CYCA-117-70 is a DCAF1 ligand (KD: 70 μM). CYCA-117-70 is an ideal chemical handles for PROTACs recruiting DCAF1[1].
Eldocasiran is a micro-ARN-193a-3p analogue, Eldocasiran has anticancer activity. Eldocasiran can be used for cancer research[1].
Methyl Salicylate-d4 is the deuterium labeled Methyl Salicylate[1]. Methyl Salicylate (Wintergreen oil) is a topical analgesic and anti-inflammatory agent. Also used as a pesticide, a denaturant, a fragrance ingredient, and a flavoring agent in food and tobacco products[2]. A systemic acquired resistance (SAR) signal in tobacco[3]. A topical nonsteroidal anti-inflammatory drug (NSAID). Methyl salicylate lactoside is a COX inhibitor[5].
Doravirine is a novel non-nucleoside inhibitor of HIV-1 reverse transcriptase with potent activity against wild-type virus (95% inhibitory concentration 19 nM, 50% human serum). target:HIV [1]In vitro: Doravirine exhibits potent antiviral activity against wild-type virus and K103N, Y181C, and K103N/Y181C mutant viruses, with IC50 value of 12, 21, 31, and 33 nM, respectively. [1] MK-1439 exhibited similar antiviral activities against 10 different HIV-1 subtype viruses (a total of 93 viruses).[2]In vivo: Administration of 50 mg doravirine with a high-fat meal is associated with slight elevations in AUC time zero to infinity (AUC0-∞) and C24 h with no change in Cmax. Midazolam AUC0-∞ is slightly reduced by coadministration of doravirine (geometric mean ratio 0.82, 90% CI 0.70, 0.97). [3]
Glutaminase C-IN-1 (968) is an allosteric inhibitor of Glutaminase C that inhibits cancer cell growth without affecting their normal cellular counterparts.
BAY-299 is a very potent, dual inhibitor with IC50s of 67 nM for BRPF2 bromodomains (BD), 8 nM for TAF1 BD2, and 106 nM for TAF1L BD2.
Orilanolimab (SYNT001) is a humanized, de-immunized and FcRn-blocking monoclonal antibody. Orilanolimab blocks the interaction between FcRn and the Fc portion of IgG molecules. Orilanolimab impedes IgG IC activation of the FcRn-mediated adaptive immune function. And Orilanolimab disrupts the associated pathways related to IgG homeostasis and innate and adaptive immunity[1][2].
Suc-Ala-Phe-Pro-Phe-pNA is a peptide substrate[1].
N-(((9H-Fluoren-9-yl)methoxy)carbonyl)-S-(tert-butyl)-L-cysteine is a cysteine derivative[1].
ST-836 is a dopamine receptor ligand; Antiparkinsonian agent.
Pentetic acid is a compound used to construct magnetic adsorbent, which can simultaneously remove heavy metal and dye from complex wastewater[1].
Elastase LasB-IN-1 (Compound 4b) has antibacterial activity. Elastase LasB-IN-1 (Compound 4b) is a selective elastase LasB inhibitor with an IC50 value of 76 nM[1].
1-O-Gentiobiosyl-3,7-dimethoxy-8-hydroxyxanthone (Compound 18) is a natural product that can be isolated from Swertia mussotii[1].
Dynorphin (2-17), amide (porcine) is a dynorphin derivative with some analgesic effects. Dynorphin is a class of opioid peptides produced by the precursor protein dynorphinogen and is involved in pain, addiction and mood regulation[1].
Ranirestat (AS-3201) is an aldose reductase inhibitor being developed for the treatment of diabetic neuropathy.
Biotin-TAT (47-57), biotin tagged TAT, is a transactivator of transcription. Biotin-TAT (47-57) is one of the most widely used PTDs into different primary cells is ATP- and temperature-dependent, indicating the involvement of endocytosis[1][2].
Salicylic acid-D6 (2-Hydroxybenzoic acid-D6) is a deuterium labeled Salicylic acid. Salicylic acid inhibits cyclo-oxygenase-2 (COX-2) activity independently of transcription factor (NF-κB) activation[1].
Lisinopril is angiotensin-converting enzyme inhibitor, used in treatment of hypertension, congestive heart failure, and heart attacks.Target: ACELisinopril is a potent, competitive inhibitor of angiotensin-converting enzyme (ACE), the enzyme responsible for the conversion of angiotensin I (ATI) to angiotensin II (ATII). ATII regulates blood pressure and is a key component of the renin-angiotensin-aldosterone system (RAAS). Lisinopril may be used to treat hypertension and symptomatic congestive heart failure, to improve survival in certain individuals following myocardial infarction, and to prevent progression of renal disease in hypertensive patients with diabetes mellitus and microalbuminuria or overt nephropathy [1, 2].
Trimethylolpropane ethoxylate triacrylate (ETPTA) is a plasticizer that can be used synthesize nanocomposites[1].
2′-Deoxy-2′-fluoro-5-methoxy-arabinouridine is a uridine analogue. Uridine has potential antiepileptic effects, and its analogs can be used to study anticonvulsant and anxiolytic activities, as well as to develop new antihypertensive agents[1].
3-Butylidenephthalide (Butylidenephthalide) is a phthalic anhydride derivative identified in Ligusticum chuanxiong Hort, and has larvicidal activity (LC50 of 1.56 mg/g for Spodoptera litura larvae)[1].
PA452, retinoic X receptor (RXR) specific antagonist, inhibits the effect of Retinoic acid (RA) on Th1/Th2 development[1].
α-Helical Corticotropin Releasing Factor (9-41) is a corticotropin releasing factor (CRF) antagonist. α-Helical Corticotropin Releasing Factor (9-41) decreases plasma growth hormone (GH) values in vivo[1][2].
diABZI STING agonist-1 (Tautomerism) is a selective stimulator of interferon genes (STING) receptor agonist, with an EC50s of 130 for human PBMCs.
Decoglurant (RO4995819) is a negative allosteric modulator of mGluR2 and mGluR3. Decoglurant is developed as an antidepressant[1].
Thalidomide-NH-PEG4-Ms is an E3 ligase ligand-linker conjugate that incorporates Thalidomide based cereblon ligand and a linker used for PROTAC BCL-XL degrader XZ739[1].
Odoratisol B is a natural product that can be isolated from Machilus odoratissima NEES[1].
GHRF, mouse, a mouse growth hormone-releasing factor, is a peptide containing 44 amino acids. GHRF, mouse stimulates the release and synthesis of growth hormone[1].
Fumarate hydratase-IN-1, an enzyme of the TCA cycle. Inhibition of fumarate hydratase-IN-1 can contribute to tumorigenicity in some cells. The use of a photoaffinity labeling strategy identified fumarate hydratase as the principal pharmacological target.[1]In vitro: The activity of this enzyme was measured using a well-established assay that monitored the conversion of fumarate into L-malate and subsequent oxidation of L-malate to oxaloacetate by malate dehydrogenase. Initial controls established that neither the carboxylic acid 3 nor ester 2 inhibited malate dehydrogenase Using this two-enzyme protocol we found that carboxylic acid 3 inhibited fumarate hydratase in a dose-dependent fashion in vitro. Besides, inhibition of fumarate hydratase can contribute to tumorigenicity in some cells.[1]
Ivangustin is a sesquiterpene isolated from the flower heads of the medicinal plant Inula britannica[1].