Withaphysalin R (compound 5) is a Withanolide that can be isolated from the Solanaceae. Withanolide is a steroid ester with an ergosterol skeleton, and some of these compounds have some significant activities, including cytotoxic and immunosuppressive, antitumor, anti-inflammatory, anticonvulsive, and antioxidant[1].
Antibacterial agent 46 is an antibacterial agent extracted from patent WO2013030735A1, example 9. Antibacterial agent 46 can be used for the research of bacterial infections[1].
NSC 694621 is a potent PCAF inhibitor, with an IC50 of 5.71 µM (PCAF/H31-21). NSC 694621 exhibits good activity of inhibiting the proliferation of cancer cells[1].
SCH 563705 is a potent and orally available CXCR2 and CXCR1 antagonist, with IC50s of 1.3 nM, 7.3 nM and Kis of 1 and 3 nM, respectively.
sEH/AChE-IN-4 (compound (+)-15) is a potent and BBB-penetrated dual inhibitor of sEH (soluble epoxide hydrolase) and AChE (acetylcholinesterase), with IC50 values of 3.1 nM (hsEH), 1660 nM (hAChE), 179 nM (hBChE, human butyrylcholinesterase), 14.5 nM (msEH), and 102 nM (mAChE), respectively[1].
Mapenterol-d6 hydrochloride is the deuterium labeled Mapenterol hydrochloride. Mapenterol hydrochloride is a type of β2-adrenoceptor agonist[1][2].
Tritoqualine is used as a histidine decarboxylase inhibitor.
Tiodazosin is a potent competitive postsynaptic alpha adrenergic receptor antagonist.
Methyltetrazine-PEG8-PFP ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
H-Ile-Pro-Pro-OH, a milk-derived peptide[1], inhibits angiotensin-converting enzyme (ACE)[1] with an IC50 of 5 μM[2]. Antihypertensive tripeptides[1].
KWAR23 is an anti-human SIRPα antibody. KWAR23 binds human SIRPα with high affinity and disrupts its binding to CD47. KWAR23 shows antitumor activity in combination with tumor-opsonizing antibodies and can be used in cancer immunotherapy research[1].
Lepunafusp alfa (JR-171) is a BBB-penetrable fusion protein consisting of J-Brain Cargo and IDUA (a lysosomal enzyme, α-L-iduronidase). Lepunafusp alfa can reduce concentration of heparan sulfate (HS) and dermatan sulfate (DS). Lepunafusp alfa can be used for research of mucopolysaccharidosis type I[1][2].
SARS-CoV-2 Mpro-IN-1 (compound 16b-3) is a potent, selective and irreversible inhibitor of SARS-CoV-2 main protease (Mpro), with an IC50 of 116 nM[1].
Boc-D-Asp(OcHex)-OH is an aspartic acid derivative[1].
2,4-D sodium salt (Sodium 2,4-dichlorophenoxyacetate) is a selective systemic herbicide for the control of broad-leaved weeds. 2,4-D sodium salt acts as a plant hormone, causing uncontrolled growth in the meristematic tissues. 2,4-D sodium salt inhibits DNA and protein synthesis and thereby prevents normal plant growth and development[1].
Shanzhiside methy lester is isolated from L. rotata. Shanzhiside methyl ester is a small molecule glucagon-like peptide-1 (GLP-1) receptor agonist and has the ability to induce anti-allodynic tolerance[1].
Mps1-IN-1 is a potent, selective and ATP-competitive Mps1 kinase inhibitor, with an IC50 and a Kd of 367 nM and 27 nM.
Darifenacin(UK88525) is a selective M3 muscarinic receptor antagonist with pKi of 8.9.IC50 value: 8.9 (pKi) [1]Target: M3 receptorin vitro: Darifenacin exerts non-parallel rightward displacement of the agonist curve and also significant depression of the maximum response (+)-cis-Dioxolane produced concentration-dependent contraction of the isolated bladder of rat [1]. Darifenacin produces a concentration dependent increase in R123 (P-gp probe) accumulation in MDCK cells. Darifenacin stimulates ATPase activity in P-gp membrane in a clear concentration dependent response manner with an estimated ED50 value of 1.6 μM. Darifenacin (100 nM) shows a significantly greater permeability for darifenacin in the basolateral to apical direction resulting in an efflux ratio in BBMEC monolayers of approximately 2.6 [2].in vivo: Darifenacin produces dose-dependent inhibition of amplitude of volume-induced bladder contractions(VIBCAMP), producing 35% inhibition at dose of 283.3 nmol/kg and maximal inhibition of approximately 50–55% [1]. Darifenacin (0.1 mg/kg i.v.) reduces bladder afferent activity in both Aδ and C fibers in female Sprague-Dawley rats, the decrease in afferent spikes in C fibers may be more pronounced than that in Aδ fibers [3].
DPNI-GABA is a nitroindoline cage compound that inhibits GABA(A) receptors and reduces GABA-evoked peak responses with an IC50 value of 0.5 mM[1].
NHS-NH-(diethylamino)ethyl benzoate is a compound that can be used for N-glycan labeling[1].
Tivanisiran (SYL1001) is a siRNA used for the study of dry eye disease. Tivanisiran was designed to silence transient receptor potential vanilloid 1 (TRPV1)[1].
(S)-3-(4-Hydroxyphenyl)-2-(methylamino)propanoic acid is a tyrosine derivative[1].
Ro-3306 is a potent and selective inhibitor of CDK1, with Kis of 20 nM, 35 nM and 340 nM for CDK1, CDK1/cyclin B1 and CDK2/cyclin E, respectively.
Telratolimod is a toll like receptors 7/8 (TLR7/8) agonist, with antitumor activity.
PTP1B-IN-3 is a potent and selective PTP1B inhibitor with IC50s of 120 nM (PTP1B) and 120 nM (TCPTP), respectively.
NCGC00029283 is a werner syndrome helicase-nuclease (WRN) helicase inhibitor with IC50s of 2.3 μM, 12.5 μM, and 3.4 μM for WRN, BLM and FANCJ helicase, respectively[1].
ZD-0892 is a selective and potent inhibitor of a neutrophil elastase with Kis of 6.7 and 200 nM for human neutrophil elastase and porcine pancreatic elastase, respectively.
Crustecdysone (20-Hydroxyecdysone) is a naturally occurring ecdysteroid hormone isolated from Cyanotis arachnoides C.B.Clarke which controls the ecdysis (moulting) and metamorphosis of arthropods, it inhibits caspase activity and induces autophagy via the 20E nuclear receptor complex, EcR-USP[1].Crustecdysone exhibits regulatory or protective roles in the cardiovascular system[2].
D-threo-PPMP hydrochloride is a potent inhibitor of glucosylceramide (GlcCer) synthase. D-threo-PPMP hydrochloride can block karyokinesis and reduce cyst production[1][2].