonyl)-L-arginine-4-methoxybenzylamide hydrochloride is an arginine derivative[1].
Gresonitamab (AMG 910) is a half-life extended (HLE) bispecific T-cell engager (BiTE) antibody targets CD3-positive T cells and CLDN18.2-expressing tumor cells. Gresonitamab can be used for the research of adenocarcinoma[1].
CPYPP is a small-molecule inhibitor of the Rac activator DOCK2 with IC50 of 22.8 uM (DOCK2DHR-2-mediated Rac GEF activity), inhibits DOCK2-Rac1 interaction; binds to DOCK2 DHR-2 domain in a reversible manner and inhibited its catalytic activity in vitro; blocks both chemokine receptor- and antigen receptor-mediated Rac activation in lymphocytes, resulting in marked reduction of chemotactic response and T cell activation.
DBCO-PEG2-DBCO is a click chemistry reagent containing an azide group. DBCO-PEG2-DBCO is a PEG linker containing two terminal DBCO groups. The DBCO groups is commonly used for copper-free Click Chemistry reactions due to its strain promoted high energy. The hydrophilic PEG chain allows for increased water solubility. T Reagent grade, for research use only[1].
RNA polymerase-IN-2 (compound 5) is s DNA-dependent RNA polymerase inhibitor. RNA polymerase-IN-2 inhibits CYP isozymes[1].
SARS-CoV-2-IN-11 is a potent and nontoxic inhibitor of SARS-CoV-2 3CL protease (3CLpro) with an IC50 and EC50 of 0.17 and 1.45 nM, respectively. SARS-CoV-2 3C-like protease (3CLpro), an enzyme essential for viral replication, is an attractive target for therapeutic intervention. SARS-CoV-2-IN-11 may lead to the emergence of effective SARS-CoV-2-specific antivirals[1].
Bromo-PEG4-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Cyclohexylglycine is a Glycine (HY-Y0966) derivative[1].
Azelnidipine(CS 905; Calblock) is a novel dihydropyridine derivative, a L-type calcium channel blocker, and an antihypertensive.IC50 value:Target: L-type calcium channelAcute administration of azelnidipine prevents a sudden drop of cardiac function after acute stress. Azelnidipine may have a protective role in inflammation associated with atherosclerosis.
Emicerfont is a corticotropin-releasing factor type 1 (CRF1) receptor antagonist with an IC50 of 66 nM.
(tert-Butoxycarbonyl)-L-valyl-L-valine is a valine derivative[1].
6-Chloromelatonin is a potent melatonin receptor agonist with greater metabolic stability than melatonin. 6-Chloromelatonin compete for [3H]-melatonin and 2-[125I]-iodomelatonin binding to MT1 receptors (pKi=8.9 and 9.1, respectively). 6-Chloromelatonin compete for [3H]-melatonin binding to MT2 receptors (pKi=9.77)[1][2].
NEP (VDP-green (NEP)) is a turn-on fluorescent probe based on the intramolecular charge transfer (ICT) mechanism for sensing vicinal dithiol-containing proteins (VDPs). NEP is exhibits high selectivity toward VDPs in live cells and in vivo and displays a strong green fluorescence signal (λex/λem=430/535 nm). NEP has the potential for parkinsonism[1].
Tenidap, a non-steroidal anti-inflammatory drug, is a selective COX-1 inhibitor, with IC50 values of 0.03 µM and 1.2 µM for COX-1 and COX-2, respectively. Tenidap has anti-inflammatory and antirheumatic properties[1][2].
Lavendustin C is a potent Ca2+ calmodulin-dependent kinase II (CaMK II) inhibitor with an IC50 of 0.2 µM. Lavendustin C inhibits EGFR-associated tyrosine kinase (IC50=0.012 µM) and pp60c-src(+) kinase (IC50=0.5 µM) [1][2].