Tris(2,4-di-tert-butylphenyl)phosphate is an active compound from the leaves of Vitex negundo L. shows anti-inflammatory activity with evidence of inhibition for secretory Phospholipase A2 (sPLA2) through molecular docking[1].
(R)-2-((tert-Butoxycarbonyl)amino)-3-(3,4-dichlorophenyl)propanoic acid is a phenylalanine derivative[1].
Lettowienolide, a geranylbenzoquinonoid, exhibits mild in vitro activity against the Plasmodium falciparum malaria parasite (IC50~20 μg/mL)[1].
Xanthine-13C,15N2 is a 15N-labeled and 13C-labled Deruxtecan. Deruxtecan is an ADC drug-linker conjugate composed of a derivative of DX-8951 (DXd) and amaleimide-GGFG peptide linker, used for synthesizing DS-8201 and U3-1402.
RAD51-IN-4 is a potent inhibitor of RAD51. RAD51 is a eukaryote gene. RAD51-IN-4 has the potential for the research of conditions involving mitochondrial defects (extracted from patent WO2019014315A1, compound R12)[1].
Dasatinib N-oxide is a minor metabolite of Dasatinib. Dasatinib is a potent and orally active dual Src/Bcr-Abl inhibitor[1][2].
Resolvin D2 is a metabolite of docosahexaenoic acid (DHA), with anti-inflammatory, anti-infective activities. Resolvin D2 is a potent regulator of leukocytes and controls microbial sepsis. Resolvin D2 is a remarkably potent inhibitor of TRPV1 (IC50 = 0.1 nM) and TRPA1 (IC50 = 2 nM) in primary sensory neurons[1][2][3].
AX-024 is an cytokine release inhibitor which can strongly inhibit the production of interleukin-6 (IL-6), tumor necrosis factor-α (TNFα), interferon-γ (IFN-γ), IL-10 and IL-17A.
5-Valine-angiotensin I is an Ang I peptide belonging to angiotensin I. 5-Valine-angiotensin I induces muscle contraction, can be used for renin-angiotensin system studies. Angiotensin I is a putative neurotransmitter, is the precursor of angiotensin II and of angiotensin fragment 1-7, which are involved in regulation of fluid volume and the release of aldosterone[1][2].
CVN417 is an orally active α6 subunit-containing nAChR antagonist, modulating phasic dopaminergic neurotransmission in an impulse-dependent manner. CVN417 inhibits Ca(2+) effluents mediated by nAChR subunits with IC50s of 0.086 μM (α6), 2.56 μM (α3) and 0.657 μM (α4), respectively. CVN417 attenuates resting tremor in Rodent models, displays the potential to improve movement dysfunction, in conditions such as Parkinson's disease[1].
Pifithrin-β is a potent p53 inhibitor with an IC50 of 23 μM.
Pirimiphos-methyl is a rapid-acting organophosphorus insecticide and acaricide, causing inhibition of AChE in target organisms. Pirimiphos-methyl is often used for prevention and control of beetles, snout beetles, moths and Ephestia cautella during storage of agricultural grains[1][2][3].
Farampator-d10 (CX-691-d10) is the deuterium labeled Farampator. Farampator (CX-691) is an AMPA receptor positive modulator.
13-Epimanool is the compound isolated from the bark of the Taiwan hemlock[1].
Valacyclovir is an antiviral drug used in the management of herpes simplex, herpes zoster, and herpes B. IC50 Value: 2.9 microg/ml (for HSV-1 W)[4]. Target: HSV infectionin vitro: VACV uptake was concentration dependent and saturable with a Michaelis-Menten constant and maximum velocity of 1.64 +/- 0.06 mM and 23.34 +/- 0.36 nmol/mg protein/5 min, respectively. A very similar Km value was obtained in hPEPT1/CHO cells and in rat and rabbit tissues and Caco-2 cells, suggesting that hPEPT1 dominates the intestinal transport properties of VACV in vitro [5]. in vivo: For treatment of a first episode of genital herpes, a large comparative trial has shown that valacyclovir (1 g twice a day) is as effective as acyclovir (200 mg five times a day) when given for 10 days. For treating recurrences, two trials show that valacyclovir is as effective as acyclovir (200 mg five times a day) with a treatment period of 5 days. A daily dose of 1 g of valacyclovir is as effective as 2 g daily. Valacyclovir can be administered once a day[1]. The concentrations of acyclovir in serum and CSF were measured at steady state after 6 days of oral treatment with 1,000 mg of valacyclovir three times a day [2]. EC50 values of PE and AC in 3T3 cells were 0.02 and 0.01 ug/ml, while values in BHK cells were 0.2 and 0.03 ug/ml. Treatment of infected immunosuppressed mice and FA and VA (b.i.d., 5.5 days) reduced the proportion with erythema from 100% to 24% and 38%, and eliminated ear paralysis, ear lesions (vesicles, etc) and death. Virus was absent from ear and brainstem by day 6, but reappeared after discontinuation in mice treated with VA [3].Clinical trial: Evaluation of Valaciclovir in Patients with Chickenpox. Phage3
AH1 is an immunodominant antigen derived from the gp70 product of an endogenous MuLV. AH1 behaves as the CTL-immunodominant epitope of CT26 colon carcinoma[1][2].
CH6953755 is a potent, orally active and selective YES1 kinase (a member of the SRC family) inhibitor with an IC50 of 1.8 nM. CH6953755 inhibits YES1 kinase, leading to antitumor activity against YES1 Gene -amplified cancers in vitro and in vivo[1].
Nicotinamide riboside tartrate, an orally active NAD+ precursor, increases NAD+ levels and activates SIRT1 and SIRT3. Nicotinamide riboside tartrate is a source of vitamin B3 (niacin) and enhances oxidative metabolism, protection against high fat diet-induced metabolic abnormalities[1]. Nicotinamide riboside tartrate reduces cognitive deterioration in a transgenic mouse model of Alzheimer’s disease[2].
Sinomenine, an alkaloid extracted from Sinomenium acutum, is a blocker of the NF-κB activation[1]. Sinomenine also is an activator of μ-opioid receptor[2].
SLEC-11 acts as a potential synthetic lethal lead for the treatment of gastric cancer. AL-GDa62 shows EC50 of 12.2 μM and 8.2 μM for isogenic mammary epithelial cells MCF10A-WT (wild-type) and MCF10A-CDH1-/-[1].
C6 NBD L-threo-ceramide is a cell-permeable analog of ceramides that is tagged with a fluorescent group C6 nitrobenzoxadiazole (C6 NBD). It is rapidly transferred between liposomes, labels the Golgi apparatus, and is metabolized to C6 NBD sphingomyelin in BHK cells and V79 fibroblasts.
Tolazamide is an oral blood glucose lowering drug used for people with Type 2 diabetes.
Tariquidar methanesulfonate, hydrate is a potent and specific inhibitor of P-glycoprotein (P-gp) with a Kd of 5.1 nM.
Pinocembrin chalcone (2',4',6'-Trihydroxychalcone) is an antibacterial compound from Helichrysum Trilineatum. Pinocembrin chalcone can prevent gastric ulcers in rats[1].
Steviol-19-O-glucoside is a metabolite of steviol in the steviol glycosides biosynthesis pathway in Stevia rebuadiana[1].
Acetyl-octreotide is a reduced linear peptide. Acetyl-octreotide can synthesize Re(V)-cyclized peptides in aqueous methanol solutions with low Sst receptor binding affinities[1].
GFB-8438 is a potent and subtype selective TRPC5 inhibitor, with IC50s of 0.18 and 0.29 μM of hTRPC5 and hTRPC4, respectively. GFB-8438 shows excellent selectivity against TRPC6, other TRP family members, NaV 1.5, as well as limited activity against the hERG channel. GFB-8438 protects mouse podocytes from injury induced by protamine sulfate model[1].
Furimazine is an imidazopyrazinone substrate. NanoLuc (Nluc) paired with Furimazine produced 2.5 million-fold brighter luminescence in mammalian cells relative to Oluc-19 with Coelenterazine.
Me-Tet-PEG4-Maleimide is an ADC Linker containing 4 PEG units. Me-Tet-PEG4-Maleimide can utilize its own Tetrazine group to undergo a specific inverse electron demand Diels-Alder reaction (iEDDA) with compounds with TCO groups. Its maleimide group (-Maleimide) degrades in aqueous media and has been used in drug delivery studies.
DMT-2'Fluoro-DG(IB) Amidite (2'-F-ibu-dG Phosphoramidite) is a nucleoside that can be used in the preparation of 4'-modified 2'-deoxy-2'-fluorouridine[1].