P2X3 antagonist 38 (compound 4) is a potent and orally active P2X3 antagonist with IC50 values of 0.132, 0.165, 0.421 µM for hP2X3, rP2X3, gpP2X3, respectively[1].
DQP-997-74 (compound 2i) is a selective inhibitor of N-methyl-d-aspartate receptor (NMDAR), specifically targeting GluN2C/D (IC50: 0.069 μM and 0.035 μM), with Blood-brain permeability. Where DQP refers to dihydroquinoline-pyrazoline. DQP-997-74 acts synergistically with the agonist glutamate to exhibit time-dependent enhanced potency in inhibiting hypersynchronous activity driven by high-frequency excitatory synaptic transmission. DQP-997-74 reduces the number of epileptogenesis in a murine model of tuberous sclerosis complex (TSC)-induced epilepsy. DQP-997-74 can be used for research on NMDAR-related neurological diseases[1].
FAK PROTAC B5 (Compound B5) is a FAK PROTAC degrader with an IC50 value of 14.9 nM. FAK PROTAC B5 presents strong FAK degradation activity, antiproliferative activity, outstanding plasma stability and moderate membrane permeability. FAK PROTAC B5 inhibits cell migration and invasion[1].
Thyminose-d2 is the deuterium labeled Thyminose. Thyminose is an endogenous metabolite[1].
Alpinetin is a flavonoid isolated from Alpinia katsumadai Hayata, activates activates PPAR-γ, with potent anti-inflammatory activity[1].
H-Ser-Ala-OH is a biologically active peptide.
TSPO ligand-1 is the ligand of AUTAC4 (HY-134640) that can be used in the synthesis of PROTACs. TSPO ligand-1 is a mitochondrial outer membrane transmembrane structural domain protein can bind to AUTAC4 and regulate mitochondrial autophagy to promote targeted mitochondrial renewal. TSPO ligand-1 is also involved in the transport of cholesterol from the outer to inner mitochondrial membrane and serves as a sensitive biomarker of brain injury and neurodegeneration[1][2].
MIF-1 (Melanostatin), an endogenous brain peptide, is a potent dopamine receptor allosteric modulator. MIF-1 inhibits melanin formation. MIF-1 blocks the effects of opioid receptor activation to modulate the analgesic effects of morphine and stress-induced analgesia (SIA). MIF-1 accesses from the blood to the CNS by directly crossing the blood-brain barrier (BBB)[1][2][3].
Nifedipine D6 is deuterium labeled nifedipine, and nifedipine is a potent calcium channel blocker.
Phenprocoumon is a coumarin derivative that acts as a long acting oral anticoagulant and an antagonist of vitamin K.
Chelerythrine Chloride is a potent, cell-permeable inhibitor of protein kinase C, with an IC50 of 660 nM.
(S)-Minzasolmin is an isomer of minzasolmin (HY-145580), an inhibitor of α-synuclein oligomerization[1].
DC-Srci-6649 is a c-Src kinase inhibitor that inhibits the phosphorylation and locks c-Src in the inactive state.
Estramustine phosphate sodium is an antimicrotubule chemotherapy agent; arrests prostate cancer cells in the G2/M phase of the cell cycle.
NMS-P515 is a potent and stereospecific PARP-1 inhibitor, with an IC50 of 27 nM in hela cells. Anti-tumor activity[1].
Isoacteoside is a natural compound which exhibit significant inhibition of advanced glycation end product formation with IC50 values of 4.6-25.7 μM, compared with those of aminoguanidine (IC50=1,056 μM) and quercetin (IC50=28.4 μM) as positive controls.IC50 value:Target:In the rat lens aldose reductase assay, acteoside, isoacteoside, and poliumoside exhibited greater inhibitory effects on rat lens aldose reductase with IC50 values of 0.83, 0.83, and 0.85 μM, respectively, than those of the positive controls, 3,3-tetramethyleneglutaric acid (IC50=4.03 μM) and quercetin (IC50=7.2 μM).
dTAG-47, heterobifunctional dTAG molecule, targets mutant FKBP12 (FKBP12F36V). FKBP12F36V serves as a degradation tag (dTAG) and is fused to a protein of interest. dTAG-47 can be used for the research of basal-like breast cancers (BBC)[1].
KNI-102 is a potent anti-HIV agent with an IC50 value of 100 nM for HIV protease[1].
NSC23005 sodium is a novel and effective p18 inhibitor (ED50=5.21 nM) in promoting Hematopoietic stem cells (HSCs) expansion in both murine and human models.
iNOS-IN-2 (Compound 53) is a potent down-regulator of inducible nitric oxide synthase (iNOS) protein. iNOS-IN-2 effectively inhibits the NO production (IC50=6.4 μM). iNOS-IN-2 has a potential therapeutic effect on chronic inflammation[1].
Unguisin B s a cyclic peptides that can be isolated from the marine-derived fungus Emericella unguis[1].
Bosutinib is a dual Src/Abl inhibitor with IC50s of 1.2 nM and 1 nM, respectively.
TD52, an Erlotinib (HY-50896) derivative, is an orally active, potent cancerous inhibitor of protein phosphatase 2A (CIP2A) inhibitor. TD52 mediates the apoptotic effect in triple-negative breast cancer (TNBC) cells via regulating the CIP2A/PP2A/p-Akt signalling pathway. TD52 indirectly reduced CIP2A by disturbing Elk1 binding to the CIP2A promoter. TD52 has less p-EGFR inhibition and has potent anti-cancer activity[1].
Laprituximab (J2898A) is a humanized IgG1 anti-EGFR antibody that can be used for the synthesis of ADC IMGN289[1].
Sialyl Lewis X-Lactose is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
H-Asp(OBzl)-Obzl.TosOH is an aspartic acid derivative[1].
[D-Arg2]Dermorphin-(1-4) amide is a N-terminal shorter peptide amide of [D-Arg2]dermorphin with the hypothermic effect. [D-Arg2]Dermorphin-(1-4) amide shows analgesic activity and degradation in soluble mouse liver and brain extracts[1].
3-O-beta-Allopyranosyl-(1->4)-beta-oleandropyranosyl-11-O-isobutyryl-12-O-acetyltenacigenin B is a chemical constituent of the plant Poria cocos [1].
TP3011 is a potent topoisomerase-1 inhibitor and is the active metabolite converted from TP3076 by aldehyde oxidase 1 (AOX1)[1]. TP3011 has robust anti-tumor activities against cancer cell lines[2].
Cyclamide (Cicloral), an oligopeptide, can be produced by cyanobacteria algae strains. Cyclamide can be used for the research of diabetes mellitus[1][2].