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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.
AT 1001 is a high-affinity and selective antagonist of the α3β4 nicotinic acetylcholine receptor (α3β4 nAChR) (Ki=2.64 nM). AT 1001 reversibly blocks inward currents induced by Epibatidine (HY-101078) in HEKcells transfected with α3β4 nAChR. AT-1001 dose-dependently inhibits nicotine self-administration behavior in rats without affecting food-reinforced responding. AT 1001 can be utilized in the research of nicotine addiction and smoking cessation therapies .
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 .
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 .
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 .
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 .
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 .
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 .
Praliciguat (IW-1973) is a potent and orally active soluble guanylate cyclase stimulator, enhances NO signaling, acts as a vasodilator. Praliciguat (IW-1973) stimulates sGC in HEK-293 cells with an EC50 of 197 nM .
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 .
MS049 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 .
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 .
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 .
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 .
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 .
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 .
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 .
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 .
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 .
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 .
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 .
(rel)-AR234960 is an active relative configuration of AR234960. AR234960, a non-peptide MAS (a G protein-coupled receptor) agonist, increases both mRNA and protein levels of CTGF via ERK1/2 signaling in HEK293-MAS cells and adult human cardiac fibroblasts .
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).
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 .
Amitifadine 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.
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 .
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 .
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).
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 .
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 .
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 .
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.
Fumagilin-105 is an autophagy targeting chimera (AUTOTAC) that induces p62 self-oligomerization with DC50 values of 0.7 μM for MetAP2 in HEK293 cells .
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 .
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 .
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 .
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 .
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.
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 .
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 HEK?293 cells, respectively. Alniditan dihydrochloride has migraine-preventive effects .
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 .
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 .
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 .
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 .
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 .
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.
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 .
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 .
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 .
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 .
Ketodarolutamide (ORM-15341) is a potent and full antagonist for human AR (hAR) with IC50 values of 38 nM as shown by transactivation assays in AR-HEK293 cells stably expressing full-length hAR and an androgen-responsive luciferase reporter gene construct.
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) .
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 .
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 .
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 .
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-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 .
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 .
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 .
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 .
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 .
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 .
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 .
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 .
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 .
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 .
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 .
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 .
(±)-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 .
ML67-33 is a selective activator of temperature- and mechano-sensitive K2P channels. ML67-33 rapidly and reversibly affects K2P2.1 (TREK-1) with EC50s of 36.3 μM and 9.7 μM in cell-free and HEK293 cells, respectively .
(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.
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 .
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 .
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.
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 .
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 .
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) .
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 .
Rapamycin (Standard) is the analytical standard of Rapamycin. 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 .
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 .
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 .
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 .
Fluoflavine (ML-090) is a selective NOX1 inhibitor with an IC50 of 90 nM. Fluoflavine has >100 selectivity for NOX1 over NOX2, NOX3, NOX4 (all IC50>10 μM). ML-090 has an IC50 of 360 nM in HEK293 cells .
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 .
RNA polymerase II-IN-2 (compound 20iii) is a potent RNA polymerase II (Pol II) inhibitor with Ki value of 9.5 nM. RNA polymerase II-IN-2 has cytotoxicity against cancer cells, and exhibits 2 and 5 fold toxicity than α-amanitin against CHO and HEK293 .
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) .
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 .
ST2-IN-1 (compound 31) is a Stimulation-2 (ST2) inhibitor, with an IC50 value of 7 μM in AlphaLISA assay, and 7.19 μM in HEK-Blue assay. ST2-IN-1 effectively attenuats the ST2/IL-33 signaling in human mast cells .
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 .
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 .
(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 .
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))
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 .
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 .
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 .
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 .
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 .
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 .
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 .
VU0529331 is a modestly selective non-GIRK1-containing G protein-gated, inwardly-rectifying, potassium channel (non-GIRK1/X) activator, with EC50s of 5.1 µM and 5.2 µM for GIRK2 and GIRK1/2 in HEK293 cells, respectively, also effective on GIRK4 homomeric channel .
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.
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 .
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 .
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 .
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 .
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 .
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.
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 shows potent antiproliferation activities on BxPC-3 and Capan-2 cells. STAT3-IN-25 has the potential for pancreatic cancer research .
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 .
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) .
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 .
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 .
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 .
OS-3-106 is a potent, BBB-penetrated 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 .
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 .
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 .
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.
(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 .
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 .
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 .
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[1].
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 .
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 HEK 293 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 .
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 .
2-Methoxyestradiol-d5 is the deuterium labeled 2-Hydroxyestradiol. 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[1][2][3][4][5][6][7].
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 .
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 .
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 .
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).
(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 .
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 .
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 .
Rapamycin- 13C,d3 (Sirolimus- 13C,d3; AY-22989- 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 .
(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 .
CB096 binds the 5′CGG/3′GGC internal loop structure of r(G4C2)exp RNA, interrupts its gain-of-function mechanism, and thus results in the regulation of nucleolar focusing, RNA splicing defects, RNA metabolism, nucleocytoplasmic transport dysfunction, and toxic dipeptide repeats (DPRs) generated by RNA translation. CB096 inhibits the RAN translation with an IC50 of 20 μM in HEK293T cells .
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 .
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- 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[1][2][3][4][5][6].
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[1][2][3][4][5][6].
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 .
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 .
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 .
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 .
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 .
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 .
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 .
(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 .
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 .
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 .
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 Degrader-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) .
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.
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 .
Ala-parafluoroPhe-Arg-Cha-Cit-Tyr-NH2 is a biological active peptide. (Protease activated receptor 1 (PAR-1) belongs to a subfamily of G-protein coupled receptors and is known to mediate the cellular effects of thrombin. This peptide is a PAR-1 selective agonist displaying a high level of specificity to PAR-1 over PAR-2. The specificity of peptide was evaluated in cell-based calcium signaling assay using HEK293 cells. PAR-1 selective agonists can be used to study PAR-1 activation in vivo. In addition to its varied cellular effects of thrombin, PAR-1 has also been shown to coordinate with PAR-4 and regulate thrombin-induced hepatocellular carcinoma harboring thrombin formation within the tumor environment classified as 'coagulation type'.)
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 .
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 .
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.
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.
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 .
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 has antiarrhythmic properties. KB130015 markedly slows the kinetics of inactivation of Na + channels. KB130015 opens large-conductance Ca 2+-activated K + channels and relaxes vascular smooth muscle .
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 .
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.
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 .
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 .
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 .
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 .
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 .
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 .
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 .
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 .
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 .
Ala-parafluoroPhe-Arg-Cha-Cit-Tyr-NH2 is a biological active peptide. (Protease activated receptor 1 (PAR-1) belongs to a subfamily of G-protein coupled receptors and is known to mediate the cellular effects of thrombin. This peptide is a PAR-1 selective agonist displaying a high level of specificity to PAR-1 over PAR-2. The specificity of peptide was evaluated in cell-based calcium signaling assay using HEK293 cells. PAR-1 selective agonists can be used to study PAR-1 activation in vivo. In addition to its varied cellular effects of thrombin, PAR-1 has also been shown to coordinate with PAR-4 and regulate thrombin-induced hepatocellular carcinoma harboring thrombin formation within the tumor environment classified as 'coagulation type'.)
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.
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 .
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.
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 .
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 .
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 .
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 .
Rapamycin (Standard) is the analytical standard of Rapamycin. 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 .
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 .
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 .
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 .
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 .
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 .
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 .
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 .
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. The total length of TREM-1 Protein, Mouse (HEK293, His) is 182 a.a., with molecular weight of ~38.0 kDa.
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. The total length of TREM-2 Protein, Cynomolgus (HEK293, His) is 156 a.a., with molecular weight of 28-40 kDa.
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 total length of SREC-I/SCARF1 Protein, Human (HEK293, His) is 402 a.a., .
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. The total length of Spondin-2/SPON2 Protein, Human (HEK293, His) is 305 a.a., with molecular weight of 38-42 kDa.
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.
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.
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. The total length of FOLR1 Protein, Human (HEK293, His-Avi) is 209 a.a., with molecular weight of 38-45 kDa.
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 (209a.a, HEK293, His) is the recombinant cynomolgus, Rhesus Macaque-derived FOLR1 protein, expressed by HEK293 , with C-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. The total length of NTAL Protein, Human (HEK293, His) is 217 a.a., with molecular weight of 35-40 kDa.
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.
The CLM9/CD300g protein is known as a receptor and is thought to be involved in mediating L-selectin-dependent lymphocyte rolling. This protein exhibits calcium-dependent binding to SELL (L-selectin ligand), indicating its ability to interact with lymphocytes and potentially influence lymphocyte-related processes. CLM9/CD300g Protein, Human (HEK293, His) is the recombinant human-derived CLM9/CD300g 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. The total length of Uteroglobin/SCGB1A1 Protein, Human (HEK293, His) is 70 a.a., with molecular weight of ~9.0 kDa.
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. The total length of TREML2 Protein, Mouse (HEK293, His) is 246 a.a., with molecular weight of 58-62 kDa.
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. The total length of TREML2 Protein, Human (HEK293, Fc) is 250 a.a., with molecular weight of 80-110 kDa.
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 (147a.a, HEK293, His) is the recombinant human-derived TREML1 protein, expressed by HEK293 , with C-6*His labeled tag. The total length of TREML1 Protein, Human (147a.a, HEK293, His) is 147 a.a., with molecular weight of ~20.0 kDa.
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. The total length of CRACC/SLAMF7 Protein, Rhesus Macaque (HEK293, His) is 204 a.a., with molecular weight of 30-50 kDa.
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. The total length of REG-1 alpha/REG1A Protein, Human (HEK293, His) is 144 a.a., with molecular weight of ~18.0 kDa.
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. The total length of FOLR1 Protein, Mouse (HEK293, His) is 208 a.a., with molecular weight of 33-37 kDa.
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 .
2-Methoxyestradiol-d5 is the deuterium labeled 2-Hydroxyestradiol. 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[1][2][3][4][5][6][7].
Rapamycin- 13C,d3 (Sirolimus- 13C,d3; AY-22989- 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 .
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 .
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[1].
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[1][2][3][4][5][6].
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[1][2][3][4][5][6].
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 .
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.
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 .
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 .
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