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Rapamycin (Sirolimus; AY 22989) is a potent and specific blood-brain barrier-transmissible mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1 . Rapamycin is an autophagy activator, an immunosuppressant .
V-9302 is a competitive antagonist of transmembrane glutamine flux. V-9302 selectively and potently targets the amino acid transporter ASCT2 (SLC1A5) not ASCT1. V-9302 inhibits ASCT2-mediated glutamine uptake (IC50=9.6 μM) in HEK-293 cells .
GSK1016790A is a potent and selective transient receptor potential vanilloid 4 (TRPV4) channel agonist. GSK1016790A can elicit Ca 2+ influx and elevate intracellular Ca 2+ in HEKcells .
Linrodostat (BMS-986205) is a selective and irreversible indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor with an IC50 value of 1.1 nM in IDO1-HEK293 cells. Linrodostat is well tolerated with potent pharmacodynamic activity in advanced cancers .
GSK717 is a potent, selective NOD2 (nucleotide-binding oligomerization domain 2) inhibitor. GSK717 inhibits muramyl dipeptide (MDP)-induced NOD2-mediated signaling, with an IC50 of 400 nM for MDP-stimulated IL-8 secretion in HEK293/hNOD2 cells .
PTC-209 is a specific BMI-1 inhibitor with an IC50 of 0.5 μM in HEK293T cell line. PTC-209 irreversibly impairs colorectal cancer-initiating cells (CICs). PTC-209 shows potent anti-myeloma activity and impairs the tumor microenvironment .
ABL127 is a selective and covalent inhibitor of protein methylesterase 1 (PME-1) with IC50s of 6.4 nM and 4.2 nM in HEK293T and MDA-MB-231 cells, respectively.
Ajmaline (Cardiorythmine) is a sodium channel blocking, class 1A anti-arrhythmic agent. Ajmaline blocks HERG currents with an IC50 of 1 μM in HEKcells and 42.3 μM in Xenopus oocytes. Ajmaline can be used for the research of the ventricular tachyarrhythmia .
JHU37160 is a potent and brain-penetrant DREADD agonist, with EC50s of 18.5 nM and 0.2 nM for hM3Dq and hM4Di DREADDs in HEK-293 cells, respectively. JHU37160 exhibits selective [ 3H]Clozapine displacement from DREADDs and not from other Clozapine-binding sites in mice brain tissue .
BMS 299897 is a sulfonamide γ-secretase inhibitor with an IC50 of 7 nM for Aβ production inhibition in HEK293 cells stably overexpressing amyloid precursor protein (APP).
Rapamycin-d3 is the deuterium labeled Rapamycin. Rapamycin is a potent and specific mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1. Rapamycin is an autophagy activator, an immunosuppressant .
Apelin-17(human, bovine) is an endogenous orphan G protein-coupled receptor APJ agonist. Apelin-17(human, bovine) binds to human APJ receptors expressed in HEK 293 cells (pIC50=9.02). Apelin-17(human, bovine) inhibits the entry of some HIV-1 and HIV-2 into the NP2/CD4 cells expressing APJ .
Venturicidin A (Aabomycin A1), from actinomycetes, is a membrane-active natural product inhibitor of ATP synthase. Venturicidin A potentiates the aminoglycoside antibiotic gentamicin against multidrug-resistant clinical isolates of Staphylococcus, Enterococcus, and Pseudomonas aeruginosa. Venturicidin A shows noticeable toxicity toward human embryonic-kidney (HEK)cells with an IC50 of 31 μg/mL.
EDP-305 is an orally active, potent and selective farnesoid X receptor (FXR) agonist, with EC50 values of 34 nM (chimeric FXR in CHO cells) and 8 nM (full-length FXR in HEKcells). EDP-305 shows a potent and consistent antifibrotic effect. EDP-305 can be used for primary biliary cholangitis (PBC) and non-alcoholic steatohepatitis (NASH) research .
Nav1.8-IN-2 (compound 35A) is a Nav1.8 voltage-gated sodium ion inhibitor with an IC50 of 0.4 nM (HEK 293 cells). Nav1.8-IN-2 inhibits the activity of Nav1.8 voltage-gated sodium ion channels, mediates sodium ion influx in excitable cells, and is associated with the initiation and conduction of action potentials. Nav1.8-IN-2 can be used for research related to pain, cough, itching, etc .
MS049, a chemical probe, is a potent, selective, and cell-active dual inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively. MS049 reduces levels of Med12me2a and H3R2me2a in HEK293 cells. MS049 is not toxic and does not affect the growth of HEK293 cells .
Gamma-Glu-Abu TFA is the TFA salt form of Gamma-Glu-Abu (HY-P4376). Gamma-Glu-Abu TFA is an agonist for calcium sensing receptor (CaSR), that activates the CaSR with an EC50 of 0.21 μM in HEK-293 cell .
AT 1001 is an orally effective α3β4 nicotinic acetylcholine receptor (α3β4 nAChR) antagonist with a Ki value of 2.64 nM. AT 1001 reversibly blocks Epibatidine (HY-101078)-induced inward currents in HEKcells transfected with α3β4 nAChR. AT 1001 dose-dependently blocks nicotine self-administration behavior in rats, alleviates gluten-induced gastrointestinal symptoms, blocks tight junction toxin-induced immune responses, and reduces the incidence of type 1 diabetes in rats. AT 1001 can be used in the research of nicotine addiction and celiac disease .
KY1220 is a compound that destabilizes both β-catenin and Ras, via targeting the Wnt/β-catenin pathway, with an IC50 of 2.1 μM in HEK293 reporter cells .
JNJ-18038683 is a 5-Hydroxytryptamine Type 7 (5-HT7) receptor antagonist, with pKis of 8.19, 8.20 for rat and human 5-HT7 in HEK293 cells, respectively.
Apelin-36(human) is an endogenous orphan G protein-coupled receptor APJ agonist, with an EC50 of 20 nM. Apelin-36(human) shows high affinity to human APJ receptors expressed in HEK 293 cells (pIC50=8.61). Apelin-36 has been linked to two major types of biological activities: cardiovascular and metabolic. Apelin-36(human) inhibits the entry of some HIV-1 and HIV-2 into the NP2/CD4 cells expressing APJ .
KB130015 (KB015) is an orally active and potent ThRα and ThRβ (thyroid hormone receptor) inhibitor, with IC50 values of 4.5 and 5.1 μM, respectively. KB130015 markedly slows the kinetics of inactivation of Na + channels. KB130015 activates hERG1 channels (EC50 = 12.2 μM) and large-conductance Ca 2+-activated K + (BKCa) channels formed by hSlo1 (α) subunits in HEK 293 cells. KB130015 has antiarrhythmic properties. KB130015 can be used for the study of cardiovascular disease .
GNE-6468 is a highly potent and selective RORγ (RORc) inverse agonist with an EC50 value of 13 nM for HEK-293 cell. GNE-6468 exhibits an EC50 of 30 nM for IL-17 PBMC .
Chenodeoxycholic acid 3-glucuronide is a metabolite of Chenodeoxycholic acid that can activate the key nuclear receptor (FXR), with an EC50 of 8 μM, and in HEK293T cells, the EC50 for activating FXR is 11 μM .
BMS-466442 is a potent and selective inhibitor of asc-1 (alanine serine cysteine transporter-1), with an IC50 of 11 nM. BMS-466442 inhibits [ 3H] D-serine uptake into rat brain synaptosomes, with an IC50 of 400 nM. BMS-466442 can be used for schizophrenia research .
MI-1851 is a potent furin inhibitor. MI-1851 prevents the proteolytic processing of the S protein of SARS-CoV-2 by endogenous flavoprotease in HEK293 cells. MI-185 has antiviral activity .
Octyl-α-ketoglutarate (1-Octyl 2-oxopentanedioate) is a stable, cell-permeable form of α-ketoglutarate which accumulates rapidly in HEK293 cells with a dysfunctional tricarboxylic acid (TCA) cycle, stimulating prolyl hydroxylase (PHD) activity. In addition, Octyl-α-ketoglutarate competitively blocks succinate- or fumarate-mediated inhibition of PHD .
MPX-004 is a potent GluN2A antagonist. MPX-004 inhibits GluN2A-containing NMDA receptors expressed in HEKcells with an IC50 of 79 nM. MPX-004 has no inhibitory effect on GluN2B or GluN2D receptor-mediated responses. MPX-004 has the potential for neuropsychiatric and developmental disorders research .
WS-898 is a highly effective ABCB1 inhibitor capable of reversing paclitaxel (PTX) resistance in drug-resistant SW620/Ad300, KB-C2, and HEK293/ABCB1 cells (IC50 = 5.0, 3.67, and 3.68 nM, respectively).
JHU37152 is a potent and brain-penetrant DREADD agonist, with EC50s of 5 nM and 0.5 nM for hM3Dq and hM4Di DREADDs in HEK-293 cells, respectively. JHU37152 exhibits selective [ 3H]Clozapine displacement from DREADDs and not from other Clozapine-binding sites in mice brain tissue .
ML352 is a noncompetitive inhibitor of the presynaptic choline transporter (CHT) with Ki
values of 92 and 166 nM for HEK293 cells expressing human CHT and mouse forebrain synaptosomes, respectively .
VU625 is an inhibitor for potassium channel, that selectively inhibits mosquito Aedes aegypti inward rectifier potassium channel 1 (AeKir), with IC50 of 96.8 nM in HEK293 cell. VU625 can be used in development of insecticide .
PTC-209 hydrobromide is a specific BMI-1 inhibitor with an IC50 of 0.5 μM in HEK293T cell line. PTC-209 hydrobromide irreversibly impairs colorectal cancer-initiating cells (CICs). PTC-209 hydrobromide shows potent anti-myeloma activity and impairs the tumor microenvironment .
ASCT2-IN-1 (compound 20k) is an ASCT2 inhibitor with IC50 values of 5.6 μM and 3.5 μM in cells A549 and HEK293, respectively. ASCT2-IN-1 induces cellapoptosis. ASCT2-IN-1 inhibits tumor growth .
Delta3,5-cholestadien-7-one is an oxysterol and a negative allosteric modulator of GABAA receptors. Delta3,5-cholestadien-7-one reduces GABA-induced currents in HEKcells expressing α1β1γ2 or α4β3γ2 subunit-containing GABAA receptors with IC50 values of 1.5 and 1 µM, respectively. Delta3,5-cholestadien-7-one reduces GABA-induced depolarization of peptidergic and non-peptidergic nociceptors, C-LTMRs, and cold thermosensors in isolated mouse dorsal root ganglion (DRG) neurons .
Apelin-36(human) TFA is an endogenous orphan G protein-coupled receptor APJ agonist, with an EC50 of 20 nM. Apelin-36(human) TFA shows high affinity to human APJ receptors expressed in HEK 293 cells (pIC550=8.61). Apelin-36(human) TFA has been linked to two major types of biological activities: cardiovascular and metabolic. Apelin-36(human) TFA inhibits the entry of some HIV-1 and HIV-2 into the NP2/CD4 cells expressing APJ .
S-22153 is a potent melatonin receptor antagonist with EC50 values of 19 nM, 4.6 nM for hMT1 and hMT2 melatonin receptor, respectively. S-22153 has Ki values of 8.6 nM (CHO cells) and 16.3 nM (HEKcells) for hMT1, and 6.0 nM (CHO cells) and 8.2 nM (HEKcells) for hMT2. S-22153 is a specific ligand of MT1 and MT2 melatonin receptors subtypes .
Amitifadine (DOV-21947; EB-1010) hydrochloride is a serotonin-norepinephrine-dopamine reuptake inhibitor (SNDRI), with IC50s of 12, 23, 96 nM for serotonin, norepinephrine and dopamine in HEK 293 cells , respectively.
JJH260 is AIG1inhibitor, and inhibit the fluorophosphonate reactivity and fatty acid esters of hydroxy fatty acid (FAHFA) hydrolysis activity of AIG1in HEK293T cells, with IC50 values of 0.50 μM and 0.57 μM, respectively .
YS-370 (compound 44) is a potent, high selective, and orally active inhibitor of P-glycoprotein (P-gp). YS-370 stimulates the P-gp ATPase activity and has moderate inhibition against CYP3A4. YS-370 effectively reverses multidrug resistance (MDR) to paclitaxel and colchicine in SW620/AD300 and HEK293T-ABCB1 cells. YS-370 in combination with paclitaxel achieves much stronger antitumor activity .
hVEGF-IN-3 (compound 9) is a potent hVEGF inhibitor. hVEGF-IN-3 inhibits HT-29, MCF-7, and HEK-293 cells proliferation with IC50s of 61, 142, and 114 μM .
PROTAC STAT6 degrader-2 is a highly efficient PROTAC degrader targeting STAT6. PROTAC STAT6 degrader-2 has a DC50 value of 1-10 nM for STAT6 in human PBMC cells and a DC50 value of less than 100 nM for STAT6 in HEK293-HIBiT-STAT6 cells. PROTAC STAT6 degrader-2 can be used for STAT6-mediated diseases .
STX-100 (Biotinylated) is a biotin-labeled STX-100 (HY-P990667). STX-100 is a humanized antibody expressed in HEK293 cells, targeting Integrin aVb6 (ITGAV & ITGB6) .
Apelin-17(human, bovine) TFA is an endogenous orphan G protein-coupled receptor APJ agonist. Apelin-17(human, bovine) TFA binds to human APJ receptors expressed in HEK 293 cells (pIC50=9.02). Apelin-17(human, bovine) TFA inhibits the entry of some HIV-1 and HIV-2 into the NP2/CD4 cells expressing APJ .
MS049 dihydrochloride is a potent, selective, and cell-active dual inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively. MS049 dihydrochloride reduces levels of Med12me2a and H3R2me2a in HEK293 cells. MS049 dihydrochloride is not toxic and does not affect the growth of HEK293 cells .
Lu AF90103 (Compound 42e) is a methyl ester prodrug of compound 42d capable of penetrating the blood-brain barrier. Compound 42d acts as a partial agonist of the GluN1/GluN2B complex, exhibiting 24% efficacy, and has an EC50 value of 78 nM. Lu AF90103 plays an important role in neuropsychiatric diseases research .
Linrodostat (BMS-986205) mesylate is a selective irreversible inhibitor of indoleamine 2,3-dioxygenase 1 (IDO1), which effectively inhibits IDO1-HEK293 mesylate cells with an IC50 value of 1.1 nM. Linrodostat mesylate demonstrates good pharmacological activity in advanced cancer .
U-101958 (PNU-101958) maleate is a highly selective ligand and antagonist for dopamine D4 receptor, with an IC50 of 2.7 nM. U-101958 maleate behaves as an agonist in HEK-293 cells expressing the human recombinant D4.4 receptor. U-101958 maleate is an antipsychotic .
Asuptegravir (Compound 1) is an inhibitor of HIV integrase activity. Asuptegravir inhibits HIV in HEK293T cells (EC50 = 1.08 nM). Asuptegravir can be studied in anti-AIDs/HIV research .
JLK-6 markedly reduce the production of amyloid β-peptide (Aβ) by amyloid-β Precursor protein (APP) expressing HEK293 cells by affecting the γ-secretase cleavage of APP, with no effect on the cleavage of the Notch receptor .
MPCI is a cell-permeant MC4R-selective ligand with pharmacological chaperone activity. MPCI is a MC4R antagonist with a Ki value of 0.218 μM on HEK293 cells expressing hMC4R. MPCI can be used for the research of MC4R-deficient obesity .
AZ513 is a reversible FAAH inhibitor with an IC50s of 551 nM and 27 nM for human FAAH and rat FAAH, respectively. AZ513 inhibits Anandamide (HY-10863) hydrolysis in human FAAH-transfected HEK293 cells (IC50 of 360 nM) .
17β-HSD10-IN-3 (compound 23) is a 17β-HSD10 inhibitor with the IC50 of 5.59 μM. 17β-HSD10-IN-3 shows no cell cytotoxicity toward the HEK-293 cell line up to 20 μM .
AGH-107 is a high selective and brain-penetrant agonist of 5-HT7 receptor, with a Ki of 6 nM and EC50 of 19 nM. AGH-107 exhibits high selectivity over related CNS targets, high metabolic stability and low toxicity in HEK-293 and HepG2 cell cultures .
JN122, a spiroindoline-containing molecule, is a MDM2 inhibitor. JN122 Inhibits MDM2/p53 protein–protein interaction and exerts robust in vivo antitumor efficacy. JN122 has antiproliferative activity in HCT-116 cells and HEK-293 cells with IC50 values of 39.6 nM and 4.28μM, respectively. JN122 can promote activation of p53 and its target genes, inhibited cell cycle progression, and induced cell apoptosis .
Photosensitizer-3 is a photosensitizer that exhibits powerful selective killing effects on transfected HEKcells and affibody-targeted A431 cancer cells when exposed to near-infrared light excitation .
Linopirdine dihydrochloride is a agonist of capsaicin receptor TRPV1. Linopirdine increases the intracellular calcium concentration in HEK293 cells. Linopirdine dihydrochloride exerts an excitatory action on mammalian nociceptors .
Antitrypanosomal agent 5 (Compound 25)is a selective anti-trypanosomal agent with IC50s of 1 nM and 483.3 µM against T. bruceicell growth and HEK293 cells growth , respectively .
CD73-IN-19 (Compound 4ab) is a CD73 inhibitor (with a 44% inhibition rate of CD73 enzymatic activity at 100 μM). CD73-IN-19 (at 10 μM and 100 μM) can completely antagonize the blockade of T cell proliferation induced by TCR (T cell receptor) triggering (which is induced by CD73 activity), and it can also inhibit the hA2A receptor activity in HEK-293 cells (Ki is 3.31 μM). CD73-IN-19 holds promise for research in the field of immune diseases .
Amitifadine (DOV-21947; EB-1010) is a serotonin-norepinephrine-dopamine reuptake inhibitor (SNDRI), with IC50s of 12, 23, 96 nM for serotonin, norepinephrine and dopamine in HEK 293 cells , respectively.
KPC-2-IN-1, boronic acid derivative, is a potent KPC-2 inhibitor with Ki of 0.032 μM. KPC-2-IN-1 enhances the activity of cefotaxime in KPC-2 expressing E. coli. KPC-2-IN-1 exhibits well tolerated in human HEK-293 cells, which can be used for the study of E. coli resistance to β-lactam antibiotics .
Dopamine D4 receptor ligand 3 (Compound 16) is a dopamine D4 receptor (D4R) antagonist (pKi: 8.86). Dopamine D4 receptor ligand 3 has pIC50 values of 5.78, 5.55, and 6.17 for Go, Gi, and βArr2 sensors in HEK-293T cells, respectively. Dopamine D4 receptor ligand 3 inhibits the viability of three human glioma cell lines, U87 MG, T98G, and U251 MG. Dopamine D4 receptor ligand 3 induces ROS production and mitochondrial dysfunction in glioma cells .
Antimalarial agent 12 (compound R-3b) is a potent antimalarial agent. Antimalarial agent 12 shows growth inhibition on P. falciparum Dd2 Strain (EC50=155 nM), 3D7 strain (EC50=136 nM). Antimalarial agent 12 has CC50 values of 10,000 to 50,000 nM for HEK-293 and hPHep cell lines. Antimalarial agent 12 has a MIC of >250,000 nM for Escherichia coli .
L-644698 is a potent and selective human recombinant prostaglandin D2 (PGD2) receptor (hDP) agonist with Ki values of 0.9, 267, 3730, 9280 nM for hDP, hEP2, hEP3, hEP4, respectively. L-644698 induces cyclic AMP production with an EC50 value of 0.5 nM .
JNJ-18038683 free base is a 5-Hydroxytryptamine Type 7 (5-HT7) receptor antagonist, with pKis of 8.19, 8.20 for rat and human 5-HT7 in HEK293 cells, respectively.
RXFP1 receptor agonist-6 (Example 7) is a RXFP1 receptor agonist. RXFP1 receptor agonist-6 stimulates cAMP production in HEK293 cells stably expressing human RXFP1, with an EC50 value of 12 nM .
RXFP1 receptor agonist-3 (Example 223) is a RXFP1 receptor agonist. RXFP1 receptor agonist-3 stimulates cAMP production in HEK293 cells stably expressing human RXFP1, with an EC50 value of 2 nM .
Anti-MRSA agent 4 (compound 7a) is a potent and selective growth inhibitor of Gram-positive Methicillin-resistant Staphylococcus aureus (MRSA), with MIC ≤ 0.26 µM. Anti-MRSA agent 4 exhibits no cytotoxic and no hemolytic activity in HEK293 cells .
RXFP1 receptor agonist-2 (Example 124) is a RXFP1 receptor agonist. RXFP1 receptor agonist-2 stimulates cAMP production in HEK293 cells stably expressing human RXFP1, with an EC50 value of 1 nM .
RXFP1 receptor agonist-8 (Example 2) is a RXFP1 receptor agonist. RXFP1 receptor agonist-8 stimulates cAMP production in HEK293 cells stably expressing human RXFP1, with an EC50 value of 1.8 nM .
RXFP1 receptor agonist-4 (Example 268) is a RXFP1 receptor agonist. RXFP1 receptor agonist-4 stimulates cAMP production in HEK293 cells stably expressing human RXFP1, with an EC50 value of 4.9 nM .
RXFP1 receptor agonist-5 (Example 98) is a RXFP1 receptor agonist. RXFP1 receptor agonist-5 stimulates cAMP production in HEK293 cells stably expressing human RXFP1, with an EC50 value of 1.3 nM .
Tembetarine chloride is a alkaloid that can be isolated from Tinospora cordifolia that exhibits antibacterial activity. Tembetarine chloride exhibits weak cytotoxicity against mouse fibroblasts (L929) and human embryonic kidney cells (HEK293) with IC50 of 1245.33 μg/mL and 1642.81 μg/mL, respectively .
RXFP1 receptor agonist-7 (Example 2) is a RXFP1 receptor agonist. RXFP1 receptor agonist-7 stimulates cAMP production in HEK293 cells stably expressing human RXFP1, with an EC50 value of 4.2 nM .
SARS-CoV-2 3CLpro-IN-33 (Compound 16) is an orally active SARS-CoV-2 3CL protease inhibitor, with an IC50 value of 1.5 nM. SARS-CoV-2 3CLpro-IN-33 shows excellent anti-SARS-CoV-2 viral activity in the HEK293T-AT cell model with an EC50 of 0.017 μM. SARS-CoV-2 3CLpro-IN-33 can be used for the study of COVID-19 infetction .
MS049 (Standard) is the analytical standard of MS049 (HY-100360). This product is intended for research and analytical applications. MS049, a chemical probe, is a potent, selective, and cell-active dual inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively. MS049 reduces levels of Med12me2a and H3R2me2a in HEK293 cells. MS049 is not toxic and does not affect the growth of HEK293 cells .
γ-glutamyltransferase, Human (HEK293) is a γ-glutamyltransferase expressed in HEK293 cells. γ-glutamyltransferase participates in glutathione metabolism. Serum γ-glutamyltransferase activity is identified as a predictor of atherosclerotic complications, and has prognostic value for cardiovascular diseases and stroke. γ-glutamyltransferase also serves as a biomarker for carcinogenesis and tumor progression .
Linrodostat (Standard) is the analytical standard of Linrodostat (HY-101560). This product is intended for research and analytical applications. Linrodostat (BMS-986205) is a selective and irreversible indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor with an IC50 value of 1.1 nM in IDO1-HEK293cells. Linrodostat is well tolerated with potent pharmacodynamic activity in advanced cancers .
HBC-12551 is an orally active BTK inhibitor (IC50 in HEK293 cells: 1.31 nM for BTK; 2.18 nM for BTK C481S). HBC-12551 has antitumor activity against diffuse large B-cell lymphoma .
Val-CDCA is a chenodeoxycholate (CDCA) and C-24 L-Valine (HY-N0717) conjugate. Val-CDCA inhibits taurocholate uptake in human NTCP-stably transfected HEK293 cells. Val-CDCA can be used for HBV infection .
Analgesic agent-2 is a selective and orally active NaV1.8 Channel inhibitor, with an IC50 of 50.18 nM in HEK293 cells stably expressing human NaV1.8 channel. Analgesic agent-2 has analgesic activity .
RXFP1 receptor agonist-1 (Example 2 peak2) is a RXFP1 receptor agonist. RXFP1 receptor agonist-1 stimulates cAMP production in HEK293 cells stably expressing human RXFP1, with an EC50 value of 300 nM .
WYJ-2 is a selective agonist for toll-like receptor 2/1 (TLR2/1) with EC50 of 18.57 nM in human TLR2 and TLR1 transient-cotransfected HEK 293T cells. WYJ-2 induces pyroptosis and exhibits anticancer activity against non-small cell lung cancer (NSCLC) .
SRI-37240 is a potent premature termination codons (PTCs) inhibitor. SRI-37240 suppresses CFTR nonsense mutations. SRI-37240 alters cellular translation termination at PTCs in HEK293T cells. SRI-37240 can also restore CFTR function in primary bronchial epithelial cells when combination with G418 .
VPC12249 is a competitive dual LPA1/LPA3 antagonist with Ki values of 137nM and 428 nM, respectively. VPC12249 inhibits calcium mobilization in HEK293T cells with a Ki value of ~130 nM. VPC12249 is promising for research of ovarian cancer and hypertensive diseases .
TREM2 agonist-5 is the microglial lipid-sensing receptor (TREM2) agonist with a Kd of 71.36 μM. TREM2 agonist-5 is a racemic structural analog of the TREM2 agonist VG-3927 and exhibits superior microglial phagocytosis and activates TREM2 signaling in HEK293-hTREM2/DAP12 cells. TREM2 agonist-5 displays a superior in vitro pharmacokinetic profile to VG-3927. TREM2 agonist-5 can used for the study of Alzheimer’s disease .
PACAP (1-38) free acid is a desamido-PACAP (1-38), human, ovine, rat (HY-P0221). PACAP (1-38) free acid can activate the human PAC1 receptor. PACAP (1-38) free acid induces cyclic AMP (cAMP) generation in both NS-1 neuroendocrine cells and non-neuroendocrine HEK293 cells .
Trans-2-butene-1,4-dicarboxylic acid (Standard) is the analytical standard of Trans-2-butene-1,4-dicarboxylic acid. This product is intended for research and analytical applications. Trans-2-butene-1,4-dicarboxylic acid (Dihydromuconic acid; trans-β-Hydromuconic acid) is an endogenous metabolite[1][2].
PF-46396 is a potent HIV-1 inhibitor with an EC50 value of 0.206 µM. PF-46396 shows antiviral activity. PF-46396 inhibits the processing of capsid (CA)/spacer peptide 1 (SP1) (p25) Gag precursor proteins and blocks maturation of the viral core particle .
(rac)-BDM88951 is the racemate of BDM88951 (HY-176778). BDM88951 (Compound 4 d) is a selective ERAP2 inhibitor with an IC50 of 19 nM. BDM88951 significantly inhibits antigen presentation in HEKcells. BDM88951 can be used for research on autoimmune diseases and cancer .
(1S,2S)-2-PCCA hydrochloride is a less active diastereomer of 2-PCCA. 2-PCCA is a GPR88 receptor agonist, and inhibits GPR88-mediated cAMP production, with an EC50 of 116 nM in HEK293 cells.
BRL-32872 is a potent human ether-a-go-go-related gene (hERG) potassium channel blocker (IC50=241 nM in isolated cardiomyocytes; 19.8 nM in HEK293 cells). BRL-32872 is promising for research of cardiac arrhythmias (e.g., atrial/ventricular rhythms) .
NY0116 is a neuromedin U receptor 2 (NMUR2) agonist with EC50 values of 27.76 μM for hNMUR1 and 13.61 μM for hNMUR2. NY0116 decreases cAMP while stimulating calcium signaling in stably expressing NMUR2 HEK293 cells .
(±)-ML 209 (compound 4n), a diphenylpropanamide, is a retinoic acid-related orphan receptor RORγ antagonist with an IC50 of 1.1 μM. (±)-ML 209 inhibits RORγt transcriptional activity with an IC50 of 300 nM in HEK293t cells. (±)-ML 209 inhibits the transcriptional activity of RORγt, but not RORα in cells. (±)-ML 209 selectively inhibits murine Th17 cell differentiation without affecting the differentiation of naïve CD4 + T cells into other lineages, including Th1 and regulatory T cells .
KP-2067 is a form of the CaSR agonist peptide. KP-2067 can result in dose-dependent activation of CaSR in HEK293T overexpressing hCaSR cell line, with an EC50 of 18.4 μM. KP-2067 significantly reduces plasma parathyroid hormone in rat model .
11β-HSD1-IN-14 (Compound 17) is a selective inhibitor for 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1), with IC50 of 74 nM for human HSD1, and 603 nM for HSD1 expressed HEK293 cell .
RAD51-IN-9 (Compound 3a) is a RAD51 inhibitor that can inhibit the binding of RAD51 to ssDNA with an IC50 of 17.85 μM. RAD51-IN-9 has a LD50 against HEK293 cells of 40.21 μM. RAD51-IN-9 can sensitize cells to Mitomycin C (HY-13316) .
M04 is an agonist of STING. It induces the expression of the IFN reporter gene in HEK293T cells expressing wild-type human STING, but does not induce this expression in HEK293T cells expressing the R71H-G230A-R293Q (HAQ) STING variant or in mouse RAW 264.7 cells, indicating that its activity is dependent on allelic and species variations. M04 induces the production of TNF-α, IL-10, IL-1β, and IL-12p70 in human peripheral blood mononuclear cells (PBMCs). At a concentration of 50 µM, M04 stimulates dendritic cells isolated from PBMCs to express the MHC class II cell surface receptor HLA-DR and co-stimulatory molecules CD40, CD80, and CD86, and also enhances their ability to activate T cells in an ex vivo assay. M04 can be used in research on inflammatory immune diseases .
KY1220 (Standard) is the analytical standard of KY1220 (HY-102028). This product is intended for research and analytical applications. KY1220 is a compound that destabilizes both β-catenin and Ras, via targeting the Wnt/β-catenin pathway, with an IC50 of 2.1 μM in HEK293 reporter cells .
Simvastatin acid (Tenivastatin) calcium hydrate is a potent HMG-CoA reductase (HMGCR) inhibitor. Simvastatin acid calcium hydrate reduces Indoxyl sulfate-mediated reactive oxygen species (ROS) production in human cardiomyocytes. Simvastatin acid calcium hydrate can also modulates OATP3A1 expression in cardiomyocytes and HEK293 cells transfected with the OATP3A1 gene .
PTGR2-IN-1 is a potent PTGR2 inhibitor with an IC50 of ~0.7 μM. PTGR2-IN-1 increases 15-keto-PGE2-dependent PPARγ transcriptional activity in PTGR2-transfected HEK293T cells .
PROTAC IRAK4 degrader-10 (compound 10) is an oral active PROTAC based on Cereblon ligand, and induces the degradation of IRAK4 with maximum degradation of 95.94% and the DC50 of 7.68 nM in HEK293 cells (Sturcture Note:(Blue: Cereblon ligand, Black: linker；Pink: IRAK4 ligand) .
Simvastatin acid (Tenivastatin) ammonium is a potent HMG-CoA reductase (HMGCR) inhibitor. Simvastatin acid ammonium reduces Indoxyl sulfate-mediated reactive oxygen species (ROS) production in human cardiomyocytes. Simvastatin acid ammonium can also modulates OATP3A1 expression in cardiomyocytes and HEK293 cells transfected with the OATP3A1 gene .
Ajmaline (Standard) is the analytical standard of Ajmaline. This product is intended for research and analytical applications. Ajmaline (Cardiorythmine) is a sodium channel blocking, class 1A anti-arrhythmic agent. Ajmaline blocks HERG currents with an IC50 of 1 μM in HEKcells and 42.3 μM in Xenopus oocytes. Ajmaline can be used for the research of the ventricular tachyarrhythmia .
BAPTA-AM is a well-known membrane permeable Ca 2+ chelator. BAPTA-AM inhibits hERG channels, hKv1.3 and hKv1.5 channels in HEK 293 cells with IC50s of 1.3 μM, 1.45 μM and 1.23 μM, respectively .
Simvastatin hydroxy acid (Tenivastatin) sodium is a potent HMG-CoA reductase (HMGCR) inhibitor. Simvastatin hydroxy acid sodium reduces Indoxyl sulfate-mediated reactive oxygen species (ROS) production in human cardiomyocytes. Simvastatin hydroxy acid sodium can also modulates OATP3A1 expression in cardiomyocytes and HEK293 cells transfected with the OATP3A1 gene .
Rapamycin (Sirolimus) (GMP) is Rapamycin (HY-10219) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Rapamycin (Sirolimus; AY 22989) is a potent and specific mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1 . Rapamycin is an autophagy activator, an immunosuppressant .
SSR240612 is a potent, and orally active specific non-peptide bradykinin B1 receptor antagonist, with Kis of 0.48 nM and 0.73 nM for B1 kinin receptors of human fibroblast MRC5 and HEKcells expressing human B1 receptors, 481 nM and 358 nM for B2 receptors of guinea pig ileum membranes and CHO cells expressing human B1 receptor, respectively.
IKE16 is a fungi-selective eukaryotic topoisomerase II inhibitor, with an IC50 value of 13.68 μM. IKE16 suppresses both the DNA relaxation activity and the decatenation activity of yTOPOII selectively. IKE16 shows moderate activity against standard fungal strains (Candida albicans ATCC 10231, Saccharomyces cerevisiae ATCC 89763) with a minimum inhibitory concentration (MIC) of 2 μg/mL against S. cerevisiae ATCC 89763. IKE16 exhibits high cytotoxicity against human cells, with an EC50 of 0.07 μM in HepG2 and 0.045 μM in HEK-293. IKE16 can be used for the study of antifungal infection .
SB 206553 is a 5-HT2C inverse agonist. SB 206553 can attenuate methamphetamine-seeking in rats. SB 206553 has activity for 5-HT2 receptor ligands in HEK-293 or CHO-K1 cells expressing human recombinant 5-HT2 receptors with pKi values of 5.6 nM (5-HT2A), 7.7 nM (5-HT2B) and 7.8 nM (5-HT2C), respectively. SB 206553 can be used for the research of psychostimulant abuse disorders .
Simvastatin acid (Tenivastatin), a hydrolysate of Simvastatin (HY-17502), is a HMG-CoA reductase (HMGCR) inhibitor. Simvastatin acid reduces Indoxyl sulfate-mediated reactive oxygen species (ROS) production in human cardiomyocytes. Simvastatin acid can also modulates OATP3A1 expression in cardiomyocytes and HEK293 cells transfected with the OATP3A1 gene .
PROTAC IRAK4 degrader-11 (compound 15) is PROTAC based on Cereblon ligand, and induces the degradation of IRAK4 with maximum degradation of 96.25% and the DC50 of 2.29 nM in HEK293 cells(Sturcture Note:(Blue: Cereblon ligand (HY-14658), Black: linker；Pink: IRAK4 inhibitor) .
Rapamycin (Standard) is the analytical standard of Rapamycin (HY-10219). This product is intended for research and analytical applications. Rapamycin (Sirolimus; AY 22989) is a potent and specific mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1 . Rapamycin is an autophagy activator, an immunosuppressant .
L-γ-Carboxyglutamic acid (H-Gla-OH) is a mGluR2 antagonist with an IC50 of 102 μM. L-γ-Carboxyglutamic acid binds to the mGluR2 receptor site via the overlapping extended amino acid conformation of its amino and carboxyl groups with glutamic acid, and its additional acidic group locates in a restricted region, thereby blocking the full activation of the receptor. L-γ-Carboxyglutamic acid can be used for the research of neurological disorders .
SID 7969543 (Standard) is the analytical standard of SID 7969543 (HY-107404). This product is intended for research and analytical applications. 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 .
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 .
Rapamycin (Sirolimus) GMP Like is Rapamycin (HY-10219) produced by using GMP like guidelines. GMP Like small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Rapamycin (Sirolimus; AY 22989) is a potent and specific mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1 . Rapamycin is an autophagy activator, an immunosuppressant .
Muscarinic M4 modulator-1 is a Muscarinic M4 receptor positive allosteric modulator. Muscarinic M4 modulator-1 activates the muscarinic M4 receptor with allosteric potency EC50 s of 14 and 3 Nm in CHO-K1 cells and HEK293 cells. Muscarinic M4 modulator-1 has an antipsychotic-like activity, promising for psychiatric and/or neurological disorders research .
BmP02 is a selective Kv1.3 channel blocker and a highly-selective Kv4.2 modulator, which can be isolated from Chinese scorpion (Buthus martensi Karsch) venom. BmP02 also delays the inactivation of Kv4.2 in HEK293T cells, with an EC50 value of ~850 nM. BmP02 inhibits the transient outward potassium currents (Ito) in ventricular muscle cells .
MDI-117740 is a dual LIMK1/2 inhibitor. MDI-117740 shows effective cellular target engagement with LIMK1 (pIC50 = 6.73) and LIMK2 (pIC50 = 7.18) in HEK293 cells. MDI-117740 exerts significant anti-migratory activity in MDA-MB-231 cells. MDI-117740 can be used for the study of cancers and neurodegenerative disorders .
AB3067 is a PROTAC degrader for BET protein, that recruits two different E3 ligase Cereblon and VHL with good affinity (IC50=559 nM for VHL in live HEK293; IC50=190 nM for CRBN in live HEK293), and degrades BRD2, BRD3, BRD4 and CRBN with DC50 of 2.1~2.3, 1.6, 15 and 75 nM, respectively. AB3067 inhibits the proliferation of RKO cell with an EC50 of 111 nM . (Pink: ligand for target protein (HY-131633A); Black: linker (HY-170391); Blue: ligand for E3 ligase VHL (HY-112078) and CRBN(HY-W998346))
VU0514009 is a competitive chemokine-like receptor 1 (CMKLR1) antagonist (EC50=2 nM). VU0514009 prevents chemerin-9-induced arrestin recruitment and receptor internalization, significantly reducing Ca 2+ flux response in HEK293 cells. VU0514009 is promising for research of inflammatory diseases and metabolic syndrome .
E197 is the inhibitor for DOCK5 that destroys the podosome belt structure of osteoclasts, thereby inhibiting the bone resorption (IC50=3.44 μM in human osteoclast). E197 inhibits the Rac in DOCK5 expressing HEK293 cell with an IC50 of 36 μM. E197 prevents the bone loss in mouse ovariectomized models .
C24:1 Ganglioside GM2 (d18:1/24:1) (ammonium) is an endogenous monosialylated ganglioside. C24:1 Ganglioside GM2 (d18:1/24:1) (ammonium) is a self-lipid that can bind to CD1d in HEK293T cells .
Fenoprofen (LILLY-53858) is a nonsteroidal anti-inflammatory agent (NSAID) and inhibits cyclooxygenase (COX). Fenoprofen is a melanocortin receptors (MCRs) positive allosteric modulator (PAM). Fenoprofen also increases ERK1/2 activation in HEK293T cells. Fenoprofen has anti-arthritic activities and can be used for the study of rheumatoid arthritis and osteoarthritis .
ERK5-IN-4 (compound 34b) is a potent and selective inhibitor of extracellular signal-related kinase 5 (ERK5). ERK5-IN-4 inhibits ERK5 (full-length) and truncated ERK5 (ERK5 ΔTAD) kinase activity in HEK293 cells with an IC50 of 77 nM and 300 nM, respectively .
Chloroguanabenz (acetate) is an antiprion agent and a derivative of the α2-adrenergic receptor agonist guanabenz. Chloroguanabenz (acetate) can inhibit the formation of prion in yeast and mammalian in vitro assays. Chloroguanabenz (acetate) can reduce the levels of truncated Huntingtin derivative Htt48 in HEK293T cells. Chloroguanabenz (acetate) can be studied in research on Huntington’s disease .
(R)-V-0219 hydrochloride is an enantiomer of V-0219 (HY-143312). V-0219 is an orally active and positive allosteric modulator (PAM) of the GLP Receptor-1 (GLP-1R). (R)-V-0219 hydrochloride activates calcium fluxes in HEKcells stably expressing hGLP-1R .
Apoptosis inducer 32 (Compound 7g) is an apoptosis inducer with a KD of 42 μM, showing anti-tumor activity. Apoptosis inducer 32 caused significant cellular morphological changes in MDA-MB-231 cells, including membrane bubbling, nuclear fragmentation, and apoptotic body formation. The IC50 of Apoptosis inducer 32 in MCF-7, MDA-MB-231, and HEKcells is 4.77, 6.56 and 337.8 μM respectively .
STAT3-IN-25 (Compound 2p) is a potent STAT3 inhibitor with a p-trifluoroethoxy benzyl substituent. STAT3-IN-25 shows STAT3 luciferase inhibition activity using HEK293T cells with an IC50 of 22.3 nM and ATP production inhibition activity using BxPC-3 cells with an IC50 of 32.5 nM. STAT3-IN-25 has the potential for pancreatic cancer research .
HIV-1 inhibitor-35 (compound 74) is a potent HIV-1 inhibitor with EC50s of 80 nM and 70 nM for LTR and CMV in HEK293 cells, respectively. HIV-1 inhibitor-35 has inhibitory activity against liver cancer cell HepG2 with a CC50 of 40 nM. HIV-1 inhibitor-35 can be used as HIV-1 latency reversing agent .
Antiproliferative agent-60 (compound 8c) is a 11-Azaartemisinin derivative with superior anticancer activities. Antiproliferative agent-60 shows IC50 values of 7.7 μM, 42.5 μM, and 15.5 μM for epidermoid carcinoma (KB), HepG2, and A549 cells, respectively. Antiproliferative agent-60 exhibits significant tumor selectivity, up to 32-fold higher compared to Hek293 normal cells .
Hi 76-0079 (NNC0076-0079; 76-0079) is a lipase inhibitor that specifically targets hormone-sensitive lipase (HSL). Hi 76-0079 inhibits PNPB Hydrolysis in cell lysates of HEK293A cells
overexpressing Lipe with an IC50 value of 0.1 μM. Hi 76-0079 synergizes with the ATGL inhibitor Atglistatin (HY-15859) to block lipolysis in vitro. Hi 76-0079 can be used for the study of lipid metabolism .
Rapaglutin E (RgE) is a glucose transporter (GLUT) inhibitor. Rapaglutin E exhibits dose-dependent inhibition of [ 3H]-2DG uptake in A549, Jurkat T, PANC10.05, and RBC, with IC50 values 8.9 nM, 3.1 nM, 35.5 nM, 74.2 nM. Rapaglutin E inhibits cell proliferation in A549, PANC10.05, HeLa, Jurkat T, and HEK293T cells .
Anticancer agent 258 is an imidazo [1,2-B][1,2,4] triazol derivative. Anticancer agent 258 regulates the activity of nuclear receptors. Anticancer agent 258 has an EC50 of 63 nM against Nurr in N2A cells. Anticancer agent 258 has IC50 of 0.1 pM for Nur77 in HEK293 cells. Anticancer agent 258 can be used in the study of cancer, metabolic diseases and neurological disorders .
Blixeprodil (GM-1020) is the orally active antagonist for NMDA receptor with an affinity of Ki=3.25 µM in rat cortical tissue. Blixeprodil inhibits NR1/2A-NMDAR-mediated currents in HEK293 cell with IC50 of 1.192 µM. Blixeprodil exhibits antidepressant in rats models. Blixeprodil can cross blood-brain barrier .
(R)-V-0219 is an enantiomer of V-0219 (HY-143312). V-0219 is an orally active and positive allosteric modulator (PAM) of the GLP Receptor-1 (GLP-1R). (R)-V-0219 activates calcium fluxes in HEKcells stably expressing hGLP-1R .
HIF-1α-IN-4 is a HIF-1α inhibitor with an IC50 value of 24 nM (in HEK293T cell). HIF-1α-IN-4 downregulates VEGF and PDK1 mRNA expressions under hypoxia. HIF-1α-IN-4 can be used in the research of cancer .
DETQ is a selective, allosteric and orally active dopamine D1 receptor (Dopamine Receptor) potentiator. In HEK293 cells expressing the human D1 receptor, DETQ increases cAMP with an EC50 of 5.8 nM and a Kb of 26 nM. DETQ shows ~30-fold less potent at rat and mouse D1 receptors and is inactive at the human D5 receptor .
gamma-secretase modulator 6 (Example 50) is a gamma-secretase modulator. gamma-secretase modulator 6 inhibits Aβ42 secretion in HEKcell line stably expressing APP (Aβ amyloid precursor protein) (pIC50: 8.1). gamma-secretase modulator 6 can be used for research of Alzheimer's disease .
LN6023 (hydrochloride) (Compound 27) is a CXCR7 agonist. LN6023 (hydrochloride) induces the recruitment of β-arrestin in HEK293T cells expressing human CXCR7 (EC50 = 3.5 µM). LN6023 (hydrochloride) reduces the surface level of P-selectin in isolated and washed human platelets. LN6023 (hydrochloride) can be used to study platelet-mediated thrombosis .
PROTAC hCAII degrader-1 is a potent PROTAC human carbonic anhydrase II (hCAII) degrader with an DC50 of 0.5 nM in HEK293 cells. PROTAC hCAII degrader-1 recruits cereblon (CRBN) E3 ubiquitin ligase to form a ternary complex. PROTAC hCAII degrader-1 enables ubiquitination and subsequent proteasomal degradation of hCAII .
PF-915275 is a potent, selective and orally active human 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) inhibitor with a Ki of 2.3 nM and an EC50 of 15 nM (in HEK293 cells). The dose-dependent effect of PF-915275 on conversion of cortisone to cortisol in primary human and monkey hepatocytes, with an EC50 of 20 and 100 nM, respectively .
AMZ30 is selective protein phosphatase methylesterase-1(PME-1) inhibitor with IC50s of 600 nM and 3.5 µM in human cell lysates and in HEK 293T cells, respectively. AMZ30 shows >100-fold selectivity relative to other serine hydrolases. AMZ30 reduces the demethylated form of PP2A in living cells. AMZ30 attenuates muscle cell differentiation. AMZ30 increases the resistance of U87MG and U251MG glioblastoma cells to t-BHP-induced oxidative stress. AMZ30can be used for the study of glioblastoma .
STAT3-IN-17 is a moderate STAT3 inhibitor (IC50=0.7 μM; HEK-Blue IL-6), with antiproliferative activity in HeLa cells. STAT3-IN-17 has good pharmacokinetic characteristics. STAT3-IN-17 also inhibits pyruvate-ferredoxin oxidoreductase (PFOR), and inhibits Helicobacter pylori .
MePT-S-N-Pme is an inhibitor of SARS-CoV-2 RdRp activity. MePT-S-N-Pme demonstrates a significant reduced reporter activity with an IC50 of 7 μM in HEK 293 cells. MePT-S-N-Pme has a slight inhibitory effect on nucleotidyltransferase activity. MePT-S-N-Pme significantly inhibits SARS-CoV-2 replication in vitro .
Fenoprofen (LILLY-53858) Calcium is a nonsteroidal anti-inflammatory agent (NSAID) and inhibits cyclooxygenase (COX). Fenoprofen Calcium is a melanocortin receptors (MCRs) positive allosteric modulator (PAM). Fenoprofen Calcium also increases ERK1/2 activation in HEK293T cells. Fenoprofen Calcium has anti-arthritic activities and can be used for the study of rheumatoid arthritis and osteoarthritis .
KN-62 is a selective and reversible inhibitor of calmodulin-dependent protein kinase II (CaMK-II) with a Ki of 0.9 μM for rat brain CaMK-II. KN-62 directly binds to the calmodulin binding site of CaMK-II. KN-62 displays noncompetitive antagonism at P2X7 receptors in HEK293 cells, with an IC50 value of approximately 15 nM.
PU02, a derivative of 6-MP (HY-13677), is a negative allosteric modulator (NAM) of 5-HT3 receptor, with IC50 values of 0.36 and 0.73 μM in HEK293 cells transfected with human 5-HT3A and 5-HT3AB receptors respectively .
Fenoprofen (LILLY-53858) Calcium hydrate is a nonsteroidal anti-inflammatory agent (NSAID) and inhibits cyclooxygenase (COX). Fenoprofen Calcium hydrate is a melanocortin receptors (MCRs) positive allosteric modulator (PAM). Fenoprofen Calcium hydrate also increases ERK1/2 activation in HEK293T cells. Fenoprofen Calcium hydrate has anti-arthritic activities and can be used for the study of rheumatoid arthritis and osteoarthritis .
2-Methoxyestradiol (2-ME2), an orally active endogenous metabolite of 17β-estradiol (E2), is an apoptosis inducer and an angiogenesis inhibitor with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules. 2-Methoxyestradio, also a potent superoxide dismutase (SOD) inhibitor and a ROS-generating agent, induces autophagy in the transformed cell line HEK293 and the cancer cell lines U87 and HeLa .
PHTPP-1304 is a PHTPP-based autophagy targeting chimera (AUTOTAC). PHTPP-1304 induces the degradation of estrogen receptor ERβ through the autophagy pathway, rather than ubiquitination (DC50 ≈ 2 nM, in HEK293T cells; < 100 nM in ACHN renal carcinoma and MCF-7 breast cancer cells). PHTPP-1304 can induce the self-oligomerization of p62. PHTPP-1304 can be used to study various cancers mediated by ERβ .
YSY01A is a proteasome inhibitor that can suppress cancer cell survival by inducing apoptosis (Apoptosis). Its IC50 values are 51.0 nM for HEK293T, 9.2 nM for A549, 5.2 nM for MCF-7, 8.9 nM for MGC-803, and 35.4 nM for PC-3M cells. Additionally, YSY01A eliminates constitutive STAT3 signaling by downregulating gp130 and JAK2 in human A549 lung cancer cells. YSY01A holds promise for research in the field of cancer therapy .
PKG1α activator 3 is a PKG1α activator (EC50 basal/partial=13/0.52 μM). PKG1α activator 3 shows anti-proliferative effects to smooth muscle cell, and can be used in cardiovascular disease research .
DSO-5a is a potent, selective, orally active BB3 agonist. DSO-5a is a representative DMAKO-00 derivative compound. DSO-5a upregulates ppar-γ activity through BB3 and activates ERK1/2 phosphorylation. DSO-5a can be used in diabetes-related research .
XY-52 (Compound 32) is a Stimulation-2 (ST2) inhibitor, with an IC50 value of 5.68 μM in AlphaLISA assay, and 4.59 μM in HEK-Blue assay. XY-52 increases proinflammatory T-cell proliferation. XY-52 reduces the plasma sST2 and IFNγ biomarkers in the graft versus host disease (GVHD) mice model .
NPS-2143 hydrochloride (SB-262470A hydrochloride), an orally active calcilytic agent, is a selective and potent calcium ion-sensing receptor (CaSR) antagonist. NPS-2143 hydrochloride (SB-262470A hydrochloride) blocks increases in cytoplasmic Ca 2+ concentrations (IC50=43 nM) elicited by activating the Ca 2+ receptor in HEK 293 cells expressing the human Ca 2+ receptor .
(S)-CE-123 is a potent, selective, and novel atypical dopamine transporter (DAT) inhibitor with an EC50 of 2.76 μM in uptake inhibition assays conducted in HEK293 cells stably expressing human isoforms of DAT. (S)-CE-123, a Modafinil analogue, is able to penetrate the blood–brain barrier. (S)-CE-123 improves cognitive and motivational processes in experimental animals .
NPS-2143 (SB-262470A), an orally active calcilytic agent, is a selective and potent calcium ion-sensing receptor (CaSR) antagonist. NPS-2143 (SB-262470A) blocks increases in cytoplasmic Ca 2+ concentrations (IC50=43 nM) elicited by activating the Ca 2+ receptor in HEK 293 cells expressing the human Ca 2+ receptor .
Rapamycin- 13C,d3 (Sirolimus- 13C,d3) is the 13C and deuterium labeled Rapamycin (HY-10219) . Rapamycin is a potent and specific mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1. Rapamycin is an autophagy activator, an immunosuppressant .
OAT1/3-IN-2 (compound 8) is a dual inhibitor of OAT1 and OAT3. OAT1/3-IN-2 can reverse the toxicity of Cys-Hg on HEK-OAT1 cells (10 μM) and has a potential protective effect on the kidneys. OAT1/3-IN-2 can be used to study mercury-induced kidney damage .
K-(D-1-Nal)-FwLL-NH2 TFA is a high affinity and potent ghrelin receptor inverse agonist (Ki values are 4.9 and 31 nM in COS7 and HEK293T cells, respectively). K-(D-1-Nal)-FwLL-NH2 blocks ghrelin receptor-mediated Gq- and G13-dependent signaling pathways.
OAT1/3-IN-1 (compound 7) is a dual inhibitor of OAT1 and OAT3. OAT1/3-IN-1 can reverse the toxicity of Cys-Hg on HEK-OAT1 cells (10 μM) and has a potential protective effect on the kidneys. OAT1/3-IN-1 can be used to study mercury-induced kidney damage .
CK2-IN-15 (Compound Biv5) is a selective and potent bivalent protein kinase CK2 inhibitor with an IC50 value of 51 pM. CK2-IN-15 significantly reduces the replication of SARS-CoV-2 in HEK-ACE2-TMPRSS2 and Vero cells, and also reduces viral replication in an ex vivo model of human nasal epithelial cells. CK2-IN-15 is promising for research of β-coronavirus infection-related diseases .
SMU-C409 is a TLR1/2 agonist with an EC50 of 65 nM in HEK-Blue hTLR2 Cells. SMU-C409 activates the TLR1/2–MyD88–NF-κB pathway, inducing TNF-α/IL-1β secretion and robust immune cell activation for antitumor immunomodulation. SMU-C409 shows low toxicity in virto. SMU-C409 can be used for cancer immunotherapy research .
(R,R)-Birelentinib ((R,R)-DZD8586) (Compound 14) is a potent BTK inhibitor with IC50 values for BTK WT and BTK C481S of 0.7 and 0.86 nM, respectively. (R,R)-Birelentinib inhibits the self-phosphorylation of BTK and its IC50 is 24.3 nM. (R,R)-Birelentinib exhibits significant anti-proliferative activity against wild-type and C481S mutant HEK293 cells. (R,R)-Birelentinib can be used for the study of drug-resistant B-cell malignancies .
AS1269574 is a potent, orally available GPR119 agonist, with an EC50 of 2.5 μM in HEK293 cells expressing human GPR119. AS1269574 activates TRPA1 cation channels to stimulate glucagon-like peptide-1 (GLP-1) secretion. AS1269574 specifically induces glucose-dependent insulin secretion from pancreatic β-cells only under high-glucose conditions. AS1269574 has the potential for the research of type 2 diabetes .
ADX68692 is an orally active negative allosteric modulators of follicle-stimulating hormone receptor with a log IC50 of -5.71. ADX68692 can inhibit hCG-induced cAMP production and s ß-arrestin 2 recruitment in HEK293 cells. ADX68692 exhibits a partial effect in both mLTC-1 and primary rat Leydig cells. ADX68692 inhibits FSHR-promoted cAMP, progesterone and estradiol production. ADX68692 can reduce the number of oocytes recovered from the ampullae .
URAT1-IN-14 is a potent and orally active Urate transporter 1 (URAT1) inhibitor. URAT1-IN-14 inhibits the human URAT1 in HEK293 cells with an IC50 of 0.72 μM. URAT1-IN-14 exhibits low cytotoxic in Hep-G2 cells. URAT1-IN-14 shows urate-lowering effect in hyperuricemia mouse models. URAT1-IN-14 can be used for the study of hyperuricemia and gout .
Ro 67-7476 is a potent positive allosteric modulator of mGluR1 and potentiates glutamate-induced calcium release in HEK293 cells expressing rat mGluR1a with an EC50 of 60.1 nM . Ro 67-7476 is a potent P-ERK1/2 agonist and activates ERK1/2 phosphorylation in the absence of exogenously added glutamate (EC50=163.3 nM) .
2'-Deoxyadenosine-5'-O-diphosphoribose sodium is a TRPM2 agonist. 2'-Deoxyadenosine-5'-O-diphosphoribose sodium enhances calcium-induced currents in inside-out patch-clamp experiments using HEK293 cells expressing human TRPM2. 2'-Deoxyadenosine-5'-O-diphosphoribose sodium is a substrate for Nucleoside Triphosphate Diphosphatase 9 (NUDT9) .
AZD6538 is a potent, selective and brain penetrant mGluR5 negative allosteric modulator. AZD6538 inhibits DHPG (HY-12598A)-stimulated intracellular Ca2+ release in HEKcells expressing rat or human mGluR5, with IC50 values of 3.2 and 13.4 nM for rat mGluR5 and human mGluR5, respectively. AZD6538 can be used for the research of neuropathic pain .
Galegine hemisulfate, a guanidine derivative, contributes to weight loss in mice. Galegine hemisulfate activates AMPK in 3T3-L1 adipocytes and L6 myotubes, as well as in the H4IIE rat hepatoma and HEK293 human kidney cell lines. Galegine hemisulfate has antibacterial activity, with minimum inhibitory concentration of 4 mg/L against Staphylococcus aureus strains .
BAPTA-AM (Standard) is the analytical standard of BAPTA-AM. This product is intended for research and analytical applications. BAPTA-AM is a well-known membrane permeable Ca2+ chelator. BAPTA-AM inhibits hERG channels, hKv1.3 and hKv1.5 channels in HEK 293 cells with IC50s of 1.3 μM, 1.45 μM and 1.23 μM, respectively .
Simvastatin acid (ammonium) (Standard) is the analytical standard of Simvastatin acid (ammonium). This product is intended for research and analytical applications. Simvastatin acid (Tenivastatin) ammonium is a potent HMG-CoA reductase (HMGCR) inhibitor. Simvastatin acid ammonium reduces Indoxyl sulfate-mediated reactive oxygen species (ROS) production in human cardiomyocytes. Simvastatin acid ammonium can also modulates OATP3A1 expression in cardiomyocytes and HEK293 cells transfected with the OATP3A1 gene .
BL-1005 (BS2463), thiophen-2-yl pyrimidine (TTP), is a potent paralytic of Schistosoma mansoni with an EC50 of 37 nM. BL-1005 shows low cytotoxicity for HEK293, HeLa and HepG2 cell with CC50 >20 μM. BL-1005 can induce paralysis in both adult and juvenile S. mansoni. BL-1005 can be used for the research of infection .
Perenostobart (SRF617) is a human IgG4 antibody with inhibitory activity against CD39 ATPase. Perenostobart inhibits CD39-mediated hydrolysis of extracellular ATP to AMP, with IC50 values of 1.9 nM (HEK293 OE cells), 0.7 nM (MOLP-8 cells), and 1.2 nM (RBC-lysed whole blood). Perenostobart enhances CD4 + T-cell proliferation, promotes dendritic cell maturation, and boosts inflammasome activation in macrophages in the presence of ATP. Perenostobart demonstrates significant single-agent anti-tumor efficacy in MOLP-8 and H520 xenograft models. Perenostobart can be used for the study of cancer .
BI-1622 is an orally active, potent and highly selective HER2 (ERBB2) inhibitor, with an IC50 of 7 nM. BI-1622 shows greater than 25-fold selectivity over EGFR. BI-1622 shows high antitumor efficacy in vivo in xenograft mouse tumor models with engineered H2170 and PC9 cells and had a favorable agent metabolism and pharmacokinetics profile .
Simvastatin acid-d6 (Tenivastatin-d6) is deuterium labeled Simvastatin acid. Simvastatin acid (Tenivastatin), a hydrolysate of Simvastatin (HY-17502), is a HMG-CoA reductase (HMGCR) inhibitor. Simvastatin acid reduces Indoxyl sulfate-mediated reactive oxygen species (ROS) production in human cardiomyocytes. Simvastatin acid can also modulates OATP3A1 expression in cardiomyocytes and HEK293 cells transfected with the OATP3A1 gene .
Simvastatin acid-d6 (ammonium)mis the deuterium labeled Simvastatin acid ammonium. Simvastatin ammonium is an active metabolite of simvastatin lactone mediated by CYP3A4/5 in the intestinal wall and liver (pKa=5.5). Simvastatin ammonium reduces indoxyl sulfate-mediated reactive oxygen species and modulates OATP3A1 expression in cardiomyocytes and HEK293 cells transfected with the OATP3A1 gene .
VU0546110 is a selective inhibitor of the sperm-specific potassium channel SLO3, with IC50s of 1.287 μM (SLO3) and 59.80 μM (SLO1) in HEK293 cells, respectively. VU0546110 blocks heterologous SLO3 currents and endogenous K + currents in human sperm. VU0546110 halts sperm hyperpolarization, induced acrosome reaction, and hyper-activated motility. VU0546110 has contraceptive potential .
Simvastatin acid-d9 ammonium is deuterated labeled Simvastatin acid ammonium (HY-119695A). Simvastatin acid (Tenivastatin) ammonium is a potent HMG-CoA reductase (HMGCR) inhibitor. Simvastatin acid ammonium reduces Indoxyl sulfate-mediated reactive oxygen species (ROS) production in human cardiomyocytes. Simvastatin acid ammonium can also modulates OATP3A1 expression in cardiomyocytes and HEK293 cells transfected with the OATP3A1 gene .
BayCysLT2, an isophthalic acid derivative, is a selective and potent cysteinyl leukotriene 2 (CysLT2) receptor antagonist with an IC50 value of 53 nM. BayCysLT2 inhibits calcium mobilization induced by leukotriene D4 in HEK293 cells expressing human CysLT2 receptors. BayCysLT2 reverses LTC4-induced increases in coronary artery perfusion pressure and decreases in contractility in isolated perfused guinea pig hearts .
HUP-55 is a prolyl endopeptidase inhibitor (IC50 = 5 nM). HUP-55 reduces the dimerization of α-synuclein in Neuro2a cells and induces autophagy (Autophagy) in HEK293 cells. It also decreases the increase in reactive oxygen species (ROS) production induced by hydrogen peroxide in SH-SY5Y cells at a concentration of 10 μM. In a mouse Parkinson’s disease model, HUP-55 (10 mg/kg) improves motor function (reduces the use frequency of the impaired paw) and decreases the levels of harmful oligomers of α-synuclein in the striatum caused by overexpression of α-synuclein .
Apelin-36(rat, mouse) TFA is an endogenous orphan G protein-coupled receptor APJ agonist. Apelin-36(rat, mouse) TFA binds to APJ receptors with an IC50 of 5.4 nM, and potently inhibits cAMP production with an EC50 of 0.52 nM. Apelin-36(rat, mouse) TFA blocks entry of some HIV-1 and HIV-2 strains into NP-2/CD4 cells expressing APJ .
AM73 is a PGC-1α1 stabilizer. AM73 increases the expression levels of Ucp1 and Cidea in brown adipocytes, and enhances basal mitochondrial respiration and uncoupled respiration. AM73 regulates hypoxia, brown adipocyte differentiation, carbohydrate metabolism and insulin signaling pathways in brown adipocytes. AM73 alters the thermogenic process of white adipocytes. AM73 is applicable to the research of obesity and related metabolic disorders .
TLR7 agonist 8 is a TLR7 agonist with an EC50 of 0.12 nM for TLR7 and an EC50 of 0.76 nM for IL-6 induction. TLR7 agonist 8 can be used for research on diseases such as fibrosis, inflammatory diseases, cancer, or pathogen infections .
OS-3-106 is a potent, and selective dopamine D3 receptor (D3R) agonist. OS-3-106 binds with high affinity (Ki = 0.2 nM) at the D3R. OS-3-106 can be used for psychoactivator addiction research .
BDM88951 (Compound 4 d) is a selective ERAP2 inhibitor with an IC50 of 19 nM. BDM88951 significantly inhibits antigen presentation. BDM88951 can be used for autoimmune diseases and cancers research .
Melicopine is an alkaloid found in Z. simulans with antimalarial and anticancer activities. It exhibits inhibitory activity against chloroquine-sensitive 3D7 and chloroquine-resistant Dd2 strains of P. falciparum, with IC50 values of 29.7 and 33.7 µg/mL, respectively. Melicopine is cytotoxic to prostate cancer cells PC-3M and LNCaP (IC50 values of 47.9 and 37.8 µg/mL), but has no effect on non-cancerous HEK293 cells (IC50 greater than 100 µg/mL). Melicopine holds promise for research in anticancer and anti-infection fields .
SNC80 (NIH 10815) is a potent, highly selective and non-peptide δ-opioid receptor agonist with a Ki of 1.78 nM and an IC50 of 2.73 nM. SNC80 also selectively activates μ-δ heteromer in HEK293 cells with an EC50 of 52.8 nM. SNC80 shows antinociceptive, antihyperalgesic and antidepressant‐like effects. SNC80 has the potential for multiple headache disorders treatment .
Flindokalner (BMS-204352) is a potassium channel modulator. Flindokalner is a positive modulator of all neuronal Kv7 channel subtypes expressed in HEK293 cells. Flindokalner is also a large conductance calcium-activated K channel (BKca) positive modulator. Flindokalner shows a negative modulatory activity at Kv7.1 channels (Ki=3.7 μM), and acts as a negative modulator of GABAA receptors. Flindokalner shows anxiolytic efficacy in vivo .
Fenoprofen (Standard) (LILLY-53858 (Standard)) is the analytical standard of Fenoprofen (HY-B1456A). This product is intended for research and analytical applications. Fenoprofenc is a nonsteroidal anti-inflammatory agent (NSAID) and inhibits cyclooxygenase (COX). Fenoprofen is a melanocortin receptors (MCRs) positive allosteric modulator (PAM). Fenoprofen also increases ERK1/2 activation in HEK293T cells. Fenoprofen has anti-arthritic activities and can be used for the study of rheumatoid arthritis and osteoarthritis.
Enpatoran (M5049) hydrochloride is a potent, orally active and dual TLR7/8 inhibitor with IC50s of 11.1 nM and 24.1 nM in HEK293 cells, respectively. Enpatoran hydrochloride is inactive against TLR3, TLR4 and TLR9. Enpatoran hydrochloride can block molecule synthetic ligands and natural endogenous RNA ligands. Enpatoran hydrochloride exhibits excellent pharmacokinetic properties in vivo. Enpatoran hydrochloride can be used for both innate and adaptive autoimmunity blocking research .
(1R,2R)-Calhex 231 hydrochloride is the isomer of Calhex 231 hydrochloride (HY-103320A), and can be used as an experimental control. Calhex 231 hydrochloride is a CaSR inhibitor via negative allosteric modulation. Calhex 231 hydrochloride blocks Ca 2+-induced accumulation of [ 3H]inositol phosphate with an IC50 of 0.39 μM in HEK293 cells. Calhex 231 hydrochloride has the potential for diabetic cardiomyopathy (DCM) treatment .
RO5323441 (TB-403) is a human IgG1 monoclonal antibody (mAb) targeting PlGF. RO5323441 inhibits the binding of human PlGF-1 or PlGF-2 to VEGFR-1 (IC50 values are 0.1 and 0.2 nM, respectively). RO5323441 blocks PlGF-induced VEGFR-1 phosphorylation in Flt-1-transfected HEK293 cells. RO5323441 has antitumor activity .
HIF-1α-IN-5 is a HIF-1α inhibitor with an IC50 value of 24 nM (in HEK293T cell). HIF-1α-IN-5 also inhibits MAO-A activity. HIF-1α-IN-5 downregulates VEGF and PDK1 mRNA expressions under hypoxia. HIF-1α-IN-5 can be used in the research of cancer .
Alniditan (Alnitidan) dihydrochloride is a potent 5-HT1B and 5-HT1D receptors agonist, with IC50s of 1.7 nM and 1.3 nM for h5-HT1B and h5-HT1D receptors in HEK293 cells, respectively. Alniditan dihydrochloride has migraine-preventive effects .
Alniditan (Alnitidan) is a potent 5-HT1B and 5-HT1D receptors agonist, with IC50s of 1.7 nM and 1.3 nM for h5-HT1B and h5-HT1D receptors in HEK293 cells, respectively. Alniditan has migraine-preventive effects .
Dooku1 is a reversibly Yoda1 antagonist with IC50 value of 1.3 μM and 1.5 μM for 2 μM Yoda1-induced Ca 2+ entry HEK 293 cells and HUVECs, respectively. Dooku1 can disrupt Yoda1-induced Piezo1 channel activity and inhibit Yoda1-induced relaxation of aorta. Dooku1 can be used for vascular physiology and disease research .
Enpatoran (M5049) is a potent, orally active and dual TLR7/8 inhibitor with IC50s of 11.1 nM and 24.1 nM in HEK293 cells, respectively. Enpatoran is inactive against TLR3, TLR4 and TLR9. Enpatoran can block molecule synthetic ligands and natural endogenous RNA ligands. Enpatoran exhibits excellent pharmacokinetic properties in vivo. Enpatoran can be used for both innate and adaptive autoimmunity blocking research .
Tolazamide (U-17835) is an orally active sulfonylurea agent that inhibits sulfonylurea receptor 1 (SUR1) linked to the inwardly rectifying potassium channel (IC50 = 4.2 µM in HEK293 cells transfected with the human receptor). Tolazamide has anti-diabetic properties. Tolazamide can lower blood glucose in sulfonylurea class. Tolazamide decreases insulin dose while continuing to maintain adequate metabolic control. Tolazamide is able to improve or normalize hyperglycemia and HbA .
Ki16425 (Debio 0719) is a subtype-selective, competitive antagonist of the EDG-family receptors, LPA1 and LPA3 with Kis of 0.34 μM and 0.93 μM, respectively. Ki16425 (Debio 0719) reduces the LPA-induced activation of p42/p44 MAPK . Ki16425 can also inhibit LPA-induced dephosphorylation of Yes-associated protein (YAP)/TAZ in HEK293A cells .
Rapamycin- 13C,d3-1 (Sirolimus- 13C,d3-1) is the deuterium labeled and 13C-labeled Rapamycin (HY-10219). Rapamycin (Sirolimus; AY 22989) is a potent and specific mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1 . Rapamycin is an autophagy activator, an immunosuppressant .
DB008 is potent and selective PARP16 inhibitor with an IC50 value of 0.27 μM, containing an acrylamide electrophilic reagent. DB008 is membrane-permeable and marks PARP16 selectively . DB008 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
ADAMTS-5-IN-4 (Compound 4b) is a selective ADAMTS5 inhibitor with an IC₅₀ of 9.4 μM. ADAMTS-5-IN-4 significantly inhibits the degradation of Aggrecan in the implants of the osteoarthritis model. ADAMTS-5-IN-4 effectively inhibits the pseudopod elongation and directional migration of ovarian cancer cells. ADAMTS-5-IN-4 shows significant cytotoxicity to HEK293T cells, human chondrocytes, and porcine chondrocyte implants. ADAMTS-5-IN-4 can be used for the study of osteoarthritis and ovarian cancer .
2-Methoxyestradiol-d5 is the deuterium labeled 2-Methoxyestradiol. 2-Methoxyestradiol (2-ME2), an orally active endogenous metabolite of 17β-estradiol (E2), is an apoptosis inducer and an angiogenesis inhibitor with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules. 2-Methoxyestradio, also a potent superoxide dismutase (SOD) inhibitor and a ROS-generating agent, induces autophagy in the transformed cell line HEK293 and the cancer cell lines U87 and HeLa .
4″-C18 EGCG is a potent inhibitor of α-amylase and α-glucosidase with IC50 values of 3.74 and 0.81 μM, respectively. 4″-C18 EGCG inhibits carbohydrate hydrolases, reduces oxidative stress and inflammation, and exhibits antidiabetic activity. 4″-C18 EGCG also downregulates proinflammatory cytokines and is cytotoxic to primary human peripheral blood mononuclear cells (PBMCs), non-cancer cell lines 3T3-L1, and HEK 293 at 50 μM .
Pyr10 is a pyrazole derivative and a selective TRP cation 3 (TRPC3) inhibitor. Pyr10 inhibits Ca 2+ influx in carbachol-stimulated TRPC3-transfected HEK293 cells with an IC50 of 0.72 μM (IC50 of 13.08 μM for store operated Ca 2+ entry in BRL-2H3 cells). Pyr10 has the ability to distinguish between receptor-operated TRPC3 and native stromal interaction molecule 1 (STIM1)/Orai1 channels .
Ketodarolutamide (ORM-15341) is a potent, high-affinity nonsteroidal competitive full antagonist of androgen receptor (AR). Ketodarolutamide displays a Ki value of 8 nM for rat wild-type AR and an IC50 value of 38 nM in AR-HEK293 cells . Ketodarolutamide inhibits testosterone-induced nuclear translocation of the AR and antagonizes both overexpressed and mutant ARs . Ketodarolutamide specifically suppresses the proliferation of AR-dependent prostate cancer cells and exhibits antitumor activity in models of castration-resistant prostate cancer (CRPC) . Ketodarolutamide is suitable for the mechanistic and therapeutic research of prostate cancer .
2-Methoxyestradiol- 13C6 is the 13C-labeled 2-Methoxyestradiol. 2-Methoxyestradiol (2-ME2), an orally active endogenous metabolite of 17β-estradiol (E2), is an apoptosis inducer and an angiogenesis inhibitor with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules. 2-Methoxyestradio, also a potent superoxide dismutase (SOD) inhibitor and a ROS-generating agent, induces autophagy in the transformed cell line HEK293 and the cancer cell lines U87 and HeLa .
Ctrl-CPF1 is a control dye for Copper Phosphorus Fluor 1 (CPF1), which exhibits no metal-dependent fluorescence response and shows no reactivity toward Cu + .
NMDAR antagonist 5 (Compound A17) is a multi-target antagonist against NMDAR and monoamine transporters (SERT、DAT and NET). NMDAR antagonist 5 shows good NMDAR antagonistic potency (IC50 = 0.3 μM) and monoamine transporter activities (SERT IC50 = 1.1 μM、DAT IC50 = 0.7 μM、NET IC50 = 2.7 μM). NMDAR antagonist 5 is highly safe and has low toxicity (hepatotoxicity and nephrotoxicity (IC50 > 100 μM); cardiotoxicity (IC50 = 24.5 μM)). NMDAR antagonist 5 has antidepressant effects and can be used in the study of depression .
THX6 is an hClpP activator with an EC50 of 1.18 μM. THX6 improves off-target profile with no affinity for hD2R and only weak affinity for hD3R (Ki = 51.1 µM) in HEK293 cells. THX6 shows good cytotoxicity in ONC201-resistant cells with an IC50 of 0.13 μM. THX6 changes the levels of fatty acids (PUFAs, MUFAs, and SFAs) in DIPG cells. THX6 decreases the level of proteins involved in oxidative phosphorylation, biogenesis, and mitophagy proteins, thereby resulting in a global collapse of mitochondrial integrity and function. THX6 can be used for diffuse intrinsic pontine glioma research .
(S)-V-0219 is an enantiomer of V-0219 (HY-143312). V-0219 is an orally active and positive allosteric modulator (PAM) of the GLP Receptor-1 (GLP-1R). (S)-V-0219 activates calcium fluxes in HEKcells stably expressing hGLP-1R. (S)-V-0219 is orally active and ameliorates high glucose levels in mice and inhibits feeding behavior in fasted mice .
Fenoprofen (LILLY-53858 (Standard)) (Standard) Calcium hydrate is the analytical standard of Fenoprofen Calcium hydrate (HY-B0288B). This product is intended for research and analytical applications. Fenoprofen is a nonsteroidal anti-inflammatory agent (NSAID) and inhibits cyclooxygenase (COX). Fenoprofen is a melanocortin receptors (MCRs) positive allosteric modulator (PAM). Fenoprofen also increases ERK1/2 activation in HEK293T cells. Fenoprofen has anti-arthritic activities and can be used for the study of rheumatoid arthritis and osteoarthritis.
PF-915275 (Standard) is the analytical standard of PF-915275. This product is intended for research and analytical applications. PF-915275 is a potent, selective and orally active human 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) inhibitor with a Ki of 2.3 nM and an EC50 of 15 nM (in HEK293 cells). The dose-dependent effect of PF-915275 on conversion of cortisone to cortisol in primary human and monkey hepatocytes, with an EC50 of 20 and 100 nM, respectively .
Galegine hydrochloride, a guanidine derivative, contributes to weight loss in mice. Guanidine hydrochloride is the compound derived from G. officinalis, which gave rise to the biguanides, metformin and phenformin. Galegine hydrochloride activates AMPK in 3T3-L1 adipocytes and L6 myotubes, as well as in the H4IIE rat hepatoma and HEK293 human kidney cell lines. Galegine hydrochloride has antibacterial activity, with minimum inhibitory concentration of 4 mg/L against Staphylococcus aureus strains .
(S)-V-0219 hydrochloride is an enantiomer of V-0219 (HY-143312). V-0219 is an orally active and positive allosteric modulator (PAM) of the GLP Receptor-1 (GLP-1R). (S)-V-0219 hydrochloride activates calcium fluxes in HEKcells stably expressing hGLP-1R. (S)-V-0219 hydrochloride is orally active and ameliorates high glucose levels in mice and inhibits feeding behavior in fasted mice .
TLR7/8 agonist 6 is a TLR7/8 agonist with EC50s of 0.18 μM and 5.34 μM in TLR7 or TLR8 HEK-SEAP reporter cells, respectively. TLR7/8 agonist 6 potently stimulates production of TNFα, IFNγ, and IL-1β. TLR7/8 agonist 6 can be used for research on cancer and infectious diseases .
Tetromycin B is a cysteine protease inhibitor with Ki values of 0.62, 1.42, 32.5, and 1.59 μM for rhodesain, falcipain-2, cathepsin L, and cathepsin B, respectively. It inhibits the growth of T. brucei in vitro (IC50=30.87 μM). Tetromycin B is also cytotoxic to HEK293T kidney cells and J774.1 macrophages (IC50s=71.77 and 20.2 μM, respectively).
6,8-Diprenylnaringenin (Lonchocarpol A; Senegalensin), a hop prenylflavonoid, is a inhibitor of breast cancer resistance protein (BCRP/ABCG2). 6,8-Diprenylnaringenin inhibits ABCG2-mediated efflux of Mitoxantrone, and 3H-Methotrexate transport (IC50=0.41 μM) in HEK293 cells. 6,8-Diprenylnaringenin exhibits some estrogenicity, but its potency is less than 1% of that of 8-Prenylnaringenin .
(E/Z)-CLH304a (GABAB receptor antagonist 1) is a mixture of (E)-CLH304a and (Z)-CLH304a. (E)-CLH304a (CLH304a; HY-129636) is a specific and noncompetitive GABAB receptor negative allosteric modulator (NAM). CLH304a inhibits Baclofen (HY-B0007)-induced ERK1/2 phosphorylation in HEK293 cells overexpressing GABAB receptors .
SIK1-IN-1 (Compound 27) is a selective Salt-inducible kinase 1 (SIK1) inhibitor with an IC50 of 0.7 nM for SIK1 over SIK2 and SIK3. SIK1-IN-1 has no cytotoxicity against HEK293 cells and PBMCs (maximum concentration of 30 μM). SIK1-IN-1 also has potent inhibitory activities for 392 kinases, in particular tyrosine kinases, such as FGR, HCK and LYN) .
LY-466195 is a selective and competitive GLUK5 receptor antagonist. LY-466195 antagonizes Kainate-induced currents with an IC50 value of 0.045 μM in rat dorsal root ganglion neurons. In HEK293 cells transfected with GLUK5, GLUK2/GLUK5, or GLUK5/GLUK66 receptors, LY466195 produces IC50 values of 0.08 μM, 0.34 μM, and 0.07 μM, respectively .
WIZ degrader 2 (Compound 142) is a degrader for widely interspaced zinc finger motifs with an AC50 of 0.011 μM. WIZ degrader 2 induces the expression of fetal hemoglobin (HbF) with an EC50 of 0.038 μM. WIZ degrader 2 can be used in research about inherited blood disorders .
AX8819 is a selective dipeptidyl peptidase II (DPP II) inhibitor with an IC50 of 0.88 nM. AX8819 induces caspase-dependent apoptosis. AX8819 exhibits low non-specific toxicity toward proliferating T cells. AX8819 can be used for the research of B cell chronic lymphocytic leukemia .
C3N-Dbn-Trp2 is an inhibitor for ATP-binding cassette transporter ABCB1. C3N-Dbn-Trp2 inhibits the ABCB1-mediated Rhodamine 123 (HY-D0816) efflux in cellsHEK293T and HCT-15 with IC50 of 5.9 µM and 2.2 µM. C3N-Dbn-Trp2 inhibits the Doxorubicin (HY-15142A) efflux, enhances the cytotoxicity of Doxorubicin in ABCB1-expressing cells .
2-Methoxyestradiol (Standard) is the analytical standard of 2-Methoxyestradiol. This product is intended for research and analytical applications. 2-Methoxyestradiol (2-ME2), an orally active endogenous metabolite of 17β-estradiol (E2), is an apoptosis inducer and an angiogenesis inhibitor with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules. 2-Methoxyestradio, also a potent superoxide dismutase (SOD) inhibitor and a ROS-generating agent, induces autophagy in the transformed cell line HEK293 and the cancer cell lines U87 and HeLa .
AS1269574 (Standard) is the analytical standard of AS1269574 (HY-107535). This product is intended for research and analytical applications. AS1269574 is a potent, orally available GPR119 agonist, with an EC50 of 2.5 μM in HEK293 cells expressing human GPR119. AS1269574 activates TRPA1 cation channels to stimulate glucagon-like peptide-1 (GLP-1) secretion. AS1269574 specifically induces glucose-dependent insulin secretion from pancreatic β-cells only under high-glucose conditions. AS1269574 has the potential for the research of type 2 diabetes .
2-Methoxyestradiol- 13C,d3 is the 13C- and deuterium labeled 2-Methoxyestradiol. 2-Methoxyestradiol (2-ME2), an orally active endogenous metabolite of 17β-estradiol (E2), is an apoptosis inducer and an angiogenesis inhibitor with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules. 2-Methoxyestradio, also a potent superoxide dismutase (SOD) inhibitor and a ROS-generating agent, induces autophagy in the transformed cell line HEK293 and the cancer cell lines U87 and HeLa .
BAY 36-7620 is a potent and noncompetitive antagonist of mGlu1 Receptor (IC50=0.16 μM) with inverse agonist activity. BAY 36-7620 inhibits tumor growth and prolongs the survival of mice with tumors by inhibiting mGlu1 receptor. BAY 36-7620 suppresses AKT phosphorylation in A549 tumors. BAY 36-762 has neuroprotective effect in acute subdural hematoma rat model.BAY 36-7620 is used in non-small cell lung cancer and breast cancer research .
Hypidone hydrochloride (YL0919) is an orally active antidepressant agent with dual activity as a highly seletive 5-HT uptake blocker and an effective 5-HT1A receptor agonist (Ki=0.19 nM). Hypidone hydrochloride inhibits the uptake of [ 3H]-5-HT into rat cerebral cortical synaptosomes and HEK293 cells with IC50s of 1.78 nM and 1.93 nM, respectively. Hypidone hydrochloride shows remarkable antidepressant effects in animal models and has the poential for the investigation of depressive disorder .
PROTAC SARS-CoV-2 Mpro degrader-6 is a PROTACs degrader targeting the SARS-CoV-2 main protease (M pro). PROTAC SARS-CoV-2 Mpro degrader-6 effectively induces the degradation of M pro and increases K48-linked polyubiquitination of M pro in HEK293 cells. PROTAC SARS-CoV-2 Mpro degrader-6 can be used in studies related to coronavirus disease 2019 (COVID-19) .
Fenoprofen- 13C6 (LILLY-53858- 13C6) sodium hydrate is the 13C labeled Fenoprofen (HY-B1456A).Fenoprofen (LILLY-53858) is a nonsteroidal anti-inflammatory agent (NSAID) and inhibits cyclooxygenase (COX). Fenoprofen is a melanocortin receptors (MCRs) positive allosteric modulator (PAM). Fenoprofen also increases ERK1/2 activation in HEK293T cells. Fenoprofen has anti-arthritic activities and can be used for the study of rheumatoid arthritis and osteoarthritis .
Cyano-myracrylamide is an inhibitor of zinc finger DHHC domain-containing palmitoyltransferase 20 (zDHHC20) with an IC50 value of 1.35 µM. Cyano-myracrylamide also inhibits the S-Acylation of EGFR and CD36. Cyano-myracrylamide also inhibits S-acylation of Legionella E3 ligase GobX, MyD88, and Ras, which are substrates of zDHHC20, zDHHC9, and zDHHC6, respectively, in HEK293T cells expressing recombinant Legionella GobX, recombinant human MyD88, or endogenous Ras .
TLR7 agonist 18 (Compound 21a) is a selective Toll-like receptor 7 (TLR7) agonist with an EC50 of 7.8 μM. TLR7 agonist 18 is not cytotoxic to hTLR7 cotransfected HEK293 cell lines and can induce the secretion of several cytokines, including IL-1β, IL-12p70, IL-8, and TNF-α. TLR7 agonist 18 can be used in vaccine, asthma, allergy and anti-cancer research .
Flindokalner (Standard) is the analytical standard of Flindokalner. This product is intended for research and analytical applications. Flindokalner (BMS-204352) is a potassium channel modulator. Flindokalner is a positive modulator of all neuronal Kv7 channel subtypes expressed in HEK293 cells. Flindokalner is also a large conductance calcium-activated K channel (BKca) positive modulator. Flindokalner shows a negative modulatory activity at Kv7.1 channels (Ki=3.7 μM), and acts as a negative modulator of GABAA receptors. Flindokalner shows anxiolytic efficacy in vivo .
TNP-ATP is an antagonist of purinergic P2Y1, P2X3, and P2X2/3 receptors (IC50 = 6, 0.9, and 7 nM, respectively, in HEK293 cells expressing human receptors). TNP-ATP reduces acetate-induced calcium flux in 1321N1 cells expressing P2X3 and P2X2/3 receptors (IC50 = 100 and 62 nM, respectively). TNP-ATP dose-dependently attenuates acetate-induced abdominal contractions in a mouse visceral pain model (ED50 = 6.35 µmol/kg) [1][2].
Adenosine receptor antagonist 7 is an orally active triple A1/A2A/A2B adenosine receptor antagonist with Ki values of 1.5, 0.6 and 21 nM. Adenosine receptor antagonist 7 shows potent inhibitory activity (IC50 = 0.8 nM) of cAMP production in A2AR-HEK293 cells. Adenosine receptor antagonist 7 can enhance infiltration of effector T cells and increase the CD8+/Treg ratio companied with Avelumab (HY-108730). Adenosine receptor antagonist 7can be used for the research of cancer, such as colon cancer .
KOR agonist 6 is a KOR agonist (Ki = 0.25 pM). KOR agonist 6 shows agonistic activity at MOR and DOR in CHO cells and inhibits Forskolin (HY-15371)-stimulated cAMP accumulation. KOR agonist 6 stimulates KOR-mediated [ 35S]GTPγS binding and inhibits cAMP accumulation in KOR-expressing HEK293 cells with potent agonistic activity, while showing lower β-arrestin recruitment potency. KOR agonist 6 demonstrates anti-nociceptive efficacy in mice. KOR agonist 6 can be used for the study of analgesics with reduced central nervous system (CNS) side effects .
YM-202074 is a selective, allosteric metabotropic glutamate receptor type 1 (mGluR1) antagonist with high affinity. YM-202074 binds to the allosteric site of rat mGluR1 with a Ki of 4.8 nM. YM-202074 fumarate also inhibits mGluR1-mediated inositol phosphate production in rat cerebellar granule cells with an IC50 of 8.6 nM. YM-202074 has potent neuroprotective effects in transient MCA (tMCA) occlusion rat models .
YM-202074 fumarate is a selective, allosteric metabotropic glutamate receptor type 1 (mGluR1) antagonist with high affinity. YM-202074 fumarate binds to the allosteric site of rat mGluR1 with a Ki of 4.8 nM. YM-202074 fumarate also inhibits mGluR1-mediated inositol phosphate production in rat cerebellar granule cells with an IC50 of 8.6 nM. YM-202074 fumarate has potent neuroprotective effects in transient MCA (tMCA) occlusion rat models .
AM79 is a PGC-1α1 stabilizer. AM79 promotes the accumulation of endogenous PGC-1α1 protein, thereby activating its target genes. AM79 increases uncoupled mitochondrial respiration in brown adipocytes. AM79 induces the expression of Ucp1 and Cidea in brown adipocytes. AM79 can be used for the research of obesity and related metabolic disorders .
NAB-14 is a potent, selective, orally active and non-competitive GluN2C/2D antagonists with an IC50 of 580 nM for GluN1/GluN2D. NAB-14 shows >800-fold selective for recombinant GluN2C and GluN2D over GluN2A and GluN2B. NAB-14 can cross the blood-brain-barrier .
FIP22 is a potent and selective IRAK4 PROTAC degrader (HEK293T cells: DC50 = 3.2 nM; THP-1 cells: DC50 = 10.6 nM). FIP22 induces the ubiquitin-proteasome system by forming an IRAK4-FIP22-CRBN ternary complex (EC50 = 12.63 nM), thereby potently blocking IRAK4-mediated NF-κB and MAPK signaling pathways. FIP22 can be used for the study of atopic dermatitis (Pink: IRAK4 ligand (HY-175765); Blue: CRBN ligand (HY-W087383); Black: Linker (HY-46871)) .
Breceptin (B 9870) is an antagonist of the bradykinin B1/B2 receptor (B1/B2R). Breceptin exhibits an irreversible antagonist effect on B2R, inhibiting the vasodilation induced by Bradykinin (HY-P0206) in the rabbit carotid vein contraction experiment. B-9870 shows partial agonist properties in HEK 293 cells with high expression of B2R, and can activate ERK1/2 phosphorylation, calcium ion mobilization, arachidonic acid release, and receptor internalization. Breceptin can be used in research to inhibit breast cancer and non-small cell lung cancer .
Cetrelimab (JNJ 63723283; JNJ 3283) is a human IgG4κ mAb targeting PD-1. Cetrelimab binds PD-1 (Kd=1.72 nM, HEK293) to block the interaction of PD-1 with PD-L1 and PD-L2 (IC50s=111.7 ng/mL and 138.6 ng/mL, respectively). Cetrelimab stimulates peripheral T cells, increases IFN-γ, IL-2, TNF-α level and inhibits tumor growth in vivo .
Tolazamide (U-17835) (Standard) is the analytical standard of Tolazamide. This product is intended for research and analytical applications. Tolazamide is an orally active sulfonylurea agent that inhibits sulfonylurea receptor 1 (SUR1) linked to the inwardly rectifying potassium channel (IC50 = 4.2 µM in HEK293 cells transfected with the human receptor). Tolazamide has anti-diabetic properties. Tolazamide can lower blood glucose in sulfonylurea class. Tolazamide decreases insulin dose while continuing to maintain adequate metabolic control. Tolazamide is able to improve or normalize hyperglycemia and HbA .
BCFTP is a potent, orally active and selective human Mas-related G protein-coupled receptor X1 (MrgprX1)-positive allosteric modulator. BCFTP selectively potentiates MrgprX1 signaling in HEK293 cells. BCFTP alleviates specific neuropathic pain-related behaviors in a humanized MrgprX1 mouse model of chronic constrictive injury (CCI) in a MrgprX1-dependent manner. BCFTP synergistically enhances psychoactive substances analgesia in CCI MrgprX1 mice. BCFTP can be used for neuropathic pain research .
APOL1-IN-2 (Compound 467) is the inhibitor for Apolipoprotein 1 (APOL1). APOL1-IN-2 reduces the APOL1 G2/G1 induced cell death in HEK293 with EC50 of 4.74 nM and 14.3 nM. APOL1-IN-2 reduces the APOL1 G2/G1/G0 induced death of trypanosomes with EC50 of 2.24, 6.03 and 3.72 nM, respectively .
NPS-2143 (Standard) is the analytical standard of NPS-2143 (HY-10007). This product is intended for research and analytical applications. NPS-2143 (SB-262470A), an orally active calcilytic agent, is a selective and potent calcium ion-sensing receptor (CaSR) antagonist. NPS-2143 (SB-262470A) blocks increases in cytoplasmic Ca2+ concentrations (IC50=43 nM) elicited by activating the Ca2+ receptor in HEK 293 cells expressing the human Ca2+ receptor .
Ro 67-7476 (Standard) is the analytical standard of Ro 67-7476 (HY-100403). This product is intended for research and analytical applications. Ro 67-7476 is a potent positive allosteric modulator of mGluR1 and potentiates glutamate-induced calcium release in HEK293 cells expressing rat mGluR1a with an EC50 of 60.1 nM . Ro 67-7476 is a potent P-ERK1/2 agonist and activates ERK1/2 phosphorylation in the absence of exogenously added glutamate (EC50=163.3 nM) .
SNC80 (Standard) is the analytical standard of SNC80 (HY-101202). This product is intended for research and analytical applications. SNC80 (NIH 10815) is a potent, highly selective and non-peptide δ-opioid receptor agonist with a Ki of 1.78 nM and an IC50 of 2.73 nM. SNC80 also selectively activates μ-δ heteromer in HEK293 cells with an EC50 of 52.8 nM. SNC80 shows antinociceptive, antihyperalgesic and antidepressant‐like effects. SNC80 has the potential for multiple headache disorders treatment .
Ki16425 (Standard) is the analytical standard of Ki16425. This product is intended for research and analytical applications. Ki16425 (Debio 0719) is a subtype-selective, competitive antagonist of the EDG-family receptors, LPA1 and LPA3 with Kis of 0.34 μM and 0.93 μM, respectively. Ki16425 (Debio 0719) reduces the LPA-induced activation of p42/p44 MAPK . Ki16425 can also inhibit LPA-induced dephosphorylation of Yes-associated protein (YAP)/TAZ in HEK293A cells .
URAT1&XO inhibitor 2 (Compound BDEO) is a dual inhibitor of xanthine oxidase and URAT1, with IC50 of 3.3 μM for xanthine oxidase. URAT1&XO inhibitor 2 blocks uptake of uric acid in HEK293 cells expressing URAT1, with a Ki value of 0.145 μM. URAT1&XO inhibitor 2 decreases serum urate level and uric acid excretion in hyperuricemic mice. URAT1&XO inhibitor 2 can be used for research of hyperuricemia .
CSF1 is a silicon-rhodamine-based, fluorescence-activatable probe with selectivity for Cu +. CSF1 colocalizes with the endoplasmic reticulum in live cells .
Ketodarolutamide-d6 (BAY 1896953-d6) is the deuterium labeled Ketodarolutamide (HY-19337). Ketodarolutamide (ORM-15341) is a potent, high-affinity nonsteroidal competitive full antagonist of androgen receptor (AR). Ketodarolutamide displays a Ki value of 8 nM for rat wild-type AR and an IC50 value of 38 nM in AR-HEK293 cells . Ketodarolutamide inhibits testosterone-induced nuclear translocation of the AR and antagonizes both overexpressed and mutant ARs . Ketodarolutamide specifically suppresses the proliferation of AR-dependent prostate cancer cells and exhibits antitumor activity in models of castration-resistant prostate cancer (CRPC) . Ketodarolutamide is suitable for the mechanistic and therapeutic research of prostate cancer .
Antiproliferative agent-53-d3 (Compound C1) is an inhibitor for theta-mediated end joining (TMEJ) in HEK293 cell with an IC50 of 0.14 µM. Antiproliferative agent-53-d3 is the inhibitor for CYP2C19 and CYP2C9 with IC50 of 0.77 and 3.1 µM. Antiproliferative agent-53-d3 inhibits the proliferation of DNA repair-compromised cells, with IC50 of 8.1 µM for BRCA2 -/- DLD-1. Antiproliferative agent-53-d3 exhibits good pharmacokinetic characteristics in CD-1 mice .
Ketodarolutamide-d3 (BAY 1896953-d3) is the deuterium labeled Ketodarolutamide (HY-19337). Ketodarolutamide (ORM-15341) is a potent, high-affinity nonsteroidal competitive full antagonist of androgen receptor (AR). Ketodarolutamide displays a Ki value of 8 nM for rat wild-type AR and an IC50 value of 38 nM in AR-HEK293 cells . Ketodarolutamide inhibits testosterone-induced nuclear translocation of the AR and antagonizes both overexpressed and mutant ARs . Ketodarolutamide specifically suppresses the proliferation of AR-dependent prostate cancer cells and exhibits antitumor activity in models of castration-resistant prostate cancer (CRPC) . Ketodarolutamide is suitable for the mechanistic and therapeutic research of prostate cancer .
MA-2029 is a selective, orally active, and competitive motilin receptor antagonist (IC50=4.9 nM). MA-2029 is selective for the motilin receptor over various other receptors and ion channels. MA-2029 may be useful for gastrointestinal disorders associated with disturbed gastrointestinal motility .
Tyrosinase-IN-49 (Compound 12) is a potent and mixed-type chalcone-based tyrosinase inhibitor with an IC50 of 0.19 μM. Tyrosinase-IN-49 has potent antioxidant potential with significant DPPH and ABTS radical scavenging capacity. Tyrosinase-IN-49 can chelate the binuclear copper ions in the active center of tyrosinase and reduce Cu 2+ to Cu +, thereby reducing the catalytic activity of the enzyme. Tyrosinase-IN-49 has low cytotoxicity for HEK293 cells and zebrafish embryo. Tyrosinase-IN-49 shows antibrowning effects to improve food quality and can be used for research of food preservation .
(1S,2S)-2-PCCA (hydrochloride) (Standard) is the analytical standard of (1S,2S)-2-PCCA (hydrochloride) (HY-100013B1). This product is intended for research and analytical applications. (1S,2S)-2-PCCA hydrochloride is a less active diastereomer of 2-PCCA. 2-PCCA is a GPR88 receptor agonist, and inhibits GPR88-mediated cAMP production, with an EC50 of 116 nM in HEK293 cells.
S1PL-IN-2 (Compound 28) is a potent sphingosine-1-phosphate lyase (S1PL) inhibitor with an IC50 of 120 nM. S1PL-IN-2 shows an IC50 of 230 nM on HEK293 cells. S1PL-IN-2 block the conversion of Vitamin B6 into the active pyridoxal-4-phosphate cofactor required for S1P lyase activity. S1PL-IN-2 can be used for the researches of inflammation and immunology, such as rheumatoid arthritis .
(E/Z)-DMU2105 (Compound 7k) is a potent and highly selective CYP1B1 inhibitor. (E/Z)-DMU2105 inhibits human CYP1B1 enzyme bound to yeast-derived microsomes with an IC50 value of 10 nM. (E/Z)-DMU2105 also potently inhibits CYP1B1 expressed within ‘live’ recombinant yeast and human HEK293 kidney cells with an IC50 value of 63.65 nM. (E/Z)-DMU2105 can be used for the research of cancer, glaucoma, ischemia and obesity .
Tyrosinase-IN-48 (Compound 3) is a potent and competitive chalcone-based tyrosinase inhibitor with an IC50 of 0.49 μM. Tyrosinase-IN-48 has potent antioxidant potential with significant DPPH and ABTS radical scavenging capacity. Tyrosinase-IN-48 can chelate the binuclear copper ions in the active center of tyrosinase and reduce Cu 2+ to Cu +, thereby reducing the catalytic activity of the enzyme. Tyrosinase-IN-48 has low cytotoxicity for HEK293 cells and zebrafish embryo. Tyrosinase-IN-48 shows antibrowning effects to improve food quality and can be used for research of food preservation .
Dezecapavir (VH-499) is a HIV-1 capsid protein inhibitor. Dezecapavir exhibits picomolar-level antiviral activity against a variety of HIV-1 laboratory strains and clinical isolates in vitro. Dezecapavir inhibits the early and late stages of the HIV-1 life cycle, blocking nuclear import, reverse transcript production, virion assembly, maturation, and post-nuclear import/pre-integration replication processes. Dezecapavir can be used in studies related to HIV-1 infection .
CD649.2 is a red-emitting copper-targeted acylimidazole-reactive Fluorescent probe and a highly specific Cu 2+ detection reagent. CD649.2 enables visualization of labile Cu 2+ pools and their dynamic changes in living cells .
O-Desmethylcarvedilol (Desmethylcarvedilol) is an active metabolite of the non-selective β-adrenergic receptor (β-AR) antagonist Carvedilol (HY-B0006). O-Desmethylcarvedilol inhibits store-overload-induced calcium release in HEK293 cells expressing the ryanodine receptor 2 (RyR2) R4496C (RyR2 R4496C) mutation (IC50 = 7.62 µM). O-Desmethylcarvedilol reduces increases in heart rate and prevents decreases in diastolic blood pressure induced by Isoproterenol (HY-B0468) in conscious rabbits (ED50s = 32 and 5 µg/kg, respectively) .
CLH304a (compound 14) is a specific and noncompetitive GABAB receptor negative allosteric modulator (NAM). CLH304a decreases GABA-induced IP3 production with an IC50 of 37.9 μM. CLH304a has no effect on other GPCR Class C members such as mGluR1, mGluR2, and mGluR5. CLH304a acts on the heptahelical domain of GB2 subunits and non-competitively inhibits the effect of agonists with inverse agonist properties. CLH304a inhibits Baclofen (HY-B0007)-induced ERK1/2 phosphorylation in HEK293 cells overexpressing GABAB receptor .
BRD9 c-1 (Compound 13-7) is a PROTACBRD9 degrader . BRD9 Degrader-1 has a micromolar binding affinity for BRD9 and a nanomolar affinity for the BRD9-VCB ternary complex. BRD9 Degrader-1 induces BRD9 proteasome degradation in HEK293T cells, which can be reversed by MLN4924 (HY-70062). (Blue: VH032-cyclopropane-F (HY-125905); Black: linker (HY-W763939); Pink: HY-168695) .
TH023 is an inhibitor for the TLR4 signaling pathway, that targets especially the formation of TLR4 homodimer. TH023 inhibits secreted embryonic alkaline phosphatase in cellHEK-Blue hTLR4 with an IC50 of 0.354 μM, and inhibits the NO expression in RAW264.7 with an IC50 of 1.61μM. TH023 also inhibits the activation of NF-κB, reduces the nuclear translocation of NF-κB p65. TH023 exhibits anti-inflammatory efficacy in LPS (HY-D1056)-induced mouse acute sepsis model, and ameliorates the mouse lung injury .
Akuammine is an indole alkaloid that has been found in Picralima nitida and has analgesic activity. It selectively binds to the μ- and κ-opioid receptors over the δ-opioid receptor (Kis=0.3, 1.68, and 10.4 μM for the human receptors, respectively). Akuammine inhibits forskolin-induced cAMP production in HEK293 cells expressing human μ- or κ-opioid receptors (IC50s=2.6 and 0.073 μM, respectively). It increases the latency to withdrawal in the tail-flick or hot plate test in mice when administered at a dose of 60 mg/kg.
VU0424465 is a potent and partial PAM (positive allosteric modulator)-agonist for mGlu5 mediated iCa 2+ mobilization. VU0424465 exhibits high affinity at MPEP allosteric binding site, with a Ki value of 11.8 nM. VU0424465 is also a agonist for pERK1/2 in cortical neurons .
H2-005 is a compound that selectively inhibits diacylglycerol acyltransferase 2 (DGAT2) and has the activity to inhibit triacylglycerol synthesis in hepatocytes and preadipocytes. H2-005 significantly reduces triacylglycerol biosynthesis in HepG2 hepatocytes and 3T3-L1 preadipocytes. H2-005 exhibits specific inhibitory activity in DGAT2-overexpressing HEK293 cells. H2-005 almost completely inhibits lipid droplet formation in 3T3-L1 cells when co-treated with a DGAT1 inhibitor. H2-005 will contribute to DGAT2-related lipid metabolism research and the development of drugs to inhibit metabolic diseases .
STAT3-IN-32 (compound 2p) is an orally active, potent STAT3 dual phosphorylation inhibitor with an indole-containing tetra-aromatic heterocycle scaffold. STAT3-IN-32 exhibits STAT3 luciferase inhibition activity using HEK293T cells with an IC50 of 5.3 nM and ATP production inhibition activity using BxPC-3 cells with an IC50 of 4.2 nM. STAT3-IN-32 significantly blocks p-Tyr705 and p-Ser727 and causes the abrogation of the corresponding nuclear transcription and mitochondrial oxidative phosphorylation functions of STAT3 by targeting the STAT3 SH2 domain (KD=21.3 nM). STAT3-IN-32 exhibits significant suppressive effects in a pancreatic cancer xenograft model .
KMR-206 is a PARP7 inhibitor with an IC50 of 13.7 nM. KMR-206 relieves AHR-mediated transcriptional repression and enhances CYP1A1 expression in the presence of TCDD. KMR-206 induces the STING-dependent IFN-β signaling pathway and increases the levels of STAT1, pSTAT1 and nuclear PARP7 in cancer cells. KMR-206 reduces the viability of lung adenocarcinoma cells, enhances radiation-induced immunogenic signals, and induces the production of immunogenic signals in glioblastoma cancer stem cells. KMR-206 destabilizes FRA1 to increase IRF1 levels and promotes the IRF3-CBP/p300 interaction. KMR-206 can be used in studies related to lung adenocarcinoma and glioblastoma .
Triptolide-6-succinate-β-D-glucose (Compound 2) is a glucose-conjugated derivative of Triptolide (HY-32735). Triptolide-6-succinate-β-D-glucose is a tumor-selective prodrug targeting glucose transporters ( GLUT). Triptolide-6-succinate-β-D-glucose can induce the degradation of the RPB subunit of RNA polymerase II. Triptolide-6-succinate-β-D-glucose inhibits the proliferation of HEK293T cells with an IC50 value of 268 nM. Triptolide-6-succinate-β-D-glucose can be used for the research of cancer, such as prostatic cancer .
Kv2.1-IN-1 is an orally active and blood-brain barrier penetrant Kv2.1 inhibitor with an IC50 of 0.07 μM. Kv2.1-IN-1 exhibits a selectivity >130 fold over other K +, Na +, and Ca 2+ ion channels. Kv2.1-IN-1 decreases the apoptosis of HEK293 cells induced by H2O2. Kv2.1-IN-1 produces significant neuroprotection efficacy in middle cerebral artery occlusion (MCAO) rat. Kv2.1-IN-1 can be used for the study of ischemic stroke .
ISR activator-5 is an eIF2B modulator and integrated stress response (ISR) activator. ISR activator-5 stabilises the inactive I-state of eIF2B, inhibits protein synthesis, and activates canonical ISR pathways without inducing eIF2α phosphorylation. ISR activator-5 can be used for the research of cancer, neurologic and metabolic disorders .
Mn1 (M1) is a BODIPY-based Mn 2+-selective "turn-on" Fluorescent sensor and fluorescence modulator. In the absence of Mn 2+, Mn1 undergoes fluorescence quenching via photoinduced electron transfer; binding to Mn 2+ inhibits this mechanism, thereby generating a fluorescence "turn-on" response. Mn1 exhibits Mn 2+-specific cellular fluorescence response .
SARS-CoV-2 Mpro-IN-43 (Compound 1) is a coronavirus main protease (Mpro) inhibitor (IC50: 72 μM). SARS-CoV-2 Mpro-IN-43 interacts with key residues in the active site of Mpro via non-covalent binding, exerting its anti-coronavirus effect. SARS-CoV-2 Mpro-IN-43 exhibits moderate to low cytotoxicity, with CC50 values of 13.24, 41.02, and 42.26 µM in HaCaT, HEK293T, and HepG2 cells, respectively. SARS-CoV-2 Mpro-IN-43 can be used in anti-SARS-CoV-2 research .
Ajmaline hydrochloride is a Class Ia antiarrhythmic agent. It inhibits HERG potassium channels with IC50s of 1.0 μmol/l and 42.3 μmol/l in HEKcells and moth spider oocytes respectively. The inhibitory effect of Ajmaline hydrochloride is rapid, reversible, and positive frequency dependent. It acts primarily on the open state of the HERG channel and may also be combined with the inactivated state. The inhibitory effect of ajmaline hydrochloride is dependent on aromatic residues in the S6 domain, and the sensitivity is significantly reduced in the inactivation-deficient HERG S620T channel. It can also slightly affect the activation voltage of HERG channels. Ajmaline hydrochloride's inhibitory effect on HERG channels may contribute to both its potent antiarrhythmic effects and its potential proarrhythmic risk.
2-Chloro-ATP sodium (2-Chloro ATP) is an adenine nucleotide and an analog of ATP. It is an antagonist of the purinergic P2Y1 receptor and inhibits intracellular calcium mobilization induced by ADP (HY-W010918) in Jurkat cells expressing the human receptor (Ki=2.3 μM). 2-Chloro-ATP sodium is an agonist of the purinergic P2X receptor and induces inward currents in HEK293 cells expressing human bladder smooth muscle or rat PC12 forms of the receptor (EC50=0.5 and 2.5 μM). 2-Chloro-ATP sodium induces relaxation of precontracted guinea pig cecal strips in a concentration-dependent manner. 2-Chloro-ATP sodium has been used to study the substrate specificity of cyclic nucleotide-dependent protein kinases such as protein kinase A (PKA) and PKG.
EP4 receptor antagonist 7 (Compound 14) is an antagonist of the prostaglandin E2 (PGE2) receptor subtype EP4 with an IC50 value of 1.1 nM. EP4 receptor antagonist 7 inhibits PGE2-induced β-arrestin recruitment in HEK293 cells with an IC50 value of 0.9 nM. EP4 receptor antagonist 7 decreases PGE2-induced expression of mRNA encoding IL-4, macrophage mannose receptor 1 (Mrc1), chitinase-like protein 3 (Chil3), chemokine (C-X-C) motif ligand 1 (Cxcl1), triggering receptor expressed on myeloid cells 2 (Trem2), and arginase-1 (Arg1), in RAW 264.7 macrophages. EP4 receptor antagonist 7 combined with an anti-PD-1 antibody inhibits tumor growth and increases infiltration of CD 8+ T cells into tumors in a CT26 murine colon cancer model .
TLR2/1 agonist-1 is a selective agonist of the TLR2/1 heterodimer. TLR2/1 agonist-1 acts as a hematopoietic recovery inducer to accelerate the recovery of peripheral blood cells. TLR2/1 agonist-1 serves as a G-CSF production inducer to increase serum G-CSF levels. TLR2/1 agonist-1 exhibits radioprotective effects in mice exposed to radiation. TLR2/1 agonist-1 can be used in studies related to acute radiation syndrome .
Ctrl-CCF1 is a control probe for CCF1. Ctrl-CCF1 can be used to distinguish copper-dependent responses from potential dye-dependent variations, such as cellular uptake, retention, subcellular accumulation, and changes in pH, redox or hydrophobic/hydrophilic environments .
CCF1 is a carbon-rhodol-based turn-on fluorescent copper sensor with high selectivity for Cu + over other biologically relevant metal ions. CCF1 detects changes in labile copper pools in living cells upon copper supplementation and/or depletion. CCF1 identifies elevations in labile copper pools in Atp7a -/ - fibroblast cell models. CCF1 can be used for the research of Menkes disease .
TRPC6-PAM-C20 is a selective positive allosteric modulator (PAM) of TRPC6 channels. TRPC6-PAM-C20 is a potent enhancer of channel activation, enabling low basal concentrations of DAG to induce activation of the ion channel. TRPC6-PAM-C20 induces increases in intracellular Ca 2+ concentrations ([Ca 2+]i) in TRPC6-expressing HEK293 cells with an EC50 of 2.37 μM. TRPC6-PAM-C20 can be used as a valuable tool to selectively exaggerate TRPC6-dependent signals .
RQ-00311651 is a T-type calcium channel blocker that specifically targets the Cav3.2 isoform with a role in neuropathic and visceral pain. RQ-00311651 significantly inhibits T currents in HEK293 cells expressing human Cav3.1 or Cav3.2. RQ-00311651 also inhibited high potassium-induced calcium signaling. RQ-00311651 also inhibits antiallergic properties in rats and mice with neuropathic pain induced by spinal nerve injury or Paclitaxel (HY-B0015). Oral and intraperitoneal injection (10-20 mg/kg) inhibits Cerulein (HY-A0190)-induced acute pancreatitis and cyclophosphamide-induced cystitis in mice .
8(9)-EET is one of the main metabolites produced by the metabolism of arachidonic acid (HY-109590) through the cytochrome P450 epoxide pathway. 8(9)-EET is an effective substrate for COX-1 and COX-2. 8(9)-EET activates PPARα in HEK293 cells and inhibits the activity of NF-κB induced by IL-1β in a PPARα-dependent and -independent manner. The (8S,9R)-isomer of 8(9)-EET ([(8S,9R)-EET]) causes vasoconstriction, thereby reducing renal plasma flow and glomerular filtration rate .
(±)8(9)-EET is one of the main metabolites produced by the metabolism of arachidonic acid (HY-109590) through the cytochrome P450 epoxide pathway. (±)8(9)-EET is an effective substrate for COX-1 and COX-2. (±)8(9)-EET activates PPARα in HEK293 cells and inhibits the activity of NF-κB induced by IL-1β in a PPARα-dependent and -independent manner. The (8S,9R)-isomer of (±)8(9)-EET ([(8S,9R)-EET]) causes vasoconstriction, thereby reducing renal plasma flow and glomerular filtration rate .
Firefly Luciferase mRNA is a reporter mRNA that can be transfected into cells to express firefly luciferase protein. Firefly Luciferase mRNA induces cytotoxicity in cancer cells at low concentrations. In cancer cells, the expression level of luciferase shows a non-linear relationship with the dose of Firefly Luciferase mRNA. When combined with the H2S-responsive bioluminescent probe (H-Luc), Firefly Luciferase mRNA enables bioluminescence-based detection of endogenous hydrogen sulfide in non-transgenic NAFLD cell models and NAFLD mouse models. Firefly Luciferase mRNA can be used in studies related to non-alcoholic fatty liver disease .
JZ-4109 is a β-Glucocerebrosidase (GCase) modulator with an IC50 of 8 nM for wild-type recombinant GCase. JZ-4109 binds to an allosteric site at the GCase dimer interface, stabilizes wild-type and GCase N370S mutant GCase, induces GCase dimerization. JZ-4109 increases GCase protein abundance. JZ-4109 can be used for the research of Parkinson's diseas .
MNP2 is a NLRP3-ASC interaction inhibitor. MNP2 selectively binds to the PYD domain of ASC (Ka=149 nM) and blocks ASC-PYM binding (Ka=58 nM), thereby inhibiting the interaction between ASC and NLRP3 and suppressing the formation of the NLRP3 inflammasome. MNP2 inhibits IL-1β release and caspase-1 maturation, and reduces the efflux of potassium and chloride ions. MNP2 prevents mitochondrial damage and reactive oxygen species production, and significantly decreases NLRP3 inflammasome formation in neurodegenerative pathologies induced by β-amyloid, Tau protein and α-synuclein. MNP2 is applicable for the research of neurodegenerative diseases .
Soyasaponin Aa is a soyasaponin that can be found in soy. Soyasaponin Aa suppresses PPARγ transcriptional activity, reduces PPARγ and C/EBPα expression, inhibits adipocyte differentiation and lipid accumulation, and reduces adipogenic marker gene expression. Soyasaponin Aa reduces hydrogen peroxide-induced reactive oxygen species (ROS) production and malondialdehyde levels. Soyasaponin Aa exhibits cellular antioxidant activity. Soyasaponin Aa can be used for the research of obesity .
AM89 is a PGC-1α1 stabilizer. AM89 activates the expression of PGC-1α1 target genes and induces the upregulation of Ucp1 gene expression. AM89 is applicable for the research of obesity and related metabolic disorders .
Deoxyandrographolide is an orally active lactone found in the Andrographis paniculata Nees. Deoxyandrographolide shows a KD of 38.4 μM of HDAC1. Deoxyandrographolide enhances GLUT4 plasma membrane translocation, activates PI3K and AMPK-dependent signaling pathways, suppresses fasting blood glucose, serum insulin, triglycerides, and LDL-cholesterol levels. Deoxyandrographolide enhances HDAC1 expression via inhibited ubiquitination degradation, represses H3K4me3, improves chromosome stability, and restrains aging biomarkers p16, p21, γH2A.X, p53 and ROS production. Deoxyandrographolide interacts with Foot-and-Mouth Disease Virus 3Cpro active site, inhibits protease and IFN-antagonist activity, derepresses ISG expression, and inhibits viral replication. Deoxyandrographolide can be used for the researches of type 2 diabetes mellitus, vascular senescenceand virus infection .
Maridebart cafraglutide (AMG 133) is a long-acting peptide-antibody conjugate that combines GLP-1 receptor agonist with glucose-dependent insulinotropic polypeptide (GIP) receptor antagonism. Maridebart cafraglutide shows antagonist activity against human, cynomolgus monkey and rat GIPR with IC50 values of 46.4 nM, 26.5 nM, 822.3 nM, respectively. Maridebart cafraglutide shows agonist activity against human, cynomolgus monkey, rat and mouse GLP-1R with EC50 values of 24.4 pM, 5.7 pM, 2.4 pM and 123 pM, respectively. Maridebart cafraglutide can be used for the study of obesity and type 2 diabetes .
Canocapavir (ZM-H1505R) is an orally active HBV core protein-targeting antiviral agent. Canocapavir binds to the hydrophobic pocket at the dimer-dimer interface of HBV core protein (HBc), stimulating intracellular accumulation of nonfunctional HBV capsids, disrupting viral replication. Canocapavir interferes with the interaction between HBc and HBV large surface protein, resulting in diminished production of empty virionsis. Canocapavir can be used for the research of hepatitis B virus (HBV) infection .
JMV 7490 is a highly potent and highly hydrophilic neurotensin receptor NTS1 probe that can be successfully labeled with 68Ga and 111In. JMV 7490 acts as an efflux inhibitor to reduce its efflux in NTS1-positive cancer cells; it also serves as an internalization inducer and is efficiently and continuously internalized by NTS1-positive cancer cells. 111In-radiolabeled JMV 7490 shows persistent uptake in NTS1-positive xenografts in nude mice, but no significant uptake in NTS1-negative xenografts. JMV 7490 can be used for in vivo tracer applications of NTS1-positive tumors and supports related research on colorectal cancer .
BX-513 is a highly potent and selective CCR1 antagonist. BX-513 effectively inhibits the binding of radiolabeled MIP-1α and RANTES to CCR1, with Ki values of 40 nM and 60 nM, respectively. BX-513 suppresses MIP-1α-induced extracellular acidification, MIP-1α- and RANTES-induced intracellular calcium mobilization, as well as MIP-1α- and RANTES-induced migration of peripheral blood mononuclear cells. BX-513 can be used for the research of rheumatoid arthritis and multiple sclerosis .
VRT-325 is a CFTR modulator. VRT-325 inhibits disulfide cross-linking between cysteines in transmembrane segments 6 and 7 of CFTR and P-gp. VRT-325 promotes maturation of CFTR and P-gp processing mutants, rescues ΔF508-CFTR folding at the endoplasmic reticulum. VRT-325 binds ΔF508-CFTR nucleotide-binding domain 1, and increases mature ΔF508-CFTR cell surface expression and chloride conductance. VRT-325 can be used for the research of cystic fibrosis [1][3].
CID 16020046 (Standard) is the analytical standard of CID 16020046. This product is intended for research and analytical applications. CID 16020046 is a potent and selective GPR55 antagonist and inhibits GPR55 constitutive activity with an IC50 of 0.15 μM. CID 16020046 inhibits GPR55-mediated Ca2+ signaling and GPR55-mediated ERK1/2 phosphorylation. CID 16020046 reduces wound healing in endothelial cells and is involved in the regulation of platelet function .
CID 16020046 is a potent and selective GPR55 antagonist and inhibits GPR55 constitutive activity with an IC50 of 0.15 μM. CID 16020046 inhibits GPR55-mediated Ca 2+ signaling and GPR55-mediated ERK1/2 phosphorylation. CID 16020046 reduces wound healing in endothelial cells and is involved in the regulation of platelet function .
AM31 is a PGC-1α1 stabilizer. AM31 enhances the protein stability of PGC-1α1, promotes protein accumulation and target gene activation. AM31 induces the expression of Ucp1 and Cidea in brown adipocytes. AM31 increases the levels of basal mitochondrial respiration and uncoupled respiration in brown adipocytes. AM31 can be used for the research of obesity and related metabolic disorders .
HZD37-5 is a humanized monoclonal antibody specifically recognizing N78 loci of IL-17A. HZD37-5 binds to human and rhesus monkeys, blocks IL-17 induced signal transduction and the release of IL-6, IL-8, CXCL-1 and GM-GSF.HZD37-5 significantly inhibited human IL-17A induced-keratinocyte chemoattractant secretion. HZD37-5 can be used for the research of autoimmune diseases including psoriasis and psoriatic arthritis .
Coptisine is an orally active and brain-penetrant alkaloid found in Coptis chinensis. Coptisine is a reversible, uncompetitive IDO inhibitor with a Ki of 5.8 μM and an IC50 of 6.3 μM. Coptisine suppresses neuroinflammation, reduces Aβ plaque burden and shows neuroprotective activity. Coptisine shows anti-inflammation activity by blocking NF-κB, MAPK, and PI3K/Akt activation. Coptisine inhibits cancer cells proliferation, induces DNA damage, G2/M phase cell cycle arrest, apoptosis, ROS production and mitochondrial dysfunction. Coptisine inhibits Rho/ROCK pathway activation, reduces arrhythmia, limits cardiac injury marker release, reduces infarct size, and preserves cardiac function in rat myocardial ischemia/reperfusion models. Coptisine downregulates HMGCR and upregulates LDLR and CYP7A1 to modulate cholesterol metabolism, reduces abnormal serum lipid levels, and promotes fecal bile acid excretion. Coptisine can be used for the research of cancer, hypercholesterolemia, Alzheimer’s disease, inflammatory disorders and cardiovascular disease .
Tagmokitug (CHS-114; SRF-114) is a fully human IgG1 antibody targeting CCR8. Tagmokitug selectively binds to human CCR8 (Kd = 502 pM) and mediates the death of CCR8-expressing cells via antibody-dependent cellular cytotoxicity and antibody-dependent cellular phagocytosis. Tagmokitug selectively eliminates intratumoral regulatory T cells, induces tumor growth inhibition, remodels the tumor immune microenvironment, and promotes the differentiation of cytotoxic CD8 + T cell subsets. Tagmokitug can be used for the research of solid tumors .
NTZ-24 is a selective STAT3 pathway inhibitor. NTZ-24 suppresses STAT3 phosphorylation at Tyr705, blocks STAT3-DNA interaction, and downregulates the levels of STAT3 downstream target proteins. NTZ-24 induces cell-cycle arrest and promotes apoptosis in cancer cells. NTZ-24 exerts significant antiproliferative activity against HeLa cells (IC50 = 3.3 μM). NTZ-24 can be used for the research of cervical cancer .
S 32212 hydrochloride is an inverse agonist of 5-HT receptors5-HT2(CINI) and 5-HT2(CVSV) (Kis=6.6, 8.9 nM) and an antagonist of 5-HT2A and α2β-adrenergic receptors (Ki=5.8, 5.8 nM). S 32212 hydrochloride can reduce the binding of GTPγS to Gαq, and reduce the activity of phospholipase C (PLC) in HEK293 cells expressing 5-HT2(CINI) receptor and CHO cells expressing 5-HT2(CVSV) receptor (EC50=38 and 18.6 nM, respectively). S 32212 hydrochloride (2.5 mg/kg) reduces 5-HT receptor agonist-induced head twitches and penile erections in mice and rats. S 32212 hydrochloride (10, 40 mg/kg) reduces immobility time in the forced swim test and marble burying behavior in mice and rats, exerting antidepressant and anxiolytic activities.
Photoactive NTR probe (Compound 1) is a covalent crosslinker and Fluorescent indicator targeting Nitroreductase. The Photoactive NTR probe undergoes a sequential activation process: it is first activated via nitroreductase-mediated nitro-to-amino conversion, and then forms a fluorescent product upon photoactivation. The Photoactive NTR probe can form covalent adducts with the side chains of cysteine, tyrosine, lysine and histidine in adjacent proteins to reduce fluorophore diffusion. The Photoactive NTR probe enables super-resolution (STORM) imaging of active mitochondrial nitroreductase microdomains in living cells .
HCN-IN-1 is a TLR4 inhibitor and HCN channel modulator with activity against HCN2 and HCN4.HCN-IN-1 inhibits TLR4-mediated alkaline phosphatase (SEAP) signal activity.HCN-IN-1 reduces HCN2 current across tested voltages, shifts voltage-dependent activation to more hyperpolarized potentials, slows activation kinetics, and does not affect deactivation process.HCN-IN-1 blocks HCN4 current.HCN-IN-1 exhibits analgesic, anti-inflammatory, and anti-anginal effects.HCN-IN-1 can be used for the research of inflammatory pain, neuropathic pain, heart failure, inflammation .
Androst-16-en-3-ol is a pheromone derived from boars that triggers mating responses in estrous sows. It also exists in human urine, plasma, saliva and sweat. As an endogenous neurosteroid, Androst-16-en-3-ol acts as a positive allosteric modulator of GABAA receptors (GABAA receptor) and exerts anxiolytic, antidepressant and anticonvulsant activities in mice.
5-HT1AR/5-HT6R ligand-1 (Compound PP13) is the ligand for 5-HT receptor that exhibits good affinity to 5-HT1AR, 5-HT6R and 5-HT7R (Ki of 19, 69 and 198 nM, respectively), thereby inhibiting the cAMP production in HEK293 cell with EC50 of 1535, 488 and 53 nM, respectively. 5-HT1AR/5-HT6R ligand-1 exhibits anti-proliferative activity against a variety of cancer cells (IC50 for 1321N1, U87MG, MCF7, and AsPC-1 is 9.6, 13.6, 19.3 and 14.6 μM, respectively). 5-HT1AR/5-HT6R ligand-1 also exhibits antagonist activity for dopamine receptor D2R with Ki of 1903 nM .
ITX5061 free base is an orally active type II non-competitive p38 MAPK inhibitor. ITX5061 free base increases HDL-C levels by inhibiting SR-BI activity. ITX5061 free base also moderately elevates ApoA-I levels. ITX5061 free base reduces early atherosclerotic lesions in the aortic arch of mice fed an atherogenic diet. ITX5061 free base can be used in the research of atherosclerosis .
ITX5061 is an orally active type II non-competitive p38 MAPK inhibitor. ITX5061 increases HDL-C levels by inhibiting SR-BI activity. ITX5061 also moderately elevates ApoA-I levels. ITX5061 reduces early atherosclerotic lesions in the aortic arch of mice fed an atherogenic diet. ITX5061 can be used in the research of atherosclerosis .
D-473 is an orally active, blood-brain barrier penetrant and serotonin-preferring reuptake inhibitor. D-473 inhibits serotonin, dopamine and norepinephrine transporters, and significantly elevates the extracellular levels of these three neurotransmitters in rat brain regions. D-473 exhibits definite antidepressant-like activity without inducing motor activation. D-473 is widely used in studies related to major depressive disorder .
CQ80 is a PEPD/XPNPEP1 inhibitor and selective CARD8 inflammasome activator. CQ80 has IC50 values of 0.91 μM for PEPD, 43 μM for XPNPEP1. CQ80 promotes the accumulation of Xaa-Pro peptides by inhibiting PEPD and XPNPEP1, releases the fragment of CARD8 for inflammasome formation, and induces pyroptosis via GSDMD cleavage. CQ80 can be used for research on inflammasome, CARD8-expressing cancer cells, HIV-1-infected cell clearance, acute myeloid leukemia (AML) .
2-Hydrazinyl-adenosine is a synthetic intermediate. Derivatives of 2-Hydrazinyl-adenosine act as A2A adenosine receptor agonists. 2-Hydrazinyl-adenosine is used in the research of neurodegenerative diseases .
VHL-IN-1 (Compound 30) is an E3 ligase VHL inhibitor with a Kd value of 37 nM. VHL-IN-1 blocks VHL-mediated ubiquitination and degradation of HIF-1α. VHL-IN-1 stabilizes the protein levels of HIF-1α and hydroxylated HIF-1α, and induces the transcriptional activity of HIF-1α. VHL-IN-1 can be used for PROTAC development. VHL-IN-1 is applicable for cancer research .
AZ-11665362 is a CRTh2 (DP2) receptor antagonist with an IC50 of 2.6 nM. AZ-11665362 shows weak activity against aldose reductase, serotonin transporter, CYP 2C19, and CYP 2C9. AZ-11665362 lacks measurable inhibitory activity againstCOX-1 and COX-2. AZ-11665362 can be used for the research of asthma, and other inflammatory diseases .
Ratio-Coppersensor-1 is a selective ratiometric copper ion Fluorescent reporter (excitation wavelength: 480 nm; emission peak central wavelengths at 505 nm and 570 nm, respectively). Ratio-Coppersensor-1 exhibits extremely high selectivity for Cu + at cellular concentrations, outperforming other competing metal ions, and shows an approximately 20-fold change in fluorescence ratio upon Cu + binding. Ratio-Coppersensor-1 is capable of reflecting changes in Cu levels .
CS790AM (Coppersensor 790 acetoxymethyl ester) is a cell-permeable, Cu +-targeted near-infrared fluorescent probe (λabs=760 nm, λem=790 nm) applicable to live cells. CS790AM can cross lipophilic cell membranes, and is converted into negatively charged CS790 under the action of intracellular esterases to be retained, thus enabling highly sensitive, reversible "turn-on" detection of labile Cu + pools in live cells and mice. CS790AM possesses excellent biocompatibility and selectivity, avoids interference from other metal ions, shows no obvious toxicity, and can be rapidly cleared. CS790AM allows long-term longitudinal monitoring of individual mice, visualizes copper levels in internal organs and isolated livers, and effectively evaluates abnormal copper accumulation in Wilson's disease models (Atp7b -/-) as well as dynamic changes after chelator treatment. CS790AM can be used for research on Wilson's disease and related copper metabolic disorders .
PI3Kα-IN-32 (Compound 11f) is a selective, orally active PI3Kα inhibitor, with an IC50 of 26.3 nM against PI3Kα H1047R. PI3Kα-IN-32 inhibits AKT phosphorylation. PI3Kα-IN-32 exhibits anticancer activity against breast cancer. PI3Kα-IN-32 can be used in the research of HR +/HER2 - breast cancer .
4-Hydroxytryptophol is an in vitro metabolite of psilocin, can be found in human liver microsomes and recombinant monoamine oxidase A systems. 4-Hydroxytryptophol is not detected in in vivo samples from mice or humans.
α-Androstenol (5α-Androst-16-en-3α-ol) is a steroid pheromone that has been found in boar testes and male axillary sweat. α-Androstenol is also a positive allosteric modulator of GABAA receptors, which enhances GABA-activated currents in primary mouse cerebellar granule cells (EC50 of 0.4 μM). α-Androstenol produces anxiolytic-like, antidepressant-like, and anticonvulsant effects in mice.α-Androstenol can be used for the research of seizures .
MK-5661 is an orally potent NaV1.8 voltage-gated sodium channel inhibitor with an EC50 of 4.3 nM. MK-5661 selectively inhibits peripheral nociceptive signaling mediators. MK-5661 reduces capsaicin-induced spontaneous nociceptive behaviors in humanized rats and attenuates capsaicin-induced skin flushing responses in rhesus monkeys. MK-5661 is applicable for pain-related research .
BD-1063 is a selective σ-1receptor antagonist with inhibitory activity against TRPC5 and TRPM3. BD-1063 exerts anti-hyperalgesic and anti-allodynic effects by inhibiting sustained calcium influx mediated by TRPC5 and TRPM3, and reverses the effects of Carrageenan (HY-125474). BD-1063 also significantly reduces excessive ethanol self-administration behavior. BD-1063 is widely used in studies on the mechanisms underlying neuropathic pain, inflammatory hyperalgesia, and alcohol abuse and dependence .
Nav1.8-IN-24 is a voltage-gated sodium channel Nav1.8 inhibitor with pIC50 values of 7.4 (resting state) and 7.5 (inactivated state), and it exhibits high selectivity for NaV1.1-1.7 subtypes. Nav1.8-IN-24 possesses in vitro safety and drug interaction profiles. Nav1.8-IN-24 can be used for the research of acute pain and chronic neuropathic pain .
Maridebart cafraglutide (AMG 133) is a long-acting peptide-antibody conjugate that combines GLP-1 receptor agonist with glucose-dependent insulinotropic polypeptide (GIP) receptor antagonism. Maridebart cafraglutide shows antagonist activity against human, cynomolgus monkey and rat GIPR with IC50 values of 46.4 nM, 26.5 nM, 822.3 nM, respectively. Maridebart cafraglutide shows agonist activity against human, cynomolgus monkey, rat and mouse GLP-1R with EC50 values of 24.4 pM, 5.7 pM, 2.4 pM and 123 pM, respectively. Maridebart cafraglutide can be used for the study of obesity and type 2 diabetes .
Rapamycin (Sirolimus) (GMP) is Rapamycin (HY-10219) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Rapamycin (Sirolimus; AY 22989) is a potent and specific mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1 . Rapamycin is an autophagy activator, an immunosuppressant .
Rapamycin (Sirolimus) GMP Like is Rapamycin (HY-10219) produced by using GMP like guidelines. GMP Like small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Rapamycin (Sirolimus; AY 22989) is a potent and specific mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1 . Rapamycin is an autophagy activator, an immunosuppressant .
Ctrl-CPF1 is a control dye for Copper Phosphorus Fluor 1 (CPF1), which exhibits no metal-dependent fluorescence response and shows no reactivity toward Cu + .
CSF1 is a silicon-rhodamine-based, fluorescence-activatable probe with selectivity for Cu +. CSF1 colocalizes with the endoplasmic reticulum in live cells .
CD649.2 is a red-emitting copper-targeted acylimidazole-reactive Fluorescent probe and a highly specific Cu 2+ detection reagent. CD649.2 enables visualization of labile Cu 2+ pools and their dynamic changes in living cells .
Mn1 (M1) is a BODIPY-based Mn 2+-selective "turn-on" Fluorescent sensor and fluorescence modulator. In the absence of Mn 2+, Mn1 undergoes fluorescence quenching via photoinduced electron transfer; binding to Mn 2+ inhibits this mechanism, thereby generating a fluorescence "turn-on" response. Mn1 exhibits Mn 2+-specific cellular fluorescence response .
Ctrl-CCF1 is a control probe for CCF1. Ctrl-CCF1 can be used to distinguish copper-dependent responses from potential dye-dependent variations, such as cellular uptake, retention, subcellular accumulation, and changes in pH, redox or hydrophobic/hydrophilic environments .
CCF1 is a carbon-rhodol-based turn-on fluorescent copper sensor with high selectivity for Cu + over other biologically relevant metal ions. CCF1 detects changes in labile copper pools in living cells upon copper supplementation and/or depletion. CCF1 identifies elevations in labile copper pools in Atp7a -/ - fibroblast cell models. CCF1 can be used for the research of Menkes disease .
Photoactive NTR probe (Compound 1) is a covalent crosslinker and Fluorescent indicator targeting Nitroreductase. The Photoactive NTR probe undergoes a sequential activation process: it is first activated via nitroreductase-mediated nitro-to-amino conversion, and then forms a fluorescent product upon photoactivation. The Photoactive NTR probe can form covalent adducts with the side chains of cysteine, tyrosine, lysine and histidine in adjacent proteins to reduce fluorophore diffusion. The Photoactive NTR probe enables super-resolution (STORM) imaging of active mitochondrial nitroreductase microdomains in living cells .
Ratio-Coppersensor-1 is a selective ratiometric copper ion Fluorescent reporter (excitation wavelength: 480 nm; emission peak central wavelengths at 505 nm and 570 nm, respectively). Ratio-Coppersensor-1 exhibits extremely high selectivity for Cu + at cellular concentrations, outperforming other competing metal ions, and shows an approximately 20-fold change in fluorescence ratio upon Cu + binding. Ratio-Coppersensor-1 is capable of reflecting changes in Cu levels .
BAPTA-AM is a well-known membrane permeable Ca 2+ chelator. BAPTA-AM inhibits hERG channels, hKv1.3 and hKv1.5 channels in HEK 293 cells with IC50s of 1.3 μM, 1.45 μM and 1.23 μM, respectively .
Rapamycin (Sirolimus) (GMP) is Rapamycin (HY-10219) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Rapamycin (Sirolimus; AY 22989) is a potent and specific mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1 . Rapamycin is an autophagy activator, an immunosuppressant .
Rapamycin (Sirolimus) GMP Like is Rapamycin (HY-10219) produced by using GMP like guidelines. GMP Like small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Rapamycin (Sirolimus; AY 22989) is a potent and specific mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1 . Rapamycin is an autophagy activator, an immunosuppressant .
BAPTA-AM (Standard) is the analytical standard of BAPTA-AM. This product is intended for research and analytical applications. BAPTA-AM is a well-known membrane permeable Ca2+ chelator. BAPTA-AM inhibits hERG channels, hKv1.3 and hKv1.5 channels in HEK 293 cells with IC50s of 1.3 μM, 1.45 μM and 1.23 μM, respectively .
PACAP (1-38) free acid is a desamido-PACAP (1-38), human, ovine, rat (HY-P0221). PACAP (1-38) free acid can activate the human PAC1 receptor. PACAP (1-38) free acid induces cyclic AMP (cAMP) generation in both NS-1 neuroendocrine cells and non-neuroendocrine HEK293 cells .
Apelin-17(human, bovine) is an endogenous orphan G protein-coupled receptor APJ agonist. Apelin-17(human, bovine) binds to human APJ receptors expressed in HEK 293 cells (pIC50=9.02). Apelin-17(human, bovine) inhibits the entry of some HIV-1 and HIV-2 into the NP2/CD4 cells expressing APJ .
Gamma-Glu-Abu TFA is the TFA salt form of Gamma-Glu-Abu (HY-P4376). Gamma-Glu-Abu TFA is an agonist for calcium sensing receptor (CaSR), that activates the CaSR with an EC50 of 0.21 μM in HEK-293 cell .
Apelin-36(human) is an endogenous orphan G protein-coupled receptor APJ agonist, with an EC50 of 20 nM. Apelin-36(human) shows high affinity to human APJ receptors expressed in HEK 293 cells (pIC50=8.61). Apelin-36 has been linked to two major types of biological activities: cardiovascular and metabolic. Apelin-36(human) inhibits the entry of some HIV-1 and HIV-2 into the NP2/CD4 cells expressing APJ .
Apelin-36(human) TFA is an endogenous orphan G protein-coupled receptor APJ agonist, with an EC50 of 20 nM. Apelin-36(human) TFA shows high affinity to human APJ receptors expressed in HEK 293 cells (pIC550=8.61). Apelin-36(human) TFA has been linked to two major types of biological activities: cardiovascular and metabolic. Apelin-36(human) TFA inhibits the entry of some HIV-1 and HIV-2 into the NP2/CD4 cells expressing APJ .
KP-2067 is a form of the CaSR agonist peptide. KP-2067 can result in dose-dependent activation of CaSR in HEK293T overexpressing hCaSR cell line, with an EC50 of 18.4 μM. KP-2067 significantly reduces plasma parathyroid hormone in rat model .
Apelin-17(human, bovine) TFA is an endogenous orphan G protein-coupled receptor APJ agonist. Apelin-17(human, bovine) TFA binds to human APJ receptors expressed in HEK 293 cells (pIC50=9.02). Apelin-17(human, bovine) TFA inhibits the entry of some HIV-1 and HIV-2 into the NP2/CD4 cells expressing APJ .
K-(D-1-Nal)-FwLL-NH2 TFA is a high affinity and potent ghrelin receptor inverse agonist (Ki values are 4.9 and 31 nM in COS7 and HEK293T cells, respectively). K-(D-1-Nal)-FwLL-NH2 blocks ghrelin receptor-mediated Gq- and G13-dependent signaling pathways.
Apelin-36(rat, mouse) TFA is an endogenous orphan G protein-coupled receptor APJ agonist. Apelin-36(rat, mouse) TFA binds to APJ receptors with an IC50 of 5.4 nM, and potently inhibits cAMP production with an EC50 of 0.52 nM. Apelin-36(rat, mouse) TFA blocks entry of some HIV-1 and HIV-2 strains into NP-2/CD4 cells expressing APJ .
BmP02 is a selective Kv1.3 channel blocker and a highly-selective Kv4.2 modulator, which can be isolated from Chinese scorpion (Buthus martensi Karsch) venom. BmP02 also delays the inactivation of Kv4.2 in HEK293T cells, with an EC50 value of ~850 nM. BmP02 inhibits the transient outward potassium currents (Ito) in ventricular muscle cells .
MNP2 is a NLRP3-ASC interaction inhibitor. MNP2 selectively binds to the PYD domain of ASC (Ka=149 nM) and blocks ASC-PYM binding (Ka=58 nM), thereby inhibiting the interaction between ASC and NLRP3 and suppressing the formation of the NLRP3 inflammasome. MNP2 inhibits IL-1β release and caspase-1 maturation, and reduces the efflux of potassium and chloride ions. MNP2 prevents mitochondrial damage and reactive oxygen species production, and significantly decreases NLRP3 inflammasome formation in neurodegenerative pathologies induced by β-amyloid, Tau protein and α-synuclein. MNP2 is applicable for the research of neurodegenerative diseases .
JMV 7490 is a highly potent and highly hydrophilic neurotensin receptor NTS1 probe that can be successfully labeled with 68Ga and 111In. JMV 7490 acts as an efflux inhibitor to reduce its efflux in NTS1-positive cancer cells; it also serves as an internalization inducer and is efficiently and continuously internalized by NTS1-positive cancer cells. 111In-radiolabeled JMV 7490 shows persistent uptake in NTS1-positive xenografts in nude mice, but no significant uptake in NTS1-negative xenografts. JMV 7490 can be used for in vivo tracer applications of NTS1-positive tumors and supports related research on colorectal cancer .
MCE PEI Transfection Reagent is designed based on 25 kDa PEI. It has high-efficiency, low-toxicity, strong-stability, and is suitable for many cell types, such as HEK-293、HEK-293T、CHO-K1、COS-1、COS-7、NIH/3T3、Sf9、HepG2 and HeLa et, even some hard-to-transfect cells. It can also be applied to large-scale recombinant protein expression and virus production. The 1 mL is defined as the base specification. All larger sizes correspond to incremental volumes of this base.
Cetrelimab (JNJ 63723283; JNJ 3283) is a human IgG4κ mAb targeting PD-1. Cetrelimab binds PD-1 (Kd=1.72 nM, HEK293) to block the interaction of PD-1 with PD-L1 and PD-L2 (IC50s=111.7 ng/mL and 138.6 ng/mL, respectively). Cetrelimab stimulates peripheral T cells, increases IFN-γ, IL-2, TNF-α level and inhibits tumor growth in vivo .
Tagmokitug (CHS-114; SRF-114) is a fully human IgG1 antibody targeting CCR8. Tagmokitug selectively binds to human CCR8 (Kd = 502 pM) and mediates the death of CCR8-expressing cells via antibody-dependent cellular cytotoxicity and antibody-dependent cellular phagocytosis. Tagmokitug selectively eliminates intratumoral regulatory T cells, induces tumor growth inhibition, remodels the tumor immune microenvironment, and promotes the differentiation of cytotoxic CD8 + T cell subsets. Tagmokitug can be used for the research of solid tumors .
Perenostobart (SRF617) is a human IgG4 antibody with inhibitory activity against CD39 ATPase. Perenostobart inhibits CD39-mediated hydrolysis of extracellular ATP to AMP, with IC50 values of 1.9 nM (HEK293 OE cells), 0.7 nM (MOLP-8 cells), and 1.2 nM (RBC-lysed whole blood). Perenostobart enhances CD4 + T-cell proliferation, promotes dendritic cell maturation, and boosts inflammasome activation in macrophages in the presence of ATP. Perenostobart demonstrates significant single-agent anti-tumor efficacy in MOLP-8 and H520 xenograft models. Perenostobart can be used for the study of cancer .
STX-100 (Biotinylated) is a biotin-labeled STX-100 (HY-P990667). STX-100 is a humanized antibody expressed in HEK293 cells, targeting Integrin aVb6 (ITGAV & ITGB6) .
RO5323441 (TB-403) is a human IgG1 monoclonal antibody (mAb) targeting PlGF. RO5323441 inhibits the binding of human PlGF-1 or PlGF-2 to VEGFR-1 (IC50 values are 0.1 and 0.2 nM, respectively). RO5323441 blocks PlGF-induced VEGFR-1 phosphorylation in Flt-1-transfected HEK293 cells. RO5323441 has antitumor activity .
HZD37-5 is a humanized monoclonal antibody specifically recognizing N78 loci of IL-17A. HZD37-5 binds to human and rhesus monkeys, blocks IL-17 induced signal transduction and the release of IL-6, IL-8, CXCL-1 and GM-GSF.HZD37-5 significantly inhibited human IL-17A induced-keratinocyte chemoattractant secretion. HZD37-5 can be used for the research of autoimmune diseases including psoriasis and psoriatic arthritis .
Rapamycin (Sirolimus; AY 22989) is a potent and specific blood-brain barrier-transmissible mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1 . Rapamycin is an autophagy activator, an immunosuppressant .
2-Methoxyestradiol (2-ME2), an orally active endogenous metabolite of 17β-estradiol (E2), is an apoptosis inducer and an angiogenesis inhibitor with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules. 2-Methoxyestradio, also a potent superoxide dismutase (SOD) inhibitor and a ROS-generating agent, induces autophagy in the transformed cell line HEK293 and the cancer cell lines U87 and HeLa .
Ajmaline (Cardiorythmine) is a sodium channel blocking, class 1A anti-arrhythmic agent. Ajmaline blocks HERG currents with an IC50 of 1 μM in HEKcells and 42.3 μM in Xenopus oocytes. Ajmaline can be used for the research of the ventricular tachyarrhythmia .
Simvastatin acid (Tenivastatin) ammonium is a potent HMG-CoA reductase (HMGCR) inhibitor. Simvastatin acid ammonium reduces Indoxyl sulfate-mediated reactive oxygen species (ROS) production in human cardiomyocytes. Simvastatin acid ammonium can also modulates OATP3A1 expression in cardiomyocytes and HEK293 cells transfected with the OATP3A1 gene .
Rapamycin (Standard) is the analytical standard of Rapamycin (HY-10219). This product is intended for research and analytical applications. Rapamycin (Sirolimus; AY 22989) is a potent and specific mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1 . Rapamycin is an autophagy activator, an immunosuppressant .
Galegine hydrochloride, a guanidine derivative, contributes to weight loss in mice. Guanidine hydrochloride is the compound derived from G. officinalis, which gave rise to the biguanides, metformin and phenformin. Galegine hydrochloride activates AMPK in 3T3-L1 adipocytes and L6 myotubes, as well as in the H4IIE rat hepatoma and HEK293 human kidney cell lines. Galegine hydrochloride has antibacterial activity, with minimum inhibitory concentration of 4 mg/L against Staphylococcus aureus strains .
Coptisine is an orally active and brain-penetrant alkaloid found in Coptis chinensis. Coptisine is a reversible, uncompetitive IDO inhibitor with a Ki of 5.8 μM and an IC50 of 6.3 μM. Coptisine suppresses neuroinflammation, reduces Aβ plaque burden and shows neuroprotective activity. Coptisine shows anti-inflammation activity by blocking NF-κB, MAPK, and PI3K/Akt activation. Coptisine inhibits cancer cells proliferation, induces DNA damage, G2/M phase cell cycle arrest, apoptosis, ROS production and mitochondrial dysfunction. Coptisine inhibits Rho/ROCK pathway activation, reduces arrhythmia, limits cardiac injury marker release, reduces infarct size, and preserves cardiac function in rat myocardial ischemia/reperfusion models. Coptisine downregulates HMGCR and upregulates LDLR and CYP7A1 to modulate cholesterol metabolism, reduces abnormal serum lipid levels, and promotes fecal bile acid excretion. Coptisine can be used for the research of cancer, hypercholesterolemia, Alzheimer’s disease, inflammatory disorders and cardiovascular disease .
Venturicidin A (Aabomycin A1), from actinomycetes, is a membrane-active natural product inhibitor of ATP synthase. Venturicidin A potentiates the aminoglycoside antibiotic gentamicin against multidrug-resistant clinical isolates of Staphylococcus, Enterococcus, and Pseudomonas aeruginosa. Venturicidin A shows noticeable toxicity toward human embryonic-kidney (HEK)cells with an IC50 of 31 μg/mL.
Deoxyandrographolide is an orally active lactone found in the Andrographis paniculata Nees. Deoxyandrographolide shows a KD of 38.4 μM of HDAC1. Deoxyandrographolide enhances GLUT4 plasma membrane translocation, activates PI3K and AMPK-dependent signaling pathways, suppresses fasting blood glucose, serum insulin, triglycerides, and LDL-cholesterol levels. Deoxyandrographolide enhances HDAC1 expression via inhibited ubiquitination degradation, represses H3K4me3, improves chromosome stability, and restrains aging biomarkers p16, p21, γH2A.X, p53 and ROS production. Deoxyandrographolide interacts with Foot-and-Mouth Disease Virus 3Cpro active site, inhibits protease and IFN-antagonist activity, derepresses ISG expression, and inhibits viral replication. Deoxyandrographolide can be used for the researches of type 2 diabetes mellitus, vascular senescenceand virus infection .
Soyasaponin Aa is a soyasaponin that can be found in soy. Soyasaponin Aa suppresses PPARγ transcriptional activity, reduces PPARγ and C/EBPα expression, inhibits adipocyte differentiation and lipid accumulation, and reduces adipogenic marker gene expression. Soyasaponin Aa reduces hydrogen peroxide-induced reactive oxygen species (ROS) production and malondialdehyde levels. Soyasaponin Aa exhibits cellular antioxidant activity. Soyasaponin Aa can be used for the research of obesity .
Melicopine is an alkaloid found in Z. simulans with antimalarial and anticancer activities. It exhibits inhibitory activity against chloroquine-sensitive 3D7 and chloroquine-resistant Dd2 strains of P. falciparum, with IC50 values of 29.7 and 33.7 µg/mL, respectively. Melicopine is cytotoxic to prostate cancer cells PC-3M and LNCaP (IC50 values of 47.9 and 37.8 µg/mL), but has no effect on non-cancerous HEK293 cells (IC50 greater than 100 µg/mL). Melicopine holds promise for research in anticancer and anti-infection fields .
Tembetarine chloride is a alkaloid that can be isolated from Tinospora cordifolia that exhibits antibacterial activity. Tembetarine chloride exhibits weak cytotoxicity against mouse fibroblasts (L929) and human embryonic kidney cells (HEK293) with IC50 of 1245.33 μg/mL and 1642.81 μg/mL, respectively .
Trans-2-butene-1,4-dicarboxylic acid (Standard) is the analytical standard of Trans-2-butene-1,4-dicarboxylic acid. This product is intended for research and analytical applications. Trans-2-butene-1,4-dicarboxylic acid (Dihydromuconic acid; trans-β-Hydromuconic acid) is an endogenous metabolite[1][2].
Ajmaline (Standard) is the analytical standard of Ajmaline. This product is intended for research and analytical applications. Ajmaline (Cardiorythmine) is a sodium channel blocking, class 1A anti-arrhythmic agent. Ajmaline blocks HERG currents with an IC50 of 1 μM in HEKcells and 42.3 μM in Xenopus oocytes. Ajmaline can be used for the research of the ventricular tachyarrhythmia .
OAT1/3-IN-2 (compound 8) is a dual inhibitor of OAT1 and OAT3. OAT1/3-IN-2 can reverse the toxicity of Cys-Hg on HEK-OAT1 cells (10 μM) and has a potential protective effect on the kidneys. OAT1/3-IN-2 can be used to study mercury-induced kidney damage .
OAT1/3-IN-1 (compound 7) is a dual inhibitor of OAT1 and OAT3. OAT1/3-IN-1 can reverse the toxicity of Cys-Hg on HEK-OAT1 cells (10 μM) and has a potential protective effect on the kidneys. OAT1/3-IN-1 can be used to study mercury-induced kidney damage .
Simvastatin acid (ammonium) (Standard) is the analytical standard of Simvastatin acid (ammonium). This product is intended for research and analytical applications. Simvastatin acid (Tenivastatin) ammonium is a potent HMG-CoA reductase (HMGCR) inhibitor. Simvastatin acid ammonium reduces Indoxyl sulfate-mediated reactive oxygen species (ROS) production in human cardiomyocytes. Simvastatin acid ammonium can also modulates OATP3A1 expression in cardiomyocytes and HEK293 cells transfected with the OATP3A1 gene .
6,8-Diprenylnaringenin (Lonchocarpol A; Senegalensin), a hop prenylflavonoid, is a inhibitor of breast cancer resistance protein (BCRP/ABCG2). 6,8-Diprenylnaringenin inhibits ABCG2-mediated efflux of Mitoxantrone, and 3H-Methotrexate transport (IC50=0.41 μM) in HEK293 cells. 6,8-Diprenylnaringenin exhibits some estrogenicity, but its potency is less than 1% of that of 8-Prenylnaringenin .
2-Methoxyestradiol (Standard) is the analytical standard of 2-Methoxyestradiol. This product is intended for research and analytical applications. 2-Methoxyestradiol (2-ME2), an orally active endogenous metabolite of 17β-estradiol (E2), is an apoptosis inducer and an angiogenesis inhibitor with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules. 2-Methoxyestradio, also a potent superoxide dismutase (SOD) inhibitor and a ROS-generating agent, induces autophagy in the transformed cell line HEK293 and the cancer cell lines U87 and HeLa .
Ajmaline hydrochloride is a Class Ia antiarrhythmic agent. It inhibits HERG potassium channels with IC50s of 1.0 μmol/l and 42.3 μmol/l in HEKcells and moth spider oocytes respectively. The inhibitory effect of Ajmaline hydrochloride is rapid, reversible, and positive frequency dependent. It acts primarily on the open state of the HERG channel and may also be combined with the inactivated state. The inhibitory effect of ajmaline hydrochloride is dependent on aromatic residues in the S6 domain, and the sensitivity is significantly reduced in the inactivation-deficient HERG S620T channel. It can also slightly affect the activation voltage of HERG channels. Ajmaline hydrochloride's inhibitory effect on HERG channels may contribute to both its potent antiarrhythmic effects and its potential proarrhythmic risk.
The TREM-1 protein is a key cell surface receptor that amplifies inflammatory responses in innate and adaptive immunity. Ligands such as PGLYRP1, HMGB1 or HSP70 activate TREM-1, leading to multimerization and complex formation with TYROBP/DAP12. TREM-1 Protein, Mouse (HEK293, His) is the recombinant mouse-derived TREM-1 protein, expressed by HEK293 , with C-6*His labeled tag.
TREM-2 protein forms a signaling complex with TYROBP, activates cells upon ligand binding, and acts as a receptor for amyloid beta, lipoproteins, and apolipoproteins. It promotes their uptake by microglia, triggering activation, proliferation, migration, apoptosis and cytokine expression. TREM-2 Protein, Cynomolgus (HEK293, His) is the recombinant cynomolgus-derived TREM-2 protein, expressed by HEK293 , with C-6*His labeled tag.
TREM-2 Protein is a receptor for amyloid beta protein 42, lipoprotein particles, and apolipoprotein. TREM-2 Protein is involved in cell proliferation and apoptosis through Wnt/β, MTOR, PI3K and NF-kappa-B signaling pathways. TREM-2 Protein is expressed by macrophages, immature monocyte-derived dendritic cells, osteoclasts, and microglia to activate the immune response. TREM-2 Protein, Human (HEK293, His) is the recombinant human-derived TREM-2 protein, expressed by HEK293 , with C-6*His labeled tag.
SREC-I/SCARF1 Protein acts as a multifunctional mediator, facilitating Ac-LDL binding and degradation, suggesting a role in lipid metabolism and adhesion. Involved in neurite-like outgrowth, it interacts with SREC2 and AVIL, forming a complex molecular network. The protein's diverse roles underscore its significance in various cellular processes beyond lipid metabolism. SREC-I/SCARF1 Protein, Human (HEK293, His) is the recombinant human-derived SREC-I/SCARF1 protein, expressed by HEK293 , with C-6*His labeled tag.
The TREM-1 protein is a cell surface receptor that critically regulates innate and adaptive immunity by enhancing inflammatory responses. TREM-1 plays a crucial role in acute and chronic inflammatory diseases, acting as a decoy receptor to balance its pro-inflammatory effects. TREM-1 Protein, Human (HEK293, His) is the recombinant human-derived TREM-1 protein, expressed by HEK293 , with C-6*His labeled tag.
Spondin-2 protein is a matricellular protein with antigen binding, lipopolysaccharide binding and metal ion binding activity. Spondin-2 is essential for recruiting lymphocytes and initiating immune responses while being involved in cell adhesion, defense response to other organism; opsonization; and positive regulation of cytokine production. Spondin-2 is found to promote infiltration of M1-like macrophages and inhibits tumor metastasis in cancer research. Spondin-2/SPON2 Protein, Human (HEK293, His) is the recombinant human-derived Spondin-2/SPON2 protein, expressed by HEK293 , with C-6*His labeled tag.
TREM-2 protein forms a signaling complex with TYROBP, activates cells upon ligand binding, and acts as a receptor for amyloid beta, lipoproteins, and apolipoproteins. It promotes their uptake by microglia, triggering activation, proliferation, migration, apoptosis and cytokine expression. TREM-2 Protein, Mouse (HEK293, His) is the recombinant mouse-derived TREM-2 protein, expressed by HEK293 , with C-6*His labeled tag.
CD94 protein is a key immune receptor for self-non-self discrimination. It forms a complex with KLRC1 or KLRC2 on lymphocyte subsets and recognizes HLA-E loaded with self-peptides. It allows cytotoxic cells to monitor MHC class I expression and promote self-tolerance. CD94 Protein, Human (HEK293, His) is the recombinant human-derived CD94 protein, expressed by HEK293 , with N-6*His labeled tag.
The FOLR1 protein is an important mediator of folate uptake, binding to folate and promoting the delivery of 5-methyltetrahydrofolate into cells. Studies show high affinity at neutral pH. FOLR1 Protein, Human (HEK293, His-Avi) is the recombinant human-derived FOLR1 protein, expressed by HEK293 , with C-Avi, C-His labeled tag.
FOLR1 is a folic acid receptor that binds to folic acid and reductive folic acid derivatives and promotes the entry of 5-methyltetrahydrofolate and folate analogs into the cell interior. FOLR1 enhances the stability and nuclear translocation of β-catenin through the EGFR/AKT/GSK3β axis, thereby promoting the proliferation and migration of laryngeal squamous cell carcinoma (LSCC). FOLR1 is highly expressed in a variety of tumors and is a potential prognostic and therapeutic target for many cancers. FOLR1 Protein, Cynomolgus/Rhesus Macaque (HEK293, His) is the recombinant cynomolgus, Rhesus Macaque-derived FOLR1 protein, expressed by HEK293 , with C-His labeled tag.
Spondin-2/SPON2 protein, as a cell adhesion molecule, plays a key role in promoting the adhesion and growth of hippocampal embryonic neurons.In addition to its role in neurodevelopment, SPON2 acts as a direct binder of bacteria and their components, functioning as an opsonin to promote phagocytosis of bacteria by macrophages.Spondin-2/SPON2 Protein, Human (Q9BUD6, HEK293, His) is the recombinant human-derived Spondin-2/SPON2 protein, expressed by HEK293 , with His labeled tag.
Linker for Activation of T-cells Family Member 2; Linker for Activation of B-cells; Membrane-Associated Adapter Molecule; Non-T-Cell Activation Linker; Williams-Beuren Syndrome Chromosomal Region 15 Protein; Williams-Beuren Syndrome Chromosomal Region 5 Protei
NTAL protein is critical for FCER1 downstream signaling in mast cells and is involved in BCR-mediated signaling in B cells and FCGR1-mediated signaling in myeloid cells. It acts as a molecular bridge, recruiting GRB2 upon phosphorylation, linking receptor activation to intracellular responses. NTAL Protein, Human (HEK293, His) is the recombinant human-derived NTAL protein, expressed by HEK293 , with C-6*His labeled tag.
Uteroglobin/SCGB1A1 protein has multiple binding abilities and can interact with phosphatidylcholine, phosphatidylinositol, PCB, and binds weakly to progesterone.As a potent phospholipase A2 inhibitor, its antiparallel homodimer structure is maintained by disulfide bonds.Uteroglobin/SCGB1A1 Protein, Mouse (HEK293, His) is the recombinant mouse-derived Uteroglobin/SCGB1A1 protein, expressed by HEK293 , with C-6*His labeled tag.
Uteroglobin; Clara cell phospholipid-binding protein; CCPBP; Clara cells 10 kDa secretory protein; CC10; Secretoglobin family 1A member 1; Urinary protein 1; UP-1; UP1; Urine protein 1; SCGB1A1; CCSP; UGB
Uteroglobin/SCGB1A1 Protein displays diverse binding, including phosphatidylcholine, phosphatidylinositol, polychlorinated biphenyls (PCB), and weakly binds progesterone. It acts as a robust inhibitor of phospholipase A2, structurally forming a disulfide-linked antiparallel homodimer. Controversy surrounds its interaction with LMBR1L, necessitating further investigation. Uteroglobin/SCGB1A1 Protein, Human (HEK293, His) is the recombinant human-derived Uteroglobin/SCGB1A1 protein, expressed by HEK293 , with C-6*His labeled tag.
TREML1 (triggering receptor expressed on myeloid cells, like 1) is a cell surface receptor that may play a role in innate and adaptive immune responses. When phosphorylated, TREML1 interacts with the proteins PTPN6 and PTPN11, suggesting that it may be involved in regulating signaling pathways related to immune processes. TREML1 Protein, Human (HEK293, His) is the recombinant human-derived TREML1 protein, expressed by HEK293 , with C-6*His labeled tag.
TREML2 protein acts as a cell surface receptor for SEMA6A and affects key intercellular signaling in cerebellar development. It regulates granule cell migration, coordinates actin cytoskeletal reorganization, and contributes significantly to axonal guidance in the central nervous system. TREML2 Protein, Mouse (HEK293, His) is the recombinant mouse-derived TREML2 protein, expressed by HEK293 , with C-6*His labeled tag.
TREML2 protein acts as a cell surface receptor, interacting with CD276 on T-cells to enhance T-cell activation and modulate immune responses, particularly in regulating T-cell activation during immune reactions. TREML2 Protein, Human (HEK293, Fc) is the recombinant human-derived TREML2 protein, expressed by HEK293 , with C-hFc labeled tag.
SLAM Family Member 7; CD2 Subset 1; CD2-Like Receptor-Activating Cytotoxic cells; CRACC; Membrane Protein FOAP-12; Novel Ly9; Protein 19A; CD319; SLAMF7; CS1
The CRACC/SLAMF7 protein is an autoligand receptor in the SLAM family that critically regulates immune cell activation and differentiation through homotypic or heterotypic interactions. It coordinates distinct immune responses, dependent on the presence or absence of the cytoplasmic linkers SH2D1A/SAP and/or SH2D1B/EAT-2. CRACC/SLAMF7 Protein, Rhesus Macaque (HEK293, His) is the recombinant Rhesus Macaque-derived CRACC/SLAMF7 protein, expressed by HEK293 , with C-6*His labeled tag.
REG1A Protein inhibits spontaneous calcium carbonate precipitation and is linked to neuronal sprouting in the brain. Additionally, it contributes to the regeneration of brain and pancreas tissues. REG-1 alpha/REG1A Protein, Human (HEK293, His) is the recombinant human-derived REG-1 alpha/REG1A protein, expressed by HEK293 , with C-6*His labeled tag.
FOLR1 Protein, binding to folate and reduced folic acid derivatives, facilitates their delivery into cells. It maintains high affinity under neutral pH but undergoes a conformational change upon endocytosis, reducing affinity and releasing folates in slightly acidic pH. Crucial for embryonic development, cell proliferation, and renal folate reabsorption. FOLR1 Protein, Mouse (HEK293, His) is the recombinant mouse-derived FOLR1 protein, expressed by HEK293 , with C-6*His labeled tag.
FOLR1 Protein, binding to folate and reduced folic acid derivatives, facilitates their delivery into cells. It maintains high affinity under neutral pH but undergoes a conformational change upon endocytosis, reducing affinity and releasing folates in slightly acidic pH. Crucial for embryonic development, cell proliferation, and renal folate reabsorption. FOLR1 Protein, Mouse (HEK293, Fc) is the recombinant mouse-derived FOLR1 protein, expressed by HEK293, with C-hFc labeled tag.
Rapamycin-d3 is the deuterium labeled Rapamycin. Rapamycin is a potent and specific mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1. Rapamycin is an autophagy activator, an immunosuppressant .
Rapamycin- 13C,d3 (Sirolimus- 13C,d3) is the 13C and deuterium labeled Rapamycin (HY-10219) . Rapamycin is a potent and specific mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1. Rapamycin is an autophagy activator, an immunosuppressant .
2-Methoxyestradiol-d5 is the deuterium labeled 2-Methoxyestradiol. 2-Methoxyestradiol (2-ME2), an orally active endogenous metabolite of 17β-estradiol (E2), is an apoptosis inducer and an angiogenesis inhibitor with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules. 2-Methoxyestradio, also a potent superoxide dismutase (SOD) inhibitor and a ROS-generating agent, induces autophagy in the transformed cell line HEK293 and the cancer cell lines U87 and HeLa .
2-Methoxyestradiol- 13C6 is the 13C-labeled 2-Methoxyestradiol. 2-Methoxyestradiol (2-ME2), an orally active endogenous metabolite of 17β-estradiol (E2), is an apoptosis inducer and an angiogenesis inhibitor with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules. 2-Methoxyestradio, also a potent superoxide dismutase (SOD) inhibitor and a ROS-generating agent, induces autophagy in the transformed cell line HEK293 and the cancer cell lines U87 and HeLa .
2-Methoxyestradiol- 13C,d3 is the 13C- and deuterium labeled 2-Methoxyestradiol. 2-Methoxyestradiol (2-ME2), an orally active endogenous metabolite of 17β-estradiol (E2), is an apoptosis inducer and an angiogenesis inhibitor with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules. 2-Methoxyestradio, also a potent superoxide dismutase (SOD) inhibitor and a ROS-generating agent, induces autophagy in the transformed cell line HEK293 and the cancer cell lines U87 and HeLa .
Simvastatin acid-d6 (Tenivastatin-d6) is deuterium labeled Simvastatin acid. Simvastatin acid (Tenivastatin), a hydrolysate of Simvastatin (HY-17502), is a HMG-CoA reductase (HMGCR) inhibitor. Simvastatin acid reduces Indoxyl sulfate-mediated reactive oxygen species (ROS) production in human cardiomyocytes. Simvastatin acid can also modulates OATP3A1 expression in cardiomyocytes and HEK293 cells transfected with the OATP3A1 gene .
Simvastatin acid-d6 (ammonium)mis the deuterium labeled Simvastatin acid ammonium. Simvastatin ammonium is an active metabolite of simvastatin lactone mediated by CYP3A4/5 in the intestinal wall and liver (pKa=5.5). Simvastatin ammonium reduces indoxyl sulfate-mediated reactive oxygen species and modulates OATP3A1 expression in cardiomyocytes and HEK293 cells transfected with the OATP3A1 gene .
Simvastatin acid-d9 ammonium is deuterated labeled Simvastatin acid ammonium (HY-119695A). Simvastatin acid (Tenivastatin) ammonium is a potent HMG-CoA reductase (HMGCR) inhibitor. Simvastatin acid ammonium reduces Indoxyl sulfate-mediated reactive oxygen species (ROS) production in human cardiomyocytes. Simvastatin acid ammonium can also modulates OATP3A1 expression in cardiomyocytes and HEK293 cells transfected with the OATP3A1 gene .
Rapamycin- 13C,d3-1 (Sirolimus- 13C,d3-1) is the deuterium labeled and 13C-labeled Rapamycin (HY-10219). Rapamycin (Sirolimus; AY 22989) is a potent and specific mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1 . Rapamycin is an autophagy activator, an immunosuppressant .
Fenoprofen- 13C6 (LILLY-53858- 13C6) sodium hydrate is the 13C labeled Fenoprofen (HY-B1456A).Fenoprofen (LILLY-53858) is a nonsteroidal anti-inflammatory agent (NSAID) and inhibits cyclooxygenase (COX). Fenoprofen is a melanocortin receptors (MCRs) positive allosteric modulator (PAM). Fenoprofen also increases ERK1/2 activation in HEK293T cells. Fenoprofen has anti-arthritic activities and can be used for the study of rheumatoid arthritis and osteoarthritis .
Antiproliferative agent-53-d3 (Compound C1) is an inhibitor for theta-mediated end joining (TMEJ) in HEK293 cell with an IC50 of 0.14 µM. Antiproliferative agent-53-d3 is the inhibitor for CYP2C19 and CYP2C9 with IC50 of 0.77 and 3.1 µM. Antiproliferative agent-53-d3 inhibits the proliferation of DNA repair-compromised cells, with IC50 of 8.1 µM for BRCA2 -/- DLD-1. Antiproliferative agent-53-d3 exhibits good pharmacokinetic characteristics in CD-1 mice .
Ketodarolutamide-d6 (BAY 1896953-d6) is the deuterium labeled Ketodarolutamide (HY-19337). Ketodarolutamide (ORM-15341) is a potent, high-affinity nonsteroidal competitive full antagonist of androgen receptor (AR). Ketodarolutamide displays a Ki value of 8 nM for rat wild-type AR and an IC50 value of 38 nM in AR-HEK293 cells . Ketodarolutamide inhibits testosterone-induced nuclear translocation of the AR and antagonizes both overexpressed and mutant ARs . Ketodarolutamide specifically suppresses the proliferation of AR-dependent prostate cancer cells and exhibits antitumor activity in models of castration-resistant prostate cancer (CRPC) . Ketodarolutamide is suitable for the mechanistic and therapeutic research of prostate cancer .
Ketodarolutamide-d3 (BAY 1896953-d3) is the deuterium labeled Ketodarolutamide (HY-19337). Ketodarolutamide (ORM-15341) is a potent, high-affinity nonsteroidal competitive full antagonist of androgen receptor (AR). Ketodarolutamide displays a Ki value of 8 nM for rat wild-type AR and an IC50 value of 38 nM in AR-HEK293 cells . Ketodarolutamide inhibits testosterone-induced nuclear translocation of the AR and antagonizes both overexpressed and mutant ARs . Ketodarolutamide specifically suppresses the proliferation of AR-dependent prostate cancer cells and exhibits antitumor activity in models of castration-resistant prostate cancer (CRPC) . Ketodarolutamide is suitable for the mechanistic and therapeutic research of prostate cancer .
DB008 is potent and selective PARP16 inhibitor with an IC50 value of 0.27 μM, containing an acrylamide electrophilic reagent. DB008 is membrane-permeable and marks PARP16 selectively . DB008 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Firefly Luciferase mRNA is a reporter mRNA that can be transfected into cells to express firefly luciferase protein. Firefly Luciferase mRNA induces cytotoxicity in cancer cells at low concentrations. In cancer cells, the expression level of luciferase shows a non-linear relationship with the dose of Firefly Luciferase mRNA. When combined with the H2S-responsive bioluminescent probe (H-Luc), Firefly Luciferase mRNA enables bioluminescence-based detection of endogenous hydrogen sulfide in non-transgenic NAFLD cell models and NAFLD mouse models. Firefly Luciferase mRNA can be used in studies related to non-alcoholic fatty liver disease .
CD63-1 aptamer sodium is a high-affinity and specific DNA aptamer targeting the CD63 protein (Kd: 38.71 nM). CD63-1 aptamer sodium efficiently binds to CD63-positive cells, including breast cancer MDA-MB-231 cells and CD63-overexpressing HEK293T cells, with moderate binding affinity (Kd~100 nM) as assessed by flow cytometry .
2-Hydrazinyl-adenosine is a synthetic intermediate. Derivatives of 2-Hydrazinyl-adenosine act as A2A adenosine receptor agonists. 2-Hydrazinyl-adenosine is used in the research of neurodegenerative diseases .
CD63-2 aptamer sodium is a high-affinity and specific DNA aptamer targeting the CD63 protein (Kd: 78.43 nM). CD63-1 aptamer sodium efficiently binds to CD63-positive cells, including breast cancer MDA-MB-231 cells and CD63-overexpressing HEK293T cells, with moderate binding affinity (Kd~100 nM) as assessed by flow cytometry .
Rapamycin (Sirolimus) (GMP) is Rapamycin (HY-10219) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Rapamycin (Sirolimus; AY 22989) is a potent and specific mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1 . Rapamycin is an autophagy activator, an immunosuppressant .
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Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
MedchemExpress Validation 03
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
MedchemExpress Validation 04
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
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