Ac-Gly-Ala-Lys(Ac)-AMC is a fluorogenic substrate for the determination of protease activity. Ac-Gly-Ala-Lys(Ac)-AMC undergoes hydrolysis and releases the fluorescent product 7-amino-4-methylcoumarin (AMC). AMC is fluorescent under UV light and can emit a fluorescent signal[1].
Flo8 is a potent anti-inflammatory and antioxidant compound. Flo8 inhibits the release of intracellular reactive oxygen species (ROS) and nitric oxide (NO) and suppresses neuronal apoptotic by inhibiting inflammatory and apoptotic signaling pathways. Flo8 can be used for Parkinson's Disease (PD) research[1].
Alimemazine is a phenothiazine derivative that is generally used as an antipruritic agent and also a hemagglutinin (HA)-receptor antagonist.Alimemazine (Trimeprazine) is also acts as a partial agonist against the histamine H1 receptor (H1R) and other GPCRs. Alimemazine displays sedative, antiserotonin, antispasmodic, and antiemetic properties[1][2].
Methylamino-PEG1-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Flavipin is an aryl hydrocarbon receptor (Ahr) agonist that induces the expression of Ahr downstream genes in mouse CD4+ T cells and CD11b+ macrophages. Flavipin inhibits the stabilizing function of Arid5a on Il23a 3′UTR, a newly identified target mRNA[1]. Flavipin exhibits the DPPH free radical scavenging ability with IC50 value of 7.2 μM, and has potent α-glucosidase inhibition with IC50 value of 33.8 μM[2].
Simufilam (PTI-125) is a low toxicity, orally active filamin A (FLNA) activator. Simufilam preferentially binds altered FLNA and restores its native conformation, restores receptor and synaptic activities, reduces its a7nAChR/TLR4 associations and downstream pathologies. Simufilam can be used for the research of Alzheimer's disease[1].
2-Chloro-9-(beta-D-ribofuranosyl)purine is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
GS-444217 is a potent and selective ATP-competitive inhibitor of apoptosis signal-regulating kinase 1 (ASK1) with an IC50 of 2.87±0.85 nM[1].
Olaratumab (IMC-3G3; LY3012207) is an anti-platelet-derived growth factor receptor alpha (PDGFRα) human monoclonal IgG1 antibody with antitumor activity[1].
Lewis a trisaccharide (Lewis a) is a trisaccharide that has been found to be present in the glycan structures of spermatozoa. Lewis a trisaccharide also is a major component of the glycan structures on the surface of HL-60 cells[1].
2’-O-Acetyl-5’-O-(p-toluoyl)-3’-deoxy-3’-fluoro-5-methyluridine is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
ERK-IN-3 is a potent and oral inhibitor of ERK. ERK-IN-3 inhibits ERK1/2 with low single-digit nM IC50 values. ERK-IN-3 has the potential to be used to study cancers driven by RAS mutations.[1].
H-D-Phg-OH is a Glycine (HY-Y0966) derivative[1].
PI3K/mTOR Inhibitor-1 is a potent, orally bioavailable dual PI3K/mTOR inhibitor with IC50s of 20/376/204/46 nM and 186 nM for PI3Kα/PI3Kβ/PI3Kγ/PI3Kδ and mTOR, respectively[1]. Antitumor activity[1].
MK-2295 (NGD-8243) is a TRPV1 antagonist. MK-2295 is an analgesic agent, and can be used for research of pain[1][2].
Methyl 12-methyltridecanoate ((R)-betaxolol hydrochloride) is a biosurfactant extracted from Brevibacterium casei LS14.Methyl 12-methyltridecanoate provides a novel approach for functionalizing the silver nanoparticles higher biocompatibility in vivo environmental[1].
Foscarbidopa (Carbidopa 4′-monophosphate) is a prodrug of Carbidopa, acts as a dopamine receptor agonist[1][2].
Ferroptosis-IN-5 (compound 9c) is a ferroptosis inhibitor with iron-chelating and reactive oxygen species (ROS) scavenging activities[1].
3-Cyanoumbelliferone is a coumarin derivative, acting as molecular probe and fluorescent dye. 3-Cyanoumbelliferone is also a macrophage migration inhibitory factor (MIF) tautomerase inhibitor with a Ki of 2.9 μM[1].
Chrysanthemol is a trans-eudesmane type sesquiterpene that can be isolated from Chrysanthemum indicum. Chrysanthemol has anti-inflammatory activity[1].
YH-306 is a candidate drug in preventing growth and metastasis of colorectal cancer by modulating FAK signalling pathway.
Leptomerine, an alkaloid from stems of Esenbeckia leiocarpa Engl. (Rutaceae) as potential treatment for Alzheimer Disease. Leptomerine inhibits acetyl cholinesterase (AChE) with an IC50 of 2.5 μM. Anticholinesterasic activity[1].
Nifurpirinol (P-7138) is a nitroaromatic antibiotic and acts as a novel substrate for the bacterial nitroreductase (NTR) enzyme. Nifurpirinol is a more potent prodrug compared to Metronidazole to trigger cell-ablation in nitroreductase expressing transgenic models[1].
N6-Dimethylamino methylidene-2’-deoxyisoguanosine is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
(R)-Zunsemetinib is the inactive isomer of Zunsemetinib (HY-139553), and can be used as an experimental control. Zunsemetinib (CDD-450) is an orally active and selective p38α mitogen-activated protein kinase-activated protein kinase 2 (MK2) pathway inhibitor. Zunsemetinib can be used for the research of immuno-inflammatory diseases[1].
Lugdunin is an antibiotic peptide. Lugdunin inhibits bacteria by dissipating their membrane potential. Lugdunin is active against Gram-positive bacteria, such as S. aureus, and reduces S. aureus skin and nasal colonization. Lugdunin induces LL-37 and CXCL8/MIP-2 in human keratinocytes and mouse skin[1].
Tubulysin family of secondary metabolites are originally isolated from the myxobacteria Archangium geophyra and Angiococcus disciformis. These compounds are potent microtubule destabilizing agents with IC50 values in the picomolar range against many cancer cell lines, including those with multidrug resistant properties. Tubulysins have limited therapeutic utility due to severe toxicity, so Tubulysins are ideal candidates to be incorporated into molecule drug conjugate (SMDC) delivery system[1].
H-Val-Obzl.HCl is a valine derivative[1].
MG-262 is a reversible proteasome inhibitor with diverse biological activities[1][2][3].
RXFP1 receptor agonist-3 (Example 223) is a RXFP1 receptor agonist. RXFP1 receptor agonist-3 inhibits cAMP production in HEK293 cells stably expressing human RXFP1, with an EC50 value of 2 nM[1].