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Bimagrumab (Anti-ACVR2B Reference Antibody) is a human monoclonal antibody that blocks activin type II receptor (ActRII), with KDs of 1.7 pM and 434 pM for human ActRIIB and ActRIIA, respectively. Bimagrumab can be used for the research of pathological muscle loss and weakness .
Chroman 1 is a highly potent and selective ROCK inhibitor. Chroman 1 is more potent against ROCK2 (IC50=1 pM) than ROCK1 (IC50=52 pM). Chroman 1 also has inhibitory activity against MRCK, with an IC50 of 150 nM .
Lurbinectedin (PM01183) is a DNA minor groove covalent binder with potent anti-tumour activity; inhibits RMG1 and RMG2 cell growth with IC50 values of 1.25 and 1.16 nM, respectively.
Plitidepsin (Aplidine) is a potent anti-cancer agent by targeting eEF1A2 ( KD=80 nM) . Plitidepsin possesses antiviral activity and is against SARS-CoV-2 with an IC90 of 0.88 nM. Plitidepsin is usually used for multiple myeloma and advanced cancer research, and has the potential for COVID-19 research .
Ledipasvir (GS-5885) is an inhibitor of the hepatitis C virus NS5A, with EC50s of 34 pM and 4 pM against genotype 1a and 1b replicon, respectively. Ledipasvir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 1.62 μM .
Maridebart cafraglutide (AMG 133) is a long-acting peptide-antibody conjugate that combines GLP-1 receptor agonist with glucose-dependent insulinotropic polypeptide (GIP) receptor antagonism. Maridebart cafraglutide shows antagonist activity against human, cynomolgus monkey and rat GIPR with IC50 values of 46.4 nM, 26.5 nM, 822.3 nM, respectively. Maridebart cafraglutide shows agonist activity against human, cynomolgus monkey, rat and mouse GLP-1R with EC50 values of 24.4 pM, 5.7 pM, 2.4 pM and 123 pM, respectively. Maridebart cafraglutide can be used for the study of obesity and type 2 diabetes .
Pumitamig (PM-8002, BNT-327) is a bispecific antibody targeting PD-L1 and VEGF-A, with immune activation and anti-angiogenic activities. By binding to PD-L1, Pumitamig restores the function of effector T cells, while neutralizing VEGF-A in the tumor microenvironment to reverse its inhibition on the infiltration and activation of immune cells and normalize tumor blood vessels. Pumitamig can also be combined with various ADCs targeting TROP2, B7H3, HER2, HER3 for the research of advanced/metastatic solid tumors, including non-small cell lung cancer, ovarian cancer, triple-negative breast cancer, cervical cancer, etc. Pumitamig also exhibits potential efficacy in "cold" tumors with low PD-L1 expression that are insensitive to immunotherapy .
ITI-214 is a potent, CNS-active, orally bioavailable PDE1 inhibitor (Ki of 58 pM) with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters and ion channels. ITI-214 inhibits recombinant full-length human PDE1A, PDE1B and PDE1C with Kis of 33 pM, 380 pM and 35 pM, respectively. ITI-214 shows efficacy in various animal models of motor and cognitive functions .
Vedaprofen (Quadrisol) is a COX-1 selective nonsteroidal anti-inflammatory agent (NSAID) for serum TxB2 and exudate PGE2 inhibition . Vedaprofen is a Escherichia coli (E. coli) sliding clamp (SC) inhibitor with the IC50 of 222 μM .
Secnidazole (RP-14539) is an orally active azole antibiotic and a imidazole mitigator of Serratia marcescens virulence. Secnidazole, as an analog of acylhomoserine lactones, effectively inhibits QS resulting in the attenuation of Pseudomonas aeruginosa pathogenesis. Secnidazole has antimicrobial activity against many anaerobic Gram-negative and Gram-positive bacterial species in vitro. Secnidazole can be used for the research of various diseases, such as amoebiasis and giardiasis, and bacterial vaginitis .
Ombitasvir is a potent inhibitor of the hepatitis C virus protein NS5A, with EC50s of 0.82 to 19.3 pM against HCV genotypes 1 to 5, and 366 pM against genotype 6a.
Ecubectedin (PM14) is a derivative. Ecteinascidins is a family of tetrahydroisoquinoline alkaloids with wide range of antitumor and antimicrobial activities .
Militarine is a plant growth inhibitor and anti-inflammatory agent. Militarine inhibits the elongation of radicles and hypocotyls in seedlings of lettuce, Italian ryegrass and timothy grass. Militarine alleviates PM2.5-induced inflammatory injury and inhibits cell migration in human alveolar epithelial A549 cells by inhibiting the NF-κB signaling pathway, reducing oxidative stress and the release of inflammatory factors. Militarine can be used in studies related to PM2.5-induced pulmonary diseases .
JJKK 048 is a highly selective and potent monoacylglycerol lipase (MAGL) inhibitor with IC50 values of 214 pM, 275 pM and 363 pM for human, rat, and mouse MAGL. JJKK 048 displays low cross-reactivity with other endocannabinoid targets. JJKK 048 can be used in the research of diseases such as cancer, neurodegenerative diseases, and pain .
Ledipasvir acetone (GS-5885 acetone) is the active ingredient of Ledipasvir. Ledipasvir is an inhibitor of the hepatitis C virus NS5A, with EC50 values of 34 pM against GT1a and 4 pM against GT1b replicon.
PM-43I is a potent STAT6 inhibitor and can reduce STAT6 phosphorylation level. PM-43I can be used in allergic lung disease, allergic rhinitis, chronic pulmonary obstructive disease and cancer research [1].
alpha-2,3-Sialyltransferase (PmST2) is a sialyltransferase produced by Pasteurella multocida (Pm) and plays an important role in the pathogenesis of Pm. alpha-2,3-Sialyltransferase (PmST2) can be used to synthesize sialyllactosyl sphingosine (lyso-GM3) .
Florzolotau (APN1607) is a positron emission tomography (PET) ligand that can be used for the detection of Alzheimer's disease (AD) and other tau proteinopathies. Its binding sites are located in the β-sheet of paired helical filaments (PHFs) and straight filaments (SFs) of tau protein, as well as in the C-shaped cavity of SFs. In addition, APN-1607 binds to intraneuronal inclusions in Alzheimer's disease (AD), primary age-related tauopathy (PART) and posterior cortical atrophy (PCA). Florzolotau shows promise for PET imaging studies of neurological disorders, particularly tau proteinopathies .
PM-1, a derivative of Thioflavin-T (ThT; HY-D0218), is a small but highly specific plasma membrane (PM) fluorescent dye for specific and long-time membrane imaging of living and fixed cells. PM-1 is embedded directly into the cell membrane and exhibits a very long retention time on the plasma membrane with a half-life of approximately 15 h. PM-1 can be used in combination with protein labeling probes to study ectodomain shedding and endocytosis processes of cell surface proteins .
SAR441255 is a GLP-1R/GCGR/GIPR agonist, with human EC50 values of 1.03 pM, 1.01 pM, and 0.73 pM, respectively. SAR441255 stimulates receptor activity and drives cAMP accumulation. SAR441255 can be used for the research of type 2 diabetes, obesity .
Relacatib (SB-462795) is a novel, potent, and orally active inhibitor of human cathepsins K, L, and V with Ki values of 41 pM, 68 pM, and 53 pM, respectively. Relacatib inhibits endogenous cathepsin K in situ in human osteoclasts and human osteoclast-mediated bone resorption with IC50 values of 45 nM and 70 nM, respectively. Relacatib inhibits bone resorption in vitro in human tissue as well as in cynomolgus monkeys in vivo .
Tibulizumab (LY 3090106) is a tetravalent bispecific monoclonal antibody targeting B-cell activating factor (BAFF) and IL-17A with Kd values of 60 pM and 14 pM, respectively. Tibulizumab can be used for autoimmune disease research .
PM-81I is a potent STAT6 inhibitor (targeting the SH2 structural domain) that effectively reduces STAT6 phosphorylation levels. PM-81I can be used in studies of allergic lung disease, allergic rhinitis, chronic obstructive pulmonary disease or cancer [1].
Ramelteon metabolite M-II is the major metabolite of Ramelteon, with IC50s of 208 pM, 1470 pM for human melatonin receptors (MT1 or MT2). Ramelteon is a selective melatonin agonist.
Chroman 1 dihydrochloride is a highly potent and selective ROCK inhibitor. Chroman 1 dihydrochloride is more potent against ROCK2 (IC50=1 pM) than ROCK1 (IC50=52 pM).
Chroman 1 dihydrochloride also has inhibitory activity against MRCK, with an IC50 of 150 nM .
alpha-1,3-N-Acetylgalactosaminyltransferase (Pm1138) (EC 2.4.1.40(Pm1138)), also namely the ABO system transferase with glycosyl transferase activity .
pm26TGF-β1 TFA peptide is a peptide that mimics a portion of the human TGF-β1 molecule. pm26TGF-β1 peptide TFA shows high affinity for the TGF-β1 receptor. pm26TGF-β1 peptide TFA displays potent anti-inflammatory properties and does not exhibit neutrophils’ chemoattraction .
Protonstatin-1 is a selective plasma membrane (PM) H +-ATPase inhibitor (IC50 of 3.9 μM) that inhibits auxin transport. Protonstatin-1 interacts with the PM H +-ATPase central loop and may thus impede the functions of the N- and/or P-domain to inhibit the pump activity .
Pyrromethene 650 (PM650) is a green-fluorescent polar tracer dye. It is used for investigations of membrane fusion, lysis, and gap-junctional communication and to detect volume changes in cells or liposomes.
Photocaged DAP (pm-DAP) is a protected version of 2,3-Diaminopropionic acid (DAP) (HY-W013673). Photocaged DAP can produce 2,3-Diaminopropionic acid after photodeprotection. Photocaged DAP can be used as an intermediate to capture biosynthetic acylase .
Pyrromethene 605 (PM605) is a green-fluorescent polar tracer dye. It is used for investigations of membrane fusion, lysis, and gap-junctional communication and to detect volume changes in cells or liposomes.
Lurbinectedin-d3 is deuterium labeled Lurbinectedin. Lurbinectedin (PM01183) is a DNA minor groove covalent binder with potent anti-tumour activity; inhibits RMG1 and RMG2 cell growth with IC50 values of 1.25 and 1.16 nM, respectively .
Secnidazole (Standard) is the analytical standard of Secnidazole. This product is intended for research and analytical applications. Secnidazole (RP-14539) is an orally active azole antibiotic and a imidazole mitigator of Serratia marcescens virulence. Secnidazole, as an analog of acylhomoserine lactones, effectively inhibits QS resulting in the attenuation of Pseudomonas aeruginosa pathogenesis. Secnidazole has antimicrobial activity against many anaerobic Gram-negative and Gram-positive bacterial species in vitro. Secnidazole can be used for the research of various diseases, such as amoebiasis and giardiasis, and bacterial vaginitis .
Ledipasvir (GS-5885) hydrochloride is an inhibitor of the hepatitis C virus NS5A, with EC50s of 34 pM and 4 pM against genotype 1a and 1b replicon, respectively. Ledipasvir hydrochloride is also a SARS-CoV 3CL pro inhibitor with an IC50 of 1.62 μM .
(+)-PM 92131 is the active enantiomer of (±)-PM 92131 (HY-177437). (+)-PM 92131 is a non-nucleoside HIV-1 inhibitor. (+)-PM 92131 has an anti-HIV-1 activity with EC50s of 0.8 and 0.6 μM for HIV-1 RF strain in XTT cytoprotection and syncytium-forming assay, respectively. (+)-PM 92131 can be used for HIV infections research .
(±)-PM 92131 is a non-nucleoside HIV-1 inhibitor. (±)-PM 92131 has an anti-HIV-1 activity with IC50s of 45.7 and 53.8 μM for HIV-1 RF strain in XTT cytoprotection and syncytium-forming assay, respectively. (±)-PM 92131 can be used for HIV infections research .
Pyrromethene 556 (PM556) is a green-fluorescent polar tracer dye. It is used for investigations of membrane fusion, lysis, and gap-junctional communication and to detect volume changes in cells or liposomes.
DC1Sme, a DC1 derivative, exhibits IC50 values of 22 pM, 10 pM, 32 pM and 250 pM for Ramos, Namalwa, HL60/s and COLO 205 cancer cells, respectively. DC1, an analogue of the minor groove-binding DNA alkylator CC-1065, is a ADC Cytotoxin. DC1 can be used in synthesis of antibody-drug conjugates for the targeted treatment of cancer.
SAR441255 TFA is a GLP-1R/GCGR/GIPR agonist, with human EC50 values of 1.03 pM, 1.01 pM, and 0.73 pM, respectively. SAR441255 TFA stimulates receptor activity and drives cAMP accumulation. SAR441255 TFA can be used for the research of type 2 diabetes, obesity .
ITI-214 free base is a potent, CNS-active, orally bioavailable PDE1 inhibitor (Ki of 58 pM) with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters and ion channels. ITI-214 free base inhibits recombinant full-length human PDE1A, PDE1B and PDE1C with Kis of 33 pM, 380 pM and 35 pM, respectively. ITI-214 free base shows efficacy in various animal models of motor and cognitive functions .
Ledipasvir diacetone (GS-5885 diacetone) is the active ingredient of Ledipasvir. Ledipasvir is an inhibitor of the hepatitis C virus NS5A, with EC50 values of 34 pM against GT1a and 4 pM against GT1b replicon.
Ledipasvir-d6 hydrochloride is deuterated labeled Ledipasvir acetone (HY-15602A). Ledipasvir acetone (GS-5885 acetone) is the active ingredient of Ledipasvir. Ledipasvir is an inhibitor of the hepatitis C virus NS5A, with EC50 values of 34 pM against GT1a and 4 pM against GT1b replicon.
pm26TGF-β1 peptide is a peptide that mimics a portion of the human TGF-β1 molecule. pm26TGF-β1 peptide shows high affinity for the TGF-β1 receptor. pm26TGF-β1 peptide displays potent anti-inflammatory properties and does not exhibit neutrophils’ chemoattraction .
Zalypsis (PM00104) has anti-tumor activity. Zalypsis binds to DNA and shows cytotoxicity. Zalypsis inhibits cell cycle and transcription, and leads to double stranded DNA breaks .
Secnidazole-d6 is the deuterium labeled Secnidazole. Secnidazole (RP-14539;PM-185184) is an orally active azole antibiotic with a longer half-life than metronidazole (HY-B0318). Secnidazole is against the vaginosis-associated bacteria and has the potential for bacterial vaginosis research .
GS-6620 PM (Compound 2) is an analog of 2′-C-methyl 4-aza-7,9-dideaza adenosine. 2′-C-methyl 4-aza-7,9-dideaza adenosine is an inhibitor of HCV replication in cell culture. GS-6620 PM can be used in the study of hepatitis C virus (HCV) infection .
Plitidepsin (Standard) is the analytical standard of Plitidepsin. This product is intended for research and analytical applications. Plitidepsin (Aplidine) is a potent anti-cancer agent by targeting eEF1A2 ( KD=80 nM) . Plitidepsin possesses antiviral activity and is against SARS-CoV-2 with an IC90 of 0.88 nM. Plitidepsin is usually used for multiple myeloma and advanced cancer research, and has the potential for COVID-19 research .
DC10SMe is a DNA alkylator, can be used in the synthesis of antibody-drug conjugate (ADC). DC10SMe exhibits IC50s of 15 pM, 12 pM, and 12 pM for Ramos, Namalwa, and HL60/s cancer cells, respectively .
Deamino-NAD is a structural analog of NAD+ (HY-B0445). Deamino-NAD is involved in glycolysis as a substrate for rabbit muscle glyceraldehyde 3-phosphate dehydrogenase (GPDH), with a Km of 2300 pm, and a Kd of 112 pm .
PM534, tubulin targeting agent, inhibits tubulin assembly with IC50 values of 0.8-3.2 nM. PM534 binds to the colchicine site of tubulin, which has high antitumor activity .
PM226 is a selective cannabinoid CB2R agonist (Ki (CB2R)=13 nM; EC50 (CB2R)=39 nM; Ki (CB1R) >40 μM;) with neuroprotective properties in vitro and vivo .
PM20D1 Human Pre-designed siRNA Set A contains three designed siRNAs for PM20D1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
Kocurin (PM181104) is a thiazolyl cyclic-peptide antibiotic. Kocurin inhibits bacterial growth by impeding bacterial protein biosynthesis during the translation phase. Kocurin has strong inhibitory activity against Gram-positive bacteria, but no activity against fungi and Gram-negative bacteria .
Sialic acid aldolase (Pm NaNa) (EC 4.1.3.3) is a type I aldolase that catalyze the reversible aldol cleavage of N-acetylneuraminic acid (Neu5Ac) to form pyruvate and N-acetyl-D-mannosamine (ManNAc) with the equilibrium favoring the Neu5Ac cleavage .
Oligomycin D (Rutamycin A) is an antibiotic. Oligomycin D can be derived from a strain of S. rutgersensis. Oligomycin D also is a potent inhibitors of K-Ras PM localization. Oligomycin D can be used for the research of various cancers .
Photocaged DAP (pm-DAP) TFA is a protected version of 2,3-Diaminopropionic acid (DAP) (HY-W013673). Photocaged DAP TFA can produce 2,3-Diaminopropionic acid after photodeprotection. Photocaged DAP TFA can be used as an intermediate to capture biosynthetic acylase .
Secnidazole-d3 (RP-14539-d3; PM-185184-d3) is the deuterium labeled Secnidazole (HY-B1118). Secnidazole (RP-14539) is an orally active azole antibiotic and a imidazole mitigator of Serratia marcescens virulence. Secnidazole, as an analog of acylhomoserine lactones, effectively inhibits QS resulting in the attenuation of Pseudomonas aeruginosa pathogenesis. Secnidazole has antimicrobial activity against many anaerobic Gram-negative and Gram-positive bacterial species in vitro. Secnidazole can be used for the research of various diseases, such as amoebiasis and giardiasis, and bacterial vaginitis .
PRB1 Human Pre-designed siRNA Set A contains three designed siRNAs for PRB1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
Secnidazole- 13C2, 15N2 is the 13C2, 15N2 labeled Secnidazole. Secnidazole (RP-14539;PM-185184) is an orally active azole antibiotic with a longer half-life than metronidazole (HY-B0318). Secnidazole is against the vaginosis-associated bacteria and has the potential for bacterial vaginosis research.
Vedaprofen (Standard) is the analytical standard of Vedaprofen. This product is intended for research and analytical applications. Vedaprofen (Quadrisol) is a COX-1 selective nonsteroidal anti-inflammatory agent (NSAID) for serum TxB2 and exudate PGE2 inhibition . Vedaprofen is a Escherichia coli (E. coli) sliding clamp (SC) inhibitor with the IC50 of 222 μM .
Secnidazole (RP-14539) hemihydrate is an orally active azole antibiotic and a imidazole mitigator of Serratia marcescens virulence. Secnidazole hemihydrate, as an analog of acylhomoserine lactones, effectively inhibits QS resulting in the attenuation of Pseudomonas aeruginosa pathogenesis. Secnidazole hemihydrate has antimicrobial activity against many anaerobic Gram-negative and Gram-positive bacterial species in vitro. Secnidazole hemihydrate can be used for the research of various diseases, such as amoebiasis and giardiasis, and bacterial vaginitis .
Hongotoxin-1, isolated from venom of Centruroides limbatus, is the inhibitor of potassium channel, with IC50 for? Kv1.1, Kv1.2, Kv1.3, and Kv1.6 of 31 pM, 170 pM, 86 pM,and 6000 pM, respectively .
VU0652925, an analog of BMS986120, is a PAR4 antagonist, with IC50 values of 43 pM and 39.2 pM for PAC1 and P-selectin, respectively. VU0652925 is able to suppress GPIIbIIIa activation .
Deamino-NAD sodium is a structural analog of NAD+ (HY-B0445). Deamino-NAD sodium is involved in glycolysis as a substrate for rabbit muscle glyceraldehyde 3-phosphate dehydrogenase (GPDH), with a Km of 2300 pm, and a Kd of 112 pm .
Militarine (Standard) is the analytical standard of Militarine (HY-122308). This product is intended for research and analytical applications. Militarine is a plant growth inhibitor and anti-inflammatory agent. Militarine inhibits the elongation of radicles and hypocotyls in seedlings of lettuce, Italian ryegrass and timothy grass. Militarine alleviates PM2.5-induced inflammatory injury and inhibits cell migration in human alveolar epithelial A549 cells by inhibiting the NF-κB signaling pathway, reducing oxidative stress and the release of inflammatory factors. Militarine can be used in studies related to PM2.5-induced pulmonary diseases .
cMCoFx1 is a potent and selective FXIIa cyclic peptide inhibitor. cMCoFx1 has high binding affinity (KD: 900 pM) and inhibitory activity (Ki: 370 pM) for FXIIa. cMCoFx1 can effectively inhibit endogenous clotting pathways, and cMCoFx1 is stable in serum and non-cytotoxic .
Ombitasvir (Standard) is the analytical standard of Ombitasvir. This product is intended for research and analytical applications. Ombitasvir is a potent inhibitor of the hepatitis C virus protein NS5A, with EC50s of 0.82 to 19.3 pM against HCV genotypes 1 to 5, and 366 pM against genotype 6a.
Secnidazole-d4 is the deuterium labeled Secnidazole . Secnidazole (RP-14539) is an orally active azole antibiotic and a imidazole mitigator of Serratia marcescens virulence. Secnidazole, as an analog of acylhomoserine lactones, effectively inhibits QS resulting in the attenuation of Pseudomonas aeruginosa pathogenesis. Secnidazole has antimicrobial activity against many anaerobic Gram-negative and Gram-positive bacterial species in vitro. Secnidazole can be used for the research of various diseases, such as amoebiasis and giardiasis, and bacterial vaginitis .
PM54 is an antitumor agent with activity across multiple cancer types. PM54 acts as a transcription and WNT/β-catenin signaling pathway inhibitor. PM54 suppresses oncogenic transcriptional programs, and key malignant pathways, while inducing DNA double-strand breaks, S-phase cell cycle arrest and apoptosis. PM54 enhances innate immune recognition, remodels the tumor microenvironment. PM54 exhibits antitumor activity as monotherapy or in combination in xenograft models. PM54 is applicable to research on various cancers and advanced solid tumors .
JJKK 048 (Standard) is the analytical standard of JJKK 048 (HY-108613). This product is intended for research and analytical applications. JJKK 048 is a highly selective and potent monoacylglycerol lipase (MAGL) inhibitor with IC50 values of 214 pM, 275 pM and 363 pM for human, rat, and mouse MAGL. JJKK 048 displays low cross-reactivity with other endocannabinoid targets. JJKK 048 can be used in the research of diseases such as cancer, neurodegenerative diseases, and pain .
UTG-4 is a GLP-1R, GIPR, and GCGR agonist with EC50 values of 126.3 pM, 29.2 pM, and 250.2 pM, respectively. UTG-4 binds to HSA (Kd = 14.6 μM). UTG-4 effectively alleviates endothelial-mesenchymal transition. UTG-4 promotes weight loss, inhibits food intake, improves glucose tolerance, and has a significant anti-atherosclerotic effect .
(+)-Niguldipine is a potent dual inhibitor targeting L-type Ca 2+ channels (Ki=85 pM) and α₁-adrenoceptor (Ki=52 pM). (+)-Niguldipine is promising for research of hypertension and cardiovascular diseases .
Relacatib (Standard) is the analytical standard of Relacatib (HY-10294). This product is intended for research and analytical applications. Relacatib (SB-462795) is a novel, potent, and orally active inhibitor of human cathepsins K, L, and V with Ki values of 41 pM, 68 pM, and 53 pM, respectively. Relacatib inhibits endogenous cathepsin K in situ in human osteoclasts and human osteoclast-mediated bone resorption with IC50 values of 45 nM and 70 nM, respectively. Relacatib inhibits bone resorption in vitro in human tissue as well as in cynomolgus monkeys in vivo .
(E/Z)-Florzolotau ((E/Z)-APN1607) is a mixed configuration or unspecified configuration of Florzolotau (HY-137557). Florzolotau (APN1607) is a positron emission tomography (PET) ligand that can be used for the detection of Alzheimer's disease (AD) and other tau proteinopathies. Its binding sites are located in the β-sheet of paired helical filaments (PHFs) and straight filaments (SFs) of tau protein, as well as in the C-shaped cavity of SFs. In addition, APN-1607 binds to intraneuronal inclusions in Alzheimer's disease (AD), primary age-related tauopathy (PART) and posterior cortical atrophy (PCA). Florzolotau shows promise for PET imaging studies of neurological disorders, particularly tau proteinopathies .
Clesrovimab (MK1654) is a humanized IgG1 monoclonal antibody targeting the respiratory syncytial virus (RSV) protein F. Clesrovimab binds to pre-fusion and post-fusion forms of RSV-A fusion protein with high affinity, with corresponding KD values of 71 pM and 480 pM, respectively. Clesrovimab is applicable for the research of RSV infection .
MEDI7814 is a humanized monoclonal antibody inhibitor targeting C5a and C5adesArg. MEDI7814 binds to recombinant human C5a and serum purified human C5a with affinities of 14 pM and 8 pM, respectively. MEDI7814 is acute inflammatory diseases such as sepsis and renal ischemia-reperfusion injury .
Ramelteon metabolite M-II-d3 is the deuterium labeled Ramelteon metabolite M-II. Ramelteon metabolite M-II is the major metabolite of Ramelteon, with IC50s of 208 pM, 1470 pM for human melatonin receptors (MT1 or MT2). Ramelteon is a selective melatonin agonist .
MJ15 is a potent and selective CB1 receptor antagonist with a Ki of 27.2 pM and an IC50 of 118.9 pM for rat CB1 receptors. MJ15 exhibits potency in obesity and hyperlipidemia models. MJ15 inhibits food intake and increases in body weight in diet-induced obese rats and mice .
Zimberelimab (GLS-010) is a fully human IgG4 anti-PD-1 monoclonal antibody with an EC50 of 210 pM for human PD-1. Zimberelimab effectively blocks the binding of PD-L1 and PD-L2 to cell-surface PD-1 in CHO-S cells, with IC50 values of 580 pM and 670 pM, respectively. Zimberelimab shows antitumor activities, and can be used for various cancers research, including cervical cancer, non-small cell lung cancer and classical Hodgkin’s lymphoma .
CE-355621 is a humanized anti-c-Met IgG1 monoclonal antibody. CE-355621 can effectively bind with human c-Met (KD = 200 pM, IC50 = 466 pM) in A549 cells and cyno c-Met (KD = 610 pM) in cynomolgus kidney cells. CE-355621 inhibits the c-Met signaling pathway by blocking HGF binding. CE-355621 significantly inhibits the growth of tumors dependent on the c-Met/HGF pathway. CE-355621 can be used for research on cancer such as glioblastoma and gastric cancer .
Conbercept (KH902) is a recombinant fusion protein composed of VEGFR-1 (second domain) and VEGFR-2 (third and fourth domains) regions fused to human IgG1 Fc. Conbercept is a VEGF inhibitor (IC50 = 8.8 pM) and is a soluble receptor decoy that blocks all isoforms of VEGF-A (Kd = 0.5 pM), VEGF-B (Kd = 8 pM), VEGF-C, and PlGF (Kd = 5 pM). Conbercept has anti-inflammatory effects, can lower the levels of VEGF, TNF-α and IL-6, and reduce the infiltration of inflammatory cells. Conbercept decreases tumor growth in several oncology studies. Conbercept can be used for various eye diseases such as polypoidal choroidal vasculopathy (PCV), diabetic macular edema (DME) and pathologic myopia choroidal neovascularization (pmCNV) .
N-0920 is a potent TMPRSS2 inhibitor with an IC50 of 0.35 nM. N-0920 effectively inhibits SARS-CoV-2 variants EG.5.1 and JN.1 entry in Calu-3 cells, with picomolar EC50s values of 300 pM and 90 pM, respectively .
Devazepide (L-364,718) is a potent, competitive, selective and orally active nonpeptide antagonist of cholecystokinin (CCK) receptor, with IC50s of 81 pM, 45 pM and 245 nM for rat pancreatic, bovine gallbladder and guinea pig brain CCK receptors, respectively. Devazepide (L-364,718) is effective for gastrointestinal disorders .
HIV-1 protease-IN-6 (compound 17d) is a potent HIV-1 protease inhibitor, with an IC50 of 21 pM and a Ki of 4.7 pM, respectively. HIV-1 protease-IN-6 exhibits potent antiviral activity to DRV (darunavir)-resistant variant, even more than wild type virus .
Ledipasvir-d6 is the deuterium labeled Ledipasvir. Ledipasvir (GS-5885) is an inhibitor of the hepatitis C virus NS5A, with EC50s of 34 pM and 4 pM against genotype 1a and 1b replicon, respectively. Ledipasvir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 1.62 μM .
Razuprotafib (AKB-9778) sodium is a potent and selective inhibitor of the catalytic activity of VE-PTP (vascular endothelial protein tyrosine phosphatase) with an IC50of 17 pM. Razuprotafib sodium promotes TIE2 activation, enhances ANG1-induced TIE2 activation, and stimulates phosphorylation of signaling molecules in the TIE2 pathway, including AKT, eNOS, and ERK. Razuprotafib sodium inhibits the structurally related phosphatase PTP1B with an IC50 of 780 nM. Razuprotafib sodium shows excellent selectivity for VE-PTP versus a variety of phosphatases, with the exception of HPTPη (IC50=36 pM) and HPTPγ (100 pM) .
Razuprotafib (AKB-9778) is a potent and selective inhibitor of the catalytic activity of VE-PTP (vascular endothelial protein tyrosine phosphatase) with an IC50of 17 pM. Razuprotafib promotes TIE2 activation, enhances ANG1-induced TIE2 activation, and stimulates phosphorylation of signaling molecules in the TIE2 pathway, including AKT, eNOS, and ERK. Razuprotafib inhibits the structurally related phosphatase PTP1B with an IC50 of 780 nM. Razuprotafib shows excellent selectivity for VE-PTP versus a variety of phosphatases, with the exception of HPTPη (IC50=36 pM) and HPTPγ (100 pM) .
Dasatinib (BMS-354825) monohydrate is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib monohydrate inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively . Dasatinib monohydrate also induces apoptosis and autophagy.
JNJ-55920839 (CNTO-6358) is a fully human immunoglobulin G1κ monoclonal antibody and a selective Interferonα/ω neutralizer, with a Kd value of 0.9-10.7 pM against hIFNα and a Kd of 1.44 pM against IFNω. JNJ-55920839 can be used in research related to systemic lupus erythematosus .
Dasatinib (BMS-354825) hydrochloride is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib hydrochloride inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively . Dasatinib hydrochloride also induces apoptosis and autophagy.
PRRSV-IN-1 (Compound 4s) is a nsp4 protease inhibitor targeting PRRSV, exhibiting an EC50 of 0.45 μM against PRRSV. It binds to the nsp4 protease with a Kd value of 29.24 pM and inhibits nsp4 protease activity with an IC50 of 80.36 pM. PRRSV-IN-1 can be used for research in the field of antiviral infections .
SYK-1106 is a potent delta-opioid receptor (DOR) agonist with an EC50 of 89 pM and a Ki of 848 pM. SYK-1106 is selective for μ and κ opioid receptors, with Ki values of 9.54 nM and 2.45 nM, respectively. SYK-1106 induces dose-dependent antidepressant-like effects. SYK-1106 can be used for the research of depression .
Cotadutide (MEDI0382) is a potent dual agonist of glucagon-like peptide-1 (GLP-1) and GCGR with EC50 values of 6.9 pM and 10.2 pM, respectively. Cotadutide exhibits ability to facilitate both weight loss and glycaemic control, and alleviate fibrosis. Cotadutide can be used in the research of obesity and type 2 diabetes (T2D) .
Cotadutide (MEDI0382) acetate is a potent dual agonist of glucagon-like peptide-1 (GLP-1) and GCGR with EC50 values of 6.9 pM and 10.2 pM, respectively. Cotadutide acetate exhibits ability to facilitate both weight loss and glycaemic control, and alleviate fibrosis. Cotadutide acetate can be used in the research of obesity and type 2 diabetes (T2D) .
Lonaprisan (ZK 230211; BAY86 5044) is an antagonist for progesterone receptor, with IC50 of 3.6 pM and 2.5 pM for PR-A and PR-B, respectively. Lonaprisan exhibits antiprogestagenic activity in rabbits, interrupts early pregnancy in rats, and exhibits antitumor efficacy against DMBA (HY-W011845)-induced mammary tumor. Lonaprisan reveals antiglucocorticoid and antiandrogenic effect .
Reslizumab (Sch 55700) is humanized monoclonal antibodies that target interleukin-5 (IL-5) for the treatment of eosinophilic asthma. Reslizumab is effective in neutralizing the function of IL-5. Reslizumab has high binding affinity for human IL-5, with KD values of 109 pM and 4.3 pM in the the Biacore surface plasmon resonance and Kinetic Exclusion Assay, respectively .
Aprotinin is a bovine pancreatic trypsin inhibitor (BPTI) inhibitor which inhibits trypsin and chymotrypsin with Kis of 0.06 pM and 9 nM, respectively.
Ledipasvir-d16 (GS-5885-d16) is deuterium labeled Ledipasvir. Ledipasvir (GS-5885) is an inhibitor of the hepatitis C virus NS5A, with EC50s of 34 pM and 4 pM against genotype 1a and 1b replicon, respectively. Ledipasvir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 1.62 μM .
Risankizumab (BI 655066) is a humanised IgG monoclonal antibody, targeting IL-23 p19 subunit (Kd <10 pM) and inhibiting IL-17 production induced by human IL-23 in mouse splenocytes (IC50 = 2 pM). Risankizumab can be used to research immunological and inflammatory disorders such as psoriasis vulgaris, psoriatic arthritis, generalized pustular psoriasis and erythrodermic psoriasis .
NAMPT inhibitor-linker 2 is a agent-linker conjugates for ADC, composed of an NAMPT inhibitor as a payload, and a linker. ADC-4 consists of an NAMPT inhibitor-linker 2 and an anti-c-Kit monoclonal antibody, exihibits potent activity against c-Kit expressing cell lines such as GIST-T1 and NCI-H526, with IC50s of <7 pM and 40 pM, respectively.
NAMPT inhibitor-linker 1 is a agent-linker conjugates for ADC, composed of an NAMPT inhibitor as a payload, and a linker. ADC-3 consists of an NAMPT inhibitor-linker 1 and an anti-c-Kit monoclonal antibody, exihibits potent activity against c-Kit expressing cell lines such as GIST-T1 and NCI-H526 cells, with IC50s of <3 pM and 9 pM, respectively.
Devazepide (Standard) is the analytical standard of Devazepide. This product is intended for research and analytical applications. Devazepide (L-364,718) is a potent, competitive, selective and orally active nonpeptide antagonist of cholecystokinin (CCK) receptor, with IC50s of 81 pM, 45 pM and 245 nM for rat pancreatic, bovine gallbladder and guinea pig brain CCK receptors, respectively. Devazepide (L-364,718) is effective for gastrointestinal disorders .
Dasatinib (BMS-354825) is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively. Dasatinib also induces apoptosis and autophagy, and can cross the blood-brain barrier .
Atz-L5 is a PD-L1PTAC (PSMA-targeted chimera) degrader (DC50: 18 pM in PC3-PIP cells; 2 pM in LNCaP cells) and LYTAC. Atz-L5 promotes lysosomal degradation of PD-L1 in PSMA-positive prostate cancer cells. Atz-L5 is applicable to the research of prostate cancer .
Corthrombin (CVS 995) is a potent alpha-keto-amide thrombin inhibitor with Ki of 1 pM. Corthrombin can be used for the research of cardiovascular disease .
Elpipodect (MK-8189) is an orally active and selective PDE10A inhibitor with a Ki value of 29 pM. Elpipodect can be used in research of schizophrenia .
Edonentan (BMS 207940) hydrate is a potent and selective antagonist of the endothelin A (ETA) receptor, with a Ki of 10 pM. In rats, Edonentan has superior (100%) oral bioavailbility .
Razuprotafib (Standard) is the analytical standard of Razuprotafib (HY-109041). This product is intended for research and analytical applications. Razuprotafib (AKB-9778) is a potent and selective inhibitor of the catalytic activity of VE-PTP (vascular endothelial protein tyrosine phosphatase) with an IC50of 17 pM. Razuprotafib promotes TIE2 activation, enhances ANG1-induced TIE2 activation, and stimulates phosphorylation of signaling molecules in the TIE2 pathway, including AKT, eNOS, and ERK. Razuprotafib inhibits the structurally related phosphatase PTP1B with an IC50 of 780 nM. Razuprotafib shows excellent selectivity for VE-PTP versus a variety of phosphatases, with the exception of HPTPη (IC50=36 pM) and HPTPγ (100 pM) .
Mirikizumab (LY3074828) is a humanized IgG4 monoclonal antibody that targets the p19 subunit of interleukin 23 (IL-23). Mirikizumab binds to human and monkey IL-23 with high affinity, with Kd values of 21 pM and 55 pM, respectively. By inhibiting the binding of IL-23 to IL-23R, Mirikizumab modulates the immune response and holds potential for research in ulcerative colitis and Crohn's disease .
Margatoxin, an alpha-KTx scorpion toxin, is a high affinity inhibitor of Kv1.3 (Kd=11.7 pM). Margatoxin inhibits the Kv1.2 (Kd=6.4 pM) and Kv1.1 (Kd=4.2 nM). Margatoxin, a 39 amino-acid-long peptide, is isolated from the venom of the scorpion Centruroides margaritatus and widely used in ion channel research .
MJ15 (Standard) is the analytical standard of MJ15 (HY-103327). This product is intended for research and analytical applications. MJ15 is a potent and selective CB1 receptor antagonist with a Ki of 27.2 pM and an IC50 of 118.9 pM for rat CB1 receptors. MJ15 exhibits potency in obesity and hyperlipidemia models. MJ15 inhibits food intake and increases in body weight in diet-induced obese rats and mice .
Antifungal agent 132 (compound 25) is a selective and potent antifungal agent. Antifungal agent 132 inhibits Cryptococcus neoformans May1 with a Ki of 180 pM .
Dasatinib (monohydrate) (Standard) is the analytical standard of Dasatinib (monohydrate). This product is intended for research and analytical applications. Dasatinib (BMS-354825) monohydrate is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib monohydrate inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively . Dasatinib monohydrate also induces apoptosis and autophagy.
Dasatinib (Standard) is the analytical standard of Dasatinib. This product is intended for research and analytical applications. Dasatinib (BMS-354825) is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively . Dasatinib also induces apoptosis and autophagy.
Dasatinib (hydrochloride) (Standard) is the analytical standard of Dasatinib (hydrochloride). This product is intended for research and analytical applications. Dasatinib (BMS-354825) hydrochloride is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib hydrochloride inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively . Dasatinib hydrochloride also induces apoptosis and autophagy.
IBG3 is a Molecular glue degrader targeting BRD2 and BRD4, with DC50 values of 8.6 pM and 6.7 pM, respectively. IBG3 binds simultaneously to the tandem bromodomains of BRD2/BRD4, induces intramolecular conformational changes, enhances the affinity of BRD2/BRD4 for DCAF16, and promotes ubiquitination and degradation. IBG3 is applicable to the research of chronic myeloid leukemia .
Margatoxin TFA, an alpha-KTx scorpion toxin, is a high affinity inhibitor of Kv1.3 (Kd=11.7 pM). Margatoxin TFA inhibits the Kv1.2 (Kd=6.4 pM) and Kv1.1 (Kd=4.2 nM). Margatoxin TFA, a 39 amino-acid-long peptide, is isolated from the venom of the scorpion Centruroides margaritatus and widely used in ion channel research .
Dasatinib (monohydrate) (Standard) is the analytical standard of Dasatinib (monohydrate). This product is intended for research and analytical applications. Dasatinib (BMS-354825) monohydrate is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib monohydrate inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively . Dasatinib monohydrate also induces apoptosis and autophagy.
VTP50469 fumarate is a potent, highly selective and orally active Menin-MLL interaction inhibitor with a Ki of 104 pM. VTP50469 fumarate has potently anti-leukemia activity .
Pinometostat (Standard) is the analytical standard of Pinometostat. This product is intended for research and analytical applications. Pinometostat (EPZ-5676) is a potent DOT1L histone methyltransferase inhibitor with a Ki of 80 pM.
VTP50469 is a potent, highly selective and orally active Menin-MLL interaction inhibitor with a Ki of 104 pM. VTP50469 has potently anti-leukemia activity .
Tebanicline dihydrochloride (Ebanicline dihydrochloride) is a nAChR modulator with potent, orally effective analgesic activity. It inhibits the binding of cytisine to α4β2 neuronal nAChRs with a Ki of 37 pM .
Pentostatin (Standard) is the analytical standard of Pentostatin. This product is intended for research and analytical applications. Pentostatin (CI-825; Deoxycoformycin) is an irreversible inhibitor of adenosine deaminase with Ki of 2.5 pM.
Cendakimab (RPC4046; ABT 308; CC-93538) is a selective, humanized, recombinant monoclonal antibody against the IL-13 molecule. Cendakimab has a high affinity and potency for both human wild-type and variant IL-13 and blocks binding of IL-13 to both IL-13Rα1 and IL-13Rα2 with IC50s of 352 pM and 631 pM by ELISA, respectively. Cendakimab recognizes both wild-type human IL-13 and the common polymorphic variant R110Q, with binding affinities of 52 and 50 pM, respectively. Cendakimab has the potential for IL-13-related allergic/inflammatory diseases (e.g., asthma and eosinophilic esophagitis) .
Povetacicept (ALPN-303) is an engineered Fc fusion protein containing the TACI domain, and acts as a dual APRIL/BAFF antagonist. The Kd value of Povetacicept for human BAFF is 59.3 pM, while its Kd value for human APRIL is 1.00 pM. Povetacicept reduces the activation, proliferation, differentiation and survival of B cells, and inhibits the production of immunoglobulins and autoantibodies. Povetacicept can be used in research related to autoimmune hemolytic anemia, immune thrombocytopenia, systemic lupus erythematosus, lupus nephritis and myasthenia gravis .
7α, 25-dihydroxycholesterol (7α,25-OHC) is a potent and selective agonist and endogenous ligand of the orphan GPCR receptor EBI2 (GPR183). 7α, 25-dihydroxycholesterol is highly potent at activating EBI2 (EC50=140 pM; Kd=450 pM). 7α, 25-dihydroxycholesterol can serve as a chemokine directing migration of B cells, T cells and dendritic cells .
Dasatinib-d4 (BMS-354825-d4) is deuterium labeled Dasatinib. Dasatinib (BMS-354825) is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively . Dasatinib also induces apoptosis and autophagy.
Nrf2 activator 18 (Compound 11a) is an orally active activator for Keap1/Nrf2/HO-1 signaling pathway, that promotes the Nrf2 nuclear translocation, and enhances the antioxidant efficacy. Nrf2 activator 18 inhibits the release of IL-6 with an IC50 of 4.816 μM. Nrf2 activator 18 exhibits anti-inflammatory efficacy in mouse PM2.5-induced lung injury model .
21-Hydroxyoligomycin A is a potent inhibitor of K-Ras PM localization with an IC50 value of 4.82 nM. 21-Hydroxyoligomycin A has cytotoxicity and can be isolated from Streptomyces .
GNE7599 is a high-affinity and orally active von Hippel-Lindau (VHL) ligand with a Kd of 540 pM. GNE7599 can be connected to the ligand for protein by a linker to form PROTACs .
Tebanicline hydrochloride (Ebanicline hydrochloride) is a nAChR modulator with potent, orally effective analgesic activity. Tebanicline hydrochloride inhibits the binding of cytisine to α4β2 neuronal nAChRs with a Ki of 37 pM .
Aprepitant (Standard) is the analytical standard of Aprepitant. This product is intended for research and analytical applications. Aprepitant (MK-0869) is a selective and high-affinity neurokinin 1 receptor antagonist with a Kd of 86 pM.
ASN06917370 is a former orphan receptor GPR17 ligand for the study of neurodegenerative diseases. ASN06917370 has an EC50 of 268 pM in [35S]GTPyS experiments .
MRTX-1257 is a selective, irreversible, covalent and orally active KRAS G12C inhibitor, with an IC50 of 900 pM for KRAS dependent ERK phosphorylation in H358 cells .
Frunevetmab (NV-02) is a felinized anti-nerve growth factor (NGF) monoclonal antibody with a Kd of 20 pM. Frunevetmab can effectively decrease osteoarthritis (OA) pain in cats .
Fluopipamine is an antagonist for Cellulose Synthase 1 (CESA1) with an IC50 of 0.78 μM. Fluopipamine leads a decrease in glucose uptake into cellulose and hyperaccumulation of CESAs at the PM in etiolated Arabidopsis seedlings .
Brolucizumab (DLX1008) is a single-chain anti-VEGF-A antibody fragment with low picomolar affinity (KD=1.05 pM). Brolucizumab can be used for the research of cancer .
PSMA-1092 is a fluorescence probe targeting prostate-specific membrane antigen (PSMA) with a Ki of 80 pM. PSMA-1092 can be used for tumor localization and imaging, such as prostate cancer .
Y-05460M-A is a substituted isocoumarin antibiotic. Y-05460M-A exhibits inhibitory activity against Gram-positive and Gram-negative bacteria. Y-05460M-A is cytotoxic against P388 lymphatic leukemia. Y-05460M-A also has antiulcer activity. Y-05460M-A is a one-carbon lower homologue of PM-04128. Y-05460M-A can be achieved from N-Boc-L-valine .
Dasatinib (BMS-354825) (GMP) is a GMP-grade Dasatinib (HY-10181). GMP-grade small molecules can be used as adjuvant agents in cell therapy. Dasatinib (BMS-354825) is an orally active, ATP-competitive, dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Ki values for Src and Bcr-Abl are 16 pM and 30 pM, respectively. Dasatinib inhibits Bcr-Abl and Src with IC50 values of less than 1.0 nM and 0.5 nM, respectively. Dasatinib also induces apoptosis and autophagy .
T26c sodium is a potent and selective MMP13 inhibitor with IC50 value of 6.9 pM. T26c sodium can inhibit the degradation of bovine nasal septal cartilage explants .
GSK256066 Trifluoroacetate is a selective and high-affinity phosphodiesterase 4 (PDE) inhibitor, with an IC50 of 3.2 pM for PDE4B. GSK256066 Trifluoroacetate is developed for the research of chronic obstructive pulmonary disease .
Norleual, an angiotensin (Ang) IV analog, is a hepatocyte growth factor (HGF)/c-Met inhibitor with an IC50 of 3 pM. Norleual is an AT4 receptor antagonist and exhibits potent antiangiogenic activities .
BMS-740808 is a potent, selective and orally active factor Xa inhibitor with a Ki of 30 pM. BMS-740808 shows >1000-fold for factor Xa than other proteases .
Lopinavir Metabolite M-1, an active metabolite of Lopinavir, inhibits HIV protease with a Ki of 0.7 pM. Lopinavir Metabolite M-1 has antiviral activities in vitro .
Saroglitazar is a novel peroxisome proliferator-activated receptor (PPAR) agonist with predominant PPARα and moderate PPARγ activity with EC50 values of 0.65 pM and 3 nM in HepG2 cells, respectively.
ARC5690 sodium is an anti-mouse P-selectin aptamer. ARC5690 bound to recombinant mouse P-selectin with a KD of approximately 15pM in vitro. ARC5690 showed a significant anti-inflammatory effect
Resolvin D5 n-3 DPA is a Docosapentaenoic acid (DPA) derived specialized proresolving lipid mediator (SPM). Resolvin D5 n-3 DPA is a GPR101, GPR12, and GPR84 agonist with EC50s of 4.6 pM, 14 pM, and 1.5 pM, respectively. Resolvin D5 n-3 DPA possesses potent pro-resolution and anti-inflammatory actions. Resolvin D5 n-3 DPA reduces cell adhesion onto TNF-α-activated human endothelial monolayers. Resolvin D5 n-3 DPA displays potent leukocyte-directed activities, upregulating the ability of neutrophils and macrophages to phagocytose bacteria. Resolvin D5 n-3 DPA can be used for the study of intestinal inflammation .
Domagrozumab is an anti-myostatin humanized monoclonal antibody with a KD value of 2.6 pM for human myostatin. Domagrozumab induces muscle anabolic activity. Domagrozumab can be used in research of duchenne muscular dystrophy (DMD) .
Govorestat (AT-007) is an orally active brain-penetrant aldose reductase inhibitor with an IC50 value of 100 pM. Govorestat has the potential for galactose-1-phosphate uridyl transferase deficiency research .
Narnatumab (IMC-RON8) is a neutralizing human monoclonal antibody that blocks RON binding to its ligand, macrophage-stimulating protein (MSP), with a Kd of 32 pM. Narnatumab can be used for the research of cancer .
Saroglitazar magnesium is a novel peroxisome proliferator-activated receptor (PPAR) agonist with predominant PPARα and moderate PPARγ activity with EC50 values of 0.65 pM and 3 nM in HepG2 cells, respectively.
GSK256066 is a selective and high-affinity phosphodiesterase 4 (PDE4) inhibitor, with an IC50 of 3.2 pM for PDE4B. GSK256066 is developed for the research of chronic obstructive pulmonary disease .
RG7697 is a dual agonist for glucagon-like peptide receptor (GLP Receptor) and glucosedependent insulinotropic polypeptide receptor (GIPR), with EC50 of 5 and 3 pM, respectively. RG7697 exhibits antihyperglycemic property .
(R)-BAY-85-8501 is the less active Enantiomer of BAY-85-8501. BAY-85-8501 is a selective and potent inhibitor of Human Neutrophil Elastase (HNE), with an IC50 of 65 pM .
Icotrokinra (JNJ-77242113) is an orally available, selective antagonist of the IL-23 receptor. Icotrokinra inhibits IL-23-induced STAT3 phosphorylation in peripheral blood mononuclear cells (IC50=5.6 pM) and inhibits IL-23-induced interferon IFN-γ production in NK cells with an IC50 of 18.4 pM. Icotrokinra exhibits anti-inflammatory activity in a rat TNBS-induced colitis model. Icotrokinra can be used in the study of psoriasis, psoriatic arthritis, and inflammatory bowel disease .
Icotrokinra (JNJ-77242113) hydrochloride is an orally available, selective antagonist of the IL-23 receptor. Icotrokinra hydrochloride inhibits IL-23-induced STAT3 phosphorylation in peripheral blood mononuclear cells (IC50=5.6 pM) and inhibits IL-23-induced interferon IFN-γ production in NK cells with an IC50 of 18.4 pM. Icotrokinra hydrochloride exhibits anti-inflammatory activity in a rat TNBS-induced colitis model. Icotrokinra hydrochloride can be used in the study of psoriasis, psoriatic arthritis, and inflammatory bowel disease .
Icotrokinra (JNJ-77242113) acetate is an orally available, selective antagonist of the IL-23 receptor. Icotrokinra acetate inhibits IL-23-induced STAT3 phosphorylation in peripheral blood mononuclear cells (IC50=5.6 pM) and inhibits IL-23-induced interferon IFN-γ production in NK cells with an IC50 of 18.4 pM. Icotrokinra acetate exhibits anti-inflammatory activity in a rat TNBS-induced colitis model. Icotrokinra acetate can be used in the study of psoriasis, psoriatic arthritis, and inflammatory bowel disease .
MOR-106 (MOR12743) is a humanized anti-IL-17C IgG1 monoclonal antibody. MOR-106 inhibits the NF-κB signaling pathway by specifically binding to IL-17C (IC50 = 59 pM for human IL-17C, IC50 = 55 pM for mouse IL-17C). MOR-106 can effectively inhibit skin inflammation and reduce related inflammatory factors in animal models of psoriasis and atopic dermatitis .
Olcegepant hydrochloride (BIBN-4096 hydrochloride) is a potent and selective non-peptide antagonist of the calcitonin gene-related peptide 1 (CGRP1) receptor with IC50 of 0.03 nM and with a Ki of 14.4 pM for human CGRP .
Olcegepant (BIBN-4096) is a potent and selective non-peptide antagonist of the calcitonin gene-related peptide 1 (CGRP1) receptor with IC50 of 0.03 nM and Ki of 14.4 pM for human CGRP .
SBE13 Hydrochloride is a potent and selective Plk1 inhibitor, with an IC50 of 200 pM; SBE13 Hydrochloride poorly inhibits Plk2 (IC50>66 μM) or Plk3 (IC50=875 nM).
AB3145 is a selective Brd4 BromoTag PROTAC degrader (DC50: 120-140 pM). AB3145 promotes the ubiquitination and degradation of Brd4. AB3145 can be used in cancer research .
Norleual TFA, an angiotensin (Ang) IV analog, is a hepatocyte growth factor (HGF)/c-Met inhibitor with an IC50 of 3 pM. Norleual TFA is an AT4 receptor antagonist and exhibits potent antiangiogenic activities .
RLH-033 is a potent and selective ligand for the sigma 1 recognition site. RLH-033 has high affinity for sigma 1 sites labeled by [ 3H](+)-pentazocine with a Ki of 50 pM .
Deltasonamide 1 is a PDE6δ-KRas inhibitor. Deltasonamide 1 can inhibit PDE6δ-KRas with a KD of 203 pM. Deltasonamide 1 can be used for the research of tumors .
ARB-272572 is an oral effective small molecule PD-L1 inhibitor, with an IC50 value of 400 pM. ARB-272572 has research significance in tumors and chronic viral infections .
Dasatinib (GMP Like) (BMS-354825 (GMP Like)) is Dasatinib (HY-10181) produced by using GMP like guidelines. GMP Like small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Dasatinib (BMS-354825) is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively . Dasatinib also induces apoptosis and autophagy.
Anti-IL25/IL17E Antibody (ABM109.2) is an antibody targeting IL-25/IL17E, with a Kd of 24 pM for hIL-25 and a Kd of 28 pM for recombinant mouse IL-25. Anti-IL25/IL17E Antibody (ABM109.2) is applicable to research related to inflammatory and immune diseases. The isotype control is Human IgG1 kappa, Isotype Control (HY-P99001) .
CCKBR agonist-1 (Compound 3r1) is a Gq-protein-preferring cholecystokinin B receptor (CCKBR) agonist with an EC50 of 35 pM. CCKBR agonist-1 significantly increases the survival rate of neurons, with an EC50 of 37 pM. CCKBR agonist-1 can improve the cognitive decline in mice by upregulating α-secretase (ADAM10) and calcium signaling molecule PLCB4, reduce the number of amyloid β (Aβ) plaques, and promote long-term potentiation (LTP). CCKBR agonist-1 can be used for the study of Alzheimer's disease .
Deltasonamide 1 TFA is a PDE6δ-KRas inhibitor. Deltasonamide 1 can inhibit PDE6δ-KRas with a KD of 203 pM. Deltasonamide 1 can be used for the research of tumors .
5-Iodo-A-85380 dihydrochloride is a selective ligand of nAChR. 5-Iodo-A-85380 dihydrochloride binds to α4β2 nAChRs in rat and human brain with Kds of 12 and 14 pM,respectively .
Ocaratuzumab (AME 133v) is an Fc-engineered humanized IgG1 anti-CD20 monoclonal antibody, with a Kd of ~100 pM. Ocaratuzumab exhibits more effective antibody-dependent cell-mediated cytotoxicity (ADCC) .
Rilapladib (SB 659032) is a selective Lp-PLA2 (lipoprotein-associated phospholipase A2) inhibitor with an IC50 of 230 pM . Rilapladib (SB 659032) is also a PAFR (Platelet Activating Factor Receptor) antagonist .
β-Secretase Inhibitor IV is a potent, cell-active BACE-1 inhibitor with IC50s of 15.6 and 16.3nM under BACE-1 concentrations of 2 nM and 100 pM, respectively.
LFS-1107 is a reversible CRM1 inhibitor (Kd: 12.5 pM). LFS-1107 can selectively eliminate extranodal natural killer/T cell lymphoma (ENKTL) cells and can be used for cancer research .
Ceralifimod (ONO-4641) is selective, high potent agonist for sphingosine 1-phosphate receptors 1 and 5, with EC50s of 27.3, 334 pM for human S1P receptor 1 and 5, respectively.
Isecarosmab (M-6495) is an anti-ADAMTS monoclonal antibody (mAb) with a KD value of 3.65 pM. Isecarosmab has chondroprotective and anti-inflammatory activities. Isecarosmab can bind albumin to extend plasma half-life .
PRV-IN-1 (compound c14) shows significant anti-pseudorabies virus (PRV) potency and safety, with an EC50 of 14 pM and a CC50 of 343.7 μM. PRV-IN-1 significantly inhibits the replication of PRV .
Zampilimab (UCB-7858) is a monoclonal antibody against transglutaminase 2 (TG2). Zampilimab inhibits TG2 crosslinking transamidation activity with an IC50 of 0.25 nM and a Kd of <50 pM. Zampilimab improves renal fibrosis .
Wnt-C59 (Standard) is the analytical standard of Wnt-C59. This product is intended for research and analytical applications. Wnt-C59 (C59) is a highly potent and oral porcupine (PORCN) inhibitor with an IC50 of 74 pM.
Elagolix is an orally active, highly effective, selective and non-peptide gonadotropin-releasing hormone receptor (GnRH receptor) antagonist (KD = 54 pM) and NFAT inhibitor, which can be used to study pain related to endometriosis .
Pibrentasvir is a novel and pan-genotypic hepatitis C virus (HCV) NS5A inhibitor with EC50s ranging from 1.4 to 5.0 pM against HCV replicons containing NS5A from genotypes 1 to 6.
Remtolumab is a bispecific variable domain immunoglobulin molecule with human affinities for TNFα and IL-17 in the low pM range of Kd. Remtolumab can be used in research related to rheumatoid arthritis, psoriatic arthritis, and moderate-to-severe plaque psoriasis .
Edonentan (BMS 207940) is an antagonist for endothelin receptor (ETA receptor), with a Ki of 10 pM. Edonentan is metabolic stable, exhibits good pharmakokinetic characters in rats. Edonentan regulates the endothelin system, blocks the big Endothelin-induced pressor response in rats model .
Corifollitropin alfa (Org 36286) is a long-acting recombinant follicle-stimulating hormone (FSH) analog. Corifollitropin alfa is a FSH Receptor agonist with an EC50 of 5.0 pM. Corifollitropin alfa stimulates ovulation and can be used in the research of infertility .
Echinomycin (Quinomycin A) is potent small-molecule and cell-permeable inhibitor of hypoxia-inducible factor-1 (HIF-1) DNA-binding activity. Echinomycin selectively inhibits the cancer stem cells (CSCs) with an IC50 of 29.4 pM .
Gartisertib (VX-803) is an ATP-competitive, orally active, and selective ATR inhibitor, with a Ki of <150 pM. Gartisertib potently inhibits ATR-driven phosphorylated checkpoint kinase-1 (Chk1) phosphorylation with an IC50 of 8 nM. Antitumor activity .
AHR antagonist 2 (Example 1) is a potent aryl hydrocarbon receptor (AHR) antagonist with IC50s of 885 pM and 2.03 nM for human and mouse AHR. AHR antagonist 2 can be used for the studies of cancers and imbalance of the immune response .
AMY109 is an anti-human interleukin-8 (IL-8) monoclonal antibody, with a Ka of 36.8 pM for human IL-8, and a Ka of 380 pM for cynomolgus monkey IL-8. AMY109 binds to human and cynomolgus monkey IL-8 in a pH-dependent manner, inhibits IL-8-mediated activation of CXCR1 and CXCR2, and blocks the downstream biological activities of IL-8. AMY109 inhibits neutrophil recruitment to endometriotic lesions and suppresses monocyte chemoattractant protein-1 production by neutrophils. AMY109 is applicable to research related to endometriosis .
AB-680 is a highly potent, reversible and selective inhibitor of CD73 (an ecto-nucleotidase), with a Ki of 4.9 pM for hCD73, displays >10,000-fold selectivity over related ecto-nucleotidases CD39. Anti-tumor activity .
T-26c, a chemical probe, is highly potent and selective matrix metalloproteinase-13 (MMP-13) inhibitor with an IC50 of 6.75 pM and more than 2600-fold selectivity over the other related metalloenzymes .
Nrf2 activator 17 (compound 10) is an Nrf2 activator that inhibits the interaction between Keap1 and Nrf2 with an IC50 of < 0.1 pM. Additionally, Nrf2 activator 17 has an EC50 of < 10 μM in HepG2 cells .
Elagolix sodium is a highly effective, selective, oral-active, short-term, non-peptide gonadotropin-releasing hormone receptor (GnRH receptor) antagonist (KD = 54 pM) and NFAT inhibitor, which can be used to study pain related to endometriosis. .
BMS-639623 is a potent and orally activeCCR3 antagonist with an IC50 of 0.3 nM. BMS-639623 picomolar inhibition potency against eosinophil chemotaxis (IC50=38 pM). BMS-639623 can be used for the research of asthma .
Elagolix is a highly effective, selective, oral-active, short-term, non-peptide gonadotropin-releasing hormone receptor (GnRH receptor) antagonist (KD = 54 pM) and NFAT inhibitor, which can be used to study pain related to endometriosis. .
GPR17 agonist 1 is a selective and potent GPR17 agonist with an EC50 of 35 pM. GPR17 agonist 1 also shows weak activation of P2Y Receptor. GPR17 agonist 1 can be used for the research of neurological disease .
Santacruzamate A (CAY-10683, STA) is a potent and selective HDAC2 inhibitor with an IC50 of 119 pM. STA also exerts neuroprotective property against amyloid-β protein fragment 25–35. STA can be used for cancer and neurological disease research .
Samatasvir (IDX71) is a potent, orally active NS5A inhibitor of HCV replication. Samatasvir is effective and selective against infectious HCV and replicons, with EC50s falling within a tight range of 2 to 24 pM in genotype 1 through 5 replicons .
Plasma kallikrein-IN-5 (Compound 20) is a potent covalent inhibitor of plasma potassium kinin peptide (Pka) with IC50 values of 66 nM and 70 pM at 1 minute and 24 hours, respectively. Plasma kallikrein-IN-5 can be used IN the study of hereditary angioedema (HAE) .
VTP50469 (Standard) is the analytical standard of VTP50469. This product is intended for research and analytical applications. VTP50469 is a potent, highly selective and orally active Menin-MLL interaction inhibitor with a Ki of 104 pM. VTP50469 has potently anti-leukemia activity .
PE154 (Compound 13) is a potent fluorescent inhibitor of human acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) (IC50s=280 pM and 16 nM, respectively) . PE154 can label β-amyloid plaques in histochemical analysis .
AB-680 ammonium is a highly potent, reversible and selective inhibitor of CD73 (an ecto-nucleotidase), with a Ki of 4.9 pM for hCD73, displays >10,000-fold selectivity over related ecto-nucleotidases CD39. Anti-tumor activity .
Sipeimine (Imperialine) is an inhibitor targeting the PI3K/AKT/NF-κB pathway and NLRP3 inflammasome, which can competitively bind to PI3K and p65. Sipeimine inhibits PI3K/AKT phosphorylation, blocks NF-κB nuclear translocation and NLRP3 inflammasome activation. Sipeimine exerts anti-inflammatory activities, inhibits pyroptosis and ferroptosis, and protects the extracellular matrix. Sipeimine can reduce cartilage degradation and synovial inflammation in osteoarthritis and improve PM2.5-induced lung injury. Sipeimine is mainly used in the study of anti-inflammatory and degenerative diseases .
Ramiprilat-d5 is deuterium labeled Ramiprilat. Ramiprilat (HOE 498 diacid), an active metabolite of Ramipril, is a potent and orally active angiotensin converting enzyme (ACE) inhibitor with a Ki value of 7 pM. Ramiprilat can be used for high blood pressure and heart failure research .
Gallinamide A TFA is a linearly depositing peptide and a potent inhibitor of cathepsin L (CatL) (IC50: 17.6 pM). Gallinamide A TFA inhibits SARS-CoV-2 infection by inhibiting CatL (EC50: 28 nM). Gallinamide A TFA also inhibits Plasmodium falciparum (IC50: 50 nM) .
Aminopterin (4-Aminofolic acid), the 4-amino derivative of folic acid, is a folic acid antagonist. Aminopterin catalyses the reduction of folic acid to tetrahydrofolic acid, and competitively inhibits dihydrofolate reductase (DHFR) with a Ki of 3.7 pM. Aminopterin has anticancer and immunosuppressive activity. Aminopterin is used in treatment of pediatric leukemia .
Rizavasertib (Standard) is the analytical standard of Rizavasertib (HY-10425). This product is intended for research and analytical applications. A-443654 is a pan-Akt inhibitor and has equal potency against Akt1, Akt2, or Akt3 within cells (Ki=160 pM) .
Gilvocarcin M is an antibiotic and can be isolated from S. gilvotanareus. Gilvocarcin M is active against S. aureus at a concentration of 32 µg/ml and inhibits growth of KB cells with the IC50 of 0.52 µg/ml. Gilvocarcin M intercalates into bacteriophage PM2 DNA .
Elsilimomab (B-E8) is a IgG1 monoclonal antibody against interleukin-6 (IL-6), with a KD of 22 pM and an IC50 of 1.4 nM. Elsilimomab can be used for the research of multiple myeloma, renal cell carcinoma, and rheumatoid arthritis (RA) .
BQ0413 exhibits good affinity to PSMA with a KD of 89 pM. BQ0413 exhibits good uptake and internalization property with an internalization rate of 44% in PC3-pip cell. BQ0413 can be used as tumor imaging agent when labeled with 99mTc .
PDE4-IN-34 is a phosphodiesterase 4 (PDE4) inhibitor, with IC50 values of 19 pM and 14 pM against PDE4B1 and PDE4D2, respectively. PDE4-IN-34 shows weak inhibitory activity against PDE8A1, with an IC50 value of 4.092 μM, and exhibits significant selectivity over other subtypes (IC50 > 10 μM). PDE4-IN-34 improves pulmonary function, reduces inflammatory responses and alleviates lung tissue damage in a rat model induced by cigarette smoke combined with LPS (HY-D1056). PDE4-IN-34 can be used for research related to chronic obstructive pulmonary disease .
DBPR110 is a nonstructural protein 5A (NS5A) inhibitor with inhibitory activity against hepatitis C virus (HCV). DBPR110 exhibited a 50% effective concentration (EC50) of 3.9 ± 0.9 pM and a selectivity index value of over 12,800,000 by reducing HCV1b replicon reporter expression. DBPR110 also effectively reduced the activity of HCV2a replicon with an EC50 of 228.8 pM and a selectivity index value of over 173,130. DBPR110 showed synergy with interferon alpha (IFN-α), NS3 protease inhibitors, and NS5B polymerase inhibitors. The results of DBPR110 suggest that it may be an effective small molecule inhibitor against HCV NS5A .
GNE-140 is an orally active and selective inhibitor of lactate dehydrogenase (LDH) A, B and C, with IC50 values of 3, 5 and 5 nM against LDHA, LDHB, LDHC, respectively. GNE-140 blocks the conversion of pyruvate to lactate, reduces lactate production and histone lysine lactylation, and inhibits glycolysis. GNE-140 attenuates cardiac hypertrophy, alleviates PM2.5-induced pulmonary inflammation and fibrosis, blocks MRSA-induced Arg1 expression, regulates metabolites of glycolysis and the pentose phosphate pathway, reduces glucose uptake, increases ROS, and induces cancer cell apoptosis. GNE-140 is applicable to research related to pathological cardiac hypertrophy, pulmonary fibrosis, MRSA infection and pancreatic cancer .
Ramiprilat (HOE 498 diacid), an active metabolite of Ramipril, is a potent and orally active angiotensin converting enzyme (ACE) inhibitor with a Ki value of 7 pM. Ramiprilat has acute antlhypertensive effect. Ramiprilat can be used for high blood pressure and heart failure research .
GSK256066 (Trifluoroacetate) (Standard) is the analytical standard of GSK256066 (Trifluoroacetate). This product is intended for research and analytical applications. GSK256066 Trifluoroacetate is a selective and high-affinity phosphodiesterase 4 (PDE) inhibitor, with an IC50 of 3.2 pM for PDE4B. GSK256066 Trifluoroacetate is developed for the research of chronic obstructive pulmonary disease .
Ru-4T is a phototherapy agent. Ru-4T has phototherapeutic efficacy (PI = 114,000) against melanoma cells (SK-MEL-28) under broad-band visible light (400-700 nm) with EC50 values of 740 pM .
MG-101 (ALLN) is an inhibitor of cysteine proteases which inhibits calpain I, calpain II, cathepsin B and cathepsin L with Kis of 190, 220, 150 and 500 pM, respectively. MG-101 induces apoptosis and inhibits tumor growth, it can be used for the research of colon cancer .
Saroglitazar-d4 is the deuterium-labeled Saroglitazar (HY-19937). Saroglitazar-d4 is a novel peroxisome proliferator-activated receptor (PPAR) agonist with predominant PPARα and moderate PPARγ activity with EC50 values of 0.65 pM and 3 nM in HepG2 cells, respectively.
AVN-492 (Standard) is the analytical standard of AVN-492 (HY-101924). This product is intended for research and analytical applications. AVN-492 is a very specific and highly-selective antagonist with picomolar affinity to 5-HT6R (Ki=91 pM).
A-134974 is a novel, high-selectivity adenosine kinase (IC50 = 60 pM) inhibitor. A-134974 enhances endogenous adenosine signaling in the spinal cord, effectively alleviates neuropathic pain, and does not cause movement disorders. A-134974 can be used for the study of neuropathic pain .
Emapalumab (NI-0501) is a human monoclonal IgG1 antibody that noncompetitively inhibits IFN-γ. Emapalumab binds with high affinity (Kd= 1.4 pM) to both free IFN-γ as well as IFN-γ bound to its receptor. Emapalumab can be used in research of hemophagocytic lymphohistiocytosis (HLH) .
PIM447 dihydrochloride (LGH447 dihydrochloride) is a potent, orally available, and selective pan-PIM kinase inhibitor, with Ki values of 6, 18, and 9 pM for PIM1, PIM2, and PIM3, respectively. PIM447 dihydrochloride displays dual antimyeloma and bone-protective effects. PIM447 dihydrochloride induces apoptosis .
Duocarmycin SA is an orally active antitumor antibiotic with an IC50 of 10 pM . Duocarmycin SA is an extremely potent cytotoxic agent capable of inducing a sequence-selective alkylation of duplex DNA. Duocarmycin SA demonstrates synergistic cytotoxicity against glioblastoma multiforme (GBM) cells treated with proton radiation in vitro .
PIM447 (LGH447) is a potent, orally available, and selective pan-PIM kinase inhibitor, with Ki values of 6, 18, and 9 pM for PIM1, PIM2, and PIM3, respectively. PIM447 displays dual antimyeloma and bone-protective effects. PIM447 induces apoptosis .
GSK256066 (Standard) is the analytical standard of GSK256066. This product is intended for research and analytical applications. GSK256066 is a selective and high-affinity phosphodiesterase 4 (PDE4) inhibitor, with an IC50 of 3.2 pM for PDE4B. GSK256066 is developed for the research of chronic obstructive pulmonary disease .
GaTx2 is a seletive and a high affinity inhibitor of ClC-2 channels with a voltage-dependent apparent KD of ∼20 pM. GaTx2 is a peptide toxin inhibitor from Leiurus quinquestriatus hebraeus venom. GaTx2 is useful in determining the role and the membrane localization of ClC-2 in specific cell types .
Ramiprilat-d4 hydrochloride is deuterated labeled Ramiprilat (HY-A0115). Ramiprilat (HOE 498 diacid), an active metabolite of Ramipril, is a potent and orally active angiotensin converting enzyme (ACE) inhibitor with a Ki value of 7 pM. Ramiprilat can be used for high blood pressure and heart failure research .
FM-381, a chemical probe, is a potent covalent reversible inhibitor of JAK3 targeting the unique Cys909. FM-381 has an IC50 of 127 pM for JAK3, with 410, 2700 and 3600-fold selectivity over JAK1, JAK2 and TYK2, respectively .
IWP-O1 is a highly potent Porcupine (Porcn) inhibitor, with an EC50 of 80 pM in L-Wnt-STF cells. IWP-O1 prevents the secretion of Wnt proteins. IWP-O1 suppresses the phosphorylation of Dvl2/3 and LRP6 in HeLa cells .
AM-7209 is a potent and selective MDM2-p53 interaction inhibitor with a Kd of 38 pM. AM-7209 inhibits the MDM2 amplified SJSA-1 osteosarcoma cell line with an IC50 of 1.6 nM. AM-7209 shows antitumor activities .
2-Iodomelatonin is a potent agonist of melatonin receptor 1 (MT1) with a Ki value of 28 pM, it is more 5-fold selective for MT1 over MT2 . 2-iodomelatonin can be used to identify, characterize and localize melatonin binding sites in the brain and peripheral tissues .
HsTX1, from the scorpion Heterometrus spinnifer, is a 34-residue, C-terminally amidated peptide cross-linked by four disulfide bridges. HsTX1, an the inhibitor of potassium channel, with IC50 for Kv1.3 of 12 pM inhibits TEM cell activation and attenuates inflammation in autoimmunity .
BETd-260 (ZBC 260) is a PROTAC connected by ligands for Cereblon and BET, with as low as 30 pM against BRD4 protein in RS4;11 leukemia cell line . BETd-260 potently suppresses cell viability and robustly induces apoptosis in hepatocellular carcinoma (HCC) cells .
ARN23765 is a corrector for F508del-CFTR with an EC50 of 38 pM in human bronchial epithelial cells. ARN23765 improves the maturation and function of F508del-CFTR on the cell membrane, affects the ions transport and secretion, and corrects the pathological mechanism of cystic fibrosis (CF) .
AMYR/CTR agonist 1 (Compound 195) is a pancreatic amylin receptor and calcitonin receptor (AMYR/CTR) agonist with EC50 values for pancreatic amylin receptor and calcitonin receptor cAMP of 99.5 and 6.16 pM respectively. AMYR/CTR agonist 1 can be used in the research of diseases such as type 2 diabetes and obesity .
HCV-IN-7 is an orally active and potent pan-genotypic HCV NS5A inhibitor with IC50s of 3-47 pM. HCV-IN-7 shows a superior pan-genotypic profile and a good pharmacokinetic profile coupled with a favorable liver uptake. HCV-IN-7 has anti-viral activity .
Streptavidin is a ~60 kDa homotetramer. Streptavidin binds four molecules of biotin with the highest affinity. The binding affinity of biotin to streptavidin is one of the highest reported for a non-covalent interaction to date, with a KD ~0.01 pM . Streptavidin has an immunosuppressive role . This product is a Streptavidin protein recombinantly expressed in an E. coli expression system.
Aprepitant- 13C2,d2 (Major) (MK-0869- 13C2,d2) is 13C labeled Aprepitant. Aprepitant (MK-0869) is a selective and high-affinity neurokinin 1 receptor antagonist with a Kd of 86 pM.
Caloxin 3A1 is a biological active peptide. (This peptide belongs to caloxins, the extracellular plasma membrane (PM) Ca2+ pump inhibitors. Caloxin 3A1 inhibits plasma membrane calcium pumps (PMCAs) but not the sarcoplasmic reticulum Ca2+-pump. This peptide does not inhibit formation of the acylphosphate intermediate from ATP.)
YM022 is a highly potent, selective and orally active gastrin/cholecystokinin (CCK)-B receptor (CCK-BR) antagonist. YM022 shows the Ki values of 68 pM and 63 nM for CCK-B and CCK-A receptor, respectively . YM022 can inhibit gastrin-induced gastric acid secretion and histidine decarboxylase activation in vivo .
Wnt-C59 (C59) GMP is a GMP grade Wnt-C59 (HY-15659). GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Wnt-C59 (C59) is a highly potent and oral porcupine (PORCN) inhibitor with an IC50 of 74 pM.
DC41SMe, a DC1 derivative, shows cytotoxicity in Ramos, Namalwa, and HL60/s cells with IC50s ranging from 18-25 pM. DC1, a simplified analogue of CC-1065, is an antibody conjugate of cytotoxic DNA alkylators for the targeted treatment of cancer .
UNC5293 is a MERTK-selective and potent inhibitor (Ki=190 pM). UNC5293 inhibits MERTK (IC50=0.9 nM) and is more selective over Axl, Tyro3 and Flt3. UNC5293 exhibits excellent mouse PK properties and is used for bone marrow leukemia research .
HCV-IN-7 hydrochloride is an orally active and potent pan-genotypic HCV NS5A inhibitor with IC50s of 3-47 pM. HCV-IN-7 hydrochloride shows a superior pan-genotypic profile and a good pharmacokinetic profile coupled with a favorable liver uptake. HCV-IN-7 hydrochloride has anti-viral activity .
MRTX-1257-d6 is the deuterium labeled MRTX-1257 (HY-114436). MRTX-1257 is a selective, irreversible, covalent and orally active KRAS G12C inhibitor, with an IC50 of 900 pM for KRAS dependent ERK phosphorylation in H358 cells .
FAP-IN-6 (Compound 21) is a selectivity FAP inhibitor with an IC50 of 13 pM. FAP-IN-6 has a high metabolic stability. FAP-IN-6 labeled with 18F can be used as a positron emission tomography (PET) tracer. FAP-IN-6 can be used for microenvironment of cancers research .
Elagolix-d9 is the deuterium labeled Elagolix. Elagolix sodium is a highly effective, selective, oral-active, short-term, non-peptide gonadotropin-releasing hormone receptor (GnRH receptor) antagonist (KD = 54 pM) and NFAT inhibitor, which can be used to study pain related to endometriosis. .
SARS-CoV-2-IN-12 (Compound 27) is a potent SARS-CoV-2-related 3C-like protease inhibitor (Ki=32.1 pM) for preventing SARS-CoV-2 viral replication and that could be useful in the research of COVID-19 .
CAY10603 (BML-281) is a potent and selective HDAC6 inhibitor, with an IC50 of 2 pM; CAY10603 (BML-281) also inhibits HDAC1, HDAC2, HDAC3, HDAC8, HDAC10, with IC50s of 271, 252, 0.42, 6851, 90.7 nM.
Olcegepant (Standard) is the analytical standard of Olcegepant (HY-10095). This product is intended for research and analytical applications. Olcegepant (BIBN-4096) is a potent and selective non-peptide antagonist of the calcitonin gene-related peptide 1 (CGRP1) receptor with IC50 of 0.03 nM and Ki of 14.4 pM for human CGRP .
Ceritinib (LDK378) dihydrochloride is a selective, orally bioavailable and ATP-competitive ALK tyrosine kinase inhibitor with an IC50 of 200 pM. Ceritinib dihydrochloride also inhibits IGF-1R, InsR, and STK22D with IC50 values of 8, 7, and 23 nM, respectively. Ceritinib dihydrochloride shows great antitumor potency .
Ceritinib (LDK378) mesylate is a selective, orally bioavailable, and ATP-competitive ALK tyrosine kinase inhibitor with an IC50 of 200 pM. Ceritinib mesylate also inhibits IGF-1R, InsR, and STK22D with IC50 values of 8, 7, and 23 nM, respectively. Ceritinib mesylate shows great antitumor potency .
TLR2 agonist 1 (Compound R-7d) is an agonist for human toll-like receptor 2 (TLR 2) with an EC50 of 116 pM. TLR2 agonist 1 enhances NF-κB promoter activation through TLR2/TLR1 heterodimers .
β2AR agonist 4 (compound A19) is a potent and selective β2-Adrenoceptor agonist with an EC50 of 3.7 pM. β2AR agonist 4 suppresses the inflammatory cytokines and leukocytes upregulation and improves lung function in COPD rat model .
Ceritinib (LDK378) is a selective, orally bioavailable, and ATP-competitive ALK tyrosine kinase inhibitor with an IC50 of 200 pM. Ceritinib also inhibits IGF-1R, InsR, and STK22D with IC50 values of 8, 7, and 23 nM, respectively. Ceritinib shows great antitumor potency .
Sipeimine (Standard) is the analytical standard of Sipeimine (HY-N0696R). Sipeimine (Imperialine) is an inhibitor targeting the PI3K/AKT/NF-κB pathway and NLRP3 inflammasome, which can competitively bind to PI3K and p65. Sipeimine inhibits PI3K/AKT phosphorylation, blocks NF-κB nuclear translocation and NLRP3 inflammasome activation. Sipeimine exerts anti-inflammatory activities, inhibits pyroptosis and ferroptosis, and protects the extracellular matrix. Sipeimine can reduce cartilage degradation and synovial inflammation in osteoarthritis and improve PM2.5-induced lung injury. Sipeimine is mainly used in the study of anti-inflammatory and degenerative diseases .
MK-8825 is an orally active, selective CGRP receptor antagonist with a Ki value of 47 pM for human CGRP receptors and 17 nM for rat CGRP receptors. MK-8825 blocks CGRP-stimulated cAMP responses and exhibits competitive-like antagonism. MK-8825 can be used in the research of migraine and temporomandibular joint disorders .
Estrone O-sulfamate (Estrone 3-O-sulfamate) is a potent steroid sulfatase (STS) inhibitor. Estrone O-sulfamate has inhibitory activity for STS in a placental microsomes (P.M.) preparation and in MCF-7 cells with IC50 values of 18 nM and 0.83 nM, respectively. Estrone O-sulfamate can be used for the research of cancer .
Emprumapimod (PF-07265803) is a potent, orally active and selective inhibitor of p38α MAPK directly inhibits LPS-induced IL-6 production from RPMI-8226 cell (IC50=100 pM). Emprumapimod can be used for the research of dilated cardiomyopathy and acute inflammatory pain .
TPM004 is an ultralong-acting, nonaggregating dual amylin (AMY3R) and calcitonin receptor (CTR) agonist with EC50 values of 0.5 and 0.7 pM. TPM004 induces weight loss, attenuates adiposity rebound, lowers glucose, and improves glucose homeostasis. TPM004 can be used for the research of obesity, diabetes .
HsTX1 (TFA) toxin, from the scorpion Heterometrus spinnifer, is a 34-residue, C-terminally amidated peptide cross-linked by four disulfide bridges. HsTX1 (TFA) is an the inhibitor of potassium channel, with IC50 for Kv1.3 of 12 pM and inhibits TEM cell activation and attenuates inflammation in autoimmunity .
Rilapladib (Standard) is the analytical standard of Rilapladib (HY-102004). This product is intended for research and analytical applications. Rilapladib (SB 659032) is a selective Lp-PLA2 (lipoprotein-associated phospholipase A2) inhibitor with an IC50 of 230 pM . Rilapladib (SB 659032) is also a PAFR (Platelet Activating Factor Receptor) antagonist .
PLK1-IN-14 (Compound Hit-4) is a selective PLK1 inhibitor. It has an IC50 of 22.61 pM against PLK1 and an IC50 of 0.09 nM for inhibiting the proliferation of DU - 145 prostate cancer cells. PLK1-IN-14 can be used in the research of prostate cancer .
AZ-4217 is an inhibitor for β-site amyloid precursor protein cleavage enzyme 1 (BACE1), with IC50 of 160 pM in human SH-SY5Y cells. AZ-4217 reduces amyloid deposition in Tg2576 mouse models, and is used for Alzheimer’s Disease research .
UNC0321 is a potent and selective histone methyltransferase G9a inhibitor with a Ki of 63 pM and with assay-dependent IC50 values of 6-9 nM. UNC0321 also inhibits GLP with assay-dependent IC50 values of 15-23 nM. UNC0321 has anti-apoptotic activity and has potential application in diabetic vascular complications .
Clonixeril (NSC 335504) is a non-nucleotide hSTING modulator. Clonixeril has weak agonist activity at micromolar concentrations and results in antagonism of the hSTING WT pathway at low femtomolar (10 -15 M) and in some cases even attomolar (10 -18 M) concentrations. Clonixeril reduces hSTING oligomerization at a concentration of 1 aM-1 pM .
Olendalizumab (ALXN1007) is a mouse-derived and humanized IgG2-G4-κ antibody, targeting to Complement protein C5a (Ki=60 pM). Olendalizumab targets the complement inflammatory pathway. Moreover, Olendalizumab can be used for research of complement mediated disorder caused by corona virus .
Foropafant (SR27417) highly potent, competitive, selective and orally active antagonist of platelet-activating factor (PAF) receptor, with a Ki value of 57 pM for [ 3H]PAF binding, at least 5-fold lower than that of unlabeled PAF itself. Foropafant potently inhibits PAF-induced aggregation of rabbit and human platelets .
PSF-IN-1 (Compound No.10-3) is a RNA-binding protein (PSF) inhibitor and can effectively inhibit the PSF-RNA interaction (IC50: 2.2 pM). PSF-IN-1 can increase histone acetylation, inhibit tumor cell proliferation and induce apoptosis. PSF-IN-1 has antitumor activity .
Murizatoclax (AMG 397) is a potent, selective and orally active inhibitor of myeloid leukemia 1 (MCL-1) inhibitor, with a Ki of 15 pM. Murizatoclax competitive binds to the BH3-binding groove of MCL1 with pro-apoptotic BCL-2 family members. Murizatoclax can be used for the research of cancer .
AP1153 aptamer sodium is a DNA aptamer that specifically binds to the cholecystokinin receptor CCKBR (Kd: ~15 pM), but does not activate CCKBR-related signaling pathways. AP1153 aptamer sodium is internalized by pancreatic ductal adenocarcinoma (PDAC) cells in a receptor-mediated manner. AP1153 aptamer sodium can bioconjugate to the surface of fluorescent nanoparticles to facilitate nanoparticle delivery to PDAC tumors in vivo .
Tildrakizumab (SCH 900222) is a humanized anti-IL-23 (p19 subunit) monoclonal antibody. IL-23 is a critical cytokine to maintain the Th17 cell phenotype. Tildrakizumab has high-affinity for single-chain IL-23 (Kd: 136 pM). Tildrakizumab is effective against moderate to severe plaque psoriasis .
(R)-Elagolix (Standard) is the analytical standard of (R)-Elagolix. This product is intended for research and analytical applications. Elagolix is a highly effective, selective, oral-active, short-term, non-peptide gonadotropin-releasing hormone receptor (GnRH receptor) antagonist (KD = 54 pM) and NFAT inhibitor, which can be used to study pain related to endometriosis. .
Ramelteon is a potent, highly selective, and orally active agonist of MT1/MT2 with Ki values of 14 and 112 pM, respectively. Ramelteon has the potential for the research of insomnia. Ramelteon consistently reduces sleep onset after long-term treatment, with no next-morning residual effects or rebound insomnia or withdrawal symptoms upon discontinuation .
Aminopterin (Standard) is the analytical standard of Aminopterin. This product is intended for research and analytical applications. Aminopterin (4-Aminofolic acid), the 4-amino derivative of folic acid, is a folic acid antagonist. Aminopterin catalyses the reduction of folic acid to tetrahydrofolic acid, and competitively inhibits dihydrofolate reductase (DHFR) with a Ki of 3.7 pM. Aminopterin has anticancer and immunosuppressive activity. Aminopterin is used in treatment of pediatric leukemia .
PL-100 is a potent HIV-1 protease inhibitor with a Ki of 36 pM and an EC50 of 16 nM. PL-100 inhibits viral replication by suppressing HIV-1 protease activity and demonstrates excellent antiviral efficacy against drug-resistant HIV strains. PL-100 can be used in research on drug-resistant HIV disease .
Santacruzamate A (Standard) is the analytical standard of Santacruzamate A. This product is intended for research and analytical applications. Santacruzamate A (CAY-10683, STA) is a potent and selective HDAC2 inhibitor with an IC50 of 119 pM. STA also exerts neuroprotective property against amyloid-β protein fragment 25–35. STA can be used for cancer and neurological disease research[1][2].
GSK2256294A (GSK 2256294) is a selective and orally active inhibitor of soluble epoxide hydrolase (sEH). GSK2256294A inhibits recombinant human sEH, rat sEH orthologs and murine sEH orthologs with IC50s of 27, 61 and 189 pM, respectively. GSK2256294A can be used for the research of chronic obstructive pulmonary disease (COPD) and cardiovascular disease .
SK48-E26 is a human interleukin-1β (IL-1β) inhibitor, with a IC50 of 400 pM against human IL-1β, a IC50 of 185 pM against cynomolgus monkey IL-1β, and a Ka value ranging from 0.048 nM to 3 nM for human IL-1β. SK48-E26 binds to the conformational epitope of human IL-1β spanning amino acid residues 95-101, and blocks the biological activity of IL-1β. SK48-E26 can be used in research related to IL-1β-mediated inflammatory diseases and osteoarthritis .
MEDI-579 is a fully human monoclonal antibody against PAI-1, with a KD value of 6 pM for human PAI-1 and 105 pM for rat PAI-1. MEDI-579 restores renal plasmin activity and inhibits PAI-1-mediated intracellular signal transduction. MEDI-579 reduces albuminuria, glomerulosclerosis severity, TGF-β1 expression level, and phosphorylated Smad2 level induced in diabetic mice. MEDI-579 decreases the levels of active PAI-1 in plasma and kidneys, and increases plasma plasmin level in a mouse model of lupus nephritis. MEDI-579 can be used in research related to diabetic nephropathy and lupus nephritis. The recommended isotype control is human IgG1 kappa (HY-P99001) .
(1R,2R)-Elpipodect ((1R,2R)-MK-8189) is the (1R,2R) enantiomer of Elpipodect (HY-153093). Elpipodect (MK-8189) is an orally active and selective PDE10A inhibitor with a Ki of 29 pM. Elpipodect can be used in research of schizophrenia .
Tesnatilimab (JNJ-64304500) is a human IgG4 monoclonal antibody targeting NKG2D, with a KD value of 9.2 pM . Tesnatilimab blocks the binding of ligands to the NKG2D receptor, thereby inhibiting downstream proinflammatory cytokine, cytotoxic mediator signaling pathways and proinflammatory immune responses. Tesnatilimab is applicable to research related to Crohn's disease .
Ac-DEVD-CHO TFA is a peptide inhibitor of caspase-3 (Ki=230 pM) and caspase-7. Ac-DEVD-CHO TFA reduces caspase-3 activity and apoptosis induced by Prostaglandin E2 (HY-101952) in rat cortical neurons. Ac-DEVD-CHO TFA is promising for research of neurodegenerative diseases and cancers .
Nidanilimab (CAN04) is a fully humanized monoclonal anti-IL1RAP antibody with a Kd value of 1.10 pM. Nidanilimab blocks IL1α and IL1β signaling and stimulates the immune system to destroy tumour cells. Nidanilimab can be used in research of non-small lung cancer (NSCLC) and pancreatic ductal adenocarcinoma (PDAC) .
HCV-IN-4 is a potent and orally active HCV NS5A inhibitor, shows great potency against GT1a, GT2b, GT3a, GT1a Y93H and GT1a L31V, with EC90s of 3 pM, 0.3 nM, 0.01 nM, 0.5 nM and 0.02 nM, respectively .
TA-0201 is a novel orally active, competitive, non-peptide endothelin receptor antagonist. TA-0201 antagonizes the specific binding of [ 125I]ET-1 to cloned human receptors of ETA and ETB with Ki values of 15 pM and 41 nM, respectively. TA-0201 inhibits the pressor response to the exogenous big ET-1 .
Elagolix-d6 (sodium) (NBI-56418-d6 (sodium)) is deuterium labeled Elagolix sodium. Elagolix sodium is a highly effective, selective, oral-active, short-term, non-peptide gonadotropin-releasing hormone receptor (GnRH receptor) antagonist (KD = 54 pM) and NFAT inhibitor, which can be used to study pain related to endometriosis. .
Calcium dobesilate is a vascular protector with oral activity that can clear hydroxyl free radicals, with an IC50 of 1.1 pM. Calcium dobesilate has antioxidant activity and helps to reduce oxidative stress and inflammation in the retinas of diabetic mice. Calcium dobesilate can be used to study chronic venous diseases, diabetic retinopathy, and the occurrence of hemorrhoids, among other conditions .
Gartisertib-d8 (VX-803-d8) is the deuterium labeled Gartisertib (HY-136270). Gartisertib (VX-803) is an ATP-competitive, orally active, and selective ATR inhibitor, with a Ki of <150 pM. Gartisertib potently inhibits ATR-driven phosphorylated checkpoint kinase-1 (Chk1) phosphorylation with an IC50 of 8 nM. Antitumor activity .
Navlimetostat is a potent, orally active, selective PRMT5-MTA complex inhibitor, with IC50 of 3.6 and 20.5 nM for PRMT5-MTA and PRMT5. Navlimetostat binds to the PRMT5-MTA complex, with KD value of 0.14 pM. Navlimetostat shows antineoplastic activity in vitro and in vivo, and can be used for cancer study .
Vobarilizumab (ALX-0061) is a humanized bispecific anti-IL-6R and anti-human serum albumin (ALB) monoclonal antibody (mAb) (Kd: 0.19 pM). Vobarilizumab consists of an anti-IL-6R domain and an anti-human serum albumin domain. Vobarilizumab can be used in the research of inflammatory autoimmune diseases, such as rheumatoid arthritis .
Nicotelline (Nicotellin) is a nicotine-related alkaloid, as well as a weak inhibitor of human cDNA-expressed cytochrome P-450 2A6 (CYP2A6). CYP2A6 mediates coumarin 7-hydroxylation, while Nicotelline fails to exhibit inhibition at 300 μM. Nicotelline can be used as a tracer and biomarker of particulate matter (PM) derived from tobacco smoke .
BPIQ-II is a linear imidazoloquinazoline that potently inhibits the tyrosine kinase activity of the epidermal growth factor receptor (EGFR; IC50=8 pM). It is selective for EGFR over an assortment of other tyrosine and serine/threonine kinases. Cellular studies indicate that BPIQ-II can enter cells and very selectively shut down EGF-stimulated signal transmission by binding competitively at the ATP site of EGFR.
PROTAC STAT6 degrader-1 (Compound I-2) is a potent STAT6 PROTAC degrader with a DC50 <1 nM. PROTAC STAT6 degrader-1 inhibits STAT6 activity with an IC50 of <0.1 pM. PROTAC STAT6 degrader-1 can be used for inflammatory and cancers research, such as non-small cell lung cancer (NSCLC) .
Ceritinib (Standard) is the analytical standard of Ceritinib (HY-15656). This product is intended for research and analytical applications. Ceritinib is a selective, orally bioavailable, and ATP-competitive ALK tyrosine kinase inhibitor with an IC50 of 200 pM. Ceritinib also inhibits IGF-1R, InsR, and STK22D with IC50 values of 8, 7, and 23 nM, respectively. Ceritinib shows great antitumor potency .
Dot1L-IN-1 is a highly potent and selective Dot1L inhibitor with a Ki of 2 pM and an IC50 of <0.1 nM. Dot1L-IN-1 potently suppresses H3K79 dimethylation (IC50=3 nM), as well as the activity of the HoxA9 promoter (IC50=17 nM) in HeLa and Molm-13 cells, respectively .
Ondansetron (GR 38032; SN 307) is a highly selective 5-HT3 receptor antagonist with an IC50 value of 103 pM. Ondansetron exerts its antiemetic effect by antagonizing 5-HT receptors located in localized neurons in the peripheral and central nervous systems. Ondansetron can inhibit nausea and vomiting induced by chemotherapy and radiotherapy .
Navlimetostat hydrochloride is a potent, orally active, selective PRMT5-MTA complex inhibitor, with IC50s of 3.6 and 20.5 nM for PRMT5-MTA and PRMT5. Navlimetostat hydrochloride binds to the PRMT5-MTA complex, with KD value of 0.14 pM. Navlimetostat shows antineoplastic activity in vitro and in vivo, and can be used for cancer study .
Calmodulin Binding Peptide 1 is a high-affinity (pM) CaM-binding peptide derived from smooth muscle myosin light chain kinase (MLCK peptide). The interface of the complex formed by Calmodulin Binding Peptide 1 and Ca 2+-CaM can be specifically bound by small-molecule inhibitors, serving as a key target for selective regulation of smooth muscle contraction and development of anti-CaM drugs .
Canakinumab (ACZ885) is a recombinant human anti-IL-1β monoclonal antibody. Canakinumab shows IC50 values of 43.6 and 40.8 pM for human and marmoset IL-1β, respectively. The mode of action of canakinumab is based on the neutralization of IL-1β signaling, resulting in suppression of inflammation related to disorders of autoimmune origin .
PROTAC BRD9 Degrader-8 is a selective, orally active BRD9 PROTAC degrader with a DC50 of 16 pM.\nPROTAC BRD9 Degrader-8 induces cell cycle arrest at the G1 phase and promotes apoptosis. PROTAC BRD9 Degrader-8 can be used for research on acute myeloid leukemia and diffuse large B-cell lymphoma .
SHR0687 is a selective tetrapeptide kappa opioid receptor (KOR) agonist with an EC50 of 0.53 pM. SHR0687 displays high potency and selectivity over MOR and DOR, with negligible blood-brain barrier penetration. SHR0687 activates KOR specifically, leading to potential modulation of neurological pathways without significant central nervous system effects. SHR0687 can be used for the research of pain .
Ondansetron (GR 38032; SN 307) hydrochloride is a highly selective 5-HT3 receptor antagonist with an IC50 value of 103 pM. Ondansetron hydrochloride exerts its antiemetic effect by antagonizing 5-HT receptors located in localized neurons in the peripheral and central nervous systems. Ondansetron hydrochloride can inhibit nausea and vomiting induced by chemotherapy and radiotherapy .
Lopinavir (ABT-378) is a highly potent, selective peptidomimetic inhibitor of the HIV-1 protease, with Kis of 1.3 to 3.6 pM for wild-type and mutant HIV protease. Lopinavir acts by arresting maturation of HIV-1 thereby blocking its infectivity . Lopinavir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 14.2 μM .
β-Secretase Inhibitor IV (Standard) is the analytical standard of β-Secretase Inhibitor IV (HY-10133). This product is intended for research and analytical applications. β-Secretase Inhibitor IV is a potent, cell-active BACE-1 inhibitor with IC50s of 15.6 and 16.3nM under BACE-1 concentrations of 2 nM and 100 pM, respectively.
Seco-Duocarmycin SA is a DNA alkylator. Seco-Duocarmycin SA is an antitumor antibiotic (IC50 = 10 pM). Seco-Duocarmycin SA can induce a concentration-dependent increase in apoptotic cell death. Seco-Duocarmycin SA can lead to significant cell cycle arrest in S and G2/M phases. Seco-Duocarmycin SA acts as an ADC cytotoxin for antibody-drug conjugates .
Daclatasvir (BMS-790052) is a potent and orally active HCV NS5A protein inhibitor with EC50s range of 9-146 pM for multiple HCV replicon genotypes. Daclatasvir is also a organic anion transporting polypeptide 1B (OATP1B) and OATP1B3 inhibitor with IC50s of 1.5 µM and 3.27 µM, respectively .
SJ44236 is a BET PROTAC degrader with activity against BRD2, BRD3 and BRD4 (DC50 = 127 pM). SJ44236 induces ubiquitination and proteasomal degradation by forming a ternary complex with BET proteins and CRBN-DDB1. SJ44236 downregulates c-Myc, upregulates p53 and reduces cancer cell viability. SJ44236 can be used for the research of leukemia and medulloblastoma .
Ramelteon-d5 is deuterium labeled Ramelteon. Ramelteon is a potent, highly selective, and orally active agonist of MT1/MT2 with Ki values of 14 and 112 pM, respectively. Ramelteon has the potential for the research of insomnia. Ramelteon consistently reduces sleep onset after long-term treatment, with no next-morning residual effects or rebound insomnia or withdrawal symptoms upon discontinuation .
CAY10603 (Standard) is the analytical standard of CAY10603. This product is intended for research and analytical applications. CAY10603 (BML-281) is a potent and selective HDAC6 inhibitor, with an IC50 of 2 pM; CAY10603 (BML-281) also inhibits HDAC1, HDAC2, HDAC3, HDAC8, HDAC10, with IC50s of 271, 252, 0.42, 6851, 90.7 nM.
GSK951 is a potent and selective Kallikrein-5 (KLK5) inhibitor amenable to epidermal delivery. GSK951 shows an IC50 of 250 pM for KLK5 and greater than 100-fold selectivity over KLK7 and KLK14. GSK951 can reduce transepidermal water loss, and decrease proinflammatory cytokine expression. GSK951 can be used for the researches of inflammation and immunology, such as Netherton syndrome .
Dot1L-IN-1 TFA is a highly potent and selective Dot1L inhibitor with a Ki of 2 pM and an IC50 of <0.1 nM. Dot1L-IN-1 TFA potently suppresses H3K79 dimethylation (IC50=3 nM), as well as the activity of the HoxA9 promoter (IC50=17 nM) in HeLa and Molm-13 cells, respectively .
2-Iodomelatonin (Standard) is the analytical standard of 2-Iodomelatonin. This product is intended for research and analytical applications. 2-Iodomelatonin is a potent agonist of melatonin receptor 1 (MT1) with a Ki value of 28 pM, it is more 5-fold selective for MT1 ?over MT2 . 2-iodomelatonin can be used to identify, characterize and localize melatonin binding sites in the brain and peripheral tissues .
Pralatrexate is an antifolate and is a potent dihydrofolate reductasean (DHFR) inhibitor with a Ki of 13.4 pM. Pralatrexate is a substrate for folylpolyglutamate synthetase with improved cellular uptake and retention. Pralatrexate has antitumor activities and has the potential for relapsed/refractory T-cell lymphoma treatment . Pralatrexate is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Ceritinib (LDK378) dihydrochloride (Standard) is the analytical standard of Ceritinib dihydrochloride (HY-15656A). This product is intended for research and analytical applications. Ceritinib dihydrochloride is a selective, orally bioavailable, and ATP-competitive ALK tyrosine kinase inhibitor with an IC50 of 200 pM. Ceritinib dihydrochloride also inhibits IGF-1R, InsR, and STK22D with IC50 values of 8, 7, and 23 nM, respectively. Ceritinib shows great antitumor potency .
Dihexa, an oligopeptide drug, is an orally active and blood-brain barrier-permeable angiotensin IV analog. Dihexa binds to hepatocyte growth factor (HGF) with high affinity (Kd=65 pM) and potentiates its activity at its receptor, c-Met. Dihexa exhibits excellent antidementia activity and improves cognitive function in animal models. Dihexa may have therapeutic potential as a treatment Alzheimer’s disease .
Daclatasvir dihydrochloride (BMS-790052 dihydrochloride) is a potent and orally active HCV NS5A protein inhibitor with EC50s range of 9-146 pM for multiple HCV replicon genotypes. Daclatasvir dihydrochloride is also an organic anion transporting polypeptide 1B (OATP1B) and OATP1B3 inhibitor with IC50s of 1.5 μM and 3.27 μM, respectively .
Ramelteon (Standard) is the analytical standard of Ramelteon. This product is intended for research and analytical applications. Ramelteon is a potent, highly selective, and orally active agonist of MT1/MT2 with Ki values of 14 and 112 pM, respectively. Ramelteon has the potential for the research of insomnia. Ramelteon consistently reduces sleep onset after long-term treatment, with no next-morning residual effects or rebound insomnia or withdrawal symptoms upon discontinuation .
seco-CBI-PBD dimer is a CBI-PBD heterodimer and a minor groove DNA crosslinker. seco-CBI-PBD dimer exhibits cytotoxicity against human tumor cells at sub-pM to low nM levels, shows low sensitivity to P-glycoprotein-mediated drug resistance, and can serve as an ADC payload. seco-CBI-PBD dimer can be used in studies of uterine cancer, breast cancer, non-small cell lung cancer, etc.
Luzopeptin A (BBM-928 A) is an actinoleukin-like antitumor antibiotic. Luzopeptin A is a bifunctional DNA intercalator which can interact with isolated DNA molecules. Luzopeptin A induces an unwinding-rewinding process of the closed superhelical PM2 DNA. Luzopeptin A is active against HIV-1 and HIV-2 reverse transcriptase with IC50s of 7 nM and 68 nM for HIV-1 RT and HIV-2 RT, respectively .
GLP-1R agonist 40 (Compound I-1) is an orally active, potent and selective GLP-1R agonist (EC50 = 26.7 pM for cAMP accumulation). GLP-1R agonist 40 shows significant decrease in blood glucose levels. GLP-1R agonist 40 can be used in the research of type 2 diabetes .
Claziprotamidum (Claziprotamide; BBP-671) is a panthothenate kinase (PANK) activator with oral activity and blood-brain barrier permeability. Claziprotamidum binds to and activates all PANK isoforms, with the highest affinity for PANK3 (KD = 97 pM; IC50 = 1.39 nM). Claziprotamidum increases the intracellular biosynthesis of Coenzyme A (HY-128851) and restores mitochondrial function. Claziprotamidum can be used in the research of pantothenate kinase-associated neurodegeneration and propionic acidemia .
T-26c (Standard) is the analytical standard of T-26c (HY-100518). This product is intended for research and analytical applications. T-26c, a chemical probe, is highly potent and selective matrix metalloproteinase-13 (MMP-13) inhibitor with an IC50 of 6.75 pM and more than 2600-fold selectivity over the other related metalloenzymes .
Ixekizumab (LY2439821) is a humanized IgG4 monoclonal antibody that selectively binds and neutralizes interleukin IL-17A (KD<3 pM). Ixekizumab directly blocks IL-17A binding to IL-17RA (IL-17A receptor) but does not bind to other IL-17 family members. Ixekizumab is used for the research of moderate-to-severe plaque psoriasis .
BIO5192 hydrate is a selective and potent integrin α4β1 (VLA-4) inhibitor (Kd<10 pM). BIO5192 hydrate selectively binds to α4β1 (IC50=1.8 nM) over a range of other integrins. BIO5192 hydrate results in a 30-fold increase in mobilization of murine hematopoietic stem and progenitors (HSPCs) over basal levels .
BIO5192 is a selective and potent integrin α4β1 (VLA-4) inhibitor (Kd<10 pM). BIO5192 selectively binds to α4β1 (IC50=1.8 nM) over a range of other integrins. BIO5192 results in a 30-fold increase in mobilization of murine hematopoietic stem and progenitors (HSPCs) over basal levels .
TYY-31 is an orally active, selective S1PR1 agonist with an EC50 of 1.13 pM. TYY-31 promotes the phosphorylation of ERK1/2. TYY-31 exerts anti-inflammatory and immunosuppressive effects, ameliorates DSS-induced colitis in mice, and reduces peripheral blood lymphocyte counts in mice in a dose-dependent manner. TYY-31 can be used for the research of ulcerative colitis .
Ondansetron (GR 38032; SN 307) hydrochloride dehydrate is a highly selective 5-HT3 receptor antagonist with an IC50 value of 103 pM. Ondansetron hydrochloride dehydrate exerts its antiemetic effect by antagonizing 5-HT receptors located in localized neurons in the peripheral and central nervous systems. Ondansetron hydrochloride dehydrate can inhibit nausea and vomiting induced by chemotherapy and radiotherapy .
Inotuzumab ozogamicin (CMC-544) is an antibody-targeted chemotherapy agent composed of a humanized anti-CD22 antibody conjugated to Calicheamicin (HY-19609). Inotuzumab ozogamicin and G544 bind human CD22 with similar affinities (Kd ≈ 150 pM). Inotuzumab ozogamicin has demonstrated efficacy against CD22 + B-cell non-Hodgkin’s lymphoma. Inotuzumab ozogamicin can be used in the research of acute lymphoblastic leukemia .
Daclatasvir-d6 is deuterium labeled Daclatasvir. Daclatasvir (BMS-790052) is a potent and orally active HCV NS5A protein inhibitor with EC50s range of 9-146 pM for multiple HCV replicon genotypes. Daclatasvir is also a organic anion transporting polypeptide 1B (OATP1B) and OATP1B3 inhibitor with IC50s of 1.5 μM and 3.27 μM, respectively .
Nesvategrast (SF0166) is a potent and selective αvβ3 antagonist with IC50 values of 0.6 nM, 8 nM, and 13 nM for αvβ3, αvβ6, and αvβ8, respectively. Nesvategrast inhibits cellular adhesion to vitronectin across human, rat, rabbit, and dog cell lines with IC50 values of 7.6 pM to 76 nM. Nesvategrast decreases neovascularization in the oxygen-induced retinopathy mouse model .
SNAP 94847 hydrochloride is a novel, high affinity selective melanin-concentrating hormonereceptor1 (MCHR1) antagonist with (Ki= 2.2 nM, Kd=530 pM), it displays >80-fold and >500-fold selectivity over MCHα1A and MCHD2 receptors respectively. SNAP 94847 hydrochloride binds with high affinity to the mouse and rat MCHR1 with minimal cross-reactivity to other GPCR, ion channels, enzymes, and transporters .
RP-001 is a picomolar short-acting S1P1 (EDG1) selective agonist, with an EC50 of 9 pM. RP-00 induces internalization and polyubiquitination of S1P1. RP-001 has little activity on S1P2-S1P4 and only moderate affinity for S1P5 .
SNAP 94847 is a novel, high affinity selective melanin-concentrating hormonereceptor1 (MCHR1) antagonist with (Ki= 2.2 nM, Kd=530 pM), it displays >80-fold and >500-fold selectivity over MCHα1A and MCHD2 receptors respectively. SNAP 94847 binds with high affinity to the mouse and rat MCHR1 with minimal cross-reactivity to other GPCR, ion channels, enzymes, and transporters .
YM022 (Standard) is the analytical standard of YM022 (HY-103355). This product is intended for research and analytical applications. YM022 is a highly potent, selective and orally active gastrin/cholecystokinin (CCK)-B receptor (CCK-BR) antagonist. YM022 shows the Ki values of 68 pM and 63 nM for CCK-B and CCK-A receptor, respectively . YM022 can inhibit gastrin-induced gastric acid secretion and histidine decarboxylase activation in vivo .
Diprovocim is a potent TLR1/TLR2 agonist. Diprovocim elicits full agonist activity in human THP-1 cells (EC50=110 pM). Diprovocim stimulates the release of TNF-α from mouse macrophages (EC50=1.3 nM). Diprovocim activates downstream MAPK and NF-κB signaling pathway. Diprovocim displays strong adjuvant activity in mice, particularly abetting cellular immune responses .
IMP-1088 is a potent human N-myristoyltransferases NMT1 and NMT2 dual inhibitor with IC50s of <1 nM for HsNMT1 and HsNMT2. IMP-1088 has a Kd of <210 pM for HsNMT1. IMP-1088 efficiently blocks rhinovirus replication by blocking rhinovirus virus-encoded protein (VP0) N-myristoylation. IMP-1088 protects host cells from the cytotoxic effects of viral infection .
Denikitug (GS-1811; JTX-1811) is a humanized monoclonal antibody against CCR8 receptor with a KD of 16.8 pM. Denikitug specifically binds to human CCR8, inhibits CCL1-induced downstreamCCR8signaling. Denikitug selectively depletes cells expressing CCR8 via antibody-dependent cellular cytotoxicity (ADCC). Denikitug promotes anti-tumor immunity and can be used for the research of cancer and immunology .
PPTN, a chemical probe, is a potent, high-affinity, competitive and highly selective P2Y14 receptor antagonist with a KB value of 434 pM. PPTN exhibits no agonist or antagonist effect at the P2Y1, P2Y2, P2Y4, P2Y6, P2Y11, P2Y12, or P2Y13 receptors. Anti-inflammatory and immune activity .
PPTN hydrochloride is a potent, high-affinity, competitive and highly selective P2Y14 receptor antagonist with a KB value of 434 pM. PPTN hydrochloride exhibits no agonist or antagonist effect at the P2Y1, P2Y2, P2Y4, P2Y6, P2Y11, P2Y12, or P2Y13 receptors. Anti-inflammatory and anti-immune activity .
FM-479 is the negative control of FM-381 (HY-102046) and has no activity on JAK3 or other kinases . FM-381 is a potent covalent reversible inhibitor of JAK3 targeting the unique Cys909. FM-381 has an IC50 of 127 pM for JAK3, with 410, 2700 and 3600-fold selectivity over JAK1, JAK2 and TYK2, respectively.
PPTN mesylate is a potent, high-affinity, competitive and highly selective P2Y14 receptor antagonist with a KB value of 434 pM. PPTN mesylate exhibits no agonist or antagonist effect at the P2Y1, P2Y2, P2Y4, P2Y6, P2Y11, P2Y12, or P2Y13 receptors. Anti-inflammatory and immune activity .
RP-001 hydrochloride is a picomolar short-acting S1P1 (EDG1) selective agonist, with an EC50 of 9 pM. RP-00 hydrochloride induces internalization and polyubiquitination of S1P1. RP-001 hydrochloride has little activity on S1P2-S1P4 and only moderate affinity for S1P5 .
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 .
ADWX 1 is a new peptide inhibitor that is potent and selective for Kv1.3 with an IC50 value of 1.89 pM. ADWX 1 inhibits Kv1.3 channel activity specifically to inhibit both the initial calcium signaling and NF-κB activation. ADWX 1 ameliorates the disease in rats of experimental autoimmune encephalomyelitis (EAE) models. ADWX 1 can be used to study T cell-mediated autoimmune diseases .
ADWX 1 TFA is a new peptide inhibitor that is potent and selective for Kv1.3 with an IC50 value of 1.89 pM. ADWX 1 inhibits Kv1.3 channel activity specifically to inhibit both the initial calcium signaling and NF-κB activation. ADWX 1 TFA ameliorates the disease in rats of experimental autoimmune encephalomyelitis (EAE) models. ADWX 1 TFA can be used to study T cell-mediated autoimmune diseases .
Daclatasvir-d16 is deuterium labeled Daclatasvir. Daclatasvir (BMS-790052) is a potent and orally active HCV NS5A protein inhibitor with EC50s range of 9-146 pM for multiple HCV replicon genotypes. Daclatasvir is also a organic anion transporting polypeptide 1B (OATP1B) and OATP1B3 inhibitor with IC50s of 1.5 μM and 3.27 μM, respectively .
ShK-Dap22 is a potent Kv1.3-specific immunosuppressive Polypeptide. ShK-Dap22 is a selective Kv1.3 channel blocker with IC50s of 23 pM, 1.8 nM, 10.5 nM, 37 nM, and 39 nM for mKv1.3, mKv1.1, hKv1.6, mKv1.4, and rKv1.2 channels, respectively .
PSF-IN-2 (Compound (C)-30) is a PSF inhibitor with an IC50 value of 0.005 pM. PSF-IN-2 exhibits anti-cancer activity, and its IC50 value for inhibiting the proliferation of 22Rv1 cells is 0.5 μM. PSF-IN-2 activates the p53 signaling pathway by inhibiting the binding of PSF to RNA, inducing the expression of related genes, promoting apoptosis, and inhibiting the cell cycle. PSF-IN-2 can be used in cancer research .
HIV-1-IN-88 (compound 20a) is a potent HIV‑1 protease inhibitor (IC50 = 10 pM) with an antiviral EC50 of 10.4 nM. HIV-1-IN-88 exhibits potency against the multidrug-resistant variants HIV-1Muta and HIV-1I50V with EC50 values of 30.0 and 34.3 nM, respectively. HIV-1-IN-88 can be used for HIV research .
Daclatasvir (Standard) is the analytical standard of Daclatasvir. This product is intended for research and analytical applications. Daclatasvir (BMS-790052) is a potent and orally active HCV NS5A protein inhibitor with EC50s range of 9-146 pM for multiple HCV replicon genotypes. Daclatasvir is also a organic anion transporting polypeptide 1B (OATP1B) and OATP1B3 inhibitor with IC50s of 1.5 µM and 3.27 µM, respectively .
ERD-12310A is a PROTAC targeting Estrogen Receptor α (ERα) with a ED50 value of 47 pM. ERD-12310A has oral activity. ERD-12310A is composed of PROTAC target protein ligand ER ligand-4 (HY-164925) (red part), E3 ligase ligand (S)-Deoxy-thalidomide (HY-168055) (blue part). ERD-12310A can be used in the research of ER + breast cancer .
Lopinavir-d8 (ABT-378-d8) is the deuterium labeled Lopinavir. Lopinavir (ABT-378) is a highly potent, selective peptidomimetic inhibitor of the HIV-1 protease, with Kis of 1.3 to 3.6 pM for wild-type and mutant HIV protease. Lopinavir acts by arresting maturation of HIV-1 thereby blocking its infectivity . Lopinavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 14.2 μM .
Lopinavir-d7 is deuterated labeled Lopinavir (HY-14588). Lopinavir (ABT-378) is a highly potent, selective peptidomimetic inhibitor of the HIV-1 protease, with Kis of 1.3 to 3.6 pM for wild-type and mutant HIV protease. Lopinavir acts by arresting maturation of HIV-1 thereby blocking its infectivity . Lopinavir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 14.2 μM .
Ceritinib (LDK378)-d7 is a deuterium labeled Ceritinib (HY-15656). Ceritinib is a selective, orally bioavailable and ATP-competitive ALK tyrosine kinase inhibitor . Ceritinib is a selective, orally bioavailable, and ATP-competitive ALK tyrosine kinase inhibitor with an IC50 of 200 pM. Ceritinib also inhibits IGF-1R, InsR, and STK22D with IC50 values of 8, 7, and 23 nM, respectively. Ceritinib shows great antitumor potency .
Etrolizumab (rhuMAb Beta7) is a gut-selective, anti-β7 integrin monoclonal antibody. Etrolizumab is specific targeting of the β7 subunit of α4β7 and αEβ7 integrins with Ki values of 18 nM and 1800 pM for Human α4β7 and Human αEβ7-293, respectively. Etrolizumab can be used in research of inflammatory bowel disease (IBD) .
Lopinavir (Standard) is the analytical standard of Lopinavir. This product is intended for research and analytical applications. Lopinavir (ABT-378) is a highly potent, selective peptidomimetic inhibitor of the HIV-1 protease, with Kis of 1.3 to 3.6 pM for wild-type and mutant HIV protease. Lopinavir acts by arresting maturation of HIV-1 thereby blocking its infectivity . Lopinavir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 14.2 μM .
Nesiritide (Brain Natriuretic Peptide-32 human) acetate is a recombinant human B-type natriuretic peptide. Nesiritide acetate is a NPRs agonist, with Kd values of 7.3 and 13 pM for NPR-A and NPR-C, respectively. Nesiritide acetate regulates V1/2 activation/inactivation of the L-type calcium channel. Nesiritide acetate shows vasodilatory, diuretic, and natriuretic activities. Nesiritide acetate is used in cardiovascular diseases such as heart failure and vascular remodeling after arterial injury .
GUB021794 is a potent and highly selective glucagon-like peptide-1 receptor (GLP-1R) agonist developed using the streaMLine platform with an EC50 value of 18 pM. GUB021794 has a very weak activity against SCTR, with an EC50 value of 190 nM. GUB021794 can significantly reduce the body weight, food intake, and total fat mass of mice in a diet-induced obesity (DIO) model. GUB021794 can be used for research on obesity/diabetes .
Daclatasvir (dihydrochloride) (Standard) is the analytical standard of Daclatasvir (dihydrochloride). This product is intended for research and analytical applications. Daclatasvir dihydrochloride (BMS-790052 dihydrochloride) is a potent and orally active HCV NS5A protein inhibitor with EC50s range of 9-146 pM for multiple HCV replicon genotypes. Daclatasvir dihydrochloride is also an organic anion transporting polypeptide 1B (OATP1B) and OATP1B3 inhibitor with IC50s of 1.5 µM and 3.27 µM, respectively .
Pralatrexate (Standard) is the analytical standard of Pralatrexate. This product is intended for research and analytical applications. Pralatrexate is an antifolate and is a potent dihydrofolate reductasean (DHFR) inhibitor with a Ki of 13.4 pM. Pralatrexate is a substrate for folylpolyglutamate synthetase with improved cellular uptake and retention. Pralatrexate has antitumor activities and has the potential for relapsed/refractory T-cell lymphoma treatment . Pralatrexate is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Ramelteon-d3 (TAK-375-d3) is a deuterium-labelled Ramelteon (HY-A0014). Ramelteon is a potent, highly selective, and orally active agonist of MT1/MT2 with Ki values of 14 and 112 pM, respectively. Ramelteon has the potential for the research of insomnia. Ramelteon consistently reduces sleep onset after long-term treatment, with no next-morning residual effects or rebound insomnia or withdrawal symptoms upon discontinuation.
TBK1-IN-2 (Compound A1) is a potent TBK1 inhibitor (IC50: 775 pM). TBK1-IN-2 binds to TBK1 through stable hydrogen bonds and π-π stacking, inhibiting IRF3 phosphorylation. TBK1-IN-2 synergizes with TNF/IFNγ to enhance immune-mediated tumor cell death. TBK1-IN-2 can be used in cancer immunotherapy research .
Nesiritide (Brain Natriuretic Peptide-32 human) is a recombinant human B-type natriuretic peptide. Nesiritide is a NPRs agonist, with Kd values of 7.3 and 13 pM for NPR-A and NPR-C, respectively. Nesiritide regulates V1/2 activation/inactivation of the L-type calcium channel. Nesiritide shows vasodilatory, diuretic, and natriuretic activities. Nesiritide is used in cardiovascular diseases such as heart failure and vascular remodeling after arterial injury .
Ctx-L3 is a selective EGFRPTAC (PSMA-targeted chimera) degrader (DC50: 4.3 pM in LNCaP cells) and LYTAC. Ctx-L3 recruits prostate-specific membrane antigen (PSMA) and mediates lysosomal degradation of EGFR in PSMA-positive prostate cancer cells. Ctx-L3 exhibits degrading activity against EGFR in prostate cancer cells. Ctx-L3 is applicable to related research on prostate cancer .
OSI-7904L (GW1843; 1843U89; OSI-7904) is a thymidylate synthase (TS) inhibitor with a Ki of 90 pM. OSI-7904L blocks de novo synthesis of thymidine nucleotides, DNA synthesis and induces cell death. OSI-7904L inhibits the growth of human cells, induces tumor regression, and achieves durable antitumor effects in mouse xenograft models. OSI-7904L can be used in research related to colon adenocarcinoma .
IDO1-IN-32 (Compound 45) is a potent and orally effective IDO1 inhibitor with an IC50 of 10 pM. IDO1-IN-32 exhibits significant anti-proliferative activity against Hela cells. IDO1-IN-32 can significantly inhibit tumor growth in CT26 and LCC transplanted mouse models by activating anti-tumor immunity. IDO1-IN-32 can be used for research on colon cancer and breast cancer .
FAK-IN-16 (compound OXA-11) is an orally active, selective focal adhesion kinase (FAK) inhibitor with an IC50 of 1.2 pM. FAK-IN-16 inhibits FAK phosphorylation at pFAK[Y397] and pFAK[Y861]. FAK-IN-16 slows tumor growth and reduces tumor vascularity, invasion. FAK-IN-16 potentiates effects of Cisplatin (HY-17394) on tumor cell proliferation and apoptosis in vitro and anti-tumor actions in mice .
CK2-IN-15 (Compound Biv5) is a selective and potent bivalent protein kinase CK2 inhibitor with an IC50 value of 51 pM. CK2-IN-15 significantly reduces the replication of SARS-CoV-2 in HEK-ACE2-TMPRSS2 and Vero cells, and also reduces viral replication in an ex vivo model of human nasal epithelial cells. CK2-IN-15 is promising for research of β-coronavirus infection-related diseases .
Ondansetron-d3 is the deuterium labeled Ondansetron (HY-B0002B ). Ondansetron (GR 38032; SN 307) is a highly selective 5-HT3 receptor antagonist with an IC50 value of 103 pM. Ondansetron exerts its antiemetic effect by antagonizing 5-HT receptors located in localized neurons in the peripheral and central nervous systems. Ondansetron can inhibit nausea and vomiting induced by chemotherapy and radiotherapy .
EGFR is a driver of tumorigenesis. EGFR is mainly found in an auto-inhibited, dimerization-incompetent, state at the plasma membrane (PM). Ligand binding promotes receptor dimerization, which determines a series of structural rearrangements that are conveyed to the cytoplasmic domain allowing the formation of asymmetric dimers between the two juxtaposed catalytic domains. EGFR has multiple mutants. EGFR G719C Recombinant Human Active Protein Kinase is a recombinant EGFR G719C protein that can be used to study EGFR G719C-related functions .
EGFR is a driver of tumorigenesis. EGFR is mainly found in an auto-inhibited, dimerization-incompetent, state at the plasma membrane (PM). Ligand binding promotes receptor dimerization, which determines a series of structural rearrangements that are conveyed to the cytoplasmic domain allowing the formation of asymmetric dimers between the two juxtaposed catalytic domains. EGFR has multiple mutants. EGFR L718Q Recombinant Human Active Protein Kinase is a recombinant EGFR L718Q protein that can be used to study EGFR L718Q-related functions .
TAK-683 acetate is a potent full KISS1 receptor (KISS1R) agonist (IC50=170 pM) with improved metabolic stability. TAK-683 acetate is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC50 values of 0.96 nM and 1.6 nM for human and rat, respectively . TAK-683 acetate depletes GnRH in the hypothalamus and reduces plasma FSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer .
palm-PrRP31 is a potent dual receptor agonist for both GPR10 (EC50=72 pM) and NPFF-R2. palm-PrRP31 activates downstream signaling pathways through binding to its receptors, GPR10 and NPFF-R2, which results in reduced appetite and increased energy expenditure. Utilizing palm-PrRP31 facilitates the study of the mechanism of action in the nervous system, thereby elucidating the complex biological processes that regulate appetite and energy expenditure .
EGFR is a driver of tumorigenesis. EGFR is mainly found in an auto-inhibited, dimerization-incompetent, state at the plasma membrane (PM). Ligand binding promotes receptor dimerization, which determines a series of structural rearrangements that are conveyed to the cytoplasmic domain allowing the formation of asymmetric dimers between the two juxtaposed catalytic domains. EGFR has multiple mutants. EGFR C797S Recombinant Human Active Protein Kinase is a recombinant EGFR C797S protein that can be used to study EGFR C797S-related functions .
EGFR is a driver of tumorigenesis. EGFR is mainly found in an auto-inhibited, dimerization-incompetent, state at the plasma membrane (PM). Ligand binding promotes receptor dimerization, which determines a series of structural rearrangements that are conveyed to the cytoplasmic domain allowing the formation of asymmetric dimers between the two juxtaposed catalytic domains. EGFR has multiple mutants. EGFR L858R Recombinant Human Active Protein Kinase is a recombinant EGFR L858R protein that can be used to study EGFR L858R-related functions .
LY2183240 is a highly potent blocker of anandamide uptake (IC50= 270 pM; Ki=540 nM). LY2183240 is a potent, covalent inhibitor of the endocannabinoid-degrading enzyme fatty acid amide hydrolase (FAAH) with an IC50 of 12.4 nM. LY2183240 inactivates FAAH by carbamylation of the enzyme's serine nucleophile. LY2183240 also inhibits several other brain serine hydrolases with IC50s of 5.3, 0.09, 8.2 nM for MAG lipase, bh6 and KIAA1363, respectively .
EGFR is a driver of tumorigenesis. EGFR is mainly found in an auto-inhibited, dimerization-incompetent, state at the plasma membrane (PM). Ligand binding promotes receptor dimerization, which determines a series of structural rearrangements that are conveyed to the cytoplasmic domain allowing the formation of asymmetric dimers between the two juxtaposed catalytic domains. EGFR has multiple mutants. EGFR L861Q Recombinant Human Active Protein Kinase is a recombinant EGFR L861Q protein that can be used to study EGFR L861Q-related functions .
Ondansetron-d5 is the deuterium labeled Ondansetron (HY-B0002B). Ondansetron (GR 38032; SN 307) is a highly selective 5-HT3 receptor antagonist with an IC50 value of 103 pM. Ondansetron exerts its antiemetic effect by antagonizing 5-HT receptors located in localized neurons in the peripheral and central nervous systems. Ondansetron can inhibit nausea and vomiting induced by chemotherapy and radiotherapy .
MG-101 (GMP) (Calpain inhibitor I (GMP)) is MG-101 (HY-18964) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. MG-101 (ALLN) is an inhibitor of cysteine proteases which inhibits calpain I, calpain II, cathepsin B and cathepsin L with Kis of 190, 220, 150 and 500 pM, respectively. MG-101 induces apoptosis and inhibits tumor growth, it can be used for the research of colon cancer .
Ondansetron (Standard) is the analytical standard of Ondansetron (HY-B0002B). This product is intended for research and analytical applications. Ondansetron (GR 38032; SN 307) is a highly selective 5-HT3 receptor antagonist with an IC50 value of 103 pM. Ondansetron exerts its antiemetic effect by antagonizing 5-HT receptors located in localized neurons in the peripheral and central nervous systems. Ondansetron can inhibit nausea and vomiting induced by chemotherapy and radiotherapy .
MIPS3526 is a potent and selective A2B adenosine receptor (A2BR) agonist with a pEC50 of 10.17 (EC50 of 58 pM). MIPS3526 shows highly receptor subtype selective versus the A1R, A2AR, and A3R. MIPS3526 ameliorates angiotensin II stimulating effects in both cardiac myocytes and fibroblasts. MIPS3526 can be used for the study of cardiovascular disease including heart failure where cardiac remodeling is a major driver .
TAK-683 is a potent full KISS1 receptor (KISS1R) agonist (IC50=170 pM) with improved metabolic stability. TAK-683 is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC50 values of 0.96 nM and 1.6 nM for human and rat, respectively . TAK-683 depletes GnRH in the hypothalamus and reduces plasma FSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer .
Disorazol A1 is an tubulin inhibitor with antifungal activity. Disorazol A1 functions by inhibiting tubulin polymerization, interfering with microtubule formation, blocking mitosis, thus arresting the cell cycle at the G2/M phase and inducing apoptosis. Disorazol A1 also exhibits an inhibitory effect against L929 mouse fibroblasts with an IC50 value of 3 pM. Disorazol A1 causes the accumulation of p53 protein in the cell nucleus. Disorazol A1 is promising for research of cancers .
EGFR is a driver of tumorigenesis. EGFR is mainly found in an auto-inhibited, dimerization-incompetent, state at the plasma membrane (PM). Ligand binding promotes receptor dimerization, which determines a series of structural rearrangements that are conveyed to the cytoplasmic domain allowing the formation of asymmetric dimers between the two juxtaposed catalytic domains. EGFR has multiple mutants. EGFR G719S Recombinant Human Active Protein Kinase is a recombinant EGFR G719S protein that can be used to study EGFR G719S-related functions .
EGFR is a driver of tumorigenesis. EGFR is mainly found in an auto-inhibited, dimerization-incompetent, state at the plasma membrane (PM). Ligand binding promotes receptor dimerization, which determines a series of structural rearrangements that are conveyed to the cytoplasmic domain allowing the formation of asymmetric dimers between the two juxtaposed catalytic domains. EGFR has multiple mutants. EGFR T790M Recombinant Human Active Protein Kinase is a recombinant EEGFR T790M protein that can be used to study EGFR T790M-related functions .
TPM003 (TG062) is a triple agonist of GLP-1R, GIPR and GCGR, with EC50 values of 33.9, 12.5 and 92.9 pM, respectively. TPM003 suppresses appetite, regulates blood glucose, enhances insulin sensitivity, reduces gastrointestinal intolerance, promotes hepatic lipid mobilization and increases energy expenditure. TPM003 induces weight loss, improves metabolic parameters, reverses hepatic steatosis and optimizes liver function markers. TPM003 is applicable for research on obesity and non-alcoholic steatohepatitis .
LY3541860 is a selective anti-CD19 antibody that both binds human CD19 with high affinity and selectively binds human B cells (Kd values: 76.8 pM and 94.5 nM for humans and cynomolgus monkeys, respectively). LY3541860 inhibits CpG-induced CD69 expression (IC50 = 0.006 nM). LY3541860 exhibits potent B cell inhibitory activities. LY3541860 can inhibit both BCR- and TLR-induced human B cell activation. LY3541860 can be used for the research of autoimmune diseases .
Cofetuzumab pelidotin (PF-06647020) is a PTK7-targeting ADC comprising a humanized anti-PTK7 mAb (hu6M024, IgG1) joined to an auristatin microtubule inhibitor payload, auristatin-0101 (Aur0101; HY-12522), by a cleavable valine-citrulline (vc)-based linker. Cofetuzumab pelidotin has a DAR of 4. Cofetuzumab pelidotin binds to cell-surface PTK7 with an EC50 of 1153 pM by flow cytometry. Cofetuzumab pelidotin has the potential for solid tumors research .
EGFR is a driver of tumorigenesis. EGFR is mainly found in an auto-inhibited, dimerization-incompetent, state at the plasma membrane (PM). Ligand binding promotes receptor dimerization, which determines a series of structural rearrangements that are conveyed to the cytoplasmic domain allowing the formation of asymmetric dimers between the two juxtaposed catalytic domains. EGFR has multiple mutants. EGFR d752-759 Recombinant Human Active Protein Kinase is a recombinant EGFR d752-759 protein that can be used to study EGFR d752-759-related functions .
BIO5192 (Standard) is the analytical standard of BIO5192 (HY-107589). This product is intended for research and analytical applications. BIO5192 is a selective and potent integrin α4β1 (VLA-4) inhibitor (Kd<10 pM). BIO5192 selectively binds to α4β1 (IC50=1.8 nM) over a range of other integrins. BIO5192 results in a 30-fold increase in mobilization of murine hematopoietic stem and progenitors (HSPCs) over basal levels .
TAK-683 TFA is a potent full KISS1 receptor (KISS1R) agonist (IC50=170 pM) with improved metabolic stability. TAK-683 TFA is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC50 values of 0.96 nM and 1.6 nM for human and rat, respectively . TAK-683 TFA depletes GnRH in the hypothalamus and reduces plasma FSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer .
EGFR is a driver of tumorigenesis. EGFR is mainly found in an auto-inhibited, dimerization-incompetent, state at the plasma membrane (PM). Ligand binding promotes receptor dimerization, which determines a series of structural rearrangements that are conveyed to the cytoplasmic domain allowing the formation of asymmetric dimers between the two juxtaposed catalytic domains. EGFR has multiple mutants. EGFR d746-750 Recombinant Human Active Protein Kinase is a recombinant EGFR d746-750 protein that can be used to study EGFR d746-750-related functions .
SNAP 94847 hydrochloride (Standard) is the analytical standard of SNAP 94847 (hydrochloride) (HY-107625A). This product is intended for research and analytical applications. SNAP 94847 hydrochloride is a novel, high affinity selective melanin-concentrating hormonereceptor1 (MCHR1) antagonist with (Ki= 2.2 nM, Kd=530 pM), it displays >80-fold and >500-fold selectivity over MCHα1A and MCHD2 receptors respectively. SNAP 94847 hydrochloride binds with high affinity to the mouse and rat MCHR1 with minimal cross-reactivity to other GPCR, ion channels, enzymes, and transporters .
Elezanumab (ABT-555; AE12-1Y-QL) is a human monoclonal antibody that selectively targets repulsive guidance molecule A (RGMa). Elezanumab potently inhibited RGMa mediated BMP signalling via the SMAD1/5/8 pathway, with an IC50 around 97 pM. Elezanumab promotes neuroregeneration and neuroprotection in neuronal injury and demyelination models binds N-terminal RGMa, blocks BMP signaling and lacks RGMc cross-reactivity. elezanumab has neuroregenerative and neuroprotective activities without impact on iron metabolism .
Ondansetron- 13C,d3 is the 13C- and deuterium labeled Ondansetron (HY-B0002B). Ondansetron (GR 38032; SN 307) is a highly selective 5-HT3 receptor antagonist with an IC50 value of 103 pM. Ondansetron exerts its antiemetic effect by antagonizing 5-HT receptors located in localized neurons in the peripheral and central nervous systems. Ondansetron can inhibit nausea and vomiting induced by chemotherapy and radiotherapy .
(rel)-Lopinavir-d8 ((rel)-ABT-378-d8) is the deuterium labeled Lopinavir (HY-14588) . Lopinavir (ABT-378) is a highly potent, selective peptidomimetic inhibitor of the HIV-1 protease, with Kis of 1.3 to 3.6 pM for wild-type and mutant HIV protease. Lopinavir acts by arresting maturation of HIV-1 thereby blocking its infectivity . Lopinavir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 14.2 μM .
HIV-1 protease-IN-1 (Compound 1e) is a potent inhibitor of HIV-1 protease with an IC50 of 90 pM. HIV-1 protease-IN-1 demonstrates antiviral activity with EC50 value of 89 nM against B-HIV. HIV-1 protease-IN-1 exhibits activity with EC50 value of 13.59 nM against C-HIV strain ZM246. HIV-1 protease-IN-1 shows remarkable activity with EC50 value of 8.23 nM against C-HIV strain Indie [1].
palm11-PrRP31 is a lipidized endogenous appetite inhibitory neuropeptide (PrRP) analogue. palm11-PrRP31 is GPR10 (EC50=39 pM) and NPFF-R2 effective dual agonists. palm11-PrRP31 is able to mimic the natural function of PrRP by binding to these receptors to reduce food intake. palm11-PrRP31 can be used as a potential anti-obesity agent and for the study of neuropeptide-receptor interaction .
Rademikibart (CBP-201) is a human monoclonal antibody targeting IL-4Rα with a KD of 20.7 pM when binding to human IL-4Rα epitopes. Rademikibart does not bind to IL-4Rα from other species. Rademikibart inhibits IL-4 and IL-13-mediated STAT6 signaling, TF-1 cell proliferation and TARC production in PBMCs. Rademikibart has the potential for moderate-to-severe Th2 inflammatory diseases research .
NS5A-IN-4 (Compound 1.12) is an orally active pan-genotypic hepatitis C virus (HCV) NS5A inhibitor with IC50 values of 1.2, 2296, 4.6, 362, 10.3 and 693 pM against gT1b, gT1a, gT2a, gT3a, gT4a and gT5a . NS5A-IN-4 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Tagmokitug (CHS-114; SRF-114) is a fully human IgG1 antibody targeting CCR8. Tagmokitug selectively binds to human CCR8 (Kd = 502 pM) and mediates the death of CCR8-expressing cells via antibody-dependent cellular cytotoxicity and antibody-dependent cellular phagocytosis. Tagmokitug selectively eliminates intratumoral regulatory T cells, induces tumor growth inhibition, remodels the tumor immune microenvironment, and promotes the differentiation of cytotoxic CD8 + T cell subsets. Tagmokitug can be used for the research of solid tumors .
Emodin-8-glucoside is an anthraquinone derivative that can be isolated from Aloe vera. Emodin-8-glucoside is the inhibitor for MAPK with an inhibition constant of 430.14 pM. Emodin-8-glucoside exhibits moderate inhibitory activity against rat lens aldose reductase (ALAR) and topoisomerases II with IC50s of 14.4 μM and 66 μM. Emodin-8-glucoside exhibits antioxidant, anti-inflammatory and anti-fibrotic activities. Emodin-8-glucoside can cross the blood brain barrier .
BTPTT-4F (Y6) is a non-fullerene acceptor-donor-acceptor (A-D-A) type small molecular acceptor (SMA) characterized by its flexible alkyl chains and centrally fused ring structure. Featuring a ladder-type electron-deficient core, BTPTT-4F can be effectively blended with PM6, showcasing significant potential for enhancing the performance of organic photovoltaic applications. Its tailored optical properties and adjustable electronic energy levels contribute to improved thermal and photochemical stability, making it a promising candidate for next-generation high-performance organic solar cells.
palm11-PrRP31 TFA is a lipidized endogenous appetite inhibitory neuropeptide (PrRP) analogue. palm11-PrRP31 TFA is GPR10 (EC50=39 pM) and NPFF-R2 effective dual agonists. palm11-PrRP31 TFA is able to mimic the natural function of PrRP by binding to these receptors to reduce food intake. palm11-PrRP31 TFA can be used as a potential anti-obesity agent and for the study of neuropeptide-receptor interaction .
Sintilimab (IBI308) is a safe and effectivel humanized IgG4 monoclonal antibody that binds to PD-1 with a KD value of 74 pM. Sintilimab blocks the interaction of PD-1 with its ligands (PD-L1 and PL-L2), consequently helping to restore the endogenous antitumour T-cell response. Sintilimab combined with prebiotics inhibits tumor volume and regulates immune cell subpopulation balance in lung adenocarcinoma mice. Sintilimab can be used for the research of classical Hodgkin's lymphoma, non-small cell lung cancer and oesophageal cancer .
Mal-Val-Ala-PAB-N(SO2Me)-Exatecan (Compound LE14) is a conjugate of an ADC toxin Exatecan (HY-13631) and a linker Mal-Val-Ala-PAB-N(SO2Me). Mal-Val-Ala-PAB-N(SO2Me)-Exatecan can be used for synthesis of ADC FZ-AD005. FZ-AD005 is a delta-like ligand 3 (DLL3, KD=58.3 pM) targeting ADC, that exhibits antitumor efficacy against SCLC cancer .
CYP1B1-IN-11 (Compound M2) is a selective CYP1B1 inhibitor with an IC50 of 0.00605 pM. CYP1B1-IN-11 effectively reverses DMBA (HY-W011845)-induced Paclitaxel (HY-B0015) resistance and CYP1B1-IN-11 suppresses tumor cells invasion and migration. CYP1B1-IN-11 can be used for tumor drug resistance research .
LY2183240 (Standard) is the analytical standard of LY2183240 (HY-10865). This product is intended for research and analytical applications. LY2183240 is a highly potent blocker of anandamide uptake (IC50= 270 pM; Ki=540 nM). LY2183240 is a potent, covalent inhibitor of the endocannabinoid-degrading enzyme fatty acid amide hydrolase (FAAH) with an IC50 of 12.4 nM. LY2183240 inactivates FAAH by carbamylation of the enzyme's serine nucleophile. LY2183240 also inhibits several other brain serine hydrolases with IC50s of 5.3, 0.09, 8.2 nM for MAG lipase, bh6 and KiAA1363, respectively .
HCGRP-(8-37) (Human α-CGRP (8-37)) is a fragment of human calcitonin gene-related peptide (hCGRP) and an antagonist of the CGRP receptor, with an IC50 of 32.1 pM against the CGRP receptor. HCGRP-(8-37) blocks adenylate cyclase activation induced by CGRP receptor ligands and attenuates vascular responses triggered by CGRP. HCGRP-(8-37) reduces capsaicin-induced vasodilation in porcine nasal mucosa and superficial skin. HCGRP-(8-37) serves as a research tool to distinguish effects mediated by CGRP or calcitonin receptors, and to investigate CGRP-induced vascular effects .
huDMB5F3 (DMB5F3; chDMB5F3) is a human monoclonal antibody against human CD227/MUC1, with a Ka value of 5.89 pM for its human target. huDMB5F3 enters MUC1-positive cancer cells via a temperature-dependent internalization process. huDMB5F3 induces cytotoxicity in MUC1-positive cancer cells. huDMB5F3 can be used in the research of various cancers including breast cancer, pancreatic cancer and gastric cancer .
[D-Ala2]-GIP (human) is a GIP receptor agonist (EC50 = 630 pM). [D-Ala2]-GIP (human) improves glucose tolerance. [D-Ala2]-GIP (human) shows neuroprotective activity in MPTP (HY-W114750)-induced Parkinson's disease model. [D-Ala2]-GIP (human) also improves cognitive function and hippocampal synaptic plasticity in obese diabetic rats. [D-Ala2]-GIP (human) can be used for research of type 2 diabetes, Parkinson's disease, etc
RKER-216 is a human monoclonal IgG antibody inhibitor targeting ALK2 with a KD of 58.7 pM. RKER-216 reduces hepcidin transcription in Hep3B.RKER-216 competes with BMP ligands for binding to the extracellular domain of ALK2, thereby inhibiting BMP-SMAD signal. RKER-216 mobilizes tissue iron effectively in inflammatory conditions. RKER-216 improves microcytic anemia in a dose-dependent manner by inhibiting SMAD signaling to reduce hepcidin and promote iron absorption and utilization in vivo. RKER-216 can be used for research on anemia of inflammation .
EZM8266 is an orally active and selective G9a (EHMT2) histone methyltransferase inhibitor with a human EHMT2IC50 of 1 pM. EZM8266 reduces repressive H3K9me2 marks at immune-stimulatory gene and endogenous retroviral element promoters. EZM8266 reduces colony formation, migration, and invasion of cancer cells. EZM8266 enhances IFN-γ response, increases MHC class I expression, and enhances CXCL10-mediated T cell recruitment in cancer cells. EZM8266 can be used for the research of hepatocellular carcinoma .
PRMT5-IN-53 is a gut-restricted and orally active PRMT5 inhibitor with pIC50s of ≥ 9.7 against hPRMT5 and mPRMT5. PRMT5-IN-53 binds to the PRMT5:MEP50 complex with a KD of 11.3 pM. PRMT5-IN-53 effectively inhibits PRMT5 locally in the intestines of mice, significantly reducing the number and area of polyps, while avoiding systemic hematological toxicity (such as anemia, neutropenia). PRMT5-IN-53 can be used for the study of colorectal cancer especially for familial adenomatous polyposis (FAP) .
EGFR is a driver of tumorigenesis. EGFR is mainly found in an auto-inhibited, dimerization-incompetent, state at the plasma membrane (PM). Ligand binding promotes receptor dimerization, which determines a series of structural rearrangements that are conveyed to the cytoplasmic domain allowing the formation of asymmetric dimers between the two juxtaposed catalytic domains. EGFR has multiple mutants. EGFR T790M/L858R Recombinant Human Active Protein Kinase is a recombinant EGFR T790M/L858R protein that can be used to study EGFR T790M/L858R-related functions .
L-771688 hydrochloride is a potent and highly selective α1A-adrenoceptor antagonist (Kd=43-90 pM). L-771688 hydrochloride is effective against cloned human, rat and dog α1A-adrenergic receptors. L-771688 exhibits high affinity (Ki ≤ 1 nM) and over 500-fold selectivity over the α1B and α1D isoforms. L-771688 potently antagonizes norepinephrine-induced responses at these receptors. Inhibits contractions induced by phenylephrine or A-61603 in rat, dog, human and monkey models .
hCYP1B1-IN-2 (compound 3n) is a potent human cytochrome P450 1B1 enzyme hCYP1B1 inhibitor. hCYP1B1-IN-2 shows the extremely potent anti-hCYP1B1 activity (IC50=0.040 nM) and blocks AhR transcription activity. hCYP1B1-IN-2 potently inhibits hCYP1B1 via a mix inhibition manner, showing a Ki value of 21.71 pM .
MRTX1133 formic is a noncovalent, potent, and selective KRAS G12D inhibitor. MRTX1133 formic optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated KD against KRAS G12D of 0.2 pM. MRTX1133 formic prevents SOS1-catalyzed nucleotide exchange and/or formation of the KRASG12D/GTP/RAF1 complex, thereby inhibiting mutant KRAS-dependent signal transduction. MRTX1133 formic shows efficacy in tumor models harboring KRAS G12D mutations .
EGFR is a driver of tumorigenesis. EGFR is mainly found in an auto-inhibited, dimerization-incompetent, state at the plasma membrane (PM). Ligand binding promotes receptor dimerization, which determines a series of structural rearrangements that are conveyed to the cytoplasmic domain allowing the formation of asymmetric dimers between the two juxtaposed catalytic domains. EGFR has multiple mutants. EGFR d747-749/A750P Recombinant Human Active Protein Kinase is a recombinant EGFR d747-749/A750P protein that can be used to study EGFR d747-749/A750P-related functions .
CL-387785 (EKI-785; WAY-EKI 785) is an orally active EGFR inhibitor with an IC50 of 370 pM. CL-387785 inhibits EGF-stimulated EGFR autophosphorylation with an IC50 of approximately 5 nM. CL-387,785 exerts selective inhibition on cell lines overexpressing EGFR or c-erbB-2, whereas it shows weak inhibitory effects on cell lines with low expression of these two receptors. CL-387785 effectively induces cell cycle arrest and apoptosis. CL-387785 can be used for the research of non-small cell lung cancer and autosomal recessive polycystic kidney disease .
Daclatasvir- 13C2,d6 (BMS-790052- 13C2,d6) is 13C and deuterium labeled Daclatasvir. Daclatasvir (BMS-790052) is a potent and orally active HCV NS5A protein inhibitor with EC50s range of 9-146 pM for multiple HCV replicon genotypes. Daclatasvir is also a organic anion transporting polypeptide 1B (OATP1B) and OATP1B3 inhibitor with IC50s of 1.5 μM and 3.27 μM, respectively .
COM503 is a high-affinity anti-IL18BP human monoclonal antibody with a Kd value of 0.291 pM. COM503 binds to IL18BP, blocks the IL18BP:IL18 interaction, displaces IL18 from preformed complexes, and enhances the activation and function of T cells and NK cells. COM503 induces anti-tumor effects by relieving the activity inhibition of endogenous IL18 in the tumor microenvironment. COM503 can be used for cancer research. The recommended isotype control is Human IgG4 (S228P) kappa, Isotype Control (HY-P99003) .
KOR agonist 6 is a KOR agonist (Ki = 0.25 pM). KOR agonist 6 shows agonistic activity at MOR and DOR in CHO cells and inhibits Forskolin (HY-15371)-stimulated cAMP accumulation. KOR agonist 6 stimulates KOR-mediated [ 35S]GTPγS binding and inhibits cAMP accumulation in KOR-expressing HEK293 cells with potent agonistic activity, while showing lower β-arrestin recruitment potency. KOR agonist 6 demonstrates anti-nociceptive efficacy in mice. KOR agonist 6 can be used for the study of analgesics with reduced central nervous system (CNS) side effects .
EGFR is a driver of tumorigenesis. EGFR is mainly found in an auto-inhibited, dimerization-incompetent, state at the plasma membrane (PM). Ligand binding promotes receptor dimerization, which determines a series of structural rearrangements that are conveyed to the cytoplasmic domain allowing the formation of asymmetric dimers between the two juxtaposed catalytic domains. EGFR has multiple mutants. EGFR C797S/L858R Recombinant Human Active Protein Kinase is a recombinant EGFR C797S/L858R protein that can be used to study EGFR C797S/L858R-related functions .
SB 201146 is an LTB4 receptor antagonist with a potency range of 10 pM to 1 μM that plays a critical role in asthma-associated airway inflammation. Studies have focused on its effects on eosinophil survival, a hallmark of asthma pathology. Studies have shown that eosinophil-derived cysteinyl leukotrienes, including LTC4 and LTD4, as well as factors such as GM-CSF and fibronectin promote eosinophil survival. SB 201146 effectively reversed mast cell- and lymphocyte-induced eosinophil survival, highlighting its potential therapeutic role in disrupting the autocrine cysteinyl leukotriene pathway that maintains eosinophil viability. This antagonist also highlights the importance of LTB4 as a paracrine mediator that influences eosinophil survival in inflammatory settings such as asthma .
EGFR is a driver of tumorigenesis. EGFR is mainly found in an auto-inhibited, dimerization-incompetent, state at the plasma membrane (PM). Ligand binding promotes receptor dimerization, which determines a series of structural rearrangements that are conveyed to the cytoplasmic domain allowing the formation of asymmetric dimers between the two juxtaposed catalytic domains. EGFR has multiple mutants. EGFR d746-750/C797S Recombinant Human Active Protein Kinase is a recombinant EGFR d746-750/C797S protein that can be used to study EGFR d746-750/C797S-related functions .
EGFR is a driver of tumorigenesis. EGFR is mainly found in an auto-inhibited, dimerization-incompetent, state at the plasma membrane (PM). Ligand binding promotes receptor dimerization, which determines a series of structural rearrangements that are conveyed to the cytoplasmic domain allowing the formation of asymmetric dimers between the two juxtaposed catalytic domains. EGFR has multiple mutants. EGFR d747-752/P753S Recombinant Human Active Protein Kinase is a recombinant EGFR d747-752/P753S protein that can be used to study EGFR d747-752/P753S-related functions .
HDB-1 is a selective inhibitor of the P2Y14 receptor (P2Y14R) with an IC50 of 26 pM. HDB-1 shows no significant inhibition on P2Y1R, P2Y2R, P2Y4R, P2Y6R, and P2Y12R. HDB-1 blocks the activation of hepatic stellate cells (HSC) by inhibiting the PKA/Raf1/MEK/ERK signaling pathway mediated by P2Y14R, thereby alleviating the core pathological process of liver fibrosis. HDB-1 can be used for the study of liver fibrosis .
Tofersen (BIIB067) is an antisense oligonucleotide and SOD1 mRNA inhibitor with an IC50 of 320 pM. Tofersen mediates RNase H-dependent degradation of SOD1 mRNA to reduce SOD1 protein levels in cerebrospinal fluid and serum. Tofersen downregulates cerebrospinal fluid neurofilament light chain, neurofilament heavy chain, amyloid-beta 1-40, amyloid-beta 1-42, neuropeptide Y, ubiquitin C-terminal hydrolase L1, neuropentraxins 1, 2, R, corticotropin-releasing hormone, IL-15, and serum neurofilament light chain, neurofilament heavy chain. Tofersen can be used for the research of superoxide dismutase 1-associated amyotrophic lateral sclerosis .
Vm24-toxin (Vaejovis mexicanus peptide 24), a 36-residue peptide, is a potent and selective Kv1.3 blocker with a Kd of ~3 pM in lymphocytes. Vm24-toxin shows >1500-fold affinity for Kv1.3 over other assayed potassium channels. Vm24-toxin folds into a distorted cystine-stabilized α/β motif consisting of a single-turn α-helix and a three-stranded antiparallel β-sheet, stabilized by four disulfide bridges. Vm24-toxin attenuates the CD4 + effector memory T cell response to T cell receptor (TCR) stimulation .
Sintilimab (Anti-PD-1) (IBI308 (Anti-PD-1)) is a safe and effectivel humanized IgG4 monoclonal antibody that binds to PD-1 with a KD value of 74 pM. Sintilimab (Anti-PD-1) blocks the interaction of PD-1 with its ligands (PD-L1 and PL-L2), consequently helping to restore the endogenous antitumour T-cell response. Sintilimab (Anti-PD-1) combined with prebiotics inhibits tumor volume and regulates immune cell subpopulation balance in lung adenocarcinoma mice. Sintilimab (Anti-PD-1) can be used for the research of classical Hodgkin's lymphoma, non-small cell lung cancer and oesophageal cancer .
Emodin-8-glucoside (Standard) is the analytical standard of Emodin-8-glucoside. This product is intended for research and analytical applications. Emodin-8-glucoside is an anthraquinone derivative that can be isolated from Aloe vera. Emodin-8-glucoside is the inhibitor for MAPK with an inhibition constant of 430.14 pM. Emodin-8-glucoside exhibits moderate inhibitory activity against rat lens aldose reductase (ALAR) and topoisomerases II with IC50s of 14.4 μM and 66 μM. Emodin-8-glucoside exhibits antioxidant, anti-inflammatory and anti-fibrotic activities. Emodin-8-glucoside can cross the blood brain barrier .
Vm24-toxin (Vaejovis mexicanus peptide 24) TFA, a 36-residue peptide, is a potent and selective Kv1.3 blocker with a Kd of ~3 pM in lymphocytes. Vm24-toxin TFA shows >1500-fold affinity for Kv1.3 over other assayed potassium channels. Vm24-toxin TFA folds into a distorted cystine-stabilized α/β motif consisting of a single-turn α-helix and a three-stranded antiparallel β-sheet, stabilized by four disulfide bridges. Vm24-toxin TFA attenuates the CD4 + effector memory T cell response to T cell receptor (TCR) stimulation .
SJ11646 is a Dasatinib (HY-10181)-based LCKPROTAC degrader with a DC50 of 0.00838 pM. SJ11646 has potent cytotoxicity against LCK-activated T-cell acute lymphoblastic leukemia (T-ALL) cells and primary leukemia samples with drastically prolonged suppression of LCK signaling, and induces T-ALL apoptosis. SJ11646 binds to 51 human kinases with a high affinity (particularly ABL1, KIT, and DDR1). SJ11646 has superior antileukemic efficacy in T-ALL mice model. . Pink: LCK ligand (HY-107447); Blue: CRBN ligase ligand (HY-163169); Black: linker (HY-76667)
5,6-DiHET lactone ((±)5,6-DiHETrE lactone) is a lactonized form of 5,6-EET and 5,6-DiHET. In solution, 5(6)-EET degrades into 5(6)-DiHET and 5(6)-δ-lactone, which can be converted to 5(6)-DiHET and quantified by GC-MS.1 5,6-DiHET potently induces vasodilation of isolated canine coronary arterioles, with 41 and 100% inhibition occurring at 0.01 and 100 pM, respectively. It also induces vasodilation in isolated human microvessels and increases intracellular calcium levels in a dose-dependent manner, an effect that can be blocked by the nitric oxide scavenger L-NAME.
IMG-008 is a fully human antagonistic antibody targeting IL-36R, acting as a high-affinity IL-36R inhibitor (Kd = 6.23 pM). IMG-008 competitively blocks the pro-inflammatory signaling pathway mediated by human IL-36R, inhibiting receptor activation and the production of inflammatory cytokines. IMG-008 suppresses Imiquimod (HY-B0180)-induced skin inflammation in humanized mice, and Fc modification increases its serum exposure and prolongs its half-life. IMG-008 can be used in studies related to IL-36R-mediated inflammatory diseases such as psoriasis .
Tofersen (BIIB067) sodium is an antisense oligonucleotide and SOD1 mRNA inhibitor with an IC50 of 320 pM. Tofersen sodium mediates RNase H-dependent degradation of SOD1 mRNA to reduce SOD1 protein levels in cerebrospinal fluid and serum. Tofersen sodium downregulates cerebrospinal fluid neurofilament light chain, neurofilament heavy chain, amyloid-beta 1-40, amyloid-beta 1-42, neuropeptide Y, ubiquitin C-terminal hydrolase L1, neuropentraxins 1, 2, R, corticotropin-releasing hormone, IL-15, and serum neurofilament light chain, neurofilament heavy chain. Tofersen sodium can be used for the research of superoxide dismutase 1-associated amyotrophic lateral sclerosis .
CL-387785 (EKI-785; WAY-EKI 785) (Standard) is the analytical standard of CL-387785 (HY-10325). This product is intended for research and analytical applications. CL-387785 is an orally active EGFR inhibitor with an IC50 of 370 pM. CL-387785 inhibits EGF-stimulated EGFR autophosphorylation with an IC50 of approximately 5 nM. CL-387,785 exerts selective inhibition on cell lines overexpressing EGFR or c-erbB-2, whereas it shows weak inhibitory effects on cell lines with low expression of these two receptors. CL-387785 effectively induces cell cycle arrest and apoptosis. CL-387785 can be used for the research of non-small cell lung cancer and autosomal recessive polycystic kidney disease.
D8P1C1 is a high-affinity ADAM17 inhibitor (with a Kd of 180 pM targeting ADAM17-ECD) that reduces the shedding and phosphorylation of EGFR ligands. D8P1C1 inhibits cancer cell proliferation in vitro and tumor growth in xenograft models. 89Zr-DFO-D8P1C1 radioimmunological PET imaging shows its substantial accumulation in ovarian tumor xenografts, serving as a platform for generating bispecific T-cell engager derivatives. D8P1C1 can be applied to research on related diseases including triple-negative breast cancer, various types of ovarian cancer, lung adenocarcinoma, glioma, and colon cancer .
AVN-101 is a potent, brain-penetrant and orally active 5-HT7 receptor antagonist (Ki of 153 pM), with slightly lesser potency toward 5-HT6, 5-HT2A, and 5HT-2C receptors (Ki values of 2.04 nM, 1.56 nM, and 1.17 nM, respectively). AVN-101 also exhibits a rather high affinity toward histamine H1 (Ki of 0.58 nM) and adrenergic α2A, α2B, and α2C (Ki= 0.41-3.6 nM) receptors. AVN-101 can be studied in such diseases as general anxiety disorders, depression, schizophrenia, Alzheimer’s disease, and multiple sclerosis .
NS101 is an anti-FAM19A5 antibody with an IC50 of 0.2 nM and a Kd of 111 pM, as well as blood-brain barrier permeability. NS101 binds to key amino acid residues of FAM19A5, thereby blocking the interaction of LRRC4B and disrupting the FAM19A5-LRRC4B complex. NS101 increases the dendritic spine density in hippocampal neurons and the prefrontal cortex, normalizes the dendritic spine elimination rate, elevates the frequencies of mEPSC and fEPSP, and promotes the transport of brain-derived FAM19A5 into the peripheral circulation. NS101 improves cognitive function in mouse models of Alzheimer's disease. NS101 can be used for research on Alzheimer's disease. The recommended isotype control is human IgG1 kappa (HY-P99001) .
MRTX1133 is a noncovalent, potent, and selective alkyne-based KRAS G12D inhibitor. MRTX1133 optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated KD against KRAS G12D of 0.2 pM. MRTX1133 prevents SOS1-catalyzed nucleotide exchange and/or formation of the KRAS G12D/GTP/RAF1 complex, thereby inhibiting mutant KRAS-dependent signal transduction. MRTX1133 selectively inhibits KRAS G12D mutant, but not KRAS wild-type, tumor cells. MRTX1133 has single digit nanomolar activity in cellular assays and marked in vivo efficacy in tumor models harboring KRAS G12D mutations .
EGFR is a driver of tumorigenesis. EGFR is mainly found in an auto-inhibited, dimerization-incompetent, state at the plasma membrane (PM). Ligand binding promotes receptor dimerization, which determines a series of structural rearrangements that are conveyed to the cytoplasmic domain allowing the formation of asymmetric dimers between the two juxtaposed catalytic domains. EGFR has multiple mutants. EGFR d746-750/T790M/C797S Recombinant Human Active Protein Kinase is a recombinant EGFR d746-750/T790M/C797S protein that can be used to study EGFR d746-750/T790M/C797S-related functions .
MCB-36 is a VHL-recruiting pan-KRAS PROTAC degrader without affecting KRAS transcription. MCB-36 exhibits minimal effects on HRAS and NRAS protein levels. MCB-36 binds to the GDP-loaded state of G12D, G12C, G12V, and wild-type KRAS with high affinities Kd ≈ 1 pM). MCB-36 decreases p-ERK levels, leading to cell apoptosis. MCB-36 effectively suppress KRAS G12C inhibitor-resistant cancer cells and remodel the tumor immune microenvironment. MCB-36 can be used for the study of colorectal cancer and lung cancer (Pink: Target protein ligand; Blue: E3 ligand (HY-112078); Black: Linker (HY-W091879)) .
AVN-101 hydrochloride is a potent, brain-penetrant and orally active 5-HT7 receptor antagonist (Ki of 153 pM), with slightly lesser potency toward 5-HT6, 5-HT2A, and 5HT-2C receptors (Ki values of 2.04 nM, 1.56 nM, and 1.17 nM, respectively). AVN-101 hydrochloride also exhibits a rather high affinity toward histamine H1 (Ki of 0.58 nM) and adrenergic α2A, α2B, and α2C (Ki= 0.41-3.6 nM) receptors. AVN-101 hydrochloride can be studied in such diseases as general anxiety disorders, depression, schizophrenia, Alzheimer’s disease, and multiple sclerosis .
BI-836880 is a humanized bispecific nanobody and a selective inhibitor of VEGF and ANG2, with a Kd of 16 pM for hANG2, an EC50 of 1.4 nM for VEGF165, and an EC50 of 2.3 nM for VEGF121. BI-836880 blocks ERK phosphorylation downstream of VEGF-A as well as TIE2 phosphorylation downstream of ANG2. BI-836880 does not inhibit ANG1-mediated TIE2 phosphorylation. BI-836880 exerts anti-angiogenic effects, reduces the number of immature endothelial vessels in tumor tissues, and inhibits tumor growth in preclinical models. BI-836880 can be used in the research of pancreatic cancer, non-small cell lung cancer, renal cell carcinoma, ovarian cancer, colon cancer, and Lewis lung cancer .
Tofersen-d27 (BIIB067-d27) is the deuterium labeled Tofersen (HY-132580). Tofersen (BIIB067) is an antisense oligonucleotide and SOD1 mRNA inhibitor with an IC50 of 320 pM. Tofersen mediates RNase H-dependent degradation of SOD1 mRNA to reduce SOD1 protein levels in cerebrospinal fluid and serum. Tofersen downregulates cerebrospinal fluid neurofilament light chain, neurofilament heavy chain, amyloid-beta 1-40, amyloid-beta 1-42, neuropeptide Y, ubiquitin C-terminal hydrolase L1, neuropentraxins 1, 2, R, corticotropin-releasing hormone, IL-15, and serum neurofilament light chain, neurofilament heavy chain. Tofersen can be used for the research of superoxide dismutase 1-associated amyotrophic lateral sclerosis.
Jujuboside B (Standard) is the analytical standard of Jujuboside B. This product is intended for research and analytical applications. Jujuboside B is a bioactive saponin component isolated from Ziziphi Spinosae Semen (sour jujube seed), with oral efficacy and blood-brain barrier permeability. Jujuboside B induces acute leukemia cell death and drives necroptosis apoptosis by activating the RIPK1/RIPK3/MLKL pathway. Jujuboside B upregulates the expression of NOXA, PARP and caspase-3, activates AMPK, inhibits the proliferation of breast cancer cells, and induces cell apoptosis and autophagy. Jujuboside B inhibits angiogenesis and tumor growth by blocking the VEGFR-2 signaling pathway. Jujuboside B alleviates liver injury in mice by regulating the Nrf2-STING signaling pathway . Jujuboside B alleviates liver injury by regulating anti-inflammatory responses and downregulating the expression of 11β-HSD2. Jujuboside B induces ferroptosis and overcomes radioresistance in non-small cell lung cancer via the PPARγ-ATF3-Gpx4 signaling pathway. Jujuboside B exerts inhibitory effects on platelet aggregation. Jujuboside B inhibits febrile seizures by suppressing the activity of AMPA receptors. Jujuboside B reverses chronic unpredictable mild stress-promoted tumor progression by blocking the PI3K/Akt and MAPK/ERK pathways and dephosphorylating CREB signaling. Jujuboside B is applicable to related studies on acute leukemia, breast cancer, PM2.5-induced lung injury, hepatotoxicity, liver injury, colorectal cancer, non-small cell lung cancer, thromboembolic diseases, cardiovascular diseases associated with high platelet aggregation, febrile seizures, and depressive-like phenotypes.
Jujuboside B is a bioactive saponin component isolated from Ziziphi Spinosae Semen (sour jujube seed), with oral efficacy and blood-brain barrier permeability. Jujuboside B induces acute leukemia cell death and drives necroptosis apoptosis by activating the RIPK1/RIPK3/MLKL pathway. Jujuboside B upregulates the expression of NOXA, PARP and caspase-3, activates AMPK, inhibits the proliferation of breast cancer cells, and induces cell apoptosis and autophagy. Jujuboside B inhibits angiogenesis and tumor growth by blocking the VEGFR-2 signaling pathway. Jujuboside B alleviates liver injury in mice by regulating the Nrf2-STING signaling pathway . Jujuboside B alleviates liver injury by regulating anti-inflammatory responses and downregulating the expression of 11β-HSD2. Jujuboside B induces ferroptosis and overcomes radioresistance in non-small cell lung cancer via the PPARγ-ATF3-Gpx4 signaling pathway. Jujuboside B exerts inhibitory effects on platelet aggregation. Jujuboside B inhibits febrile seizures by suppressing the activity of AMPA receptors. Jujuboside B reverses chronic unpredictable mild stress-promoted tumor progression by blocking the PI3K/Akt and MAPK/ERK pathways and dephosphorylating CREB signaling. Jujuboside B is applicable to related studies on acute leukemia, breast cancer, PM2.5-induced lung injury, hepatotoxicity, liver injury, colorectal cancer, non-small cell lung cancer, thromboembolic diseases, cardiovascular diseases associated with high platelet aggregation, febrile seizures, and depressive-like phenotypes .
BChE-IN-44 is a potent, brain-penetrant, highly selective BChE inhibitor [equine BChE IC50 = 18.00 pM, human BChE IC50 = 1.50 nM]. BChE-IN-44 shows neuroprotective effects against the Aβ1-42-induced injury model and inhibitory effects on Aβ1-42 self-aggregation. BChE-IN-44 reduces the levels of inflammatory factors (NO, IL-6, and TNF-α) in Lipopolysaccharides (HY-D1056)-induced BV2 cells. BChE-IN-44 can significantly ameliorate Scopolamine (HY-N0296)-induced cognition impairment. BChE-IN-44 exhibits capacity in the regulation of BChE and acetylcholine levels in the mouse hippocampus. BChE-IN-44 can be used for the study of Alzheimer’s disease (AD) .
MCB-294 is a dual-state pan-KRAS inhibitor that selectively inhibits KRAS over NRAS and HRAS. MCB-294 capable of binding both the active (GTP-bound) and inactive (GDP-bound) forms of KRAS with Kds of approximately 1 pM and 10 nM, respectively. MCB-294 broadly impairs the growth of hTERT-HPNE cells expressing G12D, G12C, G12V, G12S, G13D, and wild-type KRAS, with IC50s of approximately 700 nM. MCB-294 induces irreversible apoptosis in KRAS-mutated tumors. MCB-294 effectively suppress KRAS G12C inhibitor-resistant cancer cells and remodel the tumor immune microenvironment. MCB-294 can be used for the study of pancreatic cancer, colorectal cancer and lung cancer .
Bruceantinol is a quassinoid that can be isolated from Brucea javanica, inhibits pepper mottle virus (PepMoV) in pepper. Bruceantinol is a STAT3 inhibitor demonstrating potent antitumor activity in in vitro and in vivo human colorectal cancer (CRC) models. Bruceantinol has potent anti-leukemic activity. Bruceantinol strongly inhibits STAT3 DNA-binding ability (IC50 = 2.4 pM), blocks the constitutive and IL-6-induced STAT3 activation, and suppresses transcription of MCL-1, PTTG1, survivin and c-Myc. Bruceantinol binds with CDK2/4/6 to facilitate protein degradation through proteasome pathway. Bruceantinol can dose- and time-dependently reduces the cell growth, impede cell proliferation, disrupts the cell cycle, and induces necrosis in MCF-7 cells and apoptosis in MDA-MB-231 cells .
IMC-EB10 (LY3012218) is an anti-FLT3 monoclonal antibody. IMC-EB10 binds to FLT3 with high affinity (Kd = 158 pM) and blocks the binding of FLT3 ligand to FLT3 (IC50 ≈ 10 nM), thereby inhibiting MAPK, STAT5, and PI3K/Akt signaling in leukemia cells. IMC-EB10 can enhance the anti-leukemic effect of Methotrexate (HY-14519) and inhibit leukemias expressing wild-type or ITD-mutated FLT3 receptors. IMC-EB10 prolongs the survival of acute lymphoblastic leukemia (ALL) cells and primary leukemia samples and reduces engraftment in non-obese diabetic/severe combined immunodeficiency patients. IMC-EB10 is indicated for leukemia research .
PROTAC CBP/p300/BRD4 Degrader-1 is a dual-target PROTAC degrader with DC50 values of 8.8 pM (BRD4), 6.55 nM (CBP), and 1.05 nM (p300). PROTAC CBP/p300/BRD4 Degrader-1 induces CRBN- and proteasome-dependent degradation of BRD4 and CBP/p300, downregulates c-Myc and acetyl-H3K27, induces apoptosis. PROTAC CBP/p300/BRD4 Degrader-1 acts as an antiproliferative and antitumor agent, induces tumor growth inhibition in xenograft models. PROTAC CBP/p300/BRD4 Degrader-1 can be used for the research of prostate cancer and colorectal cancer .
EGFR is a driver of tumorigenesis. EGFR is mainly found in an auto-inhibited, dimerization-incompetent, state at the plasma membrane (PM). Ligand binding promotes receptor dimerization, which determines a series of structural rearrangements that are conveyed to the cytoplasmic domain allowing the formation of asymmetric dimers between the two juxtaposed catalytic domains. EGFR has multiple mutants. EGFR d746-750/T790M/C797S/L858R Recombinant Human Active Protein Kinase is a recombinant EGFR d746-750/T790M/C797S/L858R protein that can be used to study EGFR d746-750/T790M/C797S/L858R-related functions .
Cusatuzumab (ARGX-110) is a selective competitive blocker targeting CD70 (with an equilibrium dissociation constant of 17 pM for binding to human CD70). Cusatuzumab also possesses enhanced antibody-dependent cell-mediated cytotoxicity (ADCC) activity. It is a humanized IgG1 monoclonal antibody, artificially synthesized through humanization and genetic engineering modifications (CH2 region mutation to enhance effector function). Cusatuzumab has a dual mechanism of action: firstly, it competitively blocks the interaction between CD70 and CD27, inhibiting the CD27-NF-κB signaling pathway, reducing regulatory T cell (Treg) activation and tumor cell proliferation; secondly, by enhancing binding to FcγRIIIa, it mediates ADCC and antibody-dependent cellular phagocytosis (ADCP), directly lysing CD70-positive tumor cells. Cusatuzumab can efficiently eliminate leukemia stem cells (LSCs), induce tumor cell differentiation and apoptosis, restore immune surveillance, and target CD70-positive tumors. Cusatuzumab is used in the study of acute myeloid leukemia (AML) .
NN3201 is a c-Kit-targeting antibody-drug conjugate (ADC) with high affinity (KD = 0.19 pM). NN3201 is composed of 4-(3-Tosyl-2-(tosylmethyl)propanoyl)benzoic acid-glu(PEG24-Me)-val-cit-NH-benzyloxyformic acid-MMAE (HY-178219) and an anti-c-Kit human monoclonal antibody NN2101 (HY-P991293). NN3201 rapidly internalizes and inhibits stem cell factor (SCF)-driven signaling, thereby delivering its payload to induce cell cycle arrest and apoptosis. NN3201 exhibits no Fc-mediated effector functions antibody-dependent cell-mediated cytotoxicity (ADCC)/complement-dependent cytotoxicity (CDC) due to reduced FcγR binding. NN3201 exhibits significant c-Kit-dependent anti-tumor efficacies in various tumor models. NN3201 can be used in small cell lung cancer (SCLC) and gastrointestinal stromal tumor (GIST) and acute myeloid leukemia (AML) research [1][2].
L-699333 is a 5-lipoxygenase (5-LO) inhibitor belonging to the thieno[2,3,4-cd]indole class. This compound has a 2-ethoxybutyric acid side chain and is a potent inhibitor of the biosynthesis of 5-HPETE and LTB4 produced from human 5-LO, with ICm values of 22 nM, 7 nM, and 3.8 pM for human neutrophils and whole blood, respectively. L-699333 has shown anti-inflammatory and antiasthmatic effects in a variety of animal models, including rat pleurisy models, antigen-induced wheezing models, and awake macaque and sheep asthma models. Its inhibition of 5-LO is highly selective, with higher ICm values or stronger competitive inhibition in FLAP binding assays compared to inhibition of human 15-LO, porcine 12-LO, and ram epididymal cyclooxygenase. The racemic enantiomer 14g of L-699333 is the most potent enantiomer to date, with inhibitory effects similar to those of the known MK-0591, which has been shown in clinical trials to inhibit the biochemical effects of LTB4 biosynthesis in vitro and LTE4 excretion in urine.
Maridebart cafraglutide (AMG 133) is a long-acting peptide-antibody conjugate that combines GLP-1 receptor agonist with glucose-dependent insulinotropic polypeptide (GIP) receptor antagonism. Maridebart cafraglutide shows antagonist activity against human, cynomolgus monkey and rat GIPR with IC50 values of 46.4 nM, 26.5 nM, 822.3 nM, respectively. Maridebart cafraglutide shows agonist activity against human, cynomolgus monkey, rat and mouse GLP-1R with EC50 values of 24.4 pM, 5.7 pM, 2.4 pM and 123 pM, respectively. Maridebart cafraglutide can be used for the study of obesity and type 2 diabetes .
Wnt-C59 (C59) GMP is a GMP grade Wnt-C59 (HY-15659). GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Wnt-C59 (C59) is a highly potent and oral porcupine (PORCN) inhibitor with an IC50 of 74 pM.
PM-1, a derivative of Thioflavin-T (ThT; HY-D0218), is a small but highly specific plasma membrane (PM) fluorescent dye for specific and long-time membrane imaging of living and fixed cells. PM-1 is embedded directly into the cell membrane and exhibits a very long retention time on the plasma membrane with a half-life of approximately 15 h. PM-1 can be used in combination with protein labeling probes to study ectodomain shedding and endocytosis processes of cell surface proteins .
Pyrromethene 650 (PM650) is a green-fluorescent polar tracer dye. It is used for investigations of membrane fusion, lysis, and gap-junctional communication and to detect volume changes in cells or liposomes.
Pyrromethene 605 (PM605) is a green-fluorescent polar tracer dye. It is used for investigations of membrane fusion, lysis, and gap-junctional communication and to detect volume changes in cells or liposomes.
Pyrromethene 556 (PM556) is a green-fluorescent polar tracer dye. It is used for investigations of membrane fusion, lysis, and gap-junctional communication and to detect volume changes in cells or liposomes.
MG-101 (GMP) (Calpain inhibitor I (GMP)) is MG-101 (HY-18964) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. MG-101 (ALLN) is an inhibitor of cysteine proteases which inhibits calpain I, calpain II, cathepsin B and cathepsin L with Kis of 190, 220, 150 and 500 pM, respectively. MG-101 induces apoptosis and inhibits tumor growth, it can be used for the research of colon cancer .
PE154 (Compound 13) is a potent fluorescent inhibitor of human acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) (IC50s=280 pM and 16 nM, respectively) . PE154 can label β-amyloid plaques in histochemical analysis .
Dasatinib (GMP Like) (BMS-354825 (GMP Like)) is Dasatinib (HY-10181) produced by using GMP like guidelines. GMP Like small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Dasatinib (BMS-354825) is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively . Dasatinib also induces apoptosis and autophagy.
Streptavidin is a ~60 kDa homotetramer. Streptavidin binds four molecules of biotin with the highest affinity. The binding affinity of biotin to streptavidin is one of the highest reported for a non-covalent interaction to date, with a KD ~0.01 pM . Streptavidin has an immunosuppressive role . This product is a Streptavidin protein recombinantly expressed in an E. coli expression system.
Wnt-C59 (C59) GMP is a GMP grade Wnt-C59 (HY-15659). GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Wnt-C59 (C59) is a highly potent and oral porcupine (PORCN) inhibitor with an IC50 of 74 pM.
MG-101 (GMP) (Calpain inhibitor I (GMP)) is MG-101 (HY-18964) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. MG-101 (ALLN) is an inhibitor of cysteine proteases which inhibits calpain I, calpain II, cathepsin B and cathepsin L with Kis of 190, 220, 150 and 500 pM, respectively. MG-101 induces apoptosis and inhibits tumor growth, it can be used for the research of colon cancer .
Dasatinib (GMP Like) (BMS-354825 (GMP Like)) is Dasatinib (HY-10181) produced by using GMP like guidelines. GMP Like small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Dasatinib (BMS-354825) is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively . Dasatinib also induces apoptosis and autophagy.
Aprotinin is a bovine pancreatic trypsin inhibitor (BPTI) inhibitor which inhibits trypsin and chymotrypsin with Kis of 0.06 pM and 9 nM, respectively.
Icotrokinra (JNJ-77242113) is an orally available, selective antagonist of the IL-23 receptor. Icotrokinra inhibits IL-23-induced STAT3 phosphorylation in peripheral blood mononuclear cells (IC50=5.6 pM) and inhibits IL-23-induced interferon IFN-γ production in NK cells with an IC50 of 18.4 pM. Icotrokinra exhibits anti-inflammatory activity in a rat TNBS-induced colitis model. Icotrokinra can be used in the study of psoriasis, psoriatic arthritis, and inflammatory bowel disease .
Plitidepsin (Aplidine) is a potent anti-cancer agent by targeting eEF1A2 ( KD=80 nM) . Plitidepsin possesses antiviral activity and is against SARS-CoV-2 with an IC90 of 0.88 nM. Plitidepsin is usually used for multiple myeloma and advanced cancer research, and has the potential for COVID-19 research .
Nesiritide (Brain Natriuretic Peptide-32 human) is a recombinant human B-type natriuretic peptide. Nesiritide is a NPRs agonist, with Kd values of 7.3 and 13 pM for NPR-A and NPR-C, respectively. Nesiritide regulates V1/2 activation/inactivation of the L-type calcium channel. Nesiritide shows vasodilatory, diuretic, and natriuretic activities. Nesiritide is used in cardiovascular diseases such as heart failure and vascular remodeling after arterial injury .
[D-Ala2]-GIP (human) is a GIP receptor agonist (EC50 = 630 pM). [D-Ala2]-GIP (human) improves glucose tolerance. [D-Ala2]-GIP (human) shows neuroprotective activity in MPTP (HY-W114750)-induced Parkinson's disease model. [D-Ala2]-GIP (human) also improves cognitive function and hippocampal synaptic plasticity in obese diabetic rats. [D-Ala2]-GIP (human) can be used for research of type 2 diabetes, Parkinson's disease, etc
Cotadutide (MEDI0382) is a potent dual agonist of glucagon-like peptide-1 (GLP-1) and GCGR with EC50 values of 6.9 pM and 10.2 pM, respectively. Cotadutide exhibits ability to facilitate both weight loss and glycaemic control, and alleviate fibrosis. Cotadutide can be used in the research of obesity and type 2 diabetes (T2D) .
Cotadutide (MEDI0382) acetate is a potent dual agonist of glucagon-like peptide-1 (GLP-1) and GCGR with EC50 values of 6.9 pM and 10.2 pM, respectively. Cotadutide acetate exhibits ability to facilitate both weight loss and glycaemic control, and alleviate fibrosis. Cotadutide acetate can be used in the research of obesity and type 2 diabetes (T2D) .
HCGRP-(8-37) (Human α-CGRP (8-37)) is a fragment of human calcitonin gene-related peptide (hCGRP) and an antagonist of the CGRP receptor, with an IC50 of 32.1 pM against the CGRP receptor. HCGRP-(8-37) blocks adenylate cyclase activation induced by CGRP receptor ligands and attenuates vascular responses triggered by CGRP. HCGRP-(8-37) reduces capsaicin-induced vasodilation in porcine nasal mucosa and superficial skin. HCGRP-(8-37) serves as a research tool to distinguish effects mediated by CGRP or calcitonin receptors, and to investigate CGRP-induced vascular effects .
TAK-683 acetate is a potent full KISS1 receptor (KISS1R) agonist (IC50=170 pM) with improved metabolic stability. TAK-683 acetate is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC50 values of 0.96 nM and 1.6 nM for human and rat, respectively . TAK-683 acetate depletes GnRH in the hypothalamus and reduces plasma FSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer .
SAR441255 is a GLP-1R/GCGR/GIPR agonist, with human EC50 values of 1.03 pM, 1.01 pM, and 0.73 pM, respectively. SAR441255 stimulates receptor activity and drives cAMP accumulation. SAR441255 can be used for the research of type 2 diabetes, obesity .
RG7697 is a dual agonist for glucagon-like peptide receptor (GLP Receptor) and glucosedependent insulinotropic polypeptide receptor (GIPR), with EC50 of 5 and 3 pM, respectively. RG7697 exhibits antihyperglycemic property .
Margatoxin, an alpha-KTx scorpion toxin, is a high affinity inhibitor of Kv1.3 (Kd=11.7 pM). Margatoxin inhibits the Kv1.2 (Kd=6.4 pM) and Kv1.1 (Kd=4.2 nM). Margatoxin, a 39 amino-acid-long peptide, is isolated from the venom of the scorpion Centruroides margaritatus and widely used in ion channel research .
Calmodulin Binding Peptide 1 is a high-affinity (pM) CaM-binding peptide derived from smooth muscle myosin light chain kinase (MLCK peptide). The interface of the complex formed by Calmodulin Binding Peptide 1 and Ca 2+-CaM can be specifically bound by small-molecule inhibitors, serving as a key target for selective regulation of smooth muscle contraction and development of anti-CaM drugs .
pm26TGF-β1 TFA peptide is a peptide that mimics a portion of the human TGF-β1 molecule. pm26TGF-β1 peptide TFA shows high affinity for the TGF-β1 receptor. pm26TGF-β1 peptide TFA displays potent anti-inflammatory properties and does not exhibit neutrophils’ chemoattraction .
Norleual TFA, an angiotensin (Ang) IV analog, is a hepatocyte growth factor (HGF)/c-Met inhibitor with an IC50 of 3 pM. Norleual TFA is an AT4 receptor antagonist and exhibits potent antiangiogenic activities .
GaTx2 is a seletive and a high affinity inhibitor of ClC-2 channels with a voltage-dependent apparent KD of ∼20 pM. GaTx2 is a peptide toxin inhibitor from Leiurus quinquestriatus hebraeus venom. GaTx2 is useful in determining the role and the membrane localization of ClC-2 in specific cell types .
palm11-PrRP31 is a lipidized endogenous appetite inhibitory neuropeptide (PrRP) analogue. palm11-PrRP31 is GPR10 (EC50=39 pM) and NPFF-R2 effective dual agonists. palm11-PrRP31 is able to mimic the natural function of PrRP by binding to these receptors to reduce food intake. palm11-PrRP31 can be used as a potential anti-obesity agent and for the study of neuropeptide-receptor interaction .
SAR441255 TFA is a GLP-1R/GCGR/GIPR agonist, with human EC50 values of 1.03 pM, 1.01 pM, and 0.73 pM, respectively. SAR441255 TFA stimulates receptor activity and drives cAMP accumulation. SAR441255 TFA can be used for the research of type 2 diabetes, obesity .
CCKBR agonist-1 (Compound 3r1) is a Gq-protein-preferring cholecystokinin B receptor (CCKBR) agonist with an EC50 of 35 pM. CCKBR agonist-1 significantly increases the survival rate of neurons, with an EC50 of 37 pM. CCKBR agonist-1 can improve the cognitive decline in mice by upregulating α-secretase (ADAM10) and calcium signaling molecule PLCB4, reduce the number of amyloid β (Aβ) plaques, and promote long-term potentiation (LTP). CCKBR agonist-1 can be used for the study of Alzheimer's disease .
Caloxin 3A1 is a biological active peptide. (This peptide belongs to caloxins, the extracellular plasma membrane (PM) Ca2+ pump inhibitors. Caloxin 3A1 inhibits plasma membrane calcium pumps (PMCAs) but not the sarcoplasmic reticulum Ca2+-pump. This peptide does not inhibit formation of the acylphosphate intermediate from ATP.)
HsTX1 (TFA) toxin, from the scorpion Heterometrus spinnifer, is a 34-residue, C-terminally amidated peptide cross-linked by four disulfide bridges. HsTX1 (TFA) is an the inhibitor of potassium channel, with IC50 for Kv1.3 of 12 pM and inhibits TEM cell activation and attenuates inflammation in autoimmunity .
HCV-IN-4 is a potent and orally active HCV NS5A inhibitor, shows great potency against GT1a, GT2b, GT3a, GT1a Y93H and GT1a L31V, with EC90s of 3 pM, 0.3 nM, 0.01 nM, 0.5 nM and 0.02 nM, respectively .
ADWX 1 TFA is a new peptide inhibitor that is potent and selective for Kv1.3 with an IC50 value of 1.89 pM. ADWX 1 inhibits Kv1.3 channel activity specifically to inhibit both the initial calcium signaling and NF-κB activation. ADWX 1 TFA ameliorates the disease in rats of experimental autoimmune encephalomyelitis (EAE) models. ADWX 1 TFA can be used to study T cell-mediated autoimmune diseases .
TAK-683 is a potent full KISS1 receptor (KISS1R) agonist (IC50=170 pM) with improved metabolic stability. TAK-683 is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC50 values of 0.96 nM and 1.6 nM for human and rat, respectively . TAK-683 depletes GnRH in the hypothalamus and reduces plasma FSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer .
Vm24-toxin (Vaejovis mexicanus peptide 24) TFA, a 36-residue peptide, is a potent and selective Kv1.3 blocker with a Kd of ~3 pM in lymphocytes. Vm24-toxin TFA shows >1500-fold affinity for Kv1.3 over other assayed potassium channels. Vm24-toxin TFA folds into a distorted cystine-stabilized α/β motif consisting of a single-turn α-helix and a three-stranded antiparallel β-sheet, stabilized by four disulfide bridges. Vm24-toxin TFA attenuates the CD4 + effector memory T cell response to T cell receptor (TCR) stimulation .
pm26TGF-β1 peptide is a peptide that mimics a portion of the human TGF-β1 molecule. pm26TGF-β1 peptide shows high affinity for the TGF-β1 receptor. pm26TGF-β1 peptide displays potent anti-inflammatory properties and does not exhibit neutrophils’ chemoattraction .
Plitidepsin (Standard) is the analytical standard of Plitidepsin. This product is intended for research and analytical applications. Plitidepsin (Aplidine) is a potent anti-cancer agent by targeting eEF1A2 ( KD=80 nM) . Plitidepsin possesses antiviral activity and is against SARS-CoV-2 with an IC90 of 0.88 nM. Plitidepsin is usually used for multiple myeloma and advanced cancer research, and has the potential for COVID-19 research .
Norleual, an angiotensin (Ang) IV analog, is a hepatocyte growth factor (HGF)/c-Met inhibitor with an IC50 of 3 pM. Norleual is an AT4 receptor antagonist and exhibits potent antiangiogenic activities .
Icotrokinra (JNJ-77242113) acetate is an orally available, selective antagonist of the IL-23 receptor. Icotrokinra acetate inhibits IL-23-induced STAT3 phosphorylation in peripheral blood mononuclear cells (IC50=5.6 pM) and inhibits IL-23-induced interferon IFN-γ production in NK cells with an IC50 of 18.4 pM. Icotrokinra acetate exhibits anti-inflammatory activity in a rat TNBS-induced colitis model. Icotrokinra acetate can be used in the study of psoriasis, psoriatic arthritis, and inflammatory bowel disease .
GUB021794 is a potent and highly selective glucagon-like peptide-1 receptor (GLP-1R) agonist developed using the streaMLine platform with an EC50 value of 18 pM. GUB021794 has a very weak activity against SCTR, with an EC50 value of 190 nM. GUB021794 can significantly reduce the body weight, food intake, and total fat mass of mice in a diet-induced obesity (DIO) model. GUB021794 can be used for research on obesity/diabetes .
palm11-PrRP31 TFA is a lipidized endogenous appetite inhibitory neuropeptide (PrRP) analogue. palm11-PrRP31 TFA is GPR10 (EC50=39 pM) and NPFF-R2 effective dual agonists. palm11-PrRP31 TFA is able to mimic the natural function of PrRP by binding to these receptors to reduce food intake. palm11-PrRP31 TFA can be used as a potential anti-obesity agent and for the study of neuropeptide-receptor interaction .
Kocurin (PM181104) is a thiazolyl cyclic-peptide antibiotic. Kocurin inhibits bacterial growth by impeding bacterial protein biosynthesis during the translation phase. Kocurin has strong inhibitory activity against Gram-positive bacteria, but no activity against fungi and Gram-negative bacteria .
Hongotoxin-1, isolated from venom of Centruroides limbatus, is the inhibitor of potassium channel, with IC50 for? Kv1.1, Kv1.2, Kv1.3, and Kv1.6 of 31 pM, 170 pM, 86 pM,and 6000 pM, respectively .
cMCoFx1 is a potent and selective FXIIa cyclic peptide inhibitor. cMCoFx1 has high binding affinity (KD: 900 pM) and inhibitory activity (Ki: 370 pM) for FXIIa. cMCoFx1 can effectively inhibit endogenous clotting pathways, and cMCoFx1 is stable in serum and non-cytotoxic .
N-0920 is a potent TMPRSS2 inhibitor with an IC50 of 0.35 nM. N-0920 effectively inhibits SARS-CoV-2 variants EG.5.1 and JN.1 entry in Calu-3 cells, with picomolar EC50s values of 300 pM and 90 pM, respectively .
Margatoxin TFA, an alpha-KTx scorpion toxin, is a high affinity inhibitor of Kv1.3 (Kd=11.7 pM). Margatoxin TFA inhibits the Kv1.2 (Kd=6.4 pM) and Kv1.1 (Kd=4.2 nM). Margatoxin TFA, a 39 amino-acid-long peptide, is isolated from the venom of the scorpion Centruroides margaritatus and widely used in ion channel research .
HsTX1, from the scorpion Heterometrus spinnifer, is a 34-residue, C-terminally amidated peptide cross-linked by four disulfide bridges. HsTX1, an the inhibitor of potassium channel, with IC50 for Kv1.3 of 12 pM inhibits TEM cell activation and attenuates inflammation in autoimmunity .
ADWX 1 is a new peptide inhibitor that is potent and selective for Kv1.3 with an IC50 value of 1.89 pM. ADWX 1 inhibits Kv1.3 channel activity specifically to inhibit both the initial calcium signaling and NF-κB activation. ADWX 1 ameliorates the disease in rats of experimental autoimmune encephalomyelitis (EAE) models. ADWX 1 can be used to study T cell-mediated autoimmune diseases .
ShK-Dap22 is a potent Kv1.3-specific immunosuppressive Polypeptide. ShK-Dap22 is a selective Kv1.3 channel blocker with IC50s of 23 pM, 1.8 nM, 10.5 nM, 37 nM, and 39 nM for mKv1.3, mKv1.1, hKv1.6, mKv1.4, and rKv1.2 channels, respectively .
Nesiritide (Brain Natriuretic Peptide-32 human) acetate is a recombinant human B-type natriuretic peptide. Nesiritide acetate is a NPRs agonist, with Kd values of 7.3 and 13 pM for NPR-A and NPR-C, respectively. Nesiritide acetate regulates V1/2 activation/inactivation of the L-type calcium channel. Nesiritide acetate shows vasodilatory, diuretic, and natriuretic activities. Nesiritide acetate is used in cardiovascular diseases such as heart failure and vascular remodeling after arterial injury .
palm-PrRP31 is a potent dual receptor agonist for both GPR10 (EC50=72 pM) and NPFF-R2. palm-PrRP31 activates downstream signaling pathways through binding to its receptors, GPR10 and NPFF-R2, which results in reduced appetite and increased energy expenditure. Utilizing palm-PrRP31 facilitates the study of the mechanism of action in the nervous system, thereby elucidating the complex biological processes that regulate appetite and energy expenditure .
TAK-683 TFA is a potent full KISS1 receptor (KISS1R) agonist (IC50=170 pM) with improved metabolic stability. TAK-683 TFA is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC50 values of 0.96 nM and 1.6 nM for human and rat, respectively . TAK-683 TFA depletes GnRH in the hypothalamus and reduces plasma FSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer .
Ac-Asp-Glu-Asp(EDANS)-Glu-Glu-Abu-ψ-(COO)Ala-Ser-Lys(DABCYL)-NH2 (HCV NS3 protease substrate) is a biological active peptide. (This peptide is a HCV protease substrate incorporating an ester bond between residues P1 and P1. Due to ready transesterification of the scissile bond to the acyl-enzyme intermediate, this substrate shows very high kcat/Km values, enabling detection of activity with subnanomolar nonstructural protein 3 (NS3 protease) concentrations. It is widely used for the continuous assay of NS3 protease activity. Substrate cleavage is proportional to the enzyme concentration with a detection limit for NS3 between 1 nM and 250 pM.
Vm24-toxin (Vaejovis mexicanus peptide 24), a 36-residue peptide, is a potent and selective Kv1.3 blocker with a Kd of ~3 pM in lymphocytes. Vm24-toxin shows >1500-fold affinity for Kv1.3 over other assayed potassium channels. Vm24-toxin folds into a distorted cystine-stabilized α/β motif consisting of a single-turn α-helix and a three-stranded antiparallel β-sheet, stabilized by four disulfide bridges. Vm24-toxin attenuates the CD4 + effector memory T cell response to T cell receptor (TCR) stimulation .
UTG-4 is a GLP-1R, GIPR, and GCGR agonist with EC50 values of 126.3 pM, 29.2 pM, and 250.2 pM, respectively. UTG-4 binds to HSA (Kd = 14.6 μM). UTG-4 effectively alleviates endothelial-mesenchymal transition. UTG-4 promotes weight loss, inhibits food intake, improves glucose tolerance, and has a significant anti-atherosclerotic effect .
Icotrokinra (JNJ-77242113) hydrochloride is an orally available, selective antagonist of the IL-23 receptor. Icotrokinra hydrochloride inhibits IL-23-induced STAT3 phosphorylation in peripheral blood mononuclear cells (IC50=5.6 pM) and inhibits IL-23-induced interferon IFN-γ production in NK cells with an IC50 of 18.4 pM. Icotrokinra hydrochloride exhibits anti-inflammatory activity in a rat TNBS-induced colitis model. Icotrokinra hydrochloride can be used in the study of psoriasis, psoriatic arthritis, and inflammatory bowel disease .
TPM004 is an ultralong-acting, nonaggregating dual amylin (AMY3R) and calcitonin receptor (CTR) agonist with EC50 values of 0.5 and 0.7 pM. TPM004 induces weight loss, attenuates adiposity rebound, lowers glucose, and improves glucose homeostasis. TPM004 can be used for the research of obesity, diabetes .
Bimagrumab (Anti-ACVR2B Reference Antibody) is a human monoclonal antibody that blocks activin type II receptor (ActRII), with KDs of 1.7 pM and 434 pM for human ActRIIB and ActRIIA, respectively. Bimagrumab can be used for the research of pathological muscle loss and weakness .
Canakinumab (ACZ885) is a recombinant human anti-IL-1β monoclonal antibody. Canakinumab shows IC50 values of 43.6 and 40.8 pM for human and marmoset IL-1β, respectively. The mode of action of canakinumab is based on the neutralization of IL-1β signaling, resulting in suppression of inflammation related to disorders of autoimmune origin .
Risankizumab (BI 655066) is a humanised IgG monoclonal antibody, targeting IL-23 p19 subunit (Kd <10 pM) and inhibiting IL-17 production induced by human IL-23 in mouse splenocytes (IC50 = 2 pM). Risankizumab can be used to research immunological and inflammatory disorders such as psoriasis vulgaris, psoriatic arthritis, generalized pustular psoriasis and erythrodermic psoriasis .
Emapalumab (NI-0501) is a human monoclonal IgG1 antibody that noncompetitively inhibits IFN-γ. Emapalumab binds with high affinity (Kd= 1.4 pM) to both free IFN-γ as well as IFN-γ bound to its receptor. Emapalumab can be used in research of hemophagocytic lymphohistiocytosis (HLH) .
Ixekizumab (LY2439821) is a humanized IgG4 monoclonal antibody that selectively binds and neutralizes interleukin IL-17A (KD<3 pM). Ixekizumab directly blocks IL-17A binding to IL-17RA (IL-17A receptor) but does not bind to other IL-17 family members. Ixekizumab is used for the research of moderate-to-severe plaque psoriasis .
Cusatuzumab (ARGX-110) is a selective competitive blocker targeting CD70 (with an equilibrium dissociation constant of 17 pM for binding to human CD70). Cusatuzumab also possesses enhanced antibody-dependent cell-mediated cytotoxicity (ADCC) activity. It is a humanized IgG1 monoclonal antibody, artificially synthesized through humanization and genetic engineering modifications (CH2 region mutation to enhance effector function). Cusatuzumab has a dual mechanism of action: firstly, it competitively blocks the interaction between CD70 and CD27, inhibiting the CD27-NF-κB signaling pathway, reducing regulatory T cell (Treg) activation and tumor cell proliferation; secondly, by enhancing binding to FcγRIIIa, it mediates ADCC and antibody-dependent cellular phagocytosis (ADCP), directly lysing CD70-positive tumor cells. Cusatuzumab can efficiently eliminate leukemia stem cells (LSCs), induce tumor cell differentiation and apoptosis, restore immune surveillance, and target CD70-positive tumors. Cusatuzumab is used in the study of acute myeloid leukemia (AML) .
Pumitamig (PM-8002, BNT-327) is a bispecific antibody targeting PD-L1 and VEGF-A, with immune activation and anti-angiogenic activities. By binding to PD-L1, Pumitamig restores the function of effector T cells, while neutralizing VEGF-A in the tumor microenvironment to reverse its inhibition on the infiltration and activation of immune cells and normalize tumor blood vessels. Pumitamig can also be combined with various ADCs targeting TROP2, B7H3, HER2, HER3 for the research of advanced/metastatic solid tumors, including non-small cell lung cancer, ovarian cancer, triple-negative breast cancer, cervical cancer, etc. Pumitamig also exhibits potential efficacy in "cold" tumors with low PD-L1 expression that are insensitive to immunotherapy .
Mirikizumab (LY3074828) is a humanized IgG4 monoclonal antibody that targets the p19 subunit of interleukin 23 (IL-23). Mirikizumab binds to human and monkey IL-23 with high affinity, with Kd values of 21 pM and 55 pM, respectively. By inhibiting the binding of IL-23 to IL-23R, Mirikizumab modulates the immune response and holds potential for research in ulcerative colitis and Crohn's disease .
Povetacicept (ALPN-303) is an engineered Fc fusion protein containing the TACI domain, and acts as a dual APRIL/BAFF antagonist. The Kd value of Povetacicept for human BAFF is 59.3 pM, while its Kd value for human APRIL is 1.00 pM. Povetacicept reduces the activation, proliferation, differentiation and survival of B cells, and inhibits the production of immunoglobulins and autoantibodies. Povetacicept can be used in research related to autoimmune hemolytic anemia, immune thrombocytopenia, systemic lupus erythematosus, lupus nephritis and myasthenia gravis .
Sintilimab (IBI308) is a safe and effectivel humanized IgG4 monoclonal antibody that binds to PD-1 with a KD value of 74 pM. Sintilimab blocks the interaction of PD-1 with its ligands (PD-L1 and PL-L2), consequently helping to restore the endogenous antitumour T-cell response. Sintilimab combined with prebiotics inhibits tumor volume and regulates immune cell subpopulation balance in lung adenocarcinoma mice. Sintilimab can be used for the research of classical Hodgkin's lymphoma, non-small cell lung cancer and oesophageal cancer .
Tesnatilimab (JNJ-64304500) is a human IgG4 monoclonal antibody targeting NKG2D, with a KD value of 9.2 pM . Tesnatilimab blocks the binding of ligands to the NKG2D receptor, thereby inhibiting downstream proinflammatory cytokine, cytotoxic mediator signaling pathways and proinflammatory immune responses. Tesnatilimab is applicable to research related to Crohn's disease .
Etrolizumab (rhuMAb Beta7) is a gut-selective, anti-β7 integrin monoclonal antibody. Etrolizumab is specific targeting of the β7 subunit of α4β7 and αEβ7 integrins with Ki values of 18 nM and 1800 pM for Human α4β7 and Human αEβ7-293, respectively. Etrolizumab can be used in research of inflammatory bowel disease (IBD) .
Tildrakizumab (SCH 900222) is a humanized anti-IL-23 (p19 subunit) monoclonal antibody. IL-23 is a critical cytokine to maintain the Th17 cell phenotype. Tildrakizumab has high-affinity for single-chain IL-23 (Kd: 136 pM). Tildrakizumab is effective against moderate to severe plaque psoriasis .
Nidanilimab (CAN04) is a fully humanized monoclonal anti-IL1RAP antibody with a Kd value of 1.10 pM. Nidanilimab blocks IL1α and IL1β signaling and stimulates the immune system to destroy tumour cells. Nidanilimab can be used in research of non-small lung cancer (NSCLC) and pancreatic ductal adenocarcinoma (PDAC) .
Cofetuzumab pelidotin (PF-06647020) is a PTK7-targeting ADC comprising a humanized anti-PTK7 mAb (hu6M024, IgG1) joined to an auristatin microtubule inhibitor payload, auristatin-0101 (Aur0101; HY-12522), by a cleavable valine-citrulline (vc)-based linker. Cofetuzumab pelidotin has a DAR of 4. Cofetuzumab pelidotin binds to cell-surface PTK7 with an EC50 of 1153 pM by flow cytometry. Cofetuzumab pelidotin has the potential for solid tumors research .
Clesrovimab (MK1654) is a humanized IgG1 monoclonal antibody targeting the respiratory syncytial virus (RSV) protein F. Clesrovimab binds to pre-fusion and post-fusion forms of RSV-A fusion protein with high affinity, with corresponding KD values of 71 pM and 480 pM, respectively. Clesrovimab is applicable for the research of RSV infection .
Cendakimab (RPC4046; ABT 308; CC-93538) is a selective, humanized, recombinant monoclonal antibody against the IL-13 molecule. Cendakimab has a high affinity and potency for both human wild-type and variant IL-13 and blocks binding of IL-13 to both IL-13Rα1 and IL-13Rα2 with IC50s of 352 pM and 631 pM by ELISA, respectively. Cendakimab recognizes both wild-type human IL-13 and the common polymorphic variant R110Q, with binding affinities of 52 and 50 pM, respectively. Cendakimab has the potential for IL-13-related allergic/inflammatory diseases (e.g., asthma and eosinophilic esophagitis) .
Vobarilizumab (ALX-0061) is a humanized bispecific anti-IL-6R and anti-human serum albumin (ALB) monoclonal antibody (mAb) (Kd: 0.19 pM). Vobarilizumab consists of an anti-IL-6R domain and an anti-human serum albumin domain. Vobarilizumab can be used in the research of inflammatory autoimmune diseases, such as rheumatoid arthritis .
Reslizumab (Sch 55700) is humanized monoclonal antibodies that target interleukin-5 (IL-5) for the treatment of eosinophilic asthma. Reslizumab is effective in neutralizing the function of IL-5. Reslizumab has high binding affinity for human IL-5, with KD values of 109 pM and 4.3 pM in the the Biacore surface plasmon resonance and Kinetic Exclusion Assay, respectively .
Frunevetmab (NV-02) is a felinized anti-nerve growth factor (NGF) monoclonal antibody with a Kd of 20 pM. Frunevetmab can effectively decrease osteoarthritis (OA) pain in cats .
Domagrozumab is an anti-myostatin humanized monoclonal antibody with a KD value of 2.6 pM for human myostatin. Domagrozumab induces muscle anabolic activity. Domagrozumab can be used in research of duchenne muscular dystrophy (DMD) .
Narnatumab (IMC-RON8) is a neutralizing human monoclonal antibody that blocks RON binding to its ligand, macrophage-stimulating protein (MSP), with a Kd of 32 pM. Narnatumab can be used for the research of cancer .
MOR-106 (MOR12743) is a humanized anti-IL-17C IgG1 monoclonal antibody. MOR-106 inhibits the NF-κB signaling pathway by specifically binding to IL-17C (IC50 = 59 pM for human IL-17C, IC50 = 55 pM for mouse IL-17C). MOR-106 can effectively inhibit skin inflammation and reduce related inflammatory factors in animal models of psoriasis and atopic dermatitis .
Zampilimab (UCB-7858) is a monoclonal antibody against transglutaminase 2 (TG2). Zampilimab inhibits TG2 crosslinking transamidation activity with an IC50 of 0.25 nM and a Kd of <50 pM. Zampilimab improves renal fibrosis .
Elezanumab (ABT-555; AE12-1Y-QL) is a human monoclonal antibody that selectively targets repulsive guidance molecule A (RGMa). Elezanumab potently inhibited RGMa mediated BMP signalling via the SMAD1/5/8 pathway, with an IC50 around 97 pM. Elezanumab promotes neuroregeneration and neuroprotection in neuronal injury and demyelination models binds N-terminal RGMa, blocks BMP signaling and lacks RGMc cross-reactivity. elezanumab has neuroregenerative and neuroprotective activities without impact on iron metabolism .
Tibulizumab (LY 3090106) is a tetravalent bispecific monoclonal antibody targeting B-cell activating factor (BAFF) and IL-17A with Kd values of 60 pM and 14 pM, respectively. Tibulizumab can be used for autoimmune disease research .
Brolucizumab (DLX1008) is a single-chain anti-VEGF-A antibody fragment with low picomolar affinity (KD=1.05 pM). Brolucizumab can be used for the research of cancer .
Isecarosmab (M-6495) is an anti-ADAMTS monoclonal antibody (mAb) with a KD value of 3.65 pM. Isecarosmab has chondroprotective and anti-inflammatory activities. Isecarosmab can bind albumin to extend plasma half-life .
Remtolumab is a bispecific variable domain immunoglobulin molecule with human affinities for TNFα and IL-17 in the low pM range of Kd. Remtolumab can be used in research related to rheumatoid arthritis, psoriatic arthritis, and moderate-to-severe plaque psoriasis .
Denikitug (GS-1811; JTX-1811) is a humanized monoclonal antibody against CCR8 receptor with a KD of 16.8 pM. Denikitug specifically binds to human CCR8, inhibits CCL1-induced downstreamCCR8signaling. Denikitug selectively depletes cells expressing CCR8 via antibody-dependent cellular cytotoxicity (ADCC). Denikitug promotes anti-tumor immunity and can be used for the research of cancer and immunology .
Tagmokitug (CHS-114; SRF-114) is a fully human IgG1 antibody targeting CCR8. Tagmokitug selectively binds to human CCR8 (Kd = 502 pM) and mediates the death of CCR8-expressing cells via antibody-dependent cellular cytotoxicity and antibody-dependent cellular phagocytosis. Tagmokitug selectively eliminates intratumoral regulatory T cells, induces tumor growth inhibition, remodels the tumor immune microenvironment, and promotes the differentiation of cytotoxic CD8 + T cell subsets. Tagmokitug can be used for the research of solid tumors .
Conbercept (KH902) is a recombinant fusion protein composed of VEGFR-1 (second domain) and VEGFR-2 (third and fourth domains) regions fused to human IgG1 Fc. Conbercept is a VEGF inhibitor (IC50 = 8.8 pM) and is a soluble receptor decoy that blocks all isoforms of VEGF-A (Kd = 0.5 pM), VEGF-B (Kd = 8 pM), VEGF-C, and PlGF (Kd = 5 pM). Conbercept has anti-inflammatory effects, can lower the levels of VEGF, TNF-α and IL-6, and reduce the infiltration of inflammatory cells. Conbercept decreases tumor growth in several oncology studies. Conbercept can be used for various eye diseases such as polypoidal choroidal vasculopathy (PCV), diabetic macular edema (DME) and pathologic myopia choroidal neovascularization (pmCNV) .
Ocaratuzumab (AME 133v) is an Fc-engineered humanized IgG1 anti-CD20 monoclonal antibody, with a Kd of ~100 pM. Ocaratuzumab exhibits more effective antibody-dependent cell-mediated cytotoxicity (ADCC) .
Elsilimomab (B-E8) is a IgG1 monoclonal antibody against interleukin-6 (IL-6), with a KD of 22 pM and an IC50 of 1.4 nM. Elsilimomab can be used for the research of multiple myeloma, renal cell carcinoma, and rheumatoid arthritis (RA) .
Rademikibart (CBP-201) is a human monoclonal antibody targeting IL-4Rα with a KD of 20.7 pM when binding to human IL-4Rα epitopes. Rademikibart does not bind to IL-4Rα from other species. Rademikibart inhibits IL-4 and IL-13-mediated STAT6 signaling, TF-1 cell proliferation and TARC production in PBMCs. Rademikibart has the potential for moderate-to-severe Th2 inflammatory diseases research .
Zimberelimab (GLS-010) is a fully human IgG4 anti-PD-1 monoclonal antibody with an EC50 of 210 pM for human PD-1. Zimberelimab effectively blocks the binding of PD-L1 and PD-L2 to cell-surface PD-1 in CHO-S cells, with IC50 values of 580 pM and 670 pM, respectively. Zimberelimab shows antitumor activities, and can be used for various cancers research, including cervical cancer, non-small cell lung cancer and classical Hodgkin’s lymphoma .
Corifollitropin alfa (Org 36286) is a long-acting recombinant follicle-stimulating hormone (FSH) analog. Corifollitropin alfa is a FSH Receptor agonist with an EC50 of 5.0 pM. Corifollitropin alfa stimulates ovulation and can be used in the research of infertility .
CE-355621 is a humanized anti-c-Met IgG1 monoclonal antibody. CE-355621 can effectively bind with human c-Met (KD = 200 pM, IC50 = 466 pM) in A549 cells and cyno c-Met (KD = 610 pM) in cynomolgus kidney cells. CE-355621 inhibits the c-Met signaling pathway by blocking HGF binding. CE-355621 significantly inhibits the growth of tumors dependent on the c-Met/HGF pathway. CE-355621 can be used for research on cancer such as glioblastoma and gastric cancer .
Olendalizumab (ALXN1007) is a mouse-derived and humanized IgG2-G4-κ antibody, targeting to Complement protein C5a (Ki=60 pM). Olendalizumab targets the complement inflammatory pathway. Moreover, Olendalizumab can be used for research of complement mediated disorder caused by corona virus .
Sintilimab (Anti-PD-1) (IBI308 (Anti-PD-1)) is a safe and effectivel humanized IgG4 monoclonal antibody that binds to PD-1 with a KD value of 74 pM. Sintilimab (Anti-PD-1) blocks the interaction of PD-1 with its ligands (PD-L1 and PL-L2), consequently helping to restore the endogenous antitumour T-cell response. Sintilimab (Anti-PD-1) combined with prebiotics inhibits tumor volume and regulates immune cell subpopulation balance in lung adenocarcinoma mice. Sintilimab (Anti-PD-1) can be used for the research of classical Hodgkin's lymphoma, non-small cell lung cancer and oesophageal cancer .
IMC-EB10 (LY3012218) is an anti-FLT3 monoclonal antibody. IMC-EB10 binds to FLT3 with high affinity (Kd = 158 pM) and blocks the binding of FLT3 ligand to FLT3 (IC50 ≈ 10 nM), thereby inhibiting MAPK, STAT5, and PI3K/Akt signaling in leukemia cells. IMC-EB10 can enhance the anti-leukemic effect of Methotrexate (HY-14519) and inhibit leukemias expressing wild-type or ITD-mutated FLT3 receptors. IMC-EB10 prolongs the survival of acute lymphoblastic leukemia (ALL) cells and primary leukemia samples and reduces engraftment in non-obese diabetic/severe combined immunodeficiency patients. IMC-EB10 is indicated for leukemia research .
MEDI7814 is a humanized monoclonal antibody inhibitor targeting C5a and C5adesArg. MEDI7814 binds to recombinant human C5a and serum purified human C5a with affinities of 14 pM and 8 pM, respectively. MEDI7814 is acute inflammatory diseases such as sepsis and renal ischemia-reperfusion injury .
JNJ-55920839 (CNTO-6358) is a fully human immunoglobulin G1κ monoclonal antibody and a selective Interferonα/ω neutralizer, with a Kd value of 0.9-10.7 pM against hIFNα and a Kd of 1.44 pM against IFNω. JNJ-55920839 can be used in research related to systemic lupus erythematosus .
Anti-IL25/IL17E Antibody (ABM109.2) is an antibody targeting IL-25/IL17E, with a Kd of 24 pM for hIL-25 and a Kd of 28 pM for recombinant mouse IL-25. Anti-IL25/IL17E Antibody (ABM109.2) is applicable to research related to inflammatory and immune diseases. The isotype control is Human IgG1 kappa, Isotype Control (HY-P99001) .
AMY109 is an anti-human interleukin-8 (IL-8) monoclonal antibody, with a Ka of 36.8 pM for human IL-8, and a Ka of 380 pM for cynomolgus monkey IL-8. AMY109 binds to human and cynomolgus monkey IL-8 in a pH-dependent manner, inhibits IL-8-mediated activation of CXCR1 and CXCR2, and blocks the downstream biological activities of IL-8. AMY109 inhibits neutrophil recruitment to endometriotic lesions and suppresses monocyte chemoattractant protein-1 production by neutrophils. AMY109 is applicable to research related to endometriosis .
SK48-E26 is a human interleukin-1β (IL-1β) inhibitor, with a IC50 of 400 pM against human IL-1β, a IC50 of 185 pM against cynomolgus monkey IL-1β, and a Ka value ranging from 0.048 nM to 3 nM for human IL-1β. SK48-E26 binds to the conformational epitope of human IL-1β spanning amino acid residues 95-101, and blocks the biological activity of IL-1β. SK48-E26 can be used in research related to IL-1β-mediated inflammatory diseases and osteoarthritis .
MEDI-579 is a fully human monoclonal antibody against PAI-1, with a KD value of 6 pM for human PAI-1 and 105 pM for rat PAI-1. MEDI-579 restores renal plasmin activity and inhibits PAI-1-mediated intracellular signal transduction. MEDI-579 reduces albuminuria, glomerulosclerosis severity, TGF-β1 expression level, and phosphorylated Smad2 level induced in diabetic mice. MEDI-579 decreases the levels of active PAI-1 in plasma and kidneys, and increases plasma plasmin level in a mouse model of lupus nephritis. MEDI-579 can be used in research related to diabetic nephropathy and lupus nephritis. The recommended isotype control is human IgG1 kappa (HY-P99001) .
LY3541860 is a selective anti-CD19 antibody that both binds human CD19 with high affinity and selectively binds human B cells (Kd values: 76.8 pM and 94.5 nM for humans and cynomolgus monkeys, respectively). LY3541860 inhibits CpG-induced CD69 expression (IC50 = 0.006 nM). LY3541860 exhibits potent B cell inhibitory activities. LY3541860 can inhibit both BCR- and TLR-induced human B cell activation. LY3541860 can be used for the research of autoimmune diseases .
huDMB5F3 (DMB5F3; chDMB5F3) is a human monoclonal antibody against human CD227/MUC1, with a Ka value of 5.89 pM for its human target. huDMB5F3 enters MUC1-positive cancer cells via a temperature-dependent internalization process. huDMB5F3 induces cytotoxicity in MUC1-positive cancer cells. huDMB5F3 can be used in the research of various cancers including breast cancer, pancreatic cancer and gastric cancer .
RKER-216 is a human monoclonal IgG antibody inhibitor targeting ALK2 with a KD of 58.7 pM. RKER-216 reduces hepcidin transcription in Hep3B.RKER-216 competes with BMP ligands for binding to the extracellular domain of ALK2, thereby inhibiting BMP-SMAD signal. RKER-216 mobilizes tissue iron effectively in inflammatory conditions. RKER-216 improves microcytic anemia in a dose-dependent manner by inhibiting SMAD signaling to reduce hepcidin and promote iron absorption and utilization in vivo. RKER-216 can be used for research on anemia of inflammation .
COM503 is a high-affinity anti-IL18BP human monoclonal antibody with a Kd value of 0.291 pM. COM503 binds to IL18BP, blocks the IL18BP:IL18 interaction, displaces IL18 from preformed complexes, and enhances the activation and function of T cells and NK cells. COM503 induces anti-tumor effects by relieving the activity inhibition of endogenous IL18 in the tumor microenvironment. COM503 can be used for cancer research. The recommended isotype control is Human IgG4 (S228P) kappa, Isotype Control (HY-P99003) .
IMG-008 is a fully human antagonistic antibody targeting IL-36R, acting as a high-affinity IL-36R inhibitor (Kd = 6.23 pM). IMG-008 competitively blocks the pro-inflammatory signaling pathway mediated by human IL-36R, inhibiting receptor activation and the production of inflammatory cytokines. IMG-008 suppresses Imiquimod (HY-B0180)-induced skin inflammation in humanized mice, and Fc modification increases its serum exposure and prolongs its half-life. IMG-008 can be used in studies related to IL-36R-mediated inflammatory diseases such as psoriasis .
D8P1C1 is a high-affinity ADAM17 inhibitor (with a Kd of 180 pM targeting ADAM17-ECD) that reduces the shedding and phosphorylation of EGFR ligands. D8P1C1 inhibits cancer cell proliferation in vitro and tumor growth in xenograft models. 89Zr-DFO-D8P1C1 radioimmunological PET imaging shows its substantial accumulation in ovarian tumor xenografts, serving as a platform for generating bispecific T-cell engager derivatives. D8P1C1 can be applied to research on related diseases including triple-negative breast cancer, various types of ovarian cancer, lung adenocarcinoma, glioma, and colon cancer .
NS101 is an anti-FAM19A5 antibody with an IC50 of 0.2 nM and a Kd of 111 pM, as well as blood-brain barrier permeability. NS101 binds to key amino acid residues of FAM19A5, thereby blocking the interaction of LRRC4B and disrupting the FAM19A5-LRRC4B complex. NS101 increases the dendritic spine density in hippocampal neurons and the prefrontal cortex, normalizes the dendritic spine elimination rate, elevates the frequencies of mEPSC and fEPSP, and promotes the transport of brain-derived FAM19A5 into the peripheral circulation. NS101 improves cognitive function in mouse models of Alzheimer's disease. NS101 can be used for research on Alzheimer's disease. The recommended isotype control is human IgG1 kappa (HY-P99001) .
BI-836880 is a humanized bispecific nanobody and a selective inhibitor of VEGF and ANG2, with a Kd of 16 pM for hANG2, an EC50 of 1.4 nM for VEGF165, and an EC50 of 2.3 nM for VEGF121. BI-836880 blocks ERK phosphorylation downstream of VEGF-A as well as TIE2 phosphorylation downstream of ANG2. BI-836880 does not inhibit ANG1-mediated TIE2 phosphorylation. BI-836880 exerts anti-angiogenic effects, reduces the number of immature endothelial vessels in tumor tissues, and inhibits tumor growth in preclinical models. BI-836880 can be used in the research of pancreatic cancer, non-small cell lung cancer, renal cell carcinoma, ovarian cancer, colon cancer, and Lewis lung cancer .
Aprotinin is a bovine pancreatic trypsin inhibitor (BPTI) inhibitor which inhibits trypsin and chymotrypsin with Kis of 0.06 pM and 9 nM, respectively.
Plitidepsin (Aplidine) is a potent anti-cancer agent by targeting eEF1A2 ( KD=80 nM) . Plitidepsin possesses antiviral activity and is against SARS-CoV-2 with an IC90 of 0.88 nM. Plitidepsin is usually used for multiple myeloma and advanced cancer research, and has the potential for COVID-19 research .
7α, 25-dihydroxycholesterol (7α,25-OHC) is a potent and selective agonist and endogenous ligand of the orphan GPCR receptor EBI2 (GPR183). 7α, 25-dihydroxycholesterol is highly potent at activating EBI2 (EC50=140 pM; Kd=450 pM). 7α, 25-dihydroxycholesterol can serve as a chemokine directing migration of B cells, T cells and dendritic cells .
Santacruzamate A (CAY-10683, STA) is a potent and selective HDAC2 inhibitor with an IC50 of 119 pM. STA also exerts neuroprotective property against amyloid-β protein fragment 25–35. STA can be used for cancer and neurological disease research .
Ramiprilat (HOE 498 diacid), an active metabolite of Ramipril, is a potent and orally active angiotensin converting enzyme (ACE) inhibitor with a Ki value of 7 pM. Ramiprilat has acute antlhypertensive effect. Ramiprilat can be used for high blood pressure and heart failure research .
Sipeimine (Imperialine) is an inhibitor targeting the PI3K/AKT/NF-κB pathway and NLRP3 inflammasome, which can competitively bind to PI3K and p65. Sipeimine inhibits PI3K/AKT phosphorylation, blocks NF-κB nuclear translocation and NLRP3 inflammasome activation. Sipeimine exerts anti-inflammatory activities, inhibits pyroptosis and ferroptosis, and protects the extracellular matrix. Sipeimine can reduce cartilage degradation and synovial inflammation in osteoarthritis and improve PM2.5-induced lung injury. Sipeimine is mainly used in the study of anti-inflammatory and degenerative diseases .
Emodin-8-glucoside is an anthraquinone derivative that can be isolated from Aloe vera. Emodin-8-glucoside is the inhibitor for MAPK with an inhibition constant of 430.14 pM. Emodin-8-glucoside exhibits moderate inhibitory activity against rat lens aldose reductase (ALAR) and topoisomerases II with IC50s of 14.4 μM and 66 μM. Emodin-8-glucoside exhibits antioxidant, anti-inflammatory and anti-fibrotic activities. Emodin-8-glucoside can cross the blood brain barrier .
Jujuboside B is a bioactive saponin component isolated from Ziziphi Spinosae Semen (sour jujube seed), with oral efficacy and blood-brain barrier permeability. Jujuboside B induces acute leukemia cell death and drives necroptosis apoptosis by activating the RIPK1/RIPK3/MLKL pathway. Jujuboside B upregulates the expression of NOXA, PARP and caspase-3, activates AMPK, inhibits the proliferation of breast cancer cells, and induces cell apoptosis and autophagy. Jujuboside B inhibits angiogenesis and tumor growth by blocking the VEGFR-2 signaling pathway. Jujuboside B alleviates liver injury in mice by regulating the Nrf2-STING signaling pathway . Jujuboside B alleviates liver injury by regulating anti-inflammatory responses and downregulating the expression of 11β-HSD2. Jujuboside B induces ferroptosis and overcomes radioresistance in non-small cell lung cancer via the PPARγ-ATF3-Gpx4 signaling pathway. Jujuboside B exerts inhibitory effects on platelet aggregation. Jujuboside B inhibits febrile seizures by suppressing the activity of AMPA receptors. Jujuboside B reverses chronic unpredictable mild stress-promoted tumor progression by blocking the PI3K/Akt and MAPK/ERK pathways and dephosphorylating CREB signaling. Jujuboside B is applicable to related studies on acute leukemia, breast cancer, PM2.5-induced lung injury, hepatotoxicity, liver injury, colorectal cancer, non-small cell lung cancer, thromboembolic diseases, cardiovascular diseases associated with high platelet aggregation, febrile seizures, and depressive-like phenotypes .
Militarine is a plant growth inhibitor and anti-inflammatory agent. Militarine inhibits the elongation of radicles and hypocotyls in seedlings of lettuce, Italian ryegrass and timothy grass. Militarine alleviates PM2.5-induced inflammatory injury and inhibits cell migration in human alveolar epithelial A549 cells by inhibiting the NF-κB signaling pathway, reducing oxidative stress and the release of inflammatory factors. Militarine can be used in studies related to PM2.5-induced pulmonary diseases .
Margatoxin, an alpha-KTx scorpion toxin, is a high affinity inhibitor of Kv1.3 (Kd=11.7 pM). Margatoxin inhibits the Kv1.2 (Kd=6.4 pM) and Kv1.1 (Kd=4.2 nM). Margatoxin, a 39 amino-acid-long peptide, is isolated from the venom of the scorpion Centruroides margaritatus and widely used in ion channel research .
Bruceantinol is a quassinoid that can be isolated from Brucea javanica, inhibits pepper mottle virus (PepMoV) in pepper. Bruceantinol is a STAT3 inhibitor demonstrating potent antitumor activity in in vitro and in vivo human colorectal cancer (CRC) models. Bruceantinol has potent anti-leukemic activity. Bruceantinol strongly inhibits STAT3 DNA-binding ability (IC50 = 2.4 pM), blocks the constitutive and IL-6-induced STAT3 activation, and suppresses transcription of MCL-1, PTTG1, survivin and c-Myc. Bruceantinol binds with CDK2/4/6 to facilitate protein degradation through proteasome pathway. Bruceantinol can dose- and time-dependently reduces the cell growth, impede cell proliferation, disrupts the cell cycle, and induces necrosis in MCF-7 cells and apoptosis in MDA-MB-231 cells .
Plitidepsin (Standard) is the analytical standard of Plitidepsin. This product is intended for research and analytical applications. Plitidepsin (Aplidine) is a potent anti-cancer agent by targeting eEF1A2 ( KD=80 nM) . Plitidepsin possesses antiviral activity and is against SARS-CoV-2 with an IC90 of 0.88 nM. Plitidepsin is usually used for multiple myeloma and advanced cancer research, and has the potential for COVID-19 research .
Deamino-NAD is a structural analog of NAD+ (HY-B0445). Deamino-NAD is involved in glycolysis as a substrate for rabbit muscle glyceraldehyde 3-phosphate dehydrogenase (GPDH), with a Km of 2300 pm, and a Kd of 112 pm .
Kocurin (PM181104) is a thiazolyl cyclic-peptide antibiotic. Kocurin inhibits bacterial growth by impeding bacterial protein biosynthesis during the translation phase. Kocurin has strong inhibitory activity against Gram-positive bacteria, but no activity against fungi and Gram-negative bacteria .
Militarine (Standard) is the analytical standard of Militarine (HY-122308). This product is intended for research and analytical applications. Militarine is a plant growth inhibitor and anti-inflammatory agent. Militarine inhibits the elongation of radicles and hypocotyls in seedlings of lettuce, Italian ryegrass and timothy grass. Militarine alleviates PM2.5-induced inflammatory injury and inhibits cell migration in human alveolar epithelial A549 cells by inhibiting the NF-κB signaling pathway, reducing oxidative stress and the release of inflammatory factors. Militarine can be used in studies related to PM2.5-induced pulmonary diseases .
21-Hydroxyoligomycin A is a potent inhibitor of K-Ras PM localization with an IC50 value of 4.82 nM. 21-Hydroxyoligomycin A has cytotoxicity and can be isolated from Streptomyces .
Gallinamide A TFA is a linearly depositing peptide and a potent inhibitor of cathepsin L (CatL) (IC50: 17.6 pM). Gallinamide A TFA inhibits SARS-CoV-2 infection by inhibiting CatL (EC50: 28 nM). Gallinamide A TFA also inhibits Plasmodium falciparum (IC50: 50 nM) .
Gilvocarcin M is an antibiotic and can be isolated from S. gilvotanareus. Gilvocarcin M is active against S. aureus at a concentration of 32 µg/ml and inhibits growth of KB cells with the IC50 of 0.52 µg/ml. Gilvocarcin M intercalates into bacteriophage PM2 DNA .
Sipeimine (Standard) is the analytical standard of Sipeimine (HY-N0696R). Sipeimine (Imperialine) is an inhibitor targeting the PI3K/AKT/NF-κB pathway and NLRP3 inflammasome, which can competitively bind to PI3K and p65. Sipeimine inhibits PI3K/AKT phosphorylation, blocks NF-κB nuclear translocation and NLRP3 inflammasome activation. Sipeimine exerts anti-inflammatory activities, inhibits pyroptosis and ferroptosis, and protects the extracellular matrix. Sipeimine can reduce cartilage degradation and synovial inflammation in osteoarthritis and improve PM2.5-induced lung injury. Sipeimine is mainly used in the study of anti-inflammatory and degenerative diseases .
Santacruzamate A (Standard) is the analytical standard of Santacruzamate A. This product is intended for research and analytical applications. Santacruzamate A (CAY-10683, STA) is a potent and selective HDAC2 inhibitor with an IC50 of 119 pM. STA also exerts neuroprotective property against amyloid-β protein fragment 25–35. STA can be used for cancer and neurological disease research[1][2].
Luzopeptin A (BBM-928 A) is an actinoleukin-like antitumor antibiotic. Luzopeptin A is a bifunctional DNA intercalator which can interact with isolated DNA molecules. Luzopeptin A induces an unwinding-rewinding process of the closed superhelical PM2 DNA. Luzopeptin A is active against HIV-1 and HIV-2 reverse transcriptase with IC50s of 7 nM and 68 nM for HIV-1 RT and HIV-2 RT, respectively .
Disorazol A1 is an tubulin inhibitor with antifungal activity. Disorazol A1 functions by inhibiting tubulin polymerization, interfering with microtubule formation, blocking mitosis, thus arresting the cell cycle at the G2/M phase and inducing apoptosis. Disorazol A1 also exhibits an inhibitory effect against L929 mouse fibroblasts with an IC50 value of 3 pM. Disorazol A1 causes the accumulation of p53 protein in the cell nucleus. Disorazol A1 is promising for research of cancers .
Emodin-8-glucoside (Standard) is the analytical standard of Emodin-8-glucoside. This product is intended for research and analytical applications. Emodin-8-glucoside is an anthraquinone derivative that can be isolated from Aloe vera. Emodin-8-glucoside is the inhibitor for MAPK with an inhibition constant of 430.14 pM. Emodin-8-glucoside exhibits moderate inhibitory activity against rat lens aldose reductase (ALAR) and topoisomerases II with IC50s of 14.4 μM and 66 μM. Emodin-8-glucoside exhibits antioxidant, anti-inflammatory and anti-fibrotic activities. Emodin-8-glucoside can cross the blood brain barrier .
Dasatinib (monohydrate) (Standard) is the analytical standard of Dasatinib (monohydrate). This product is intended for research and analytical applications. Dasatinib (BMS-354825) monohydrate is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib monohydrate inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively . Dasatinib monohydrate also induces apoptosis and autophagy.
Jujuboside B (Standard) is the analytical standard of Jujuboside B. This product is intended for research and analytical applications. Jujuboside B is a bioactive saponin component isolated from Ziziphi Spinosae Semen (sour jujube seed), with oral efficacy and blood-brain barrier permeability. Jujuboside B induces acute leukemia cell death and drives necroptosis apoptosis by activating the RIPK1/RIPK3/MLKL pathway. Jujuboside B upregulates the expression of NOXA, PARP and caspase-3, activates AMPK, inhibits the proliferation of breast cancer cells, and induces cell apoptosis and autophagy. Jujuboside B inhibits angiogenesis and tumor growth by blocking the VEGFR-2 signaling pathway. Jujuboside B alleviates liver injury in mice by regulating the Nrf2-STING signaling pathway . Jujuboside B alleviates liver injury by regulating anti-inflammatory responses and downregulating the expression of 11β-HSD2. Jujuboside B induces ferroptosis and overcomes radioresistance in non-small cell lung cancer via the PPARγ-ATF3-Gpx4 signaling pathway. Jujuboside B exerts inhibitory effects on platelet aggregation. Jujuboside B inhibits febrile seizures by suppressing the activity of AMPA receptors. Jujuboside B reverses chronic unpredictable mild stress-promoted tumor progression by blocking the PI3K/Akt and MAPK/ERK pathways and dephosphorylating CREB signaling. Jujuboside B is applicable to related studies on acute leukemia, breast cancer, PM2.5-induced lung injury, hepatotoxicity, liver injury, colorectal cancer, non-small cell lung cancer, thromboembolic diseases, cardiovascular diseases associated with high platelet aggregation, febrile seizures, and depressive-like phenotypes.
EXOSC9 is a noncatalytic RNA exosome complex component that critically drives 3'->5' exoribonuclease activity and contributes to a variety of cellular RNA processing and degradation events. In the nucleus, it helps stabilize the maturation of RNA species and eliminates processing by-products, non-coding transcripts and defective mRNAs, thereby inhibiting their cytoplasmic export. EXOSC9 Protein, Human (sf9, His) is the recombinant human-derived EXOSC9 protein, expressed by Sf9 insect cells , with N-His labeled tag.
Galectin-1/LGALS1 is a lectin that binds β-galactoside and complex carbohydrates and regulates apoptosis, proliferation, and differentiation. It inhibits CD45 phosphatase activity, blocks Lyn kinase dephosphorylation, and induces T cell apoptosis. Animal-Free Galectin-1/LGALS1 Protein, Human (His) is the recombinant human-derived animal-FreeGalectin-1/LGALS1 protein, expressed by E. coli , with N-His labeled tag. This product is for cell culture use only.
Galectin-1/LGALS1 is a lectin that binds β-galactoside and complex carbohydrates and regulates apoptosis, proliferation, and differentiation. It inhibits CD45 phosphatase activity, blocks Lyn kinase dephosphorylation, and induces T cell apoptosis. Galectin-1/LGALS1 Protein, Human (His) is the recombinant human-derived Galectin-1/LGALS1 protein, expressed by E. coli , with C-6*His labeled tag.
Ramelteon metabolite M-II-d3 is the deuterium labeled Ramelteon metabolite M-II. Ramelteon metabolite M-II is the major metabolite of Ramelteon, with IC50s of 208 pM, 1470 pM for human melatonin receptors (MT1 or MT2). Ramelteon is a selective melatonin agonist .
MCB-294 is a dual-state pan-KRAS inhibitor that selectively inhibits KRAS over NRAS and HRAS. MCB-294 capable of binding both the active (GTP-bound) and inactive (GDP-bound) forms of KRAS with Kds of approximately 1 pM and 10 nM, respectively. MCB-294 broadly impairs the growth of hTERT-HPNE cells expressing G12D, G12C, G12V, G12S, G13D, and wild-type KRAS, with IC50s of approximately 700 nM. MCB-294 induces irreversible apoptosis in KRAS-mutated tumors. MCB-294 effectively suppress KRAS G12C inhibitor-resistant cancer cells and remodel the tumor immune microenvironment. MCB-294 can be used for the study of pancreatic cancer, colorectal cancer and lung cancer .
Ramelteon-d3 (TAK-375-d3) is a deuterium-labelled Ramelteon (HY-A0014). Ramelteon is a potent, highly selective, and orally active agonist of MT1/MT2 with Ki values of 14 and 112 pM, respectively. Ramelteon has the potential for the research of insomnia. Ramelteon consistently reduces sleep onset after long-term treatment, with no next-morning residual effects or rebound insomnia or withdrawal symptoms upon discontinuation.
Lurbinectedin-d3 is deuterium labeled Lurbinectedin. Lurbinectedin (PM01183) is a DNA minor groove covalent binder with potent anti-tumour activity; inhibits RMG1 and RMG2 cell growth with IC50 values of 1.25 and 1.16 nM, respectively .
Dasatinib-d4 (BMS-354825-d4) is deuterium labeled Dasatinib. Dasatinib (BMS-354825) is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively . Dasatinib also induces apoptosis and autophagy.
Ramiprilat-d5 is deuterium labeled Ramiprilat. Ramiprilat (HOE 498 diacid), an active metabolite of Ramipril, is a potent and orally active angiotensin converting enzyme (ACE) inhibitor with a Ki value of 7 pM. Ramiprilat can be used for high blood pressure and heart failure research .
Ramelteon-d5 is deuterium labeled Ramelteon. Ramelteon is a potent, highly selective, and orally active agonist of MT1/MT2 with Ki values of 14 and 112 pM, respectively. Ramelteon has the potential for the research of insomnia. Ramelteon consistently reduces sleep onset after long-term treatment, with no next-morning residual effects or rebound insomnia or withdrawal symptoms upon discontinuation .
Ondansetron-d5 is the deuterium labeled Ondansetron (HY-B0002B). Ondansetron (GR 38032; SN 307) is a highly selective 5-HT3 receptor antagonist with an IC50 value of 103 pM. Ondansetron exerts its antiemetic effect by antagonizing 5-HT receptors located in localized neurons in the peripheral and central nervous systems. Ondansetron can inhibit nausea and vomiting induced by chemotherapy and radiotherapy .
Ledipasvir-d6 hydrochloride is deuterated labeled Ledipasvir acetone (HY-15602A). Ledipasvir acetone (GS-5885 acetone) is the active ingredient of Ledipasvir. Ledipasvir is an inhibitor of the hepatitis C virus NS5A, with EC50 values of 34 pM against GT1a and 4 pM against GT1b replicon.
MRTX-1257-d6 is the deuterium labeled MRTX-1257 (HY-114436). MRTX-1257 is a selective, irreversible, covalent and orally active KRAS G12C inhibitor, with an IC50 of 900 pM for KRAS dependent ERK phosphorylation in H358 cells .
Secnidazole-d6 is the deuterium labeled Secnidazole. Secnidazole (RP-14539;PM-185184) is an orally active azole antibiotic with a longer half-life than metronidazole (HY-B0318). Secnidazole is against the vaginosis-associated bacteria and has the potential for bacterial vaginosis research .
Ledipasvir-d6 is the deuterium labeled Ledipasvir. Ledipasvir (GS-5885) is an inhibitor of the hepatitis C virus NS5A, with EC50s of 34 pM and 4 pM against genotype 1a and 1b replicon, respectively. Ledipasvir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 1.62 μM .
Ceritinib (LDK378)-d7 is a deuterium labeled Ceritinib (HY-15656). Ceritinib is a selective, orally bioavailable and ATP-competitive ALK tyrosine kinase inhibitor . Ceritinib is a selective, orally bioavailable, and ATP-competitive ALK tyrosine kinase inhibitor with an IC50 of 200 pM. Ceritinib also inhibits IGF-1R, InsR, and STK22D with IC50 values of 8, 7, and 23 nM, respectively. Ceritinib shows great antitumor potency .
Lopinavir-d8 (ABT-378-d8) is the deuterium labeled Lopinavir. Lopinavir (ABT-378) is a highly potent, selective peptidomimetic inhibitor of the HIV-1 protease, with Kis of 1.3 to 3.6 pM for wild-type and mutant HIV protease. Lopinavir acts by arresting maturation of HIV-1 thereby blocking its infectivity . Lopinavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 14.2 μM .
Tofersen-d27 (BIIB067-d27) is the deuterium labeled Tofersen (HY-132580). Tofersen (BIIB067) is an antisense oligonucleotide and SOD1 mRNA inhibitor with an IC50 of 320 pM. Tofersen mediates RNase H-dependent degradation of SOD1 mRNA to reduce SOD1 protein levels in cerebrospinal fluid and serum. Tofersen downregulates cerebrospinal fluid neurofilament light chain, neurofilament heavy chain, amyloid-beta 1-40, amyloid-beta 1-42, neuropeptide Y, ubiquitin C-terminal hydrolase L1, neuropentraxins 1, 2, R, corticotropin-releasing hormone, IL-15, and serum neurofilament light chain, neurofilament heavy chain. Tofersen can be used for the research of superoxide dismutase 1-associated amyotrophic lateral sclerosis.
Secnidazole-d3 (RP-14539-d3; PM-185184-d3) is the deuterium labeled Secnidazole (HY-B1118). Secnidazole (RP-14539) is an orally active azole antibiotic and a imidazole mitigator of Serratia marcescens virulence. Secnidazole, as an analog of acylhomoserine lactones, effectively inhibits QS resulting in the attenuation of Pseudomonas aeruginosa pathogenesis. Secnidazole has antimicrobial activity against many anaerobic Gram-negative and Gram-positive bacterial species in vitro. Secnidazole can be used for the research of various diseases, such as amoebiasis and giardiasis, and bacterial vaginitis .
Secnidazole- 13C2, 15N2 is the 13C2, 15N2 labeled Secnidazole. Secnidazole (RP-14539;PM-185184) is an orally active azole antibiotic with a longer half-life than metronidazole (HY-B0318). Secnidazole is against the vaginosis-associated bacteria and has the potential for bacterial vaginosis research.
Ledipasvir-d16 (GS-5885-d16) is deuterium labeled Ledipasvir. Ledipasvir (GS-5885) is an inhibitor of the hepatitis C virus NS5A, with EC50s of 34 pM and 4 pM against genotype 1a and 1b replicon, respectively. Ledipasvir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 1.62 μM .
Secnidazole-d4 is the deuterium labeled Secnidazole . Secnidazole (RP-14539) is an orally active azole antibiotic and a imidazole mitigator of Serratia marcescens virulence. Secnidazole, as an analog of acylhomoserine lactones, effectively inhibits QS resulting in the attenuation of Pseudomonas aeruginosa pathogenesis. Secnidazole has antimicrobial activity against many anaerobic Gram-negative and Gram-positive bacterial species in vitro. Secnidazole can be used for the research of various diseases, such as amoebiasis and giardiasis, and bacterial vaginitis .
Saroglitazar-d4 is the deuterium-labeled Saroglitazar (HY-19937). Saroglitazar-d4 is a novel peroxisome proliferator-activated receptor (PPAR) agonist with predominant PPARα and moderate PPARγ activity with EC50 values of 0.65 pM and 3 nM in HepG2 cells, respectively.
Ramiprilat-d4 hydrochloride is deuterated labeled Ramiprilat (HY-A0115). Ramiprilat (HOE 498 diacid), an active metabolite of Ramipril, is a potent and orally active angiotensin converting enzyme (ACE) inhibitor with a Ki value of 7 pM. Ramiprilat can be used for high blood pressure and heart failure research .
Aprepitant- 13C2,d2 (Major) (MK-0869- 13C2,d2) is 13C labeled Aprepitant. Aprepitant (MK-0869) is a selective and high-affinity neurokinin 1 receptor antagonist with a Kd of 86 pM.
Elagolix-d6 (sodium) (NBI-56418-d6 (sodium)) is deuterium labeled Elagolix sodium. Elagolix sodium is a highly effective, selective, oral-active, short-term, non-peptide gonadotropin-releasing hormone receptor (GnRH receptor) antagonist (KD = 54 pM) and NFAT inhibitor, which can be used to study pain related to endometriosis. .
Daclatasvir-d6 is deuterium labeled Daclatasvir. Daclatasvir (BMS-790052) is a potent and orally active HCV NS5A protein inhibitor with EC50s range of 9-146 pM for multiple HCV replicon genotypes. Daclatasvir is also a organic anion transporting polypeptide 1B (OATP1B) and OATP1B3 inhibitor with IC50s of 1.5 μM and 3.27 μM, respectively .
Daclatasvir-d16 is deuterium labeled Daclatasvir. Daclatasvir (BMS-790052) is a potent and orally active HCV NS5A protein inhibitor with EC50s range of 9-146 pM for multiple HCV replicon genotypes. Daclatasvir is also a organic anion transporting polypeptide 1B (OATP1B) and OATP1B3 inhibitor with IC50s of 1.5 μM and 3.27 μM, respectively .
Lopinavir-d7 is deuterated labeled Lopinavir (HY-14588). Lopinavir (ABT-378) is a highly potent, selective peptidomimetic inhibitor of the HIV-1 protease, with Kis of 1.3 to 3.6 pM for wild-type and mutant HIV protease. Lopinavir acts by arresting maturation of HIV-1 thereby blocking its infectivity . Lopinavir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 14.2 μM .
Ondansetron-d3 is the deuterium labeled Ondansetron (HY-B0002B ). Ondansetron (GR 38032; SN 307) is a highly selective 5-HT3 receptor antagonist with an IC50 value of 103 pM. Ondansetron exerts its antiemetic effect by antagonizing 5-HT receptors located in localized neurons in the peripheral and central nervous systems. Ondansetron can inhibit nausea and vomiting induced by chemotherapy and radiotherapy .
(rel)-Lopinavir-d8 ((rel)-ABT-378-d8) is the deuterium labeled Lopinavir (HY-14588) . Lopinavir (ABT-378) is a highly potent, selective peptidomimetic inhibitor of the HIV-1 protease, with Kis of 1.3 to 3.6 pM for wild-type and mutant HIV protease. Lopinavir acts by arresting maturation of HIV-1 thereby blocking its infectivity . Lopinavir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 14.2 μM .
Ondansetron- 13C,d3 is the 13C- and deuterium labeled Ondansetron (HY-B0002B). Ondansetron (GR 38032; SN 307) is a highly selective 5-HT3 receptor antagonist with an IC50 value of 103 pM. Ondansetron exerts its antiemetic effect by antagonizing 5-HT receptors located in localized neurons in the peripheral and central nervous systems. Ondansetron can inhibit nausea and vomiting induced by chemotherapy and radiotherapy .
Daclatasvir- 13C2,d6 (BMS-790052- 13C2,d6) is 13C and deuterium labeled Daclatasvir. Daclatasvir (BMS-790052) is a potent and orally active HCV NS5A protein inhibitor with EC50s range of 9-146 pM for multiple HCV replicon genotypes. Daclatasvir is also a organic anion transporting polypeptide 1B (OATP1B) and OATP1B3 inhibitor with IC50s of 1.5 μM and 3.27 μM, respectively .
Elagolix-d9 is the deuterium labeled Elagolix. Elagolix sodium is a highly effective, selective, oral-active, short-term, non-peptide gonadotropin-releasing hormone receptor (GnRH receptor) antagonist (KD = 54 pM) and NFAT inhibitor, which can be used to study pain related to endometriosis. .
Gartisertib-d8 (VX-803-d8) is the deuterium labeled Gartisertib (HY-136270). Gartisertib (VX-803) is an ATP-competitive, orally active, and selective ATR inhibitor, with a Ki of <150 pM. Gartisertib potently inhibits ATR-driven phosphorylated checkpoint kinase-1 (Chk1) phosphorylation with an IC50 of 8 nM. Antitumor activity .
MRTX1133 is a noncovalent, potent, and selective alkyne-based KRAS G12D inhibitor. MRTX1133 optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated KD against KRAS G12D of 0.2 pM. MRTX1133 prevents SOS1-catalyzed nucleotide exchange and/or formation of the KRAS G12D/GTP/RAF1 complex, thereby inhibiting mutant KRAS-dependent signal transduction. MRTX1133 selectively inhibits KRAS G12D mutant, but not KRAS wild-type, tumor cells. MRTX1133 has single digit nanomolar activity in cellular assays and marked in vivo efficacy in tumor models harboring KRAS G12D mutations .
Pralatrexate is an antifolate and is a potent dihydrofolate reductasean (DHFR) inhibitor with a Ki of 13.4 pM. Pralatrexate is a substrate for folylpolyglutamate synthetase with improved cellular uptake and retention. Pralatrexate has antitumor activities and has the potential for relapsed/refractory T-cell lymphoma treatment . Pralatrexate is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
MCB-36 is a VHL-recruiting pan-KRAS PROTAC degrader without affecting KRAS transcription. MCB-36 exhibits minimal effects on HRAS and NRAS protein levels. MCB-36 binds to the GDP-loaded state of G12D, G12C, G12V, and wild-type KRAS with high affinities Kd ≈ 1 pM). MCB-36 decreases p-ERK levels, leading to cell apoptosis. MCB-36 effectively suppress KRAS G12C inhibitor-resistant cancer cells and remodel the tumor immune microenvironment. MCB-36 can be used for the study of colorectal cancer and lung cancer (Pink: Target protein ligand; Blue: E3 ligand (HY-112078); Black: Linker (HY-W091879)) .
MCB-294 is a dual-state pan-KRAS inhibitor that selectively inhibits KRAS over NRAS and HRAS. MCB-294 capable of binding both the active (GTP-bound) and inactive (GDP-bound) forms of KRAS with Kds of approximately 1 pM and 10 nM, respectively. MCB-294 broadly impairs the growth of hTERT-HPNE cells expressing G12D, G12C, G12V, G12S, G13D, and wild-type KRAS, with IC50s of approximately 700 nM. MCB-294 induces irreversible apoptosis in KRAS-mutated tumors. MCB-294 effectively suppress KRAS G12C inhibitor-resistant cancer cells and remodel the tumor immune microenvironment. MCB-294 can be used for the study of pancreatic cancer, colorectal cancer and lung cancer .
Tofersen (BIIB067) is an antisense oligonucleotide and SOD1 mRNA inhibitor with an IC50 of 320 pM. Tofersen mediates RNase H-dependent degradation of SOD1 mRNA to reduce SOD1 protein levels in cerebrospinal fluid and serum. Tofersen downregulates cerebrospinal fluid neurofilament light chain, neurofilament heavy chain, amyloid-beta 1-40, amyloid-beta 1-42, neuropeptide Y, ubiquitin C-terminal hydrolase L1, neuropentraxins 1, 2, R, corticotropin-releasing hormone, IL-15, and serum neurofilament light chain, neurofilament heavy chain. Tofersen can be used for the research of superoxide dismutase 1-associated amyotrophic lateral sclerosis .
Tofersen (BIIB067) sodium is an antisense oligonucleotide and SOD1 mRNA inhibitor with an IC50 of 320 pM. Tofersen sodium mediates RNase H-dependent degradation of SOD1 mRNA to reduce SOD1 protein levels in cerebrospinal fluid and serum. Tofersen sodium downregulates cerebrospinal fluid neurofilament light chain, neurofilament heavy chain, amyloid-beta 1-40, amyloid-beta 1-42, neuropeptide Y, ubiquitin C-terminal hydrolase L1, neuropentraxins 1, 2, R, corticotropin-releasing hormone, IL-15, and serum neurofilament light chain, neurofilament heavy chain. Tofersen sodium can be used for the research of superoxide dismutase 1-associated amyotrophic lateral sclerosis .
ARC5690 sodium is an anti-mouse P-selectin aptamer. ARC5690 bound to recombinant mouse P-selectin with a KD of approximately 15pM in vitro. ARC5690 showed a significant anti-inflammatory effect
AP1153 aptamer sodium is a DNA aptamer that specifically binds to the cholecystokinin receptor CCKBR (Kd: ~15 pM), but does not activate CCKBR-related signaling pathways. AP1153 aptamer sodium is internalized by pancreatic ductal adenocarcinoma (PDAC) cells in a receptor-mediated manner. AP1153 aptamer sodium can bioconjugate to the surface of fluorescent nanoparticles to facilitate nanoparticle delivery to PDAC tumors in vivo .
Tofersen-d27 (BIIB067-d27) is the deuterium labeled Tofersen (HY-132580). Tofersen (BIIB067) is an antisense oligonucleotide and SOD1 mRNA inhibitor with an IC50 of 320 pM. Tofersen mediates RNase H-dependent degradation of SOD1 mRNA to reduce SOD1 protein levels in cerebrospinal fluid and serum. Tofersen downregulates cerebrospinal fluid neurofilament light chain, neurofilament heavy chain, amyloid-beta 1-40, amyloid-beta 1-42, neuropeptide Y, ubiquitin C-terminal hydrolase L1, neuropentraxins 1, 2, R, corticotropin-releasing hormone, IL-15, and serum neurofilament light chain, neurofilament heavy chain. Tofersen can be used for the research of superoxide dismutase 1-associated amyotrophic lateral sclerosis.
PM20D1 Human Pre-designed siRNA Set A contains three designed siRNAs for PM20D1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
PRB1 Human Pre-designed siRNA Set A contains three designed siRNAs for PRB1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
Dasatinib (BMS-354825) (GMP) is a GMP-grade Dasatinib (HY-10181). GMP-grade small molecules can be used as adjuvant agents in cell therapy. Dasatinib (BMS-354825) is an orally active, ATP-competitive, dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Ki values for Src and Bcr-Abl are 16 pM and 30 pM, respectively. Dasatinib inhibits Bcr-Abl and Src with IC50 values of less than 1.0 nM and 0.5 nM, respectively. Dasatinib also induces apoptosis and autophagy .
Dasatinib (GMP Like) (BMS-354825 (GMP Like)) is Dasatinib (HY-10181) produced by using GMP like guidelines. GMP Like small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Dasatinib (BMS-354825) is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively . Dasatinib also induces apoptosis and autophagy.
Wnt-C59 (C59) GMP is a GMP grade Wnt-C59 (HY-15659). GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Wnt-C59 (C59) is a highly potent and oral porcupine (PORCN) inhibitor with an IC50 of 74 pM.
MG-101 (GMP) (Calpain inhibitor I (GMP)) is MG-101 (HY-18964) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. MG-101 (ALLN) is an inhibitor of cysteine proteases which inhibits calpain I, calpain II, cathepsin B and cathepsin L with Kis of 190, 220, 150 and 500 pM, respectively. MG-101 induces apoptosis and inhibits tumor growth, it can be used for the research of colon cancer .
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Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
MedchemExpress Validation 03
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
MedchemExpress Validation 04
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
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