Cefamandole nafate is a pro-drug that is hydrolyzed by plasma esterases to produce cefamandole, second-generation cephalosporin antibiotic with bactericidal activity. Cefamandole nafate is used to study the effects of expression and inhibition of PBP 2A and other penicillin-binding proteins (PDPs) on bacterial cell wall mucopeptide synthesis. Cefamandole binds to and inactivates penicillin-binding proteins (PBP) located on the inner membrane of the bacterial cell wall. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. This results in the weakening of the bacterial cell wall and causes cell lysis. 了解更多

Neuraminidase-IN-1 is a neuraminidase inhibitor, with an IC50 of 0.21 μM. Neuraminidase-IN-1 has excellent activity against H1N1 influenza virus. 了解更多

DiZPK is a photocrosslinker for identifying direct protein-protein interactions in living prokaryotic and eukaryotic cells. 了解更多

ML191 (CCG-152883, CID-23612552) is an antagonist of GPR55 with EC50 of 1.076 ?M in U2OS cells overexpressing GPR55. 了解更多

SW155246 is a potent and selective DNMT1 (DNA methyltransferase 1) inhibitor with IC50 of 1.2 μM. SW155246 induces re-expression of the tumor suppressor geneRASSF1 in A549 cells. 了解更多

MSBN is a highly selective fluorogenic probe for thiols, selectively imaging thiols in live cells and specifically label protein thiols with a turn-on signal to determine diverse reversible protein thiol modifications. 了解更多

FLTX1 is a fluorescent Tamoxifen derivative that can specifically label intracellular Tamoxifen-binding sites (estrogen receptors) under permeabilized and non-permeabilized conditions. FLTX1 exhibits the potent antiestrogenic properties of Tamoxifen in breast cancer cells. FLTX1 is devoid of the estrogenic agonistic effect on the uterus. 了解更多

FOY 251, an anti-proteolytic active metabolite Camostate (HY-13512), acts as a proteinase inhibitor. FOY 251 inhibits SARS-CoV-2 infection in cells assay. 了解更多

SR18662 is a potent inhibitor of Kr??ppel-like factor five (KLF5) with an IC50 of 4.4 nM and an analogue of ML264 (HY-19994) with improved inhibitory potency against colorectal cancer cells. SR18662 can be used for the study of colorectal cancer. 了解更多

Citronellol (Dihydrogeraniol, (±)-β-Citronellol), a constituent of rose and geranium oils, is used in perfumes and insect repellents. Citronellol can cause necrotic apoptosis of NCI-H1299 cells by up-regulating TNF-α, RIP1 / RIP3 activities, and down-regulating caspase-3 / caspase-8 activities. 了解更多

Tomatidine hydrochloride acts as an anti-inflammatory agent by blocking NF-κB and JNK signaling. Tomatidine hydrochloride activates autophagy either in mammal cells or C elegans. 了解更多

Amarogentin (AG), a secoiridoid glycoside mainly extracted from Swertia and Gentiana roots, exhibits anti-oxidative, anti-tumour, and anti-diabetic activities. Amarogentin is an agonist for the bitter taste receptor TAS2R1 and inhibits in LAD-2 cells substance P-induced production of newly synthesized TNF-α. 了解更多

3'-Hydroxypterostilbene, a natural pterostilbene analogue, effectively inhibits the growth of human colon cancer cells (IC50s of 9.0, 40.2, and 70.9 ?M for COLO 205, HCT-116, and HT-29 cells, respectively) by inducing apoptosis and autophagy. 了解更多

BMP signaling agonist sb4 is a potent benzoxazole bone morphogenetic protein 4 (BMP4) signaling agonist with a EC50 value of 74 nM, activates BMP signaling by stabilizing intracellular p-SMAD-1/5/9. 了解更多

MQAE is a fluorescent indicator that is quenched via collision with chloride, and is more sensitive and selective than 36Cl and microelectrode-based methods for chloride measurement in cells. 了解更多

HS-1793 is a resveratrol analogue. HS-1793 downregulates the expression of hypoxia-induced HIF-1 and VEGF and inhibits tumor growth of human breast cancer cells in a nude mouse xenograft model. 了解更多

UK-371804 is a potent and selective urokinase-type plasmogen activator (uPA) inhibitor with excellent enzyme potency (Ki=10 nM) and selectivity profile (4000-fold versus tPA and 2700-fold versus plasmin). 了解更多

TP0427736 is a potent inhibitor of ALK5 kinase activity with an IC50 of 2.72 nM and this effect is 300-fold higher than the inhibitory effect on ALK3 (IC50 = 836 nM for ALK3). It also inhibits Smad2/3 phosphorylation in A549 cells induced by TGF-β1 with an IC50 value of 8.68 nM. 了解更多

(E)-Methyl 4-coumarate (Methyl 4-hydroxycinnamate), found in several plants, such as green onion (Allium cepa) or noni (Morinda citrifolia L.) leaves. (E)-Methyl 4-coumarate cooperates with Carnosic Acid in inducing apoptosis and killing acute myeloid leukemia cells, but not normal peripheral blood mononuclear cells. Antioxidant and antimicrobial activity. 了解更多

(E/Z)-BCI (NSC 150117) is a dual-specificity phosphatase 6 (DUSP6) inhibitor with anti-inflammatory activities. (E/Z)-BCI attenuates LPS-induced inflammatory mediators and ROS production in macrophage cells via activating the Nrf2 signaling axis and inhibiting the NF-κB pathway. 了解更多

5,7,4'-Trimethoxyflavone is isolated from Kaempferia parviflora (KP) that is a famous medicinal plant from Thailand. 5,7,4'-Trimethoxyflavone induces apoptosis, as evidenced by increments of sub-G1 phase, DNA fragmentation, annexin-V/PI staining, the Bax/Bcl-xL ratio, proteolytic activation of caspase-3, and degradation of poly (ADP-ribose) polymerase (PARP) protein.5,7,4'-Trimethoxyflavone is significantly effective at inhibiting proliferation of SNU-16 human gastric cancer cells in a concentration dependent manner. 了解更多

ODQ is a potent and selective soluble guanylyl cyclase (sGC, nitric oxide-activated enzyme) inhibitor. ODQ enhances the pro-apoptotic effects of Cisplatin in human mesothelioma cells. 了解更多

Perillyl alcohol, a monoterpene, is active in inducing apoptosis in tumor cells without affecting normal cells. 了解更多

Ursolic acid, a naturally occurring triterpenoid, induces the apoptosis of human cancer cells through multiple signaling pathways. 了解更多

Pyridostatin stabilizes G-quadruplexes (G4s) in cells and elicits a DNA damage response by causing the formation of DNA double strand breaks (DSB). 了解更多

Merafloxacin, also known as CI 934, is a fluoroquinolone antibacterial, which was also identified as a ?1 PRF inhibitor of SARS-CoV-2. Frameshift inhibition by merafloxacin is robust to mutations within the pseudoknot region and is similarly effective on ?1 PRF of other beta coronaviruses. Importantly, frameshift inhibition by merafloxacin substantially impedes SARS-CoV-2 replication in Vero E6 cells, thereby providing the proof of principle of targeting ?1 PRF as an effective antiviral strategy for SARS-CoV-2. 了解更多

RO6889678 is an inhibitor of HBV with a complex ADME profile. RO6889678 showed an intracellular enrichment of 78-fold in hepatocytes, with an apparent intrinsic clearance of 5.2 ?l/min per mg protein and uptake and biliary clearances of 2.6 and 1.6 ?l/min per mg protein, respectively. 了解更多

PF-04995274 is a partial agonist of the serotonin (5-HT) receptor subtypes 5-HT4A, 5-HT4B, 5-HT4D, and 5-HT4E (Kis = 0.36, 0.46, 0.15, and 0.32 nM, respectively, in a radioligand binding assay).1 It increases cAMP levels in HEK293 cells expressing 5-HT4A, 5-HT4B, 5-HT4D, and 5-HT4E receptors (EC50s = 0.47, 0.36, 0.37, and 0.26 nM, respectively, for the human recombinant receptors). PF-04995274 decreases scopolamine-induced increases in the distance traveled in the Morris water maze in rats when administered at a dose of 0.032 mg/kg. 了解更多

Tenofovir exalidex, also known as HDP-Tenofovir and CMX-157, is a novel lipid acyclic nucleoside phosphonate that delivers high intracellular concentrations of the active antiviral agent tenofovir. 了解更多

MK 212 hydrochloride is a 5-HT receptor agonist; displays selectivity for 5-HT2C over 5-HT2A (IC50 values are 0.028 and 0.42 μM for human 5-HT2C and 5-HT2A receptors expressed in HEK293 cells respectively). 了解更多

EAD1 is a potent autophagy inhibitor with antiproliferative activity in lung and pancreatic cancer cells. EAD1 also induces apoptosis. 了解更多

Triptorelin is a synthetic gonadotropin-releasing hormone (GnRH) peptide agonist that binds to the GnRH receptor. It inhibits the growth of DU145, LNCaP, and PC3 prostate and OVCAR-3 ovarian cancer cells. 了解更多

FL118 is an inhibitor of human survivin expression, activating tumor suppressor p53 as a novel MOA in p53 wild-type cancer cells. 了解更多

TC-I 2000 is a TRPM8 channel blocker that inhibits icilin-induced TRPM8 channel activation in rTRPM8-expressing CHO cells 了解更多

Oct3/4-inducer-1 (compound 2) is a potent Oct3/4 inducer. Oct3/4-inducer-1 promotes expression and stabilization of Oct3/4, and enhances its transcriptional activity in diverse human somatic cells. 了解更多

THPP-1, a SGC chemical probe, is a potent and orally bioavailable phosphodiesterase 10A (PDE10A) inhibitor, with Ki values of 1 nM and 1.3 nM for human and rat PDE10A, respectively. THPP-1 has excellent pharmacokinetic properties in preclinical species. 了解更多

BLT-1, a thiosemicarbazone copper chelator, is a selective scavenger receptor B, type 1 (SR-BI) inhibitor. BLT-1 inhibits the transfer of lipids between high-density lipoproteins (HDL) and cells mediated by SR-BI. BLT-1 is a potent HCV entry inhibitor. 了解更多

Sinapinic acid (Sinapic acid) is a phenolic compound isolated from Hydnophytum formicarum Jack. Rhizome, acts as an inhibitor of HDAC, with an IC50 of 2.27 mM, and also inhibits ACE-I activity. Sinapinic acid posssess potent anti-tumor activity, induces apoptosis of tumor cells. 了解更多

α-Lipoic Acid is an antioxidant, which is an essential cofactor of mitochondrial enzyme complexes. α-Lipoic Acid inhibits NF-κB-dependent HIV-1 LTR activation. α-Lipoic Acid induces endoplasmic reticulum (ER) stress-mediated apoptosis in hepatoma cells. 了解更多

Taurolidine is a broad-spectrum antimicrobial for the prevention of central venous catheter-related infections. Taurolidine has a direct and selective antineoplastic effect on brain tumor cells by the induction of apoptosis. 了解更多

Gardenoside is a natural compound found in Gardenia fruits, with hepatoprotective properties. Gardenoside suppresses the pain of chronic constriction injury by regulating the P2X3 and P2X7 receptors. Gardenoside has an inhibitory effect on free fatty acids (FFA)-induced cellular steatosis. 了解更多

Hexylresorcinol (4-Hexylresorcinol) is a natural compound found in plants with antimicrobial, anthelmintic, antiseptic and antitumor activities. Hexylresorcinol can induce apoptosis in squamous carcinoma cells. Hexylresorcinol is a reversible and noncompetitive inhibitor of α-glucosidase. Hexylresorcinol has protective effects against oxidative DNA damage. 了解更多

L-SelenoMethionine, an L-isomer of Selenomethionine, is a major natural food-form of selenium. L-SelenoMethionin is a cancer chemopreventive agent that can reduce cancer incidence by dietary supplementation and induce apoptosis of cancer cells. 了解更多

(S)-(+)-Rolipram ((+)-Rolipram) is a cyclic AMP(cAMP)-specific phosphodiesterase 4 (PDE4) inhibitor, with an IC50 of 1100 nM. (S)-(+)-Rolipram can suppresse tumor necrosis factor-alpha (TNFα) production by human mononuclear cells. 了解更多

Dexrazoxane is an intracellular iron chelator and an inhibitor of topoisomerase IIα. 了解更多

Selective TRPM4 blocker (IC50 = 20 μM in HEK293 cells). Exhibits no effect on CFTR or TRPM5 (at 0.25 and 1 mM respectively). Abolishes arrhythmias induced by hypoxia in a mouse heart model. 了解更多

Rubitecan (RFS 2000), a Camptothecin derivative, is an orally active topoisomerase I inhibitor with broad antitumor activity, and induces protein-linked DNA single-strand breaks, thereby blocking DNA and RNA synthesis in dividing cells. 了解更多

Hydroxystilbamidine bis(methanesulfonate), a dye capable of binding to both DNA and RNA, has been found to be a powerful inhibitor of cellular ribonucleases. 了解更多

Helioxanthin derivative 5-4-2 is an analogue of helioxanthin, exhibites significant in vitro anti-HBV activity with EC50 of 0.08 uM in HepG2.2.15 cells. 了解更多