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CellTracker CM-DiI (CM-DiI) is a lipophilic fluorochrome that can be used for tracking the migration of lymphocytes. CellTracker CM-DiI is feasible to detect labeled cells in histological sections (excitation 553 nm; emission 570 nm) .
CM-675 is a dual phosphodiesterase 5 (PDE5) and class I histone deacetylases-selective inhibitor, with IC50 values of 114 nM and 673 nM for PDE5 and HDAC1, respectively. CM-675 has potential to treat Alzheimer’s disease .
CM-272 is a first-in-class, potent, selective, substrate-competitive and reversible dual G9a/DNA methyltransferases (DNMTs) inhibitor with antitumor activities. CM-272 inhibits G9a, DNMT1, DNMT3A, DNMT3B and GLP with IC50s of 8 nM, 382 nM, 85 nM, 1200 nM and 2 nM, respectively. CM-272 inhibits cell proliferation and promotes apoptosis, inducing IFN-stimulated genes and immunogenic cell death .
CM-1758 is a histone deacetylase (HDAC) inhibitor. CM-1758 inhibits tumor growth in vivo. CM-1758 induces acetylation of non-histone proteins in acute myeloid leukemia cells .
CM-10-18 is a potent and orally active inhibitor of both α-glucosidases I and II in vitro and in treated animals. CM-10-18 inhibits DENV infection of cultured human cells and reduces the peak viremia of DENV in mice .
CM572 is a selective irreversible partial sigma-2 receptor agonist. CM572 has antitumor activity. CM572 induces dose-dependent cell death, with an EC50 of 7.6 μM in SK-N-SH neuroblastoma cells. CM572 can be used for the research of kinds of diseases such as neuroblastoma, breast cancer .
CM10 is a potent and selective aldehyde dehydrogenase 1A (ALDH1A) family inhibitor, with IC50s of 1700, 740, and 640 nM for ALDH1A1, ALDH1A2, and ALDH1A3, respectively. CM10 does not inhibit any of the other ALDH family members. CM10 can regulate metabolism and has anti-cancer activity .
CM03 is a potent DNA G-quadruplexes (G4s) ligand. CM03 can stabilise G4s, downregulating more G4-containing genes as well as increasing incidence of double-strand break events (DSBs) due to torsional strain on DNA and chromatin structure. CM03 has selective potency for pancreatic cancer cells .
CM-579 trihydrochloride is a first-in-class reversible, dual inhibitor of G9a and DNMT, with IC50 values of 16 nM, 32 nM for G9a and DNMT, respectively. Has potent in vitro cellular activity in a wide range of cancer cells .
CM-579 is a first-in-class reversible, dual inhibitor of G9a and DNMT, with IC50 values of 16 nM, 32 nM for G9a and DNMT, respectively. Has potent in vitro cellular activity in a wide range of cancer cells .
CM-H2DCFDA is a derivative of H2DCFDA (HY-D0940). CM-H2DCFDA can be used to determine cellular oxidant levels (Ex/Em: 495/530 nm). CM-H2DCFDA is light-sensitive .
CM398 is a highly selective, orally active sigma-2 receptor ligand (Ki=0.43 nM), with high sigma-1/sigma-2 selectivity rato (1000-fold). CM398 shows notable affinity for dopamine (Ki=32.90 nM) and serotonin transporters (Ki=244.2 nM). CM398 shows promising anti-inflammatory analgesic effects in the formalin model of inflammatory pain in mice .
Zegocractin (CM-4620) is a calcium-release activated calcium-channel (CRAC channel) inhibitor, with IC50s of 119 nM and 895 nM for Orai1/STIM1 and Orai2/STIM1 channels, respectively .
Fabomotizole hydrochloride (CM346 hydrochloride) is an anxiolytic agent. Fabomotizole hydrochloride produces anxiolytic and neuroprotective effects without any muscle relaxant actions.
Murraol (CM-c2), a coumarin, can be isolated from the leaves of Madagascar pine cork (Apiaceae). Murraol has cyclooxygenase (COX) and lipoxygenase inhibitory properties and has an inhibitory effect on the growth of cancer cells .
Vorolanib (CM082) is an orally active, potent multikinase VEGFR/PDGFR inhibitor. Vorolanib is a potent ATP-binding cassette (ABC) transporter inhibitor. Vorolanib is an angiogenesis inhibitor and has antitumor activity combined with ZD1839 (HY-50895) .
Stapokibart (CM310) is a humanised monoclonal antibody targeting IL-4Rα and efficiently blocks the interaction of cytokines IL-4 and IL-13 with their co-receptor subunit IL-4Rα. Stapokibart has the capacity to interact with IL-4Rα in humans, cynomolgus monkeys, and rats .
L-798106 is potent and highly selective prostanoid EP3 receptor antagonist (Ki=0.3 nM), it also has micromolar activities at the EP4, EP1 and EP2 receptors with Ki values of 916 nM, >5000 nM and >5000 nM, respectively .
CMP98, a PROTAC, is unable to induce degradation of VHL. CMP98 can be used as a negative control compound for CM11 . CMP98 consists of two von Hippel-Lindau ligands on their active domain.
SN-38-CM2 is a split esterase, and shows >95% conversion to SN-38 within 5 min in vitro. SN-38-CM2 induces protein-protein interactions (PPI)-dependent esterase to mediate cell death in MDA-MB-231 cells .
Fluorescein-CM2 is a fluorogenic molecule that can be used to rapidly screen esterase cut sites for protein-protein interaction-dependent (PPI-dependent) esterase activity in E. coli .
APX2039 is an orally active and potent inhibitor of the fungal Gwt1 enzyme. APX2039 has extremely potent anticryptococcal activity against C. neoformans and C. gattii. APX2039 blocks the localization of GPI (glycosylphosphatidyl inositol)-anchored cell wall mannoproteins. APX2039 can be used for Cryptococcal meningitis (CM) research .
(-)-trans-Myrtanol is an antimicrobial and acaricide agent. (-)-trans-Myrtanol exhibits potent antimicrobial activities against harmful intestinal bacteria. (-)-trans-Myrtanol shows acaricidal activities for D. farinae, D. pteronyssinus, T. putrescentiae with LD50 values of 2.30 µg/cm2, 2.22 µg/cm2, 12.95 µg/cm2, respectively .
Egaptivon pegol (ARC1779) is an aptamer, which blocks binding of the von Willebrand Factor (VWF) to platelet GPIb receptors. Egaptivon pegol has anti-thrombotic efficacy.
Vutrisiran (ALN-TTRsc02) is a liver-directed, investigational, small interfering ribonucleic acid (siRNA) agent. Vutrisiran can be used for transthyretin (TTR)-mediated amyloidosis research .
Givosiran (ALN-AS1) is a small interfering RNA that targets hepatic aminolevulinate synthase 1 (ALAS1) messenger RNA. Givosiran downregulates ALAS1 mRNA and prevents accumulation of neurotoxic δ-aminolevulinic acid and porphobilinogen levels. Givosiran can be used for the research of acute intermittent porphyria .
Drisapersen, a antisense oligonucleotide, induces exon 51 skipping during dystrophin pre-mRNA splicing and allows synthesis of partially functional dystrophin in Duchenne muscular dystrophy (DMD) patients with amenable mutations.
Remlarsen (MRG-201), a miR-29b mimic, acts a miR-29b agonist. Remlarsen has the potential for preventiong formation of a fibrotic scar or cutaneous fibrosis .
Patisiran sodium is a double-stranded small interfering RNA that targets a sequence within the transthyretin (TTR) messenger RNA. Patisiran sodium specifically inhibits hepatic synthesis of mutant and wild-type TTR. Patisiran sodium can be used for the research of hereditary TTR amyloidosis .
Inclisiran (ALN-PCSsc) is a double-stranded small interfering RNA (siRNA) molecule that inhibits the transcription of PCSK-9. Inclisiran can be used for hyperlipidemia and cardiovascular disease (CVD) research .
Fazirsiran (ARO-AAT) is a second-generation RNAi agent. Fazirsiran consistes of a cholesterol-conjugated RNAi trigger (chol-RNAi) to selectively degrade Alpha1-antitrypsin (AAT) mRNA by RNAi and a melittin-derived peptide conjugated to N-acetylgalactosamine (NAG) formulated as the excipient EX1 to promote endosomal escape of the chol-RNAi in hepatocytes . Fazirsiran can be used in the study of Alpha-1 Antitrypsin Deficiency (AATD) liver disease.
Lumasiran sodium, an investigational RNA interference (RNAi) therapeutic agent, reduces hepatic oxalate production by targeting glycolate oxidase. Lumasiran sodium reduces urinary oxalate excretion, the cause of progressive kidney failure in primary hyperoxaluria type 1 (PH1) .
Lumasiran (ALN-G01), a siRNA product, reduces hepatic oxalate production by targeting glycolate oxidase. By silencing the gene encoding glycolate oxidase, Lumasiran depletes glycolate oxidase and thereby inhibits the synthesis of oxalate, which is the toxic metabolite that is directly associated with the clinical manifestations of Primary hyperoxaluria type 1 (PH1) .
Cemdisiran is an N-acetylgalactosamine (GalNAc) conjugated siRNA for the research of complement-mediated diseases by suppressing liver production of complement 5 (C5) protein.
Ioversol hydrolysate-1 is a hydrolyzate of Ioversol (HY-B1410), a non-ionic iodinated contrast agent (CM) used in CT scans or X-rays in animal experiments .
Ceratotoxin-1 (CcoTx1), a peptide toxin, is an voltage-gated sodium channel subtypes inhibitor. Ceratotoxin-1 inhibits Nav1.1/β1, Nav1.2/β1, Nav1.4/β1, and Nav1.5/β1 with IC50 of 523 nM, 3 nM, 888 nM, and 323 nM, respectively. Ceratotoxin-1 also inhibits Nav1.8/β1 .
Fitusiran (ALN-AT3SC), an small interfering RNA, specifically targets antithrombin (AT) messenger RNA to lower production of AT in the liver. Fitusiran increases thrombin generation and has the potential for the research of the hemophilia .
Ioversol (MP-328) is a nonionic iodinated contrast medium (CM) that is used during a CT scan or x-ray in animal experiment. Ioversol does not damage the blood-brain barrier (BBB) in animal .
5-ROX (5-Carboxy-X-rhodamine), a rhodamine dye, exhibits strong fluorescence property in aqueous buffer with the λexit of 580 nm (ε=3.6×10 4 M -1cm-1), and λemit of 604 nm (=0.94) .
m-Tolualdehyde (3-Methylbenzaldehyde) is a compound that can be isolated from Ficus carica L. and Myosotis arvensis. m-Tolualdehyde has food protective effects. m-Tolualdehyde shows acaricidal activities for Tyrophagus putrescentiae with a LD50 of 1.97 μg/cm3 .
Antitumor agent-96 (Compound D34) is a potent MRE11 inhibitor. Antitumor agent-96 down-regulates the HR pathway by binding with MRE11 and suppressing its endonuclease functions. Antitumor agent-96 induces CM cells apoptosis .
CP-312 is a potent Heme Oxygenase-1 (HO-1) inducer. CP-312 protects hiPSC-CM viability by targeting the antioxidant response network through induction of HMOX1 expression. CP-312 protects human iPSC-derived cardiomyocytes from oxidative stress .
3′-O-N3-dATP (3′-O-Azidomethyl dATP) is a modified nucleotide, which is utilized for DNA polymerase. 3′-O-N3-dATP acts as reversible terminator with enhanced raman scattering (SERS) at 2125 cm-1, which determines the DNA sequences continuously .
Dehydrotumulosic acid is one of the effective constituents of Poria cocos. Poria cocos, a popular Chinese medicinal herb of fungal origin, has been included in many combinations with other CM herbs for its traditionally claimed activities of inducing diuresis, excreting dampness, invigorating the spleen and tranquilizing the mind and its modern pharmacological use of modulating the immune system of the body .
N4-Acetyl-2'-O-methylcytidine (ac4Cm) is an RNA with dual acetylation and methoxidation modifications found in thermophilic archaea. N4-Acetyl-2'-O-methylcytidine has been implicated in the adaptability of archaea in extreme environments, enhancing RNA stability through dual modification .
Sotatercept (ACE-011) is a soluble activin receptor 2A (ACVR2A) type IgG Fc fusion protein. Sotatercept combines activin and growth differentiation factor to try to restore the balance between growth promotion and growth inhibition signal pathways. Sotatercept has potential application in pulmonary arterial hypertension, anemia, bone loss, erythropoiesis, multiple myeloma (MM) osteolytic lesions .
Antifungal agent 22 (compound D16) is a potential and orally active antifungal agent for CM (cryptococcal meningitis), with an IC50 of 0.5 μg/mL. Antifungal agent 22 can penetrate the blood-brain barrier and kill the C. neoformans H99 cells by destroying the integrity of fungal cell membranes. Antifungal agent 22 shows selective anti-Cryptococcus activity with good metabolic stability and low cytotoxicity .
Malachite Green Carbinol base (MGOH, MGCB) is a derivative of Malachite green (MG) with not fluorescence. Malachite green carbinol base (MGOH, MGCB), as a pH regulation reagent,MGCB molecule could release OH - under UV light irradiation and generate a progressive shift in pH values. MGCB solution turns from colorless to deep green rapidly when exposed to a high-pressure UV lamp (500 W, 50 W/cm) .
Cyanines are formally compounds with two nitrogen atoms linked by an odd number of methene units. 26 28 The nitrogen atoms are parts of the heterocyclic units (such as indole, benzoxazol, or benzothiazol) . The structures and optical properties of representative cyanine dyes used for in vivo imaging are presented . Cyanines are characterized by long wavelength, tunable absorption and emission, very high extinction coefficient (up to 300,000 M 1 cm 1), good water solubility, and relatively straightforward synthesis .
Dersimelagon (MT-7117) is an orally active, selective melanocortin 1 receptor (MC1R) agonist with EC50 values of 8.16, 3.91, 1.14 and 0.251 nM for human (h), cynomolgus monkey (cm), mouse (m) and rat (r) MC1R, respectively. Dersimelagon shows good affinity for hMC1R and hMC4R with Ki values of 2.26, 32.9 nM, respectively. Dersimelagon can be used for the research of skin pigmentation .
3′-O-N3-dATP trisodium (3′-O-Azidomethyl dATP trisodium) is the trisodium salt form of 3′-O-N3-dATP. 3′-O-N3-dATP trisodium is a modified nucleotide, which is utilized for DNA polymerase. 3′-O-N3-dATP trisodium acts as reversible terminator with enhanced raman scattering (SERS) at 2125 cm-1, which determines the DNA sequences continuously .
Ultevursen (QR-421a) is a single-stranded RNA based oligonucleotide that is designed to skip exon 13 in the RNA with the aim to stop vision loss in people that have retinitis pigmentosa due to a mutation in exon 13 of the USH2A gene (encoding usherin). Ultevursen sequence: (P-thio)[2′-O-(2-methoxyethyl)](A-G-m 5C-m 5U-m 5U-m 5C-G-G-A-G-A-A-A-m 5U-m 5U-m 5U-A-A-A-m 5U-m 5C) .
CellTracker CM-DiI (CM-DiI) is a lipophilic fluorochrome that can be used for tracking the migration of lymphocytes. CellTracker CM-DiI is feasible to detect labeled cells in histological sections (excitation 553 nm; emission 570 nm) .
CM-H2DCFDA is a derivative of H2DCFDA (HY-D0940). CM-H2DCFDA can be used to determine cellular oxidant levels (Ex/Em: 495/530 nm). CM-H2DCFDA is light-sensitive .
Fluorescein-CM2 is a fluorogenic molecule that can be used to rapidly screen esterase cut sites for protein-protein interaction-dependent (PPI-dependent) esterase activity in E. coli .
5-ROX (5-Carboxy-X-rhodamine), a rhodamine dye, exhibits strong fluorescence property in aqueous buffer with the λexit of 580 nm (ε=3.6×10 4 M -1cm-1), and λemit of 604 nm (=0.94) .
Cyanines are formally compounds with two nitrogen atoms linked by an odd number of methene units. 26 28 The nitrogen atoms are parts of the heterocyclic units (such as indole, benzoxazol, or benzothiazol) . The structures and optical properties of representative cyanine dyes used for in vivo imaging are presented . Cyanines are characterized by long wavelength, tunable absorption and emission, very high extinction coefficient (up to 300,000 M 1 cm 1), good water solubility, and relatively straightforward synthesis .
Nitroso-PSAP is a sensitive and specific chromogenic reagent for iron (Fe 2+), which is used for the colorimetric determination of iron in blood after mineralization with periodic acid. TNitroso-PSAP chelates with iron (Fe 2+) to produce a green complex (λmax=756 nm, Epsilon = 4.5 x 10 < sup > 4 < / sup > dm < sup > 3 < / sup > mol < sup > 1 < / sup > cm < sup > 1 < / sup >) .
Ceratotoxin-1 (CcoTx1), a peptide toxin, is an voltage-gated sodium channel subtypes inhibitor. Ceratotoxin-1 inhibits Nav1.1/β1, Nav1.2/β1, Nav1.4/β1, and Nav1.5/β1 with IC50 of 523 nM, 3 nM, 888 nM, and 323 nM, respectively. Ceratotoxin-1 also inhibits Nav1.8/β1 .
Stapokibart (CM310) is a humanised monoclonal antibody targeting IL-4Rα and efficiently blocks the interaction of cytokines IL-4 and IL-13 with their co-receptor subunit IL-4Rα. Stapokibart has the capacity to interact with IL-4Rα in humans, cynomolgus monkeys, and rats .
Sotatercept (ACE-011) is a soluble activin receptor 2A (ACVR2A) type IgG Fc fusion protein. Sotatercept combines activin and growth differentiation factor to try to restore the balance between growth promotion and growth inhibition signal pathways. Sotatercept has potential application in pulmonary arterial hypertension, anemia, bone loss, erythropoiesis, multiple myeloma (MM) osteolytic lesions .
Priliximab (CEN 000029) is an anti-CD4 humanized monoclonal antibody. Priliximab binds to CD4 on the surface of T cells, resulting in a significant and sustained reduction in circulating CD4 + T cells. Priliximab can be used in research of rheumatoid arthritis (RA) .
m-Tolualdehyde (3-Methylbenzaldehyde) is a compound that can be isolated from Ficus carica L. and Myosotis arvensis. m-Tolualdehyde has food protective effects. m-Tolualdehyde shows acaricidal activities for Tyrophagus putrescentiae with a LD50 of 1.97 μg/cm3 .
Dehydrotumulosic acid is one of the effective constituents of Poria cocos. Poria cocos, a popular Chinese medicinal herb of fungal origin, has been included in many combinations with other CM herbs for its traditionally claimed activities of inducing diuresis, excreting dampness, invigorating the spleen and tranquilizing the mind and its modern pharmacological use of modulating the immune system of the body .
Murraol (CM-c2), a coumarin, can be isolated from the leaves of Madagascar pine cork (Apiaceae). Murraol has cyclooxygenase (COX) and lipoxygenase inhibitory properties and has an inhibitory effect on the growth of cancer cells .
(-)-trans-Myrtanol is an antimicrobial and acaricide agent. (-)-trans-Myrtanol exhibits potent antimicrobial activities against harmful intestinal bacteria. (-)-trans-Myrtanol shows acaricidal activities for D. farinae, D. pteronyssinus, T. putrescentiae with LD50 values of 2.30 µg/cm2, 2.22 µg/cm2, 12.95 µg/cm2, respectively .
Envelope glycoprotein gp160 Protein (HIV-1 gp160 Protein) is the sole antigenic protein on the surface of the HIV-1 virion and mediates HIV-1 entry into target cells. The endoproteolytic processing of HIV-1 gp160 membrane glycoprotein precursor into gp120 and gp41 is necessary for formation of infectious HIV particles. HIV-1 gp160 induces endothelial cell apoptosis, which is mediated by CXCR4 chemokine receptor. envelope glycoprotein gp160 Protein, HIV-1 (ADD25380, HEK293, His) is the recombinant Virus-derived envelope glycoprotein gp160 protein, expressed by HEK293 , with C-His labeled tag. The total length of envelope glycoprotein gp160 Protein, HIV-1 (ADD25380, HEK293, His) is 473 a.a., with molecular weight of ~54.4 KDa.
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