(Rac)-Etavopivat ((Rac)-FT-4202) is an isomer of Etavopivat (HY-139573). Etavopivat is an orally active erythrocyte pyruvate kinase-R (PKR) activator that can be used in studies of sickle cell disease and other haemoglobinopathies[1].
H-Ile-His-OH is a biologically active peptide.
CYT-1010 hydrochloride is a mu-opioid receptor agonist extracted from patent WO2013173730A2, with EC50s of 13.1 nM and 0.0053 nM on beta-arrestin recruitment and inhibition of cAMP production, respectively[1].
9-cis-Retinoic acid-d5 (ALRT1057-d5) is the deuterium labeled 9-cis-Retinoic acid. 9-cis-Retinoic acid (ALRT1057), a vitamin A derivative, is a potent RAR/RXR agonist. 9-cis-Retinoic acid induces apoptosis, regulates cell cycle and has anticancer, anti-inflammatory and neuroprotection activities[1][2][3][4][5][6].
Vilobelimab (CaCP-29, IFX-1) is a monoclonal anti-C5a antibody to the allergen C5a, a pro-inflammatory complement division product that plays a central role in mediating organ dysfunction. Vilobelimab acts as a C5a inhibitor, inhibiting neutrophil activation, chemotaxis, and reducing inflammatory signalling, and may be used in studies related to sepsis, COVID-19, etc[1].
EPZ020411 hydrochloride is a potent and selective inhibitor of PRMT6 with IC50 of 10 nM, has ＞10 fold selectivity for PRMT6 over PRMT1 and PRMT8.IC50 value: 10 nMTarget: PRMT6in vitro: EPZ020411 inhibits methylation of PRMT6 substrates in cells. EPZ020411 does-dependently inhibits H3R2 methylation in PRMT6-overexpressing cells.in vivo: EPZ020411 shows good bioavailability following subcutaneous (SC) dosing in rats making it a suitable tool for in vivo studies.
AZ628 is a pan-Raf kinase inhibitor with IC50s of 105, 34 and 29 nM for B-Raf, B-RafV600E, and c-Raf-1, respectively.
KRAS G12C inhibitor 39 is a potent inhibitor of KRAS G12C. KRas is a highly attractable target of the pharmaceutical industry for cancer research. KRAS G12C inhibitor 39 has the potential for the research of KRAS G12C-mediated cancer (extracted from patent WO2019099524A1, compound 494)[1].
Antibacterial agent 158 (compound 6c), a Micrococcin analogue, and is effective against impetigo and C. difficile infection (CDI)[1].
Amido Black 10B (Naphthol Blue Black) is a highly toxic azo dye for amino acid staining. Amido Black 10B can create several problems in the human respiratory system and may also cause skin and eye irritations[1].
Protein kinase C (alpha) peptide (TFA) is a peptide of PKC-α. PKC-α acts as a lipid-dependent ser/thr protein kinase, can modulate various cellular processes, including cell survival, proliferation, differentiation, migration, adhesion and so on[1].
L-Carnitine-d9 chloride is the deuterium labeled L-Carnitine chloride. L-Carnitine chloride, a highly polar, small zwitterion, is an essential co-factor for the mitochondrial β-oxidation pathway. L-Carnitine chloride functions to transport long chain fatty acyl-CoAs into the mitochondria for degradation by β-oxidation. L-Carnitine chloride is an antioxidant. L-Carnitine chloride can ameliorate metabolic imbalances in many inborn errors of metabolism[1][2][3].
DGKα-IN-2 (example 48) is a DGKα inhibitor with the IC50 of 0.9 nM, extracted from patent WO2021105115. DGKα-IN-2 significantly enhances the anti-tumor effect of anti-PD-1 by increasing the proliferation and function of T cells. DGKα-IN-2 has the potential for cancer and immunology study.
Orphenadrine-d3 (hydrochloride) is the deuterium labeled Orphenadrine hydrochloride[1]. Orphenadrine hydrochloride is an orally active and non-competitive NMDA receptor antagonist (crosses the blood-brain barrier) with a Ki of 6.0 μM. Orphenadrine hydrochloride relieves stiffness, pain and discomfort due to muscle strains, sprains or other injuries. Orphenadrine hydrochloride is also used to relieve tremors associated with parkinson's disease. Orphenadrine citrate has good neuroprotective properties, can be used in studies of neurodegenerative diseases[2][3].
Dansylphenylalanine is a phenylalanine derivative[1].
AZ'6421 acts as Protcolysis Targeting Chimera (PROTAC) to selectively degrade estrogen receptor alpha. AZ'6421 has a potent anti-tumour effect to inhibit the uncontrolled cellular proliferation which arises from malignant disease. AZ'6421 can be used for the research of cancer such as breast cancer[1].
3-Feruloyl-1-Sinapoyl sucrose (compound 1) is a glycoside isolated from the aerial parts of Polygala chamaebuxus[1].
β-Lactamase-IN-5 is a β-lactamase inhibitor extracted from patent WO2013149121A1, compound 720. β-Lactamase-IN-5 can be used for the research of bacterial infections[1].
(-)-Carvone is an insect neurotoxin and a irreversible acetylcholinesterase (AChE) inhibitor. (-)-Carvone can be used as a bird repellent, inhibits larval growth, decreases pupatation rate, and increases mortality of larvae[1][2].
Manghaslin is a flavonoid glycoside with anti-inflammatory activities. Manghaslin shows inhibitory activity against AChE with an IC50 of 94.92 µM[1][2].
Mulberrofuran Q inhibits the formation of 12-hydroxy-5,8,10-heptadecatrienoic acid (HHT) and thromboxane B2 (cyclooxygenase products)[1].
BODIPY 558/568 C12 is a fatty acid-conjugated fluorescent probe for lipid droplets. It displays excitation/emission maxima of 558/568 nm, respectively, and has been used to monitor the localization and dynamics of lipid droplets in live cells.
Dabcyl-YVADAPV-EDANS is a fluorogenic interleukin-1β converting enzyme (ICE) substrate for measuring ICE-like protease activity. Dabcyl-YVADAPV-EDANS detects fluorescence at 360 nm excitation and 480 nm emission wavelengths. ICE-like protease is a critical mediator of K+ deprivation-induced apoptosis of cerebellar granule neurons[1].
UT-155 is a selective androgen receptor (AR) antagonist, with a Ki of 267 nM for AR-RBD.
Influenza A virus-IN-6 (compound 16j) is a potent and selective influenza A virus inhibitor with an IC50 of 3.88 µM and CC50 of 36.64 µM. Influenza A virus-IN-6 shows anti-IAV activity with low cytotoxicity[1].
2-(1,3-Dioxoisoindolin-2-yl)pentanedioic acid is a glutamic acid derivative[1].
L-838417 is a selective partial agonist at the α2, α3 and α5 subtypes of the GABAA receptor and an antagonist at the α1, with binding Ki values of 0.79 nM, 0.67 nM, 1.67 nM, 267 nM, 2.25 nM and 2183 nM for α1β3γ2, α2β3γ2, α3β3γ2, α4β3γ2, α5β3γ2 and α6β3γ2[1].
Omesdafexor is a FXR agonist. Omesdafexor can be used in the research of liver disease or a metabolic inflammation-mediated disease[1][2].
Arjunic acid (Arjuntriterpenic acid) (compound 13) is a triterpenoid compound isolated from Sanguisorba officinalis L[1].
Okadaic acid, a marine toxin, is an inhibitor of protein phosphatases (PP), including PP1 (IC50=15-50 nM), PP2A (IC50=0.1-0.3 nM), PP3 (IC50=3.7-4 nM), PP4 (IC50=0.1 nM), PP5 (IC50=3.5 nM), with a significantly higher affinity for PP2A. Okadaic acid increase of phosphorylation of a number of proteins by inhibiting PP, and acts a tumor promoter[1] [2].