From 11:00 pm to 12:00 pm EST ( 8:00 pm to 9:00 pm PST ) on January 6th, the website will be under maintenance. We are sorry for the inconvenience. Please arrange your schedule properly.
Incensole acetate is a main constituent of Boswellia carterii resin, has neuroprotective effects against neuronal damage in traumatic and ischemic head injury. Incensole acetate reduces Aβ25–35-triggeredapoptosis in hOBNSCs .
SID 7969543 is a selective SF-1 (steroidogenic factor 1, NR5A1) inhibitor with an IC50 of 760 nM. SID 7969543 inhibits SF-1-triggered luciferase expression with IC50 of 30 nM. SF-1 is a transcription factor belonging to the nuclear receptor superfamily .
GPLGIAGQ, a MMP2-cleavable polypeptide, is used as a stimulus-sensitive linker in both liposomal and micellar nanocarriers for MMP2-triggered tumor targeting. GPLGIAGQ can be used to synthesis unique MMP2-targeted photosensitizer in photodynamic therapy (PDT) .
GPLGIAGQ TFA, a MMP2-cleavable polypeptide, is used as a stimulus-sensitive linker in both liposomal and micellar nanocarriers for MMP2-triggered tumor targeting. GPLGIAGQ TFA can be used to synthesis unique MMP2-targeted photosensitizer in photodynamic therapy (PDT) .
RGD Trifluoroacetate is a tripeptide that effectively triggers cell adhesion, addresses certain cell lines and elicits specific cell responses; RGD Trifluoroacetate binds to integrins.
Eledoisin Related Peptide is a Substance P analog that excites neurons and triggers behavioral responses. Eledoisin Related Peptide is also a tachykinin receptor ligand.
Graveoline (Rutamine) is an anti-cancer agent that can trigger apoptosis and autophagy in skin melanoma cells. Graveoline also exhibits antifungal activity .
Odetiglucan, a novel beta glucan, is a potent immunostimulant. Odetiglucan activates innate immune effector cells and triggers a coordinated anti-cancer immune response .
Biotinylated isoxazole is a biotinylated derivative of Isoxazole (HY-W010649). Biotinylated isoxazole is capable of triggering the formation of aggregates related to RNA granules .
Nerol is a constituent of neroli oil. Nerol Nerol triggers mitochondrial dysfunction and induces apoptosis via elevation of Ca 2+ and ROS. Antifungal activity .
IPTG is a molecular mimic of allolactose, a lactose metabolite that triggers transcription of the lac operon, and it is therefore used to induce protein expression where the gene is under the control of the lac operator.
FT3967385 is a novel USP30 inhibitor that recapitulates genetic loss of USP30 and sets the trigger for PINK1-PARKIN amplification of mitochondrial ubiquitylation.
Apoptosis inducer 3 (Compound 3) is an apoptosis inducer that selectively triggers apoptosis and late-apoptosis. Apoptosis inducer 3 shows cytotoxicity against cancer cells .
S-72 inhibits tubulin polymerization and further triggers mitosis-phase cell cycle arrest and cell apoptosis, in addition to suppressing STAT3 signaling .
{Boc}-Phe-Leu-Phe-Leu-Phe TFA is a formyl peptide receptor (FPR) family antagonist that preferentially inhibits activity triggered through the formyl peptide receptor .
Apoptosis inducer 6 (compound 4e) is an anticancer agent with a broad-spectrum anticancer activity. Apoptosis inducer 6 triggers cell death through the induction of apoptosis .
Anticancer agent 161 (Compound 3b) is a bioactive alkynol with anti-cancer potential. Anticancer agent 161 can trigger autophagy and mitochondrial membrane potential depletion .
{Boc}-Phe-Leu-Phe-Leu-Phe ({Boc}-FLFLF) is a formyl peptide receptor (FPR) family antagonist that preferentially inhibits activity triggered through the formyl peptide receptor .
Zingiberene (α-Zingiberene) is a monocyclic sesquiterpene which is the predominant constituent of ginger with oil content (Zingiber officinale). Neuroprotective potential . Zingiberene triggersautophagy. Anticancer activity .
Vazegepant (Zavegepant) is an orally active calcitonin gene-related peptide CGRP receptor antagonist with potential for acute research in migraine. CGRP is an important trigger in migraine pathophysiology .
GSK-LSD1 is a LSD1 inhibitor. GSK-LSD1 reduces food intake and body weight, and improves insulin sensitivity and glycemic control in mouse models of obesity. GSK-LSD1 also ameliorates NAFLD. GSK-LSD1 inhibits SARS-CoV-2-triggered cytokine release in COVID-19 PBMCs. GSK-LSD1 also inhibits cancer growth and metastasis .
Metformin hydrochloride (1,1-Dimethylbiguanide hydrochloride) inhibits the mitochondrial respiratory chain in the liver, leading to activation of AMPK, enhancing insulin sensitivity for type 2 diabetes research. Metformin hydrochloride triggersautophagy .
Microtubule inhibitor 2 is a potent and selective, orally active microtubule inhibitor. Microtubule inhibitor 2 triggers cell death through ferroptosis . Microtubule inhibitor 2 shows antitumor activity .
Azobenzene-d10 is the deuterium labeled Azobenzene[1]. Azobenzene can be used as an optical trigger for the design and synthesis of a large variety of photoresponsive systems[2][3][4].
Galloflavin potassium is a novel lactate dehydrogenase inhibitor that can be used for the research of cancer. Galloflavin inhibits aerobic glycolysis in PLC/PRF/5 cells and triggers cell death via apoptosis .
DPBQ activates p53 and triggersapoptosis in a polyploid-specific manner, but does not inhibit topoisomerase or bind DNA. DPBQ elicits expression and phosphorylation of p53 and this effect is specific to tetraploid cells .
SARS-CoV-2-IN-72 (compound 12) is a potent allosteric inhibitor of the SARS-COV-2 papain-like protease domain that can trigger the degradation of NSP3 .
Euxanthone, a xanthone derivative, attenuates Aβ1-42-induced oxidative stress and apoptosis by triggeringautophagy. Euxanthone exhibits anti-neoplastic and neuroprotective activities .
TRP-601 is a caspase inhibitor. TRP-601 reversed the increased expression of active caspase-2, the activation of endogenous apoptotic pathway and the up-regulation of key protein triggered by hyperoxia .
N6F11 is a ferroptosis inducer, and can trigger the degradation of glutathione peroxidase 4 (GPX4) specifically in cancer cells. N6F11 can be used for ferroptosis study .
Antitumor agent-128 (compound 1a) is an antitumor agent that elicits cell cycle arrest in both the G2/M and S phases, triggeringapoptosis in A549 cells .
Nifurpirinol (P-7138) is a nitroaromatic antibiotic and acts as a novel substrate for the bacterial nitroreductase (NTR) enzyme. Nifurpirinol is a more potent proagent compared to Metronidazole to trigger cell-ablation in nitroreductase expressing transgenic models .
Domperidone (R33812) is an orally active and selective dopamine-2 receptor antagonist. Domperidone acts as an antiemetic and a prokinetic agent through its effects on the chemoreceptor trigger zone and motor function of the stomach and small intestine .
FSEN1 is a potent and non-competitive FSP1 inhibitor with an IC50 value of 313 nM. FSEN1 triggers iron death in cancer cells by inhibiting FSP1. FSEN1 can be used in research of cancer .
(+)-Erinacin A is an anticancer compound that can be isolated from the mushroom Hericium erinaceum. (+)-Erinacin A has the capacity to trigger cancer cell death dependent on the production of reactive oxygen species (ROS). (+)-Erinacin A has anticancer and neuroprotective activity .
Maropitant is a selective and orally active neurokinin (NK1) receptor antagonist. Maropitant acts by blocking the binding of substance P within the emetic center and the chemoreceptor trigger zone (CRTZ). Maropitant is highly effective in preventing vomiting .
G150 is a highly selective human cyclic GMP-AMP synthase (h-cGAS) inhibitor with an IC50 of 10.2 nM. G150 represses dsDNA-triggered interferon expression, and G150 can be used for the research of inflammatory .
Metformin (1,1-Dimethylbiguanide) inhibits the mitochondrial respiratory chain in the liver, leading to activation of AMPK, enhancing insulin sensitivity for type 2 diabetes research. Metformin can cross the blood-brain barrier and triggersautophagy .
D-Tyrosine is the D-isomer of tyrosine. D-Tyrosine negatively regulates melanin synthesis by inhibiting tyrosinase activity. D-Tyrosine inhibits biofilm formation and trigger the self-dispersal of biofilms without suppressing bacterial growth .
SDOX is the Doxorubicin (DOX) proagent. The loaded DOX proagents (SDOX) which can release the parent agents DOX triggered by excessive GSH in tumor cells, minimize the unexpected side effects on normal tissues without compromising the potency .
Vidutolimod sodium is a CpG-A oligodeoxynucleotide. Vidutolimod sodium is a Toll-like receptor 9 (TLR9) agonist, which activates plasmacytoid dendritic cells (pDCs) and triggers interferon alpha (IFNα) release, leading to a cascade of anti-tumor immune effects.
Microtubule inhibitor 8 (MP-HJ-1b) is a potent inhibitor of microtubule. Microtubule inhibitor 8 triggers cell death through ferroptosis. Microtubule inhibitor 8 has anti-tumor effect .
DHODH-IN-26 (compound B2) is a mitochondria-targeting DHODH inhibitor. DHODH-IN-26 shows anticancer activity, triggers the formation of reactive oxygen species (ROS), promots mitochondrial lipid peroxidation, and induces ferroptosis .
Metformin-d6 (hydrochloride)e is a deuterium labeled Metformin hydrochloride. Metformin hydrochloride inhibits the mitochondrial respiratory chain in the liver, leading to activation of AMPK, enhancing insulin sensitivity for type 2 diabetes research. Metformin hydrochloride triggers autophagy[1].
Hellebrigenin, one of bufadienolides belonging to cardioactive steroids, is isolated from traditional Chinese medicine Venenum Bufonis. Hellebrigenin induces DNA damage and cell cycle G2/M arrest. Hellebrigenin triggers mitochondria-mediated apoptosis.
Domperidone (R33812) monomaleate is an orally active and selective dopamine-2 receptor antagonist. Domperidone monomaleate acts as an antiemetic and a prokinetic agent through its effects on the chemoreceptor trigger zone and motor function of the stomach and small intestine .
FBBBE is used to detect the production of H2O2 by cells. FBBBE can be triggered by intracellular H2O2 and converted to fluorescein, resulting in an increase in intracellular fluorescence (Ex=4480 nm, Em=512 nm) .
Nerol (Standard) is the analytical standard of Nerol. This product is intended for research and analytical applications. Nerol is a constituent of neroli oil. Nerol Nerol triggers mitochondrial dysfunction and induces apoptosis via elevation of Ca 2+ and ROS. Antifungal activity .
iRGD peptide is a 9-amino acid cyclic peptide, triggers tissue penetration of agents by first binding to αv-integrins, then proteolytically cleaved in the tumor to produce CRGDK/R to interact with neuropilin-1, and has tumor-targeting and tumor-penetrating properties.
BI-0115 is a selective inhibitor of LOX-1 (IC50=5.4 µM) that blocks cellular uptake of oxLDL. BI-0115 binding triggers receptor inhibition by formation of dimers of the homodimeric ligand binding domain .
Anti-inflammatory agent 13 (Compound 3) is a pentacyclic triterpene compound. Anti-inflammatory agent 13 exhibits a considerable inhibitory effect on inflammation models. Anti-inflammatory agent 13 has the potential for the research of either DAMPs or PAMPs triggered inflammation .
VK-II-36 is a carvedilol analog that suppresses sarcoplasmic reticulum Ca 2+release but does not block the β-receptor.VK-II-36 inhibits triggered activities evoked by both early and delayed after depolarizations .
Berubicin hydrochloride (RTA 744) is a Doxorubicin (HY-15142A) analogue. Berubicin hydrochloride triggersapoptosis and cell killing in NB cells by activating proapoptotic mediators. Berubicin hydrochloride has proapoptotic and anti-leukemia activities. Berubicin hydrochloride can be used for cancer research .
Vidutolimod (CMP-001) is a CpG-A oligodeoxynucleotide. Vidutolimod is a Toll-like receptor 9 (TLR9) agonist, which activates plasmacytoid dendritic cells (pDCs) and triggers interferon alpha (IFNα) release, leading to a cascade of anti-tumor immune effects.
Ara-SH is a Cytarabine mercaptopropionic acid-substituted derivative. Ara-SH is used as the trigger to fabricate a smart Cytarabine and Venetoclax-coloaded nanoparticle (AV-NP) through self-assembly. Ara-SH exhibits remarkable synergistic antileukemia effects in vitro and in vivo .
Anticancer agent 193 (compound D3-3) is an inducer of ferritinophagy, eventually triggeringferroptosis. Anticancer agent 193 induces the production of lipid ROS, and significantly promoted colorectal cancer cells to release the ferrous ion in an autophagy-dependent manner .
DFPM activates plant resistance protein signaling in roots, and triggers root growth arrest. DFPM decreases root cell viability in accession Col-0. DFPM is light sensitive in aqueous solutions. DFPM becomes bioactive during light and oxygen-dependent modification .
ChemR23-IN-1 (compound 2) is a ChemR23 inhibitor with IC50s of 38 nM and 100 nM for human and mouse ChemR23, respectively. ChemR23-IN-1 inhibits chemotaxis of CAL-1 triggered by Chemerin in vitro .
Topoisomerase II inhibitor 4 (compound E17) is a potent Topoisomerase II inhibitor. Topoisomerase II inhibitor 4 triggers G2/M cell cycle arrest and shows anti-tumor activity with strong cytotoxic and anti-proliferative effect .
Nadunolimab is a human monoclonal IgG1 antibody targeting IL1RAP. Nadunolimab blocks IL-1α and IL-1β signaling and triggering antibody-dependent cellular cytotoxicity. Nadunolimab can be used in research of cancer .
Urokinase (peptidolytic) (EC 3.4.21.73) is a serine protease, an inactive form (zymogen) of the serine protease plasminogen. Activation of plasmin triggers a proteolytic cascade reaction, which in turn participates in thrombolysis or extracellular matrix degradation, implicated in vascular disease and cancer-related research .
Metformin (hydrochloride) (Standard) is the analytical standard of Metformin (hydrochloride). This product is intended for research and analytical applications. Metformin hydrochloride (1,1-Dimethylbiguanide hydrochloride) inhibits the mitochondrial respiratory chain in the liver, leading to activation of AMPK, enhancing insulin sensitivity for type 2 diabetes research. Metformin hydrochloride triggersautophagy .
ORIC-533 is an orally active, selective CD73 inhibitor with AMP-competition. ORIC-533 restores immunosuppressed CD8+ T cell proliferation and activation, triggers significant lysis and cell death of multiple myeloma cells in the bone marrow microenvironment .
Domperidone-d6 is the deuterium labeled Domperidone. Domperidone (R33812) is a selective dopamine-2 receptor antagonist. Domperidone acts as an antiemetic and a prokinetic agent through its effects on the chemoreceptor trigger zone and motor function of the stomach and small intestine[1][2].
KRA-533 is a potent KRAS agonist. KRA-533 binds to the GTP/GDP binding pocket in the KRAS protein to prevent GTP cleavage, resulting in the accumulation of constitutively active GTP-bound KRAS that triggers both apoptotic and autophagic cell death pathways in cancer cells.
Skp2 Inhibitor C1 (SKPin C1) is an S-phase kinase-related protein 2 (Skp2) inhibitor with an inhibitory effect on metastatic melanoma cells. Skp2 Inhibitor C1 slows the cell cycle, inhibits cell proliferation, and triggersapoptosis .
Imetit dihydrobromide (VUF 8325 dihydrobromide) is a high affinity and potent agonist of histamine H3 and H4 receptors, with Ki values of 0.3 and 2.7 nM, respectively. Imetit mimics histamine effect in triggering a shape change in eosinophils (EC50=25 nM) .
Mitochondria-Targeted Photoactivatable Proagent accumulates in the mitochondria and shows light-triggered temporally controlled cell death. Mitochondria-Targeted Photoactivatable Proagent can be used in a novel drug delivery platform that provides on-demand, real-time, organelle-specific agent release and monitoring upon photoactivation .
Gue1654 is a modulator of OXE-R. Gue1654 inhibits Gβγ but not Gα signaling triggered upon activation of Gα(i)-βγ by the chemoattractant receptor OXE-R. Gue1654 does not interfere nonspecifically with signaling directly at or downstream of Gβγ .
Cusatuzumab is a human αCD70 monoclonal antibody. Cusatuzumab shows cytotoxicity activity with enhanced antibody-dependent cellular. Cusatuzumab reduces leukemia stem cells (LSCs) and triggers gene signatures related to myeloid differentiation and apoptosis. Cusatuzumab has the potential for the research of Acute myeloid leukemia (AML) .
cGAMP (Cyclic GMP-AMPP) functions as an endogenous second messenger in metazoans and triggers interferon production in response to cytosolic DNA. cGAMP activates stimulator of interferon genes (STING), which activates a signaling cascade leading to the production of type I interferons and other immune mediators .
Estramustine phosphate sodium, an estradiol analog, is an orally active antimicrotubule chemotherapy agent. Estramustine phosphate sodium depolymerises microtubules by binding to microtubule associated proteins (MAPs) and/or to tubulin. Estramustine phosphate sodium can interfere mitosis, trigger cell death and induce apoptosis, which can be used for the research of cancer like prostate cancer .
AhR agonist 2 (Compound 12a) is a potent agonist of aryl hydrocarbon receptor (AhR) with an EC50 of 0.03 nM. AhR agonist 2 induces rapid nuclear enrichment of AhR, triggers the transcription of downstream genes and promote skin barrier repair. AhR agonist 2 has the potential for the research of psoriasis .
Estramustine phosphate, an estradiol analog, is an orally active antimicrotubule chemotherapy agent. Estramustine phosphate depolymerises microtubules by binding to microtubule associated proteins (MAPs) and/or to tubulin. Estramustine phosphate can interfere mitosis, trigger cell death and induce apoptosis, which can be used for the research of cancer like prostate cancer .
Dazostinag disodium (TAK-676) is an agonist of STING, triggering the activation of STING signaling pathway and type I interferons. Dazostinag disodium is also a modulator of immune system, resulting complete regressions and durable memory T-cell immunity. Dazostinag disodium promotes durable IFN-dependent antitumor immunity .
Virodhamine is an endocannabinoid, it regulates neurotransmission by activating the cannabinoid (CB) receptors. Virodhamine is an antagonist of CB1 receptor and an agonist of CB2 receptor. Virodhamine induces megakaryocytic differentiation by triggeringMAPK signaling and ROS production. Virodhamine can be used for the research of various neurological disorders such as Alzheimer's and Parkinson's diseases .
AJH-836 is an activator of Munc13-1 and PKC ε/α (Kd: 4.5 nM for PKCα) . AJH-836 triggers the translocation of Munc13-1 from the cytoplasm to the plasma membrane. AJH-836 can be used for research of neurodegenerative diseases .
Darapladib (SB-480848) is an orally active, selective and reversible Lp-PLA2 inhibitor (IC50=0.25 nM). Darapladib can trigger irreversible actions on glioma cell apoptosis and induce cycle arrest. Darapladib can be used in the study of atherosclerosis and cancer .
AGI-24512 is a potent methionine adenosyltransferase 2α (MAT2A) inhibitor, with an IC50 of 8 nM. AGI-24512 triggers DNA damage response. AGI-24512 can block proliferation of MTAP-deleted cancer cells in vitro. AGI-24512 can be used for researching anticancer .
Eriocitrin is a flavonoid isolated from lemons that is a powerful antioxidant. Eriocitrin inhibits the proliferation of liver cancer cells by arresting the cell cycle in the S phase by upregulating p53, cyclin A, cyclin D3 and CDK6. Eriocitrin triggers apoptosis by activating intrinsic signaling pathways involving mitochondria .
RAMB4 is a ubiquitin-proteasome system (UPS)-stressor. RAMB4 inhibits ubiquitin-mediated protein degradation upstream of the 20S proteasomal catalytic activites. RAMB4 triggers a ubiquitin-proteasome-system (UPS)-stress response without affecting 20S proteasome catalytic activities. Anticancer activity .
cGAMP (Cyclic GMP-AMPP) disodium functions as an endogenous second messenger in metazoans and triggers interferon production in response to cytosolic DNA. cGAMP diammonium activates stimulator of interferon genes (STING), which activates a signaling cascade leading to the production of type I interferons and other immune mediators .
CL075 (3M002) is a selective TLR8 agonist with immunomodulating properties. CL075 triggers a MyD88-dependent signaling pathway to elicit production of inflammatory cytokines and type I interferons (IFNs) via activation of NF-κB and IRF7, respectively .
cGAMP (Cyclic GMP-AMPP) diammonium functions as an endogenous second messenger in metazoans and triggers interferon production in response to cytosolic DNA. cGAMP diammonium activates stimulator of interferon genes (STING), which activates a signaling cascade leading to the production of type I interferons and other immune mediators .
D-Tyrosine-d2 is the deuterium labeled D-Tyrosine. D-Tyrosine is the D-isomer of tyrosine. D-Tyrosine negatively regulates melanin synthesis by inhibiting tyrosinase activity. D-Tyrosine inhibits biofilm formation and trigger the self-dispersal of biofilms without suppressing bacterial growth[1][2].
D-Tyrosine-d4 is the deuterium labeled D-Tyrosine. D-Tyrosine is the D-isomer of tyrosine. D-Tyrosine negatively regulates melanin synthesis by inhibiting tyrosinase activity. D-Tyrosine inhibits biofilm formation and trigger the self-dispersal of biofilms without suppressing bacterial growth[1][2].
D-Tyrosine-d7 is the deuterium labeled D-Tyrosine. D-Tyrosine is the D-isomer of tyrosine. D-Tyrosine negatively regulates melanin synthesis by inhibiting tyrosinase activity. D-Tyrosine inhibits biofilm formation and trigger the self-dispersal of biofilms without suppressing bacterial growth[1][2].
Hyaluronate lyase can cleat hyaluronate (HA) and produce unsaturated disaccharides through a β-elimination reaction. The resulting disaccharides further trigger the downstream pathway and catalyze the next reaction. Hyaluronate lyase helps Streptococcus dysgalactiae subsp.equisimilis (SDSE) acquire nutrients from the host, causing bacterial pathogenicity .
icFSP1 is a potent ferroptosis suppressor protein-1 (FSP1) inhibitor. icFSP1 does not competitively inhibit FSP1 enzyme activity, but instead triggers subcellular relocalization of FSP1 from the membrane and FSP1 condensation before ferroptosis induction, in synergism with GPX4 inhibition .
Eprenetapopt (APR-246) is a first-in-class, small molecule that restores wild-type p53 functions in TP53-mutant cells. Eprenetapopt triggers apoptosis in tumor cells. Eprenetapopt also targets the selenoprotein thioredoxin reductase 1 (TrxR1), a key regulator of cellular redox balance .
HDAC-IN-33 is a potent HDAC inhibitor with IC50s of 24, 46, and 47 nM for HDAC1, HDAC2 and HDAC6, respectively. HDAC-IN-33 possesses potent antiproliferation activities against tumor cells. HDAC-IN-33 shows potent antitumor efficacy in vivo That trigger antitumor immunity .
GD3 Ganglioside is a prominent ganglioside of human melanoma. GD3 Ganglioside is an inducer of mitochondrial permeability. GD3 ganglioside directly targets mitochondria in a bcl-2-controlled fashion. GD3 ganglioside is rapidly synthesized from accumulated ceramide after the clustering of death-inducing receptors and triggers apoptosis .
Naphthazarin (DHNQ) is a naturally occurring compound. Naphthazarin is effective by various cellular mechanisms including oxidative stress, activation of mitochondrial apoptosis-inducing factor (AIF), depolymerization of microtubules, interference with lysosomal function and p53-dependent p21 activation. Naphthazarin triggersapoptosis and has anti-tumor effects .
Anticancer agent 194 (compound 10p) is a ferroptosis and autophagy inducer. Anticancer agent 194 arrests colon cancer cell cycle at G2/M phase, but can't induce cell apoptosis. Anticancer agent 194 independently triggeres cell ferroptosis and autophagy through the massive accumulation of ROS .
Rostafuroxin (PST 2238), a digitoxigenin derivative, is an orally active and potent Na +,K +-ATPase (ATP1A1) antognist. Rostafuroxin binds specifically to the ATP1A1 extracellular domain and blocks respiratory syncytial virus (RSV)-triggered EGFR Tyr845 phosphorylation. Rostafuroxin has antihypertensive and anti-RSV activity .
PR-924 is a selective tripeptide epoxyketone immunoproteasome subunit LMP-7 inhibitor with an IC50 of 22 nM. PR-924 covalently modifies proteasomal N-terminal threonine active sites. PR-924 inhibits growth and triggersapoptosis in multiple myeloma (MM) cells. PR-924 has antitumor activities .
Lycopodine, a pharmacologically important bioactive component derived from Lycopodium clavatumspores, triggersapoptosis by modulating 5-lipoxygenase, and depolarizing mitochondrial membrane potential in refractory prostate cancer cells without modulating p53 activity . Lycopodine inhibits proliferation of HeLa cells through induction of apoptosis via caspase-3 activation .
Ecdysone (α-Ecdysone), a major steroid hormone in insects and herbs, triggersmineralocorticoid receptor (MR) activation and induces cellular apoptosis. Ecdysone plays essential roles in coordinating developmental transitions and homeostatic sleep regulation through its active metabolite 20-hydroxyecdysone (Crustecdysone; 20E; HY-N6979) .
Pifusertib (TAS-117) hydrochloride is a potent, selective, orally active allosteric Akt inhibitor (with IC50s of 4.8, 1.6, and 44 nM for Akt1, 2, and 3, respectively). Pifusertib hydrochloride triggers anti-myeloma activities and enhances fatal endoplasmic reticulum (ER) stress induced by proteasome inhibition. Pifusertib hydrochloride induces apoptosis and autophagy .
Pifusertib (TAS-117) is a potent, selective, orally active allosteric Akt inhibitor (with IC50s of 4.8, 1.6, and 44 nM for Akt1, 2, and 3, respectively). Pifusertib triggers anti-myeloma activities and enhances fatal endoplasmic reticulum (ER) stress induced by proteasome inhibition. Pifusertib induces apoptosis and autophagy .
Famitinib (SHR1020), an orally active multi-targeted kinase inhibitor, inhibits the activity of c-kit, VEGFR-2 and PDGFRβ with IC50 values of 2.3 nM, 4.7 nM and 6.6 nM, respectively . Famitinib exerts powerful antitumor activity in human gastric cancer cells and xenografts. Famitinib triggersapoptosis .
HDAC-IN-32 is a potent HDAC inhibitor with IC50s of 5.2, 11, and 28 nM for HDAC1, HDAC2 and HDAC6, respectively. HDAC-IN-32 possesses potent antiproliferation activities against tumor cells. HDAC-IN-32 shows potent antitumor efficacy in vivo That trigger antitumor immunity .
HQ461 is a molecular glue that promotes CDK12-DDB1 interaction to triggercyclin K degradation. HQ461-mediated degradation of cyclin K impairs CDK12 function, resulting in decreased CDK12 substrate phosphorylation, downregulation of DNA damage response genes, and cell death .
Maropitant- 13C,d3 is the 13C- and deuterium labeled Maropitant. Maropitant is a selective and orally active neurokinin (NK1) receptor antagonist. Maropitant acts by blocking the binding of substance P within the emetic center and the chemoreceptor trigger zone (CRTZ). Maropitant is highly effective in preventing vomiting[1][2].
ZLHQ-5f is a dual CDK2 and Topo I inhibitor with an IC50 of 0.145 μM against CDK2/CycA2. ZLHQ-5f arrests the cell cycle in S-phase, triggersapoptosis in HCT116 cells, and has a good safety profile .
Loncastuximab tesirine is a human cluster of differentiation 19 (CD19)-directed antibody-drug conjugate (ADC). Once bound to CD19 on the cell membrane, loncastuximab tesirine is rapidly internalised and triggers cell death. Loncastuximab tesirin induces cell apoptosis, it can be used for the research of diffuse large B-cell lymphoma .
Picrasidine I is an anti-inflammatory and anti-osteoclastogenic dimeric alkaloid that can be isolated from Picrasma quassioides. Picrasidine I inducs cell cycle arrest, and triggers cell apoptosis by downregulats ERK and Akt pathways. Picrasidine I inhibits the activation of MAPKs, NF-κB and ROS generation, and suppresses the expression of c-Fos and NFATc1 .
Bozepinib is a PKR (RNA-dependent protein kinase) activator and potently inhibits the HER-2 signaling pathway as well as JNK and ERK kinases. Bozepinib induces PKR-mediated apoptosis and synergizes with IFNα to triggerapoptosis, autophagy and senescence. Bozepinib also demonstrates in vivo antitumor and antimetastatic efficacy in xenografted nude mice .
Ziyuglycoside I isolated from S. officinalis root, has anti-wrinkle activity, and increases the expression of type I collagen. Ziyuglycoside I could be used as an active ingredient for cosmetics . Ziyuglycoside I triggers cell cycle arrest and apoptosis mediated by p53, it can be a potential agent candidate for treating triple-negative breast cancer (TNBC) .
Physalin B, one of the major active steroidal constituents of Cape gooseberry, induces cell cycle arrest and triggersapoptosis in breast cancer cells through modulating p53-dependent apoptotic pathway. Physalin B inhibits the ubiquitin-proteasome pathway and induces incomplete autophagic response in human colon cancer cells in vitro .
Cibisatamab (CEA-TCB), a T cell bispecific antibody, binds Carcino-Embryonic Antigen (CEA) on cancer cells and CD3 on T cells. Cibisatamab (CEA-TCB) triggers T cell killing of cancer cell lines expressing moderate to high levels of CEA at the cell surface. Cibisatamab (CEA-TCB) can be used for colorectal cancer research .
Poly(styrenyl acetal trehalose) (pSAT) is composed of trehalose side chains linked to a polystyrene backbone via acetals. Poly(styrenyl acetal trehalose) stabilizes a variety of proteins and enzymes against fluctuations in temperature, and does not trigger the innate immune response. Poly(styrenyl acetal trehalose) can be used in synthesis of protein-polymer conjugates for reduced renal clearance of the biomolecule .
CDN-A is a cyclic di-nucleotide, it can be used to synthesis antibody-drug conjugate (ADC). Cyclic di-nucleotides are potent stimulators of innate and adaptive immune responses. In humans, cyclic di-nucleotide, which are either produced endogenously in response to foreign DNA or by invading bacterial pathogens, trigger the innate immune system by activating the expression of interferon genes .
R1530 is a highly potent, orally active, dual-acting mitosis/angiogenesis inhibitor, with anti-tumor and anti-angiogenic activities. R1530 is a multikinase inhibitor which binds to 31 kinases with Kd values of <500 nM. R1530 inhibits VGFR2 and FGFR1 with IC50 of 10 nM and 28 nM, respectively. R1530 triggers apoptosis (mitotic catastrophe) or senescence .
(E)-Methyl 3,4,5-trimethoxycinnamate is a bioactive natural phenylpropanoid. (E)-Methyl 3,4,5-trimethoxycinnamate suppresses inflammation in RAW264.7 macrophages and blocks macrophage-adipocyte interaction. (E)-Methyl 3,4,5-trimethoxycinnamate also has antiarrhythmic effect, leads to suppression of triggered activities in rabbit myocytes .
(Pyr3)-Amyloid β-Protein (3-42) is the predominant amyloid β-peptide structure deposited in human brain of Alzheimer's disease and Down's syndrome patients. (Pyr3)-Amyloid β-Protein (3-42) is suggested to accumulate in the brain and to trigger the formation of insoluble amyloid β-peptide deposits .
Chelerythrine is a natural alkaloid, acts as a potent and selective Ca 2+/phospholopid-dependent PKC antagonist, with an IC50 of 0.7 μM . Chelerythrine has antitumor, antidiabetic and anti-inflammatory activity . Chelerythrine inhibits the BclXL-Bak BH3 peptide binding with IC50 of 1.5 μM and displaces Bax from BclXL. Chelerythrine triggersapoptosis and autophagy .
BT2 is a BCKDC kinase (BDK) inhibitor with an IC50 of 3.19 μM. BT2 binding to BDKtriggers helix movements in the N-terminal domain, resulting in the dissociation of BDK from the branched-chain α-ketoacid dehydrogenase complex (BCKDC) . BT2 (compound 4) is also a potent and selective Mcl-1 inhibitor with a Ki value of 59 μM .
HE-S2 is an antibody-drug conjugate triggering a potent antitumor immune response. HE-S2 acts by blocking the PD-1/PD-L1 interaction and activating the Toll-like receptor 7/8 (TLR7/8) signaling pathway. HE-S2 has remarkable antitumor activity .
Bonannione A (6-Geranylnaringenin; Mimulone), a prenylflavonoid, is an orally active and potent protein tyrosine phosphatase 1B (PTP1B) inhibitor with an IC50 of 14 µM. Bonannione A triggers caspase-dependent apoptosis. Bonannione A induces autophagy through p53-mediated AMPK/mTOR pathway. Bonannione A shows anti-inflammatory, antiradical and anti-cancer activity .
Ganoderic acid T1 is a deacetylated derivative of Ganoderic acid T. Ganoderic acid T1 attenuates antioxidant defense system and induces apoptosis of cancer cells. Ganoderic acid T1 decreases mitochondrial membrane potential and activates caspase-9 and caspase-3, to trigger apoptosis. Ganoderic acid T1 also increases the generation of intracellular ROS to produce pro-oxidant activities and cytotoxicity .
(Pyr3)-Amyloid β-Protein (3-42) TFA is the predominant amyloid β-peptide structure deposited in human brain of Alzheimer's disease and Down's syndrome patients. (Pyr3)-Amyloid β-Protein (3-42) TFA is suggested to accumulate in the brain and to trigger the formation of insoluble amyloid β-peptide deposits .
CBI1 is a covalent BAX inhibitor. CBI1 selectively derivatizes BAX at C126 and inhibits BAX activation by triggering ligands or point mutagenesis. CBI1 blocks t-2-hex lipidation and oligomerization of BAX. CBI1 inhibits BAX activation induced by BH3 ligands, F116A mutagenesis or t-2-hex .
Trimetazidine dihydrochloride is a selective long chain 3-ketoyl coenzyme A thiolase inhibitor with an IC50 of 75 nM, which can inhibit β-oxidation of free fatty acid (FFA). Trimetazidine dihydrochloride is an effective antianginal agent and a cytoprotective agent, has anti-oxidant, anti-inflammatory, antinociceptive and gastroprotective properties. Trimetazidine dihydrochloride triggers autophagy. Trimetazidine dihydrochloride is also a 3-hydroxyacyl-CoA dehydrogenase (HADHA) inhibitor .
Polyphyllin VI, an active saponin, possess anti-cancer activities. Polyphyllin VI induces G2/M cell cycle arrest and triggersapoptosis. Polyphyllin VI induces caspase-1-mediated pyroptosis via the induction of ROS/NF-κB/NLRP3/GSDMD signal axis in non-small cell lung cancer .
Trimetazidine is a selective long chain 3-ketoyl coenzyme A thiolase inhibitor with an IC50 of 75 nM, which can inhibit β-oxidation of free fatty acid (FFA). Trimetazidine is an effective antianginal agent and a cytoprotective agent, has anti-oxidant, anti-inflammatory, antinociceptive and gastroprotective properties. Trimetazidine triggersautophagy. Trimetazidine is also a 3-hydroxyacyl-CoA dehydrogenase (HADHA) inhibitor .
Antitumor agent-78 is an antitumor agent, inhibits cancer cells growth and migration. Antitumor agent-78 triggersferroptosis by inhibiting GPx-4 and elevating COX2. Antitumor agent-78 also activates intrinsic apoptotic pathway (Bax-Bcl-2-caspase-3) and hinders Epithelial-mesenchymal transition (EMT) process of cancer cells .
Antitumor agent-77 is an antitumor agent, inhibits cancer cells growth and migration. Antitumor agent-77 triggersferroptosis by inhibiting GPx-4 and elevating COX2. Antitumor agent-77 also activates intrinsic apoptotic pathway (Bax-Bcl-2-caspase-3) and hinders Epithelial-mesenchymal transition (EMT) process of cancer cells .
MOPIPP is a novel indolebased chalcone, and vacuolin-1, is a non-lethal vacuoleinducing 2-propyl analog of MOMIPP (HY-148114). MOPIPP induces cellular vacuolization and increases autophagosomes numbers. MOPIPP also triggersmethuosis, and interrupts glucose uptake and glycolytic metabolism. MOPIPP can cross the blood-brain barrier and shows efficacy in suppressing tumor progression agaisnt glioblastoma cells .
FtsZ-IN-5 is a potent FtsZ inhibitor, to promote FtsZ polymerization and inhibit GTPase activity of FtsZ. Thus, FtsZ-IN-5 inhibits bacterial division to lead to death of bacterial cells. FtsZ-IN-5 shows bactericidal activity with no significant tendency to trigger bacterial resistance as well as rapid bactericidal properties. And FtsZ-IN-5 shows low hemolytic activity and cytotoxicity to mammalian cells .
FtsZ-IN-6 is a potent FtsZ inhibitor, to promote FtsZ polymerization and inhibit GTPase activity of FtsZ. Thus, FtsZ-IN-6 inhibits bacterial division to lead to death of bacterial cells. FtsZ-IN-6 shows bactericidal activity with no significant tendency to trigger bacterial resistance as well as rapid bactericidal properties. And FtsZ-IN-6 shows low hemolytic activity and cytotoxicity to mammalian cells .
FtsZ-IN-7 is a potent FtsZ inhibitor, to promote FtsZ polymerization and inhibit GTPase activity of FtsZ. Thus, FtsZ-IN-7 inhibits bacterial division to lead to death of bacterial cells. FtsZ-IN-7 shows bactericidal activity with no significant tendency to trigger bacterial resistance as well as rapid bactericidal properties. And FtsZ-IN-7 shows low hemolytic activity and cytotoxicity to mammalian cells .
FtsZ-IN-8 is a potent FtsZ inhibitor, to promote FtsZ polymerization and inhibit GTPase activity of FtsZ. Thus, FtsZ-IN-8 inhibits bacterial division to lead to death of bacterial cells. FtsZ-IN-8 shows bactericidal activity with no significant tendency to trigger bacterial resistance as well as rapid bactericidal properties. And FtsZ-IN-8 shows low hemolytic activity and cytotoxicity to mammalian cells .
HL23 is a histone deacetylase (HDAC) inhibitor with activity against hepatocellular carcinoma (HCC). HL23 enhances acetylation of the TXNIP promoter and upregulates TXNIP expression, thereby mediating potassium channel activity and triggering TXNIP-dependent potassium deprivation. HL23 inhibits HCC progression and metastasis and has a synergistic effect with Sorafenib (HY-10201) and is more potent than Sorafenib+Vorinostat (HY-10221) .
17R-Resolvin D1 (17R-RvD1; AT-RvD1) is an aspirin-triggered epimer of Resolvin D1, which exhibits anti-inflammatory activity in mice and human PMNs cells . 17R-Resolvin D1 specificially inhibits TRPV3 with an IC50 of 398 nM and exhibits peripheral anti-nociceptive efficacy .
RO2959 hydrochloride is a potent and selective CRAC channel inhibitor with an IC50 of 402 nM. RO2959 hydrochloride is a potent blocker of store operated calcium entry (SOCE) mediated by Orai1/Stim1 channels with an IC50 of 25 nM. RO2959 hydrochloride is also a potent inhibitor of human IL-2 production, and potently blocks T cell receptor triggered gene expression and T cell functional pathways .
Topoisomerase II inhibitor 3 (Compound 6 h ) is a acridone derivatives, as well as a Type II DNA topoisomerase (topo II) inhibitor , as a topo IIα/β inhibitor with the value of IC50 is 0.17 μM for topo IIα and the value of IC50 is 0.23 μM for topo IIβ subtypes, caused obvious DNA damage, and induced apoptosis by triggering the loss of mitochondrial membrane potential .
SOS1 agonist-1 (compound 79) is an agonist for the Son of sevenless homologue SOS1. SOS1 is a guanine nucleotide exchange factor that catalyzes the exchange of GDP to GTP on RAS and regulates RAS activation. SOS1 agonists increase nucleotide exchange on RAS, enhance cellular RAS-GTP levels, and trigger biphasic signaling changes in ERK1/2 phosphorylation. Play an anti-cancer role [1] .
PROTAC GPX4 degrader-2 (compound 18a) is a proteolysis targeting chimeras (PROTACs) that can degrade glutathione peroxidase 4 (GPX4), with the DC50, 48h value of 1.68 μM. PROTAC GPX4 degrader-2 induces the accumulation of lipid peroxides and mitochondrial depolarization, subsequently triggeringferroptosis. PROTAC GPX4 degrader-2 has anti-proliferative effect .
RRx-001, a hypoxia-selective epigenetic agent and studied as a radio- and chem-sensitizer, triggersapoptosis and overcomes agent resistance in myeloma. RRx-001 exhibits potent anti-tumor activity with minimal toxicity . RRx-001 is a dual small molecule checkpoint inhibitor by downregulating CD47 and SIRP-α . RRx-001 is a potent inhibitor of G6PD and shows potent antimalarial activity .
Polyinosinic-polycytidylic acid (Poly(I:C)) sodium is a synthetic analog of double-stranded RNA and an agonist of toll-like receptor 3 (TLR3) and retinoic acid inducible gene I (RIG-I)-like receptors (RIG-I and MDA5). Polyinosinic-polycytidylic acid sodium can be used as a vaccine adjuvant to enhance innate and adaptive immune responses, and to alter the tumor microenvironment. Polyinosinic-polycytidylic acid sodium can directly trigger cancer cells to undergo apoptosis .
Polyinosinic-polycytidylic acid (Poly(I:C)) is a synthetic analog of double-stranded RNA and an agonist of toll-like receptor 3 (TLR3) and retinoic acid inducible gene I (RIG-I)-like receptors (RIG-I and MDA5). Polyinosinic-polycytidylic acid can be used as a vaccine adjuvant to enhance innate and adaptive immune responses, and to alter the tumor microenvironment. Polyinosinic-polycytidylic acid can directly trigger cancer cells to undergo apoptosis .
Polyinosinic-polycytidylic acid potassium (Poly(I:C) potassium) is a synthetic analog of double-stranded RNA and an agonist of toll-like receptor 3 (TLR3) and retinoic acid inducible gene I (RIG-I)-like receptors (RIG-I and MDA5). Polyinosinic-polycytidylic acid sodium can be used as a vaccine adjuvant to enhance innate and adaptive immune responses, and to alter the tumor microenvironment. Polyinosinic-polycytidylic acid potassium can directly trigger cancer cells to undergoApoptosis .
KHK-IN-3 (Example 1) is a ketohexokinase (KHK) inhibitor. KHK-IN-3 can be used in the study of kidney disease, nonalcoholic steatohepatitis (NASH), diabetes and heart failure. KHK is a rate-limiting enzyme and fructokinase involved in fructose metabolism. KHK catalyzes the phosphorylation of fructose to fructose-1-phosphate (FIP) at the expense of ATP. The lack of feedback inhibition of fructose metabolism triggers the accumulation of downstream intermediates such as lipogenesis, gluconeogenesis, and oxidative phosphorylation .
BKN-1 is a bifunctional ligand that can not only track the formation of mtG4s (G-quadruplexes, four-stranded DNA structures containing Hoogsteen bonds) through far-red emission, but can also induce mitochondrial dysfunction. BKN-1 has anti-tumor activity and may cause mtDNA loss, damage mitochondrial integrity, reduce ATP levels, and trigger ROS imbalance, leading to apoptosis and autophagy .
SC144 is a first-in-class, orally active gp130 (IL6-beta) inhibitor. SC144 binds gp130, induces gp130 phosphorylation (S782) and deglycosylation, abrogates Stat3 phosphorylation and nuclear translocation, and further inhibits the expression of downstream target genes. SC144 shows potent inhibition of gp130 ligand-triggered signaling. SC144 induces apoptosis in human ovarian cancer cells .
SC144 hydrochloride is a first-in-class, orally active gp130 (IL6-beta) inhibitor. SC144 hydrochloride binds gp130, induces gp130 phosphorylation (S782) and deglycosylation, abrogates Stat3 phosphorylation and nuclear translocation, and further inhibits the expression of downstream target genes. SC144 hydrochloride shows potent inhibition of gp130 ligand-triggered signaling. SC144 hydrochloride induces apoptosis in human ovarian cancer cells .
AX-024 hydrochloride is an orally available, first-in-class inhibitor of the TCR-Nck interaction that selectively inhibits TCR-triggered T cell activation with an IC50 ~1 nM. AX-024 hydrochloride modulates cell signaling by targeting SH3 domains. AX-024 hydrochloride has low-acute toxicity and high potency and selectivity, and strongly inhibit the production of IL-6, TNF-α, IFN-γ, IL-10 and IL-17A.
AX-024 is an orally available, first-in-class inhibitor of the TCR-Nck interaction that selectively inhibits TCR-triggered T cell activation with an IC50 ~1 nM. AX-024 modulates cell signaling by targeting SH3 domains. AX-024 has low-acute toxicity and high potency and selectivity, and strongly inhibit the production of IL-6, TNF-α, IFN-γ, IL-10 and IL-17A.
Trimetazidine-d8 (dihydrochloride) is the deuterium labeled Trimetazidine dihydrochloride. Trimetazidine dihydrochloride is a selective long chain 3-ketoyl coenzyme A thiolase inhibitor with an IC50 of 75 nM, which can inhibit β-oxidation of free fatty acid (FFA). Trimetazidine dihydrochloride is an effective antianginal agent and a cytoprotective agent, has anti-oxidant, anti-inflammatory, antinociceptive and gastroprotective properties. Trimetazidine dihydrochloride triggers autophagy. Trimetazidine dihydrochloride is also a 3-hydroxyacyl-CoA dehydrogenase (HADHA) inhibitor[1][2][3][4].
Foxy-5, a WNT5A agonist, is a mimicking peptide of WNT5A which is a non-canonical member of the Wnt family. Foxy-5 triggers cytosolic free calcium signaling without affecting β-catenin activation and it impairs the migration and invasion of epithelial cancer cells. Foxy-5 effectively reduces the metastatic spread of WNT5A-low prostate cancer cells in an orthotopic mouse model .
Targaprimir-96 is a potent inhibitor of microRNA-96 (miR-96) processing. Targaprimir-96 selectively modulates miR-96 production in cancer cells and triggersapoptosis. Targaprimir-96 binds primary miR-96 (pri-miR-96) with low nanomolar affinity. Targaprimir-96 directly engages pri-miR-96 in breast cancer cells and is ineffective on healthy breast cells .
N-decanoyl-L-homoserine lactone (C10-HSL) is a N-acyl-homoserine lactone (AHL) N-decanoyl-L-homoserine lactone can inhibit primary root growth in Arabidopsis. N-decanoyl-L-homoserine lactone triggers a transient and immediate increase in the concentrations of cytosolic free Ca 2+ and reactive oxygen species (ROS), increases the activity of mitogen-activated protein kinase 6 (MPK6), and induces nitric oxide (NO) production in Arabidopsis roots .
RO2959 monohydrochloride is a potent and selective CRAC channel inhibitor with an IC50 of 402 nM. RO2959 monohydrochloride is a potent blocker of store operated calcium entry (SOCE) mediated by Orai1/Stim1 channels with an IC50 of 25 nM. RO2959 monohydrochloride is also a potent inhibitor of human IL-2 production, and potently blocks T cell receptor triggered gene expression and T cell functional pathways .
Benzyl butyl phthalate, a member of phthalic acid esters (PAEs), can trigger the migration and invasion of hemangioma (HA) cells via upregulation of Zeb1. Benzyl butyl phthalate activates aryl hydrocarbon receptor (AhR) in breast cancer cells to stimulate SPHK1/S1P/S1PR3 signaling and enhances formation of metastasis-initiating breast cancer stem cells (BCSCs) .
AES-350 is a potent and orally active HDAC6 inhibitor with an IC50 and a Ki of 0.0244 μM and 0.035 μM, respectively. AES-350 is also against HDAC3, HDAC8 in an enzymatic activity assay with IC50 values of 0.187 μM and 0.245 μM, respectively. AES-350 triggers apoptosis in AML cells through HDAC inhibition and can be used for acute myeloid leukemia (AML) research .
Fazirsiran (ARO-AAT) is a second-generation RNAi agent. Fazirsiran consistes of a cholesterol-conjugated RNAi trigger (chol-RNAi) to selectively degrade Alpha1-antitrypsin (AAT) mRNA by RNAi and a melittin-derived peptide conjugated to N-acetylgalactosamine (NAG) formulated as the excipient EX1 to promote endosomal escape of the chol-RNAi in hepatocytes . Fazirsiran can be used in the study of Alpha-1 Antitrypsin Deficiency (AATD) liver disease.
DYSP-C34 is a potent, biocompatible, and ultrasound (US)-triggered multifunctional molecular machine. DYSP-C34 has multiple favorable properties, such as improved lipophilic/hydrophilic balance, intensified US-induced ROS production capacity, and better cellular permeability, resulting in the excellent tumor target efficiency and notable sonodynamic therapy (SDT)-mediated tumor regression. DYSP-C34 exhibits mild immunogenicity by stimulating APCs directly .
CDK1/Cyc B-IN-1 (Compound 5) is a selective CDK1/Cyc B complex inhibitor with an IC50 of 97 nM. CDK1/Cyc B-IN-1 triggersapoptosis and G2/M cell cycle arrest. CDK1/Cyc B-IN-1 shows broad-spectrum cytotoxic action against cancer cell lines .
(R)-PR-924 is the isomer of PR-924 (HY-123587), and can be used as an experimental control. PR-924 is a selective tripeptide epoxyketone immunoproteasome subunit LMP-7 inhibitor with an IC50 of 22 nM. PR-924 covalently modifies proteasomal N-terminal threonine active sites. PR-924 inhibits growth and triggersapoptosis in multiple myeloma (MM) cells. PR-924 has antitumor activities .
TP4 (Nile tilapia piscidin) is an orally active piscidin-like antimicrobial peptide. TP4 inhibits multiple gram positive and negative strains (MIC: 0.03-10 μg/mL). TP4 shows hemolytic activities. TP4 enhances immune response, antioxidant activity, and intestinal health against bacterial infections. TP4 also has anti-tumor effect, and induces necrosis by triggering mitochondrial dysfunction in cancer cells .
Fazirsiran sodium is a second-generation RNAi agent. Fazirsiran sodium consistes of a cholesterol-conjugated RNAi trigger (chol-RNAi) to selectively degrade Alpha1-antitrypsin (AAT) mRNA by RNAi and a melittin-derived peptide conjugated to N-acetylgalactosamine (NAG) formulated as the excipient EX1 to promote endosomal escape of the chol-RNAi in hepatocytes . Fazirsiran sodium can be used in the study of Alpha-1 Antitrypsin Deficiency (AATD) liver disease.
Siramesine (Lu 28-179) is a potent sigma-2 receptor agonist. Siramesine has a subnanomolar affinity for sigma-2 receptors (IC50=0.12 nM) and exhibits a 140-fold selectivity for sigma-2 receptors over sigma-1 receptors (IC50=17 nM). Siramesine triggers cell death through destabilisation of mitochondria, but not lysosomes. Anti-cancer activity .
Siramesine (Lu 28-179) hydrochloride is a potent sigma-2 receptor agonist. Siramesine hydrochloride has a subnanomolar affinity for sigma-2 receptors (IC50=0.12 nM) and exhibits a 140-fold selectivity for sigma-2 receptors over sigma-1 receptors (IC50=17 nM). Siramesine hydrochloride triggers cell death through destabilisation of mitochondria, but not lysosomes. Anti-cancer activity .
MPT0B392, an orally active quinoline derivative, induces c-Jun N-terminal kinase (JNK) activation, leading to apoptosis. MPT0B392 inhibits tubulin polymerization and triggers induction of the mitotic arrest, followed by mitochondrial membrane potential loss and caspases cleavage by activation of JNK and ultimately leads to apoptosis. MPT0B392 is demonstrated to be a novel microtubule-depolymerizing agent and enhances the cytotoxicity of sirolimus in sirolimus-resistant acute leukemic cells and the multidrug resistant cell line .
Foxy-5 TFA, a WNT5A agonist, is a mimicking peptide of WNT5A which is a non-canonical member of the Wnt family. Foxy-5 TFA triggers cytosolic free calcium signaling without affecting β-catenin activation and it impairs the migration and invasion of epithelial cancer cells. Foxy-5 TFA effectively reduces the metastatic spread of WNT5A-low prostate cancer cells in an orthotopic mouse model .
Targaprimir-96 TFA is a potent inhibitor of microRNA-96 (miR-96) processing. Targaprimir-96 TFA selectively modulates miR-96 production in cancer cells and triggersapoptosis. Targaprimir-96 TFA binds primary miR-96 (pri-miR-96) with low nanomolar affinity. Targaprimir-96 TFA directly engages pri-miR-96 in breast cancer cells and is ineffective on healthy breast cells .
Anticancer agent 56 (compound 4d) is a potent anti-cancer agent with agent-likeness properties, possessing anticancer activity against several cancer cell lines (IC50<3 μM). Anticancer agent 56 induces cell cycle arrest at G2/M phase and triggers mitochondrial apoptosis pathway. Anticancer agent 56 acts by accumulation of ROS, up regulation of BAX, down regulation of Bcl-2 and activation of caspases 3, 7, 9 .
SHP2/HDAC-IN-1 is a dual allosteric SHP2/HDAC inhibitor with IC50 values of 20.4 nM (SHP2) and 25.3 nM (HDAC1) respectively. SHP2/HDAC-IN-1 triggers efficient antitumor immunity by activating T cells, enhancing the antigen presentation function and promoting cytokine secretion. SHP2/HDAC-IN-1 can be used in the research of cancer immunoresearch .
W1131 is a potent STAT3 inhibitor, triggeringferroptosis. W1131 suppresses cancer progression in gastric cancer cell subcutaneous xenograft model, organoids model, and PDX model. W1131 effectively alleviates chemical resistance of cancer cells to 5-FU (HY-90006). W1131 regulates cell cycle, DNA damage response, and oxidative phosphorylation, including IL6-JAK-STAT3 pathway and ferroptosis pathway .
KIN1400 is a potent IRF3 activator. KIN1400 triggers IRF3-dependent innate immune antiviral genes (RIG-I, MDA5, IFIT1, and Mx1) and IFN-β expression. KIN1400 inhibits WNV and DV, two mosquito-borne members of the Flaviviridae and the genus Flavivirus. KIN1400 also inhibits HCV replication. KIN1400 induces innate antiviral immunity through a MAVS-IRF3 axis .
Siramesine (Lu 28-179) fumarate is a potent sigma-2 receptor agonist. Siramesine fumarate has a subnanomolar affinity for sigma-2 receptors (IC50=0.12?nM) and exhibits a 140-fold selectivity for sigma-2 receptors over sigma-1 receptors (IC50=17?nM). Siramesine fumarate triggers cell death through destabilisation of mitochondria, but not lysosomes. Anti-cancer activity .
Gambogic amide is a potent and selective agonist of TrkA and also induces its tyrosine phosphorylation and activation of downstream signaling, including Akt and MAPK. Gambogic amide specifically interacts with the cytoplasmic juxtamembrane domain of the TrkA receptor and triggers its dimerization, leading to activation. Gambogic amide has neuroprotective activity preventing glutamate-induced neuronal cell death. Gambogic amide has improved efficacy in a transient middle cerebral artery occlusion model of stroke and could be used to study neurodegenerative diseases and stroke .
Trimetazidine (dihydrochloride) (Standard) is the analytical standard of Trimetazidine (dihydrochloride). This product is intended for research and analytical applications. Trimetazidine dihydrochloride is a selective long chain 3-ketoyl coenzyme A thiolase inhibitor with an IC50 of 75 nM, which can inhibit β-oxidation of free fatty acid (FFA). Trimetazidine dihydrochloride is an effective antianginal agent and a cytoprotective agent, has anti-oxidant, anti-inflammatory, antinociceptive and gastroprotective properties. Trimetazidine dihydrochloride triggers autophagy. Trimetazidine dihydrochloride is also a 3-hydroxyacyl-CoA dehydrogenase (HADHA) inhibitor .
BRAF V600E/CRAF-IN-1 (Compound 8b) is a potent inhibitor of BRAF V600E/CRAF. BRAF V600E/CRAF-IN-1 triggers apoptosis and cell cycle arrest at G0/G1 phase in HCT-116 colon cancer cell. BRAF V600E/CRAF-IN-1 has the potential for the research of cancer diseases .
OTS193320, a imidazo[1,2-a]pyridine compound, is a SUV39H2 methyltransferase activity inhibitor. OTS193320 decreases global histone H3 lysine 9 tri-methylation levels in breast cancer cells and triggersapoptotic cell death. Combination of OTS193320 with Doxorubicin (DOX; HY-15142A) results in reduction of γ-H2AX levels as well as cancer cell viability compared to a single agent OTS193320 or DOX .
NEO214 is an autophagy inhibitor and a covalent conjugate of the PDE4 inhibitor Rolipram (HY-16900) and perillyl alcohol (HY-N7000). It has anti-cancer activity and blood-brain barrier (BBB) permeability. Over sex. NEO214 prevents autophagy-lysosome fusion, thereby blocking autophagic flux and triggering glioma cell death. The process involves mTOR activation, andTFEB(Transcription Factor EB) aggregation. NEO214 inhibitionMacroautophagy/autophagy in glioblastoma cells has the potential to overcome chemotherapy resistance in glioblastoma .
c-di-AMP (Cyclic diadenylate) sodium is a STING agonist, which binds to the transmembrane protein STING thereby activating the TBK3-IRF3 signaling pathway, subsequently triggering the production of type I IFN and TNF. c-di-AMP sodium is also a bacterial second messenger, which regulates cell growth, survival, and virulence, primarily within Gram-positive bacteria, and also regulates host immune response. c-di-AMP sodium acts as a potent mucosal adjuvant stimulating both humoral and cellular responses .
c-di-AMP diammonium is a STING agonist, which binds to the transmembrane protein STING thereby activating the TBK3-IRF3 signaling pathway, subsequently triggering the production of type I IFN and TNF. c-di-AMP diammonium is also a bacterial second messenger, which regulates cell growth, survival, and virulence, primarily within Gram-positive bacteria, and also regulates host immune response. c-di-AMP diammonium acts as a potent mucosal adjuvant stimulating both humoral and cellular responses .
c-di-AMP (Cyclic diadenylate) is a STING agonist, which binds to the transmembrane protein STING thereby activating the TBK3-IRF3 signaling pathway, subsequently triggering the production of type I IFN and TNF. c-di-AMP (Cyclic diadenylate) is also a bacterial second messenger, which regulates cell growth, survival, and virulence, primarily within Gram-positive bacteria, and also regulates host immune response. c-di-AMP (Cyclic diadenylate) acts as a potent mucosal adjuvant stimulating both humoral and cellular responses .
OSU-T315 (ILK-IN-1) is a small Integrin-linked kinase (ILK) inhibitor with an IC50 of 0.6 μM, inhibiting PI3K/AKT signaling by dephosphorylation of AKT-Ser473 and other ILK targets (GSK-3β and myosin light chain) . OSU-T315 abrogates AKT activation by impeding AKT localization in lipid rafts and triggers caspase-dependent apoptosis in an ILK-independent manner . OSU-T315 causes cell death through apoptosis and autophagy .
Dehydroaltenusin is a small molecule selective inhibitor of eukaryotic DNA polymerase α, a type of antibiotic produced by a fungus with an IC50 value of 0.68 μM. The inhibitory mode of action of dehydroaltenusin against mammalian pol α activity is competitive with respect to the DNA template primer (Ki=0.23 µM) and non-competitive with respect to the 2'-deoxyribonucleoside 5'-triphosphate substrate (Ki=0.18 µM) . Dehydroaltenusin arrests the cancer cell cycle at the S-phase and triggersapoptosis . Dehydroaltenusin possesses anti-tumor activity against human adenocarcinoma tumor in vivo .
TrxR-IN-3 (Compound 2c) is a potent inhibitor of TrxR. TrxR-IN-3 exhibits potent antiproliferative activities against five human cancer cell lines, especially against breast tumor cells. TrxR-IN-3 increases ROS levels and resulted in marked apoptosis by regulating apoptosis-related proteins expressed in the breast cancer cells. TrxR-IN-3 also triggers the formation of autophagosomes and autolysosomes by promoting the expression of LC3-II and Beclin-1 and diminishing the expression of LC3-I and p62 proteins .
BRAF V600E/CRAF-IN-2 (Compound 9c) is a potent inhibitor of BRAF V600E/CRAF with IC50s of 0.888 and 0.229 μM, respectively. BRAF V600E/CRAF-IN-2 triggers apoptosis and cell cycle arrest at G0/G1 phase in HCT-116 colon cancer cell. BRAF V600E/CRAF-IN-2 has the potential for the research of cancer diseases .
Benzyl butyl phthalate-d4 is the deuterium labeled Benzyl butyl phthalate[1]. Benzyl butyl phthalate, a member of phthalic acid esters (PAEs), can trigger the migration and invasion of hemangioma (HA) cells via upregulation of Zeb1. Benzyl butyl phthalate activates aryl hydrocarbon receptor (AhR) in breast cancer cells to stimulate SPHK1/S1P/S1PR3 signaling and enhances formation of metastasis-initiating breast cancer stem cells (BCSCs)[2][3][4].
GNA002 is a highly potent, specific and covalent EZH2 (Enhancer of zeste homolog 2) inhibitor with an IC50 of 1.1 μM. GNA002 can specifically and covalently bind to Cys668 within the EZH2-SET domain, triggering EZH2 degradation through COOH terminus of Hsp70-interacting protein (CHIP)-mediated ubiquitination. GNA002 efficiently reduces EZH2-mediated H3K27 trimethylation, reactivates polycomb repressor complex 2 (PRC2)-silenced tumor suppressor genes .
ODN 2216 is a human-specific TLR9 (toll-like receptor 9) ligand or agonist. ODN 2216 induces high amounts of IFN-α and IFN-β. ODN 2216 induces IFN-α by pDC (plasmacytoid DC) and IL-12 (p40) production by DC (dendritic cells). ODN 2216 stimulates IFN-γ production in peripheral blood mononuclear cells (PBMC), which is indirect and mediated by IFN-α/β. ODN 2216 can activate NK cells and promote IFN-γ production of TCR-triggered CD4 + T cells .
Cudraflavone B is a prenylated flavonoid with anti-inflammatory and anti-tumor properties. Cudraflavone B is also a dual inhibitor of COX-1 and COX-2. Cudraflavone B blocks the translocation of nuclear factor κB (NF-κB) from the cytoplasm to the nucleus in macrophages. Thus, Cudraflavone B inhibits tumor necrosis factor α (TNFα) gene expression and secretion. Cudraflavone B also triggers the mitochondrial apoptotic pathway, activates NF-κB, the MAPK p38, and ERK, and induced the expression of SIRT1. Thus Cudraflavone B inhibits the growth of human oral squamous cell carcinoma cells .
ODN?2216 sodium is a human-specific TLR9 (toll-like receptor 9) ligand or agonist. ODN?2216 sodium induces high amounts of IFN-α and IFN-β. ODN 2216 sodium induces IFN-α by pDC (plasmacytoid DC) and IL-12 (p40) production by DC (dendritic cells). ODN 2216 sodium stimulates IFN-γ production in peripheral blood mononuclear cells (PBMC), which is indirect and mediated by IFN-α/β. ODN 2216 sodium can activate NK cells and promote IFN-γ production of TCR-triggered CD4 + T cells .
Daphnetin (7,8-dihydroxycoumarin), one coumarin derivative can be found in plants of the Genus Daphne, is a potent, oral active protein kinase inhibitor, with IC50s of 7.67 μM, 9.33 μM and 25.01 μM for EGFR, PKA and PKC in vitro, respectively. Daphnetin triggers ROS-induced cell apoptosis and induces cytoprotective autophagy by modulating the AMPK/Akt/mTOR pathway. Daphnetin has anti-inflammation activitity and inhibits TNF-α, IL-1ß, ROS, and MDA production. Daphnetin has schizontocidal activity against malaria parasites. Daphnetin can be used for rheumatoid arthritis , cancer and anti-malarian research .
Ginsenoside Rk1 is a unique component created by processing the ginseng plant (mainly Sung Ginseng, SG) at high temperatures .
Ginsenoside Rk1 has anti-inflammatory effect, suppresses the activation of Jak2/Stat3 signaling pathway and NF-κB .
Ginsenoside Rk1 has anti-tumor effect, antiplatelet aggregation activities, anti-insulin resistance, nephroprotective effect, antimicrobial effect, cognitive function enhancement, lipid accumulation reduction and prevents osteoporosis .
Ginsenoside Rk1 induces cell apoptosis by triggering intracellular reactive oxygen species (ROS) generation and blocking PI3K/Akt pathway .
c-di-AMP (Standard) is the analytical standard of c-di-AMP. This product is intended for research and analytical applications. c-di-AMP (Cyclic diadenylate) is a STING agonist, which binds to the transmembrane protein STING thereby activating the TBK3-IRF3 signaling pathway, subsequently triggering the production of type I IFN and TNF. c-di-AMP (Cyclic diadenylate) is also a bacterial second messenger, which regulates cell growth, survival, and virulence, primarily within Gram-positive bacteria, and also regulates host immune response. c-di-AMP (Cyclic diadenylate) acts as a potent mucosal adjuvant stimulating both humoral and cellular responses .
NSC 194308, a U2AF2-RNA complexes enhancer, increases association of the U2AF1-U2AF2-SF1-splice site RNA complex by binding a site between the U2AF2 RNA recognition motifs (RRM1 and RRM2). NSC 194308 inhibits pre-mRNA splicing by stalling spliceosome assembly at the point where U2AF helps recruit U2 snRNP to the branchpoint. NSC 194308 enhances the binding of pre-mRNA to U2AF2, selectively triggering cell death in leukemia cell lines containing spliceosome mutations .
MIR96-IN-1 targets the Drosha site in the miR-96 (miRNA-96, microRNA-96) hairpin precursor, inhibiting its biogenesis, derepressing downstream targets, and triggeringapoptosis in breast cancer cells. MIR96-IN-1 binds to RNAs with Kds of 1.3, 9.4, 3.4, 1.3 and 7.4 μM for RNA1, RNA2, RNA3, RNA4 and RNA5, respectively . MIR96-IN-1 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
Endoplasmic reticulum (ER) contributes to the production and folding of approximately one third of cellular proteins, and is thus inextricably linked to the maintenance of cellular homeostasis and the fine balance between health and disease. However, some adverse factors negatively impact ER functions and protein synthesis, resulting in the activation of Endoplasmic reticulum stress (ER stress, ERS) and unfolded protein response (UPR) signaling pathways. The UPR is triggered when ER protein folding capacity is overwhelmed by cellular demand and the UPR initially aims to restore ER homeostasis and normal cellular functions. However, if this fails, then the UPR triggers cell death. Chronic ER stress and defects in UPR signaling are emerging as key contributors to a growing list of human diseases, including diabetes, neurodegeneration and cancer.
MCE Endoplasmic Reticulum Stress Compound Library contains 219 ER stress-related compounds that mainly target PERK, IRE1, ATF6, etc. MCE ER stress library is a useful tool for researching ER stress and related diseases.
Agonistic drugs activate or stimulate their receptors, triggering responses that increase or decrease cell activity. The highly selective activators can act on specific biological or molecular targets, while non-selective activators may interfere with multiple targets or targets simultaneously. The highly selective activators reduce the likelihood of these non-specific effects by targeting specific targets, making research more precise and reliable. The Highly Selective Activators Library contains 1468 compounds, covering multiple targets and subtypes, such as GPCR protein family, Ion channel, multiple kinases, etc. The Highly Selective Activators Library is an effective tool for screening different phenotypes.
GPCRs are a large family of cell surface receptors that respond to a variety of external signals. Binding of a signaling molecule to a GPCR results in G protein activation, which in turn triggers the production of any number of second messengers. GPCRs play an important role in the human body, and increased understanding of these receptors has greatly affected modern medicine. In fact, researchers estimate that between one-third to one-half of all approved drugs act by binding to GPCRs. GPCRs are a large group of drug targets in drug discovery.
MCE provides a unique collection of 2286 small molecules targeting GPCRs that can be used in the screening for various GPCRs-related research and drug development projects.
Sodium channels conduct sodium ions (Na+) through a cell's plasma membrane that are the source of excitatory currents for the nervous system and muscle. Na channels are classified according to the trigger that opens the channel for such ions, i.e. either a voltage-change (Voltage-gated, voltage-sensitive, or voltage-dependent sodium channel also called VGSCs or Nav channel) or a binding of a substance (a ligand) to the channel (ligand-gated sodium channels). Dysfunction in voltage-gated sodium channels correlates with neurological and cardiac diseases, including epilepsy, myopathies, pain and cardiac arrhythmias. Sodium channel blockers are used in the treatment of cardiac arrhythmia, pain and convulsion.
MCE offers a unique collection of 128 sodium channel blocker and antagonists, all of which have the identified inhibitory effect on sodium channels. MCE Sodium Channel Blocker Library can be used for neurological and cardiac diseases drug discovery and sodium channel research.
Neurotransmitter (NT) receptors, also known as neuroreceptors, are a broadly diverse group of membrane proteins that bind neurotransmitters for neuronal signaling. There are two major types of neurotransmitter receptors: ionotropic and metabotropic. Ionotropic receptors are ligand-gated ion channels, meaning that the receptor protein includes both a neurotransmitter binding site and an ion channel. The binding of a neurotransmitter molecule (the ligand) to the binding site induces a conformational change in the receptor structure, which opens, or gates, the ion channel. The term “metabotropic receptors” is typically used to refer to transmembrane G-protein-coupled receptors. Metabotropic receptors trigger second messenger-mediated effects within cells after neurotransmitter binding.
In some neurological diseases, the neurotransmitter receptor itself appears to be the target of the disease process. Many neuroactive drugs act by modifying neurotransmitter receptors. A better understanding of neurotransmitter receptor changes in disease may lead to improvements in therapy.
MCE designs a unique collection of 1785 compounds targeting a variety of neurotransmitter receptors. MCE Neurotransmitter Receptor Compound Library is a useful tool for neurological diseases drug discovery.
FBBBE is used to detect the production of H2O2 by cells. FBBBE can be triggered by intracellular H2O2 and converted to fluorescein, resulting in an increase in intracellular fluorescence (Ex=4480 nm, Em=512 nm) .
IPTG is a molecular mimic of allolactose, a lactose metabolite that triggers transcription of the lac operon, and it is therefore used to induce protein expression where the gene is under the control of the lac operator.
Hyaluronate lyase can cleat hyaluronate (HA) and produce unsaturated disaccharides through a β-elimination reaction. The resulting disaccharides further trigger the downstream pathway and catalyze the next reaction. Hyaluronate lyase helps Streptococcus dysgalactiae subsp.equisimilis (SDSE) acquire nutrients from the host, causing bacterial pathogenicity .
GPLGIAGQ TFA, a MMP2-cleavable polypeptide, is used as a stimulus-sensitive linker in both liposomal and micellar nanocarriers for MMP2-triggered tumor targeting. GPLGIAGQ TFA can be used to synthesis unique MMP2-targeted photosensitizer in photodynamic therapy (PDT) .
RGD Trifluoroacetate is a tripeptide that effectively triggers cell adhesion, addresses certain cell lines and elicits specific cell responses; RGD Trifluoroacetate binds to integrins.
GPLGIAGQ, a MMP2-cleavable polypeptide, is used as a stimulus-sensitive linker in both liposomal and micellar nanocarriers for MMP2-triggered tumor targeting. GPLGIAGQ can be used to synthesis unique MMP2-targeted photosensitizer in photodynamic therapy (PDT) .
Eledoisin Related Peptide is a Substance P analog that excites neurons and triggers behavioral responses. Eledoisin Related Peptide is also a tachykinin receptor ligand.
{Boc}-Phe-Leu-Phe-Leu-Phe TFA is a formyl peptide receptor (FPR) family antagonist that preferentially inhibits activity triggered through the formyl peptide receptor .
{Boc}-Phe-Leu-Phe-Leu-Phe ({Boc}-FLFLF) is a formyl peptide receptor (FPR) family antagonist that preferentially inhibits activity triggered through the formyl peptide receptor .
TRP-601 is a caspase inhibitor. TRP-601 reversed the increased expression of active caspase-2, the activation of endogenous apoptotic pathway and the up-regulation of key protein triggered by hyperoxia .
TAT-PAK18 R192A is an inactive Tat-Pak peptide. TAT-PAK18 R192A does not have any effect in the translocation of Rac1 triggered by any of the interrogated proteins .
LQVTDSGLYRCVIYHPP (LP17) is a triggering receptor expressed on myeloid cells (TREM-1) inhibitory peptide. LQVTDSGLYRCVIYHPP substantially alleviates ischemia-induced infarction and neuronal injury. LQVTDSGLYRCVIYHPP can get access into brain and block TREM-1 .
LQVTDSGLYRCVIYHPP (LP17) TFA is a triggering receptor expressed on myeloid cells (TREM-1) inhibitory peptide. LQVTDSGLYRCVIYHPP TFA substantially alleviates ischemia-induced infarction and neuronal injury. LQVTDSGLYRCVIYHPP TFA can get access into brain and block TREM-1 .
Egg Laying Hormone, aplysia is a neuropeptide synthesized by the bag cell neurons, which contains 36 amino acids and can stimulate egglaying and ovulation in Aplysia via electrical discharge triggering of neurons. Egg-laying hormone of Aplysia induces a voltage-dependent slow inward current carried by Na' in an identified motoneuron .
IA9 TFA (human TREM-2 182-190 TFA) is a TREM-2 inhibitor , and can diminish release of proinflammatory cytokines and dramatically suppressed joint inflammation and damage in collagen-Induced Arthritis (CIA) mice model .
IA9 (human TREM-2 182-190) is a TREM-2 inhibitor , and can diminish release of proinflammatory cytokines and dramatically suppressed joint inflammation and damage in collagen-Induced Arthritis (CIA) mice model .
(Pyr3)-Amyloid β-Protein (3-42) is the predominant amyloid β-peptide structure deposited in human brain of Alzheimer's disease and Down's syndrome patients. (Pyr3)-Amyloid β-Protein (3-42) is suggested to accumulate in the brain and to trigger the formation of insoluble amyloid β-peptide deposits .
(Pyr3)-Amyloid β-Protein (3-42) TFA is the predominant amyloid β-peptide structure deposited in human brain of Alzheimer's disease and Down's syndrome patients. (Pyr3)-Amyloid β-Protein (3-42) TFA is suggested to accumulate in the brain and to trigger the formation of insoluble amyloid β-peptide deposits .
Foxy-5, a WNT5A agonist, is a mimicking peptide of WNT5A which is a non-canonical member of the Wnt family. Foxy-5 triggers cytosolic free calcium signaling without affecting β-catenin activation and it impairs the migration and invasion of epithelial cancer cells. Foxy-5 effectively reduces the metastatic spread of WNT5A-low prostate cancer cells in an orthotopic mouse model .
C5aR1 antagonist peptide is a biological active peptide. (This linear peptide is derived from the C-terminus of the chemokine, complement fragment 5 anaphylatoxin (C5a). This peptide functions to inhibit C5a binding and function at human and rat C5a receptors. C5a is crucial to triggering cellular immune responses and its overexpression is involved in arthritis, Alzheimer’s disease, cystic fibrosis, systemic lupus erythematosus, and other immunoinflammatory diseases.)
TP4 (Nile tilapia piscidin) is an orally active piscidin-like antimicrobial peptide. TP4 inhibits multiple gram positive and negative strains (MIC: 0.03-10 μg/mL). TP4 shows hemolytic activities. TP4 enhances immune response, antioxidant activity, and intestinal health against bacterial infections. TP4 also has anti-tumor effect, and induces necrosis by triggering mitochondrial dysfunction in cancer cells .
Foxy-5 TFA, a WNT5A agonist, is a mimicking peptide of WNT5A which is a non-canonical member of the Wnt family. Foxy-5 TFA triggers cytosolic free calcium signaling without affecting β-catenin activation and it impairs the migration and invasion of epithelial cancer cells. Foxy-5 TFA effectively reduces the metastatic spread of WNT5A-low prostate cancer cells in an orthotopic mouse model .
Nadunolimab is a human monoclonal IgG1 antibody targeting IL1RAP. Nadunolimab blocks IL-1α and IL-1β signaling and triggering antibody-dependent cellular cytotoxicity. Nadunolimab can be used in research of cancer .
Dezamizumab (GSK 2398852) is a fully humanized recombinant monoclonal IgG1 anti-serum amyloid P component (SAP) antibody, with potential anti-amyloid activity. Dezamizumab triggers immunotherapeutic clearance of amyloid. Dezamizumab can be used in research of Amyloid light-chain (AL) amyloidosis .
Cusatuzumab is a human αCD70 monoclonal antibody. Cusatuzumab shows cytotoxicity activity with enhanced antibody-dependent cellular. Cusatuzumab reduces leukemia stem cells (LSCs) and triggers gene signatures related to myeloid differentiation and apoptosis. Cusatuzumab has the potential for the research of Acute myeloid leukemia (AML) .
Loncastuximab tesirine is a human cluster of differentiation 19 (CD19)-directed antibody-drug conjugate (ADC). Once bound to CD19 on the cell membrane, loncastuximab tesirine is rapidly internalised and triggers cell death. Loncastuximab tesirin induces cell apoptosis, it can be used for the research of diffuse large B-cell lymphoma .
Cibisatamab (CEA-TCB), a T cell bispecific antibody, binds Carcino-Embryonic Antigen (CEA) on cancer cells and CD3 on T cells. Cibisatamab (CEA-TCB) triggers T cell killing of cancer cell lines expressing moderate to high levels of CEA at the cell surface. Cibisatamab (CEA-TCB) can be used for colorectal cancer research .
Incensole acetate is a main constituent of Boswellia carterii resin, has neuroprotective effects against neuronal damage in traumatic and ischemic head injury. Incensole acetate reduces Aβ25–35-triggeredapoptosis in hOBNSCs .
Graveoline (Rutamine) is an anti-cancer agent that can trigger apoptosis and autophagy in skin melanoma cells. Graveoline also exhibits antifungal activity .
Nerol is a constituent of neroli oil. Nerol Nerol triggers mitochondrial dysfunction and induces apoptosis via elevation of Ca 2+ and ROS. Antifungal activity .
Zingiberene (α-Zingiberene) is a monocyclic sesquiterpene which is the predominant constituent of ginger with oil content (Zingiber officinale). Neuroprotective potential . Zingiberene triggersautophagy. Anticancer activity .
Euxanthone, a xanthone derivative, attenuates Aβ1-42-induced oxidative stress and apoptosis by triggeringautophagy. Euxanthone exhibits anti-neoplastic and neuroprotective activities .
(+)-Erinacin A is an anticancer compound that can be isolated from the mushroom Hericium erinaceum. (+)-Erinacin A has the capacity to trigger cancer cell death dependent on the production of reactive oxygen species (ROS). (+)-Erinacin A has anticancer and neuroprotective activity .
D-Tyrosine is the D-isomer of tyrosine. D-Tyrosine negatively regulates melanin synthesis by inhibiting tyrosinase activity. D-Tyrosine inhibits biofilm formation and trigger the self-dispersal of biofilms without suppressing bacterial growth .
Hellebrigenin, one of bufadienolides belonging to cardioactive steroids, is isolated from traditional Chinese medicine Venenum Bufonis. Hellebrigenin induces DNA damage and cell cycle G2/M arrest. Hellebrigenin triggers mitochondria-mediated apoptosis.
Nerol (Standard) is the analytical standard of Nerol. This product is intended for research and analytical applications. Nerol is a constituent of neroli oil. Nerol Nerol triggers mitochondrial dysfunction and induces apoptosis via elevation of Ca 2+ and ROS. Antifungal activity .
Virodhamine is an endocannabinoid, it regulates neurotransmission by activating the cannabinoid (CB) receptors. Virodhamine is an antagonist of CB1 receptor and an agonist of CB2 receptor. Virodhamine induces megakaryocytic differentiation by triggeringMAPK signaling and ROS production. Virodhamine can be used for the research of various neurological disorders such as Alzheimer's and Parkinson's diseases .
Eriocitrin is a flavonoid isolated from lemons that is a powerful antioxidant. Eriocitrin inhibits the proliferation of liver cancer cells by arresting the cell cycle in the S phase by upregulating p53, cyclin A, cyclin D3 and CDK6. Eriocitrin triggers apoptosis by activating intrinsic signaling pathways involving mitochondria .
cGAMP (Cyclic GMP-AMPP) disodium functions as an endogenous second messenger in metazoans and triggers interferon production in response to cytosolic DNA. cGAMP diammonium activates stimulator of interferon genes (STING), which activates a signaling cascade leading to the production of type I interferons and other immune mediators .
cGAMP (Cyclic GMP-AMPP) diammonium functions as an endogenous second messenger in metazoans and triggers interferon production in response to cytosolic DNA. cGAMP diammonium activates stimulator of interferon genes (STING), which activates a signaling cascade leading to the production of type I interferons and other immune mediators .
Naphthazarin (DHNQ) is a naturally occurring compound. Naphthazarin is effective by various cellular mechanisms including oxidative stress, activation of mitochondrial apoptosis-inducing factor (AIF), depolymerization of microtubules, interference with lysosomal function and p53-dependent p21 activation. Naphthazarin triggersapoptosis and has anti-tumor effects .
Ecdysone (α-Ecdysone), a major steroid hormone in insects and herbs, triggersmineralocorticoid receptor (MR) activation and induces cellular apoptosis. Ecdysone plays essential roles in coordinating developmental transitions and homeostatic sleep regulation through its active metabolite 20-hydroxyecdysone (Crustecdysone; 20E; HY-N6979) .
Picrasidine I is an anti-inflammatory and anti-osteoclastogenic dimeric alkaloid that can be isolated from Picrasma quassioides. Picrasidine I inducs cell cycle arrest, and triggers cell apoptosis by downregulats ERK and Akt pathways. Picrasidine I inhibits the activation of MAPKs, NF-κB and ROS generation, and suppresses the expression of c-Fos and NFATc1 .
Ziyuglycoside I isolated from S. officinalis root, has anti-wrinkle activity, and increases the expression of type I collagen. Ziyuglycoside I could be used as an active ingredient for cosmetics . Ziyuglycoside I triggers cell cycle arrest and apoptosis mediated by p53, it can be a potential agent candidate for treating triple-negative breast cancer (TNBC) .
Physalin B, one of the major active steroidal constituents of Cape gooseberry, induces cell cycle arrest and triggersapoptosis in breast cancer cells through modulating p53-dependent apoptotic pathway. Physalin B inhibits the ubiquitin-proteasome pathway and induces incomplete autophagic response in human colon cancer cells in vitro .
(E)-Methyl 3,4,5-trimethoxycinnamate is a bioactive natural phenylpropanoid. (E)-Methyl 3,4,5-trimethoxycinnamate suppresses inflammation in RAW264.7 macrophages and blocks macrophage-adipocyte interaction. (E)-Methyl 3,4,5-trimethoxycinnamate also has antiarrhythmic effect, leads to suppression of triggered activities in rabbit myocytes .
Chelerythrine is a natural alkaloid, acts as a potent and selective Ca 2+/phospholopid-dependent PKC antagonist, with an IC50 of 0.7 μM . Chelerythrine has antitumor, antidiabetic and anti-inflammatory activity . Chelerythrine inhibits the BclXL-Bak BH3 peptide binding with IC50 of 1.5 μM and displaces Bax from BclXL. Chelerythrine triggersapoptosis and autophagy .
Bonannione A (6-Geranylnaringenin; Mimulone), a prenylflavonoid, is an orally active and potent protein tyrosine phosphatase 1B (PTP1B) inhibitor with an IC50 of 14 µM. Bonannione A triggers caspase-dependent apoptosis. Bonannione A induces autophagy through p53-mediated AMPK/mTOR pathway. Bonannione A shows anti-inflammatory, antiradical and anti-cancer activity .
Ganoderic acid T1 is a deacetylated derivative of Ganoderic acid T. Ganoderic acid T1 attenuates antioxidant defense system and induces apoptosis of cancer cells. Ganoderic acid T1 decreases mitochondrial membrane potential and activates caspase-9 and caspase-3, to trigger apoptosis. Ganoderic acid T1 also increases the generation of intracellular ROS to produce pro-oxidant activities and cytotoxicity .
Polyphyllin VI, an active saponin, possess anti-cancer activities. Polyphyllin VI induces G2/M cell cycle arrest and triggersapoptosis. Polyphyllin VI induces caspase-1-mediated pyroptosis via the induction of ROS/NF-κB/NLRP3/GSDMD signal axis in non-small cell lung cancer .
c-di-AMP (Cyclic diadenylate) sodium is a STING agonist, which binds to the transmembrane protein STING thereby activating the TBK3-IRF3 signaling pathway, subsequently triggering the production of type I IFN and TNF. c-di-AMP sodium is also a bacterial second messenger, which regulates cell growth, survival, and virulence, primarily within Gram-positive bacteria, and also regulates host immune response. c-di-AMP sodium acts as a potent mucosal adjuvant stimulating both humoral and cellular responses .
c-di-AMP diammonium is a STING agonist, which binds to the transmembrane protein STING thereby activating the TBK3-IRF3 signaling pathway, subsequently triggering the production of type I IFN and TNF. c-di-AMP diammonium is also a bacterial second messenger, which regulates cell growth, survival, and virulence, primarily within Gram-positive bacteria, and also regulates host immune response. c-di-AMP diammonium acts as a potent mucosal adjuvant stimulating both humoral and cellular responses .
c-di-AMP (Cyclic diadenylate) is a STING agonist, which binds to the transmembrane protein STING thereby activating the TBK3-IRF3 signaling pathway, subsequently triggering the production of type I IFN and TNF. c-di-AMP (Cyclic diadenylate) is also a bacterial second messenger, which regulates cell growth, survival, and virulence, primarily within Gram-positive bacteria, and also regulates host immune response. c-di-AMP (Cyclic diadenylate) acts as a potent mucosal adjuvant stimulating both humoral and cellular responses .
Dehydroaltenusin is a small molecule selective inhibitor of eukaryotic DNA polymerase α, a type of antibiotic produced by a fungus with an IC50 value of 0.68 μM. The inhibitory mode of action of dehydroaltenusin against mammalian pol α activity is competitive with respect to the DNA template primer (Ki=0.23 µM) and non-competitive with respect to the 2'-deoxyribonucleoside 5'-triphosphate substrate (Ki=0.18 µM) . Dehydroaltenusin arrests the cancer cell cycle at the S-phase and triggersapoptosis . Dehydroaltenusin possesses anti-tumor activity against human adenocarcinoma tumor in vivo .
Cudraflavone B is a prenylated flavonoid with anti-inflammatory and anti-tumor properties. Cudraflavone B is also a dual inhibitor of COX-1 and COX-2. Cudraflavone B blocks the translocation of nuclear factor κB (NF-κB) from the cytoplasm to the nucleus in macrophages. Thus, Cudraflavone B inhibits tumor necrosis factor α (TNFα) gene expression and secretion. Cudraflavone B also triggers the mitochondrial apoptotic pathway, activates NF-κB, the MAPK p38, and ERK, and induced the expression of SIRT1. Thus Cudraflavone B inhibits the growth of human oral squamous cell carcinoma cells .
Daphnetin (7,8-dihydroxycoumarin), one coumarin derivative can be found in plants of the Genus Daphne, is a potent, oral active protein kinase inhibitor, with IC50s of 7.67 μM, 9.33 μM and 25.01 μM for EGFR, PKA and PKC in vitro, respectively. Daphnetin triggers ROS-induced cell apoptosis and induces cytoprotective autophagy by modulating the AMPK/Akt/mTOR pathway. Daphnetin has anti-inflammation activitity and inhibits TNF-α, IL-1ß, ROS, and MDA production. Daphnetin has schizontocidal activity against malaria parasites. Daphnetin can be used for rheumatoid arthritis , cancer and anti-malarian research .
Ginsenoside Rk1 is a unique component created by processing the ginseng plant (mainly Sung Ginseng, SG) at high temperatures .
Ginsenoside Rk1 has anti-inflammatory effect, suppresses the activation of Jak2/Stat3 signaling pathway and NF-κB .
Ginsenoside Rk1 has anti-tumor effect, antiplatelet aggregation activities, anti-insulin resistance, nephroprotective effect, antimicrobial effect, cognitive function enhancement, lipid accumulation reduction and prevents osteoporosis .
Ginsenoside Rk1 induces cell apoptosis by triggering intracellular reactive oxygen species (ROS) generation and blocking PI3K/Akt pathway .
c-di-AMP (Standard) is the analytical standard of c-di-AMP. This product is intended for research and analytical applications. c-di-AMP (Cyclic diadenylate) is a STING agonist, which binds to the transmembrane protein STING thereby activating the TBK3-IRF3 signaling pathway, subsequently triggering the production of type I IFN and TNF. c-di-AMP (Cyclic diadenylate) is also a bacterial second messenger, which regulates cell growth, survival, and virulence, primarily within Gram-positive bacteria, and also regulates host immune response. c-di-AMP (Cyclic diadenylate) acts as a potent mucosal adjuvant stimulating both humoral and cellular responses .
Trigger protein is essential for protein export, acting as chaperone and peptidyl prolyl cis-trans isomerase. In its chaperone role, it keeps nascent polypeptides in an open conformation, facilitating correct protein folding. Trigger factor Protein, E.coli (P.pastoris, His) is the recombinant E. coli-derived Trigger factor protein, expressed by P. pastoris , with N-His labeled tag. The total length of Trigger factor Protein, E.coli (P.pastoris, His) is 432 a.a., with molecular weight (affected by relative charge) of ~60 KDa.
Metformin-d6 (hydrochloride)e is a deuterium labeled Metformin hydrochloride. Metformin hydrochloride inhibits the mitochondrial respiratory chain in the liver, leading to activation of AMPK, enhancing insulin sensitivity for type 2 diabetes research. Metformin hydrochloride triggers autophagy[1].
D-Tyrosine-d4 is the deuterium labeled D-Tyrosine. D-Tyrosine is the D-isomer of tyrosine. D-Tyrosine negatively regulates melanin synthesis by inhibiting tyrosinase activity. D-Tyrosine inhibits biofilm formation and trigger the self-dispersal of biofilms without suppressing bacterial growth[1][2].
Azobenzene-d10 is the deuterium labeled Azobenzene[1]. Azobenzene can be used as an optical trigger for the design and synthesis of a large variety of photoresponsive systems[2][3][4].
Domperidone-d6 is the deuterium labeled Domperidone. Domperidone (R33812) is a selective dopamine-2 receptor antagonist. Domperidone acts as an antiemetic and a prokinetic agent through its effects on the chemoreceptor trigger zone and motor function of the stomach and small intestine[1][2].
D-Tyrosine-d2 is the deuterium labeled D-Tyrosine. D-Tyrosine is the D-isomer of tyrosine. D-Tyrosine negatively regulates melanin synthesis by inhibiting tyrosinase activity. D-Tyrosine inhibits biofilm formation and trigger the self-dispersal of biofilms without suppressing bacterial growth[1][2].
D-Tyrosine-d7 is the deuterium labeled D-Tyrosine. D-Tyrosine is the D-isomer of tyrosine. D-Tyrosine negatively regulates melanin synthesis by inhibiting tyrosinase activity. D-Tyrosine inhibits biofilm formation and trigger the self-dispersal of biofilms without suppressing bacterial growth[1][2].
Maropitant- 13C,d3 is the 13C- and deuterium labeled Maropitant. Maropitant is a selective and orally active neurokinin (NK1) receptor antagonist. Maropitant acts by blocking the binding of substance P within the emetic center and the chemoreceptor trigger zone (CRTZ). Maropitant is highly effective in preventing vomiting[1][2].
Trimetazidine-d8 (dihydrochloride) is the deuterium labeled Trimetazidine dihydrochloride. Trimetazidine dihydrochloride is a selective long chain 3-ketoyl coenzyme A thiolase inhibitor with an IC50 of 75 nM, which can inhibit β-oxidation of free fatty acid (FFA). Trimetazidine dihydrochloride is an effective antianginal agent and a cytoprotective agent, has anti-oxidant, anti-inflammatory, antinociceptive and gastroprotective properties. Trimetazidine dihydrochloride triggers autophagy. Trimetazidine dihydrochloride is also a 3-hydroxyacyl-CoA dehydrogenase (HADHA) inhibitor[1][2][3][4].
Benzyl butyl phthalate-d4 is the deuterium labeled Benzyl butyl phthalate[1]. Benzyl butyl phthalate, a member of phthalic acid esters (PAEs), can trigger the migration and invasion of hemangioma (HA) cells via upregulation of Zeb1. Benzyl butyl phthalate activates aryl hydrocarbon receptor (AhR) in breast cancer cells to stimulate SPHK1/S1P/S1PR3 signaling and enhances formation of metastasis-initiating breast cancer stem cells (BCSCs)[2][3][4].
MIR96-IN-1 targets the Drosha site in the miR-96 (miRNA-96, microRNA-96) hairpin precursor, inhibiting its biogenesis, derepressing downstream targets, and triggeringapoptosis in breast cancer cells. MIR96-IN-1 binds to RNAs with Kds of 1.3, 9.4, 3.4, 1.3 and 7.4 μM for RNA1, RNA2, RNA3, RNA4 and RNA5, respectively . MIR96-IN-1 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
Inquiry Online
Your information is safe with us. * Required Fields.
