From 11:00 pm to 12:00 pm EST ( 8:00 pm to 9:00 pm PST ) on January 6th, the website will be under maintenance. We are sorry for the inconvenience. Please arrange your schedule properly.
SMCC-DM1 (DM1-SMCC) is a agent-linker conjugate composed of a potent microtubule-disrupting agent DM1 and a linker SMCC to make antibody agent conjugate (ADC) .
DM3 (Maytansinoid DM3) is a maytansine analog bearing disulfide or thiol groups and a tubulin inhibitor, and is a cytotoxic moiety of antibody-drug conjugates (ADCs) .
DM1-SMe is an unconjugated form of the Maytansinoid in IMGN901. DM1-SMe is about 3-10-fold more potent than the parent agent Maytansine, with IC50s ranging from 0.003 to 0.01 nM for DM1-SMe in a panel of human tumor cell lines .
DM4-d6 is deuterium labeled DM4. DM4 is is an antitubulin agent that inhibit cell division. DM4 can be used in the preparation of antibody agent conjugate.
DM3-SMe is a maytansine derivative and a tubulin inhibitor, and is a cytotoxic moiety of antibody-drug conjugates (ADCs), which can be linked to antibody through disulfide bond or stable thioether bond. DM3-SMe shows highly cytotoxic activity in vitro with an IC50 of 0.0011 nM .
DM4-SMe is a metabolite of antibody-maytansin conjugates (AMCs) and a tubulin inhibitor, and also a cytotoxic moiety of antibody-drug conjugates (ADCs), which can be linked to antibody through disulfide bond or stable thioether bond. DM4-SMe inhibits KB cells with an IC50 of 0.026 nM .
DM-Nitrophen tertasodium is a Ca 2+ cage. DM-Nitrophen releases Ca 2+ when cleaved upon illumination with near-ultraviolet light . DM-Nitrophen tertasodium can be used for study of Ca 2+ signaling .
Sunifiram (DM-235) is a piperazine derived ampakine-like drug which has nootropic effects in animal studies with significantly higher potency than piracetam.
DM4-SPDP is a agent-linker conjugate composed of a potent antitubulin agent DM4 and a linker SMCC to make antibody agent conjugate . SPDP is a short-chain crosslinker for amine-to-sulfhydryl conjugation via NHS-ester and pyridyldithiol reactive groups that form cleavable (reducible) disulfide bonds with cysteine sulfhydryls .
Unifiram (DM232) is acts as a potent cognition enhancer through the activation of the AMPA-mediated neurotransmission system. Unifiram (DM232) has the potential for amnesia prevention and neurodegenerative disorder research .
DM1-(PEG)4-DBCO is a agent-linker conjugate composed of a potent microtubulin inhibitor DM1 and a linker DBCO-PEG4-Ahx to make antibody agent conjugate (ADC). Mertansine (DM1) is a microtubulin inhibitor and is an antibody-conjugatable maytansinoid that is developed to overcome systemic toxicity associated with maytansine and to enhance tumor-specific delivery. DM1-PEG4-DBCO is a click chemistry reagent, it contains a DBCO group that can undergo strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing Azide groups.
DM-01 is a powerful and selective EZH2 inhibitor for the research of diffuse large B-cell lymphoma (DLBCL), follicular lymphoma (FL), and SNF5/INI-1/SMARCB1 genetically defined solid tumors .
Mertansine (DM1) is a microtubulin inhibitor and is an antibody-conjugatable maytansinoid that is developed to overcome systemic toxicity associated with maytansine and to enhance tumor-specific delivery. Mertansine can be attached to a monoclonal antibody with a linker to create an antibody-drug conjugate (ADC) .
LDN193189 (DM-3189) (GMP) is LDN193189 (HY-12071) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. LDN193189 is selective BMP type I receptor inhibitor .
DM-PIT-1 is a PIP3/PH (phosphatidylinositol-3,4,5-triphosphate/Pleckstrin) interaction inhibitor . DM-PIT-1 has the potential for the research of ovarian cancer .
Brexpiprazole S-oxide (DM-3411) is a main metabolite of Brexpiprazole and is metabolized by cytochrome P450 3A4 (CYP3A4). Brexpiprazole is an atypical antipsychotic agent and a partial agonist of human 5-HT1A and dopamine receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM .
DM-CO-(CH2)5-SMe is an anticancer agent derived from antibody-drug conjugates (ADC) metabolite with cytotoxicity to H1703, H1975, COLO704 and Colo720E cells .
DM-β-CD (2,6-Di-O-methyl-β-cyclodextrin) is a cyclic molecule consisting of seven glucose units modified with two methyl groups at the 2- and 6-positions. It is usually used as a solubilizer and carrier for poorly soluble drugs in pharmaceutical preparations. Furthermore, it has applications in analytical chemistry, food science, and environmental remediation due to its ability to form clathrates with various guest molecules, such as aromatic compounds, pesticides, and heavy metals.
LDN193189 is a potent selective BMP type I receptor (BMP I) inhibitor. LDN-193189 efficiently inhibits transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50 values of 5 nM and 30 nM, respectively. LDN-193189 can be used for the research of bone morphogenetic protein signalling, such as fibrodysplasia ossificans progressiva .
LDN-193189 (dihydrochloride) is a potent selective BMP type I receptor (BMP I) inhibitor. LDN-193189 efficiently inhibits transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50 values of 5 nM and 30 nM, respectively. LDN-193189 can be used for the research of bone morphogenetic protein signalling, such as fibrodysplasia ossificans progressiva .
Dehydroaripiprazole (OPC-14857) is an active metabolite of Aripiprazole. Aripiprazole is an antipsychotic agent and is metabolized by CYP3A4 and CYP2D6 forming mainly Dehydroaripiprazole. Dehydroaripiprazole has with antipsychotic activity equivalent to Aripiprazole .
Dehydroaripiprazole (OPC-14857) hydrochloride is an active metabolite of Aripiprazole. Aripiprazole is an antipsychotic agent and is metabolized by CYP3A4 and CYP2D6 forming mainly Dehydroaripiprazole hydrochloride. Dehydroaripiprazole hydrochloride has with antipsychotic activity equivalent to Aripiprazole .
LDN193189 Tetrahydrochloride is a selective BMP type I receptor inhibitor, which efficiently inhibits ALK2 and ALK3 (IC50=5 nM and 30 nM, respectively), with weaker effects on ALK4, ALK5 and ALK7 (IC50≥500 nM) .
Dehydroaripiprazole (Standard) is the analytical standard of Dehydroaripiprazole. This product is intended for research and analytical applications. Dehydroaripiprazole (OPC-14857) is an active metabolite of Aripiprazole. Aripiprazole is an antipsychotic agent and is metabolized by CYP3A4 and CYP2D6 forming mainly Dehydroaripiprazole. Dehydroaripiprazole has with antipsychotic activity equivalent to Aripiprazole .
Brexpiprazole S-oxide-d8 is a deuterium labeled Brexpiprazole S-oxide. Brexpiprazole S-oxide is a main metabolite of Brexpiprazole and is metabolized by cytochrome P450 3A4 (CYP3A4). Brexpiprazole is an atypical antipsychotic agent and a partial agonist of human 5-HT1A and dopamine receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM[1][2][3].
Dehydroaripiprazole-d8 is deuterium labeled Dehydroaripiprazole. Dehydroaripiprazole (OPC-14857) is an active metabolite of Aripiprazole. Aripiprazole is an antipsychotic agent and is metabolized by CYP3A4 and CYP2D6 forming mainly Dehydroaripiprazole. Dehydroaripiprazole has with antipsychotic activity equivalent to Aripiprazole[1][2][3].
MA-PEG4-VC-PAB-DMEA-duocarmycin DM is a drug-linker conjugate for ADC by using the anticancer antibiotic Duocarmycin DM (HY-130978), linked via MA-PEG4-vc-PAB-DMEA (HY-126668) .
Lys-SMCC-DM1 (Lys-Nε-MCC-DM1) is a agent-linker conjugates for ADC that can inhibit tubulin polymerization. Lys-SMCC-DM1 is the active metabolite of T-DM1. T-DM1 is a HER2-targeting ADC with a tubulin polymerization inhibitor DM1. Lys-SMCC-DM1 can be used in the research of breast cancer .
(Rac)-Lys-SMCC-DM1 ((Rac)-Lys-Nε-MCC-DM1) is the racemate of Lys-SMCC-DM1 (HY-101982). Lys-SMCC-DM1 is a linker-payload component that has the potential to inhibit tubulin polymerization. Lys-SMCC-DM1 is the active metabolite of T-DM1 .
S-Me-DM4 is a metabolite of DM4 S-methylated by intracellular enzyme. DM4 (HY-100503) is a microtubule-depolymerizing maytansinoid with strong cytotoxicity. DM4 can be used as an ADC Cytotoxin molecule .
Duocarmycin DM, a DNA minor-groove alkylator, is an antibody agent conjugates (ADCs) toxin. Duocarmycin DM is based on its characteristic curved indole structure and a spirocyclopropylcyclohexadienone electrophile to act anticancer activity .
Ganoderic acid DM, a natural triterpenoid isolated from Ganoderma lucidum, induces DNA damage, G1 cell cycle arrest and apoptosis in human breast cancer cells. Ganoderic acid DM as a specific inhibitor of osteoclastogenesis .
SPDB-DM4 is a agent-linker conjugate for ADC by using the maytansinebased payload (DM4, a tubulin inhibitor) via a SPDB linker, exhibiting potent anti-tumor activity.
S-methyl DM1 is a thiomethyl derivative of Maytansine. S-methyl DM1 binds to tubulin with a Kd of 0.93 μM and inhibts microtubule polymerization. S-methyl DM1 potently suppresses microtubule dynamic instability and has anticancer effects .
SPP-DM1 is a agent-linker conjugate for ADC with potent antitumor activity by using DM1 (a potent microtubule-disrupting agent), linked via the ADC linker SPP .
Sulfo-PDBA-DM4 is a agent-linker conjugate composed of a potent a tubulin inhibitor DM4 and a linker Sulfo-PDBA to make antibody agent conjugate (ADC). Sulfo-PDBA is a gluthatione cleavable linker.
Duocarmycin DM free base, a DNA minor-groove alkylator, is an antibody agent conjugates (ADCs) toxin. Duocarmycin DM free base is based on its characteristic curved indole structure and a spirocyclopropylcyclohexadienone electrophile to act anticancer activity .
SC-VC-PAB-DM1 is a agent-linker conjugate for ADC with with potent antitumor activity by using DM1 (Mertansine, a tubulin inhibitor) , linked via the ADC linker SC-VC-PAB .
Tomaymycin DM, a DNA alkylator, is a derivative of Tomaymycin, it is a PBD dimer, which is attached to tumor targeting antibodies to create antibody-drug conjugates (ADCs).
Mal-VC-PAB-DM1 is a agent-linker conjugate for ADC with potent antitumor activity by using DM1 (a potent microtubule-disrupting agent), linked via the ADC linker Mal-VC-PAB .
Cantuzumab ravtansine (IMGN242; huC242-DM4), an ADC, is a humanized monoclonal antibody, huC242, covalently linked via a disulfide bond to DM4 (DM4 (HY-12454)). Cantuzumab ravtansine has broad antitumor efficacy against a range of CanAg-positive human tumor xenografts .
Lys-Nε-SPDB-DM4 is a agent-linker conjugate composed of a potent a tubulin inhibitor DM4 and a linker Lys-Nε-SPDB to make antibody agent conjugate (ADC) .
DBCO-PEG4-Ahx-DM1 is a agent-linker conjugate composed of a potent microtubulin inhibitor DM1 and a linker DBCO-PEG4-Ahx to make antibody agent conjugate (ADC). Mertansine (DM1) is a microtubulin inhibitor and is an antibody-conjugatable maytansinoid that is developed to overcome systemic toxicity associated with maytansine and to enhance tumor-specific delivery. DBCO-PEG4-Ahx-DM1 is a click chemistry reagent, it contains a DBCO group that can undergo strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing Azide groups.
Cantuzumab mertansine (SB-408075; huC242-DM1), an ADC, is an immunoconjugate of the potent maytansine derivative (DM1; HY-19792) and the humanized monoclonal antibody (huC242) directed to CanAg. Cantuzumab mertansine has cytotoxic toward colon cancer cells and has broad antitumor efficacy against a range of CanAg-positive human tumor xenografts .
Trastuzumab emtansine (Ado-Trastuzumab emtansine) is an antibody-drug conjugate (ADC) that incorporates the HER2-targeted antitumor properties of trastuzumab with the cytotoxic activity of the microtubule-inhibitory agent DM1 (derivative of maytansine). Trastuzumab emtansine can be used for the research of advanced breast cancer .
Trastuzumab emtansine (Ado-Trastuzumab emtansine) is an antibody-drug conjugate (ADC) that incorporates the HER2-targeted antitumor properties of trastuzumab with the cytotoxic activity of the microtubule-inhibitory agent DM1 (derivative of maytansine). Trastuzumab emtansine can be used for the research of advanced breast cancer .
Tusamitamab ravtansine (SAR-408701) is a targeted ADC against tumor cells expressing CEACAM5, composed of a humanized anti-CEACAM5 monoclonal antibody covalently linked to the potent cytotoxic agent, maytansinoid DM4 (HY-12454), via a cleavable linker. Tusamitamab ravtansine has an average drug-to-antibody ratio (DAR) of 3.8 .
Heptamidine dimethanesulfonate (SBi4211 dimethanesulfonate) is a potent Pentamidine-related inhibitor of the calcium-binding protein S100B (Kd=6.9 μM), selectively kills melanoma cells with S100B over those without S100B . Heptamidine is a useful tool for the investigation of Myotonic dystrophy (DM) .
RK-582 is an orally active, spiroindoline-based selective inhibitor of tankyrase. The IC50s of RK-582 against TNKS1/PARP5A and PARP1 are 36.1 nM and 18.168 nM, respectively. RK-582 inhibits rectal cancer COLO-320DM cells (GI50=0.23 μM) and significantly inhibits tumor growth in a COLO-320DM mouse xenograft model .
Izeltabart is a high-affinity humanized antibody targeting ADAM9. Izeltabart can be used as ADC Antibody for site-specific conjugation with Maytansinoid-based DM21-C (a Drug-Linker Conjugates for ADC), to synthesize IMGC936 (Antibody-Drug Conjugates (ADCs)) with strong anti-cancer activity. DM21-C is composed of Maytansinoid (microtubule inhibitor) and a stable tripeptide linker. IMGC936 exhibits cytotoxicity against ADAM9-positive human tumor cell lines and potent antitumor activity in xenograft tumor models .
α-Glucosidase-IN-22 (compound 7i), a benzimidazole, is a potent α-glucosidase inhibitor with an IC50 of 0.64 μM. α-Glucosidase-IN-22 is a potent anti-diabetic agent and has the potential for type 2 diabetes mellitus (T2DM) research .
PF-06291874 is a highly potent, non-peptide and orally active glucagon receptor antagonist. PF-06291874 is under the study for type 2 diabetes mellitus (T2DM) .
Ecnoglutide (XW003) is a long-acting, cAMP-biased glucagon-like peptide 1 (GLP-1) receptor agonist. Ecnoglutide can be used for research of T2DM and obesity .
Prucalopride succinate is an orally active, selective and specific 5-HT 4 receptor agonist (high affinity), with pKis of 8.6 and 8.1 for human 5-HT4a/4b receptors, respectively. Prucalopride succinate improves intestinal motility by promoting regeneration of the intestinal nervous system in rats. Prucalopride succinate also shows anticancer activity by blocking of the PI3K/AKT/mTor signaling pathway. Prucalopride succinate can be used in studies of chronic constipation, pseudo-intestinal obstruction and cancer .
Retagliptin phosphate (SP2086 phosphate) is a selective, competitive and orally active dipeptidyl peptidase-4 (DPP-4) inhibitor. Retagliptin phosphate can be used for type 2 diabetes mellitus (T2DM) research .
Retagliptin (SP2086) is a selective, competitive and orally active dipeptidyl peptidase-4 (DPP-4) inhibitor. Retagliptin can be used for type 2 diabetes mellitus (T2DM) research .
SSTR5 antagonist 2 hydrochloride is a highly potent, oral active and selective somatostatin (receptor) subtype 5 (SSTR5) antagonist and has potential for the research of type 2 diabetes mellitus (T2DM) .
Lotiglipron (PF-07081532) is an orally active GLP-1R agonist. Lotiglipron reduces glucose and body weight, and can be used for research of Type 2 diabetes mellitus (T2DM) .
Rongliflozin (DJT1116PG) is a selective and orally active inhibitor of sodium-glucose co-transporter-2 (SGLT-2). Rongliflozin can be used for the research of type 2 diabetes mellitus (T2DM) .
Cryptophycin analog 1 is an ADC payload. Cryptophycin analog 1 shows anticancer activity. Cryptophycin analog 1 displays cell activity an order of magnitude more potent than approved ADC payloads MMAE and DM1 .
SSTR5 antagonist 2 (compound 10) is a highly potent, oral active and selective somatostatin (receptor) subtype 5 (SSTR5) antagonist and has potential for the research of treat type 2 diabetes mellitus (T2DM) .
SSTR5 Antagonist 1 (compound 10) is a highly potent, oral active and selective somatostatin (receptor) subtype 5 (SSTR5) antagonist and has potential for the research of treat type 2 diabetes mellitus (T2DM) .
α-Glucosidase-IN-38 (Compound 11j) is a potent inhibitor of α-glucosidase inhibitor with IC50 of 12.44±0.38 μM.α-Glucosidase-IN-38 plays an important role in Diabetes mellitus (DM) .
Trelagliptin (SYR-472) is a potent, orally active and highly selective DPP-4 inhibitor with an IC50 of 4 nM. Trelagliptin succinate improves glycemic control in vivo and can be used for the study of type 2 diabetes mellitus (T2DM) .
AMG131 (INT131), a potent and highly selective PPARγ partial agonist, binds to PPARγ and displaces Rosiglitazone with a Ki of ~10 nM. AMG131 can be used for research of type-2 diabetes mellitus (T2DM) .
Anticancer agent 149 (compound 3) is an anticancer agent isolated from the rhizome of Dioscorea dioscorea (DM). Anticancer agent 149 exhibits selective cytotoxic activity against MCF-7 cells (IC50=31.41 μM) .
Trelagliptin (SYR-472) succinate is a potent, orally active and highly selective DPP-4 inhibitor with an IC50 of 4 nM. Trelagliptin succinate improves glycemic control in vivo and can be used for the study of type 2 diabetes mellitus (T2DM) .
Luseogliflozin (TS 071) hydrate is a selective potent and orally active second-generation sodium-glucose co-transporter 2 (SGLT2) inhibitor with an IC50 of 2.26 nM. Luseogliflozin hydrate can be used for the research of type 2 diabetes mellitus (T2DM) .
GSK-1292263 is an orally available GPR119 agonist with pEC50s of 6.9 and 6.7 for human and rat GPR119, respectively. GSK-1292263 can be used for the research of type 2 diabetes mellitus (T2DM) .
OM-1700 is a potent tankyrase inhibitor with IC50s of 127 and 14 nM for tankyrase 1 and tankyrase 2, respectively. OM-1700 reduces cell growth in the colon cancer cell line COLO 320DM (GI50=650 nM) .
Cofrogliptin (HSK7653) (compound 2), a tetrahydropyran derivative, is a potent oral dipeptidyl aminopeptidase 4 (DPP-4) inhibitor with Long-acting antidiabetic efficacy. Cofrogliptin (compound 2) has a great potential for type 2 diabetes mellitus (T2DM) .
α-Glucosidase-IN-26 (Compound 7i) is an α-glucosidase inhibitor (IC50=4.63 µM). α-Glucosidase-IN-26 can be used in the study of type 2 diabetes mellitus (T2DM) .
Glucagon receptor antagonists-5 (compound 13K) is a potent and orally bioavailable indazole-based glucagon receptor antagonist (Ki=32 nM). Glucagon receptor antagonists-5 has potential for the treatment of type 2 diabetes mellitus (T2DM) .
Dapagliflozin (BMS-512148), a new type of agent used to treat diabetes mellitus (DM), is a competitive sodium/glucose cotransporter 2 (SGLT2) inhibitor, which results in excretion of glucose into the urine . Dapagliflozin induces HIF1 expression and attenuates renal IR injury .
Fazpilodemab (BFKB8488A) is a humanized, agonistic, bispecific antibody targeting fibroblast growth factor receptor 1c (FGFR1c) and Klothoβ. Fazpilodemab can be used for the research of type 2 diabetes mellitus (T2DM) or nonalcoholic fatty liver disease (NAFLD) .
Beta-Sitosterol (purity>75%) is a phytosterol with oral activity. Beta-Sitosterol (purity>75%) interferes with a variety of cell signaling pathways, including the cell cycle, apoptosis and cell proliferation. Beta-Sitosterol (purity>75%) has anti-inflammatory, antioxidant, and antitumor activities .
Heptamidine (SBi4211) is a potent Pentamidine-related inhibitor of the calcium-binding protein S100B (Kd=6.9 μM), selectively kills melanoma cells with S100B over those without S100B . Heptamidine is a useful tool for the investigation of Myotonic dystrophy (DM) .
GLP-1 receptor agonist 10 (compound 42) is an agonist of GLP Receptor. GLP-1 receptor agonist 10 inhibits food intake and reduces glucose excursion in mice. GLP-1 receptor agonist 10 can be used in the study of type 2 diabetes (T2DM) and obesity .
OPC-163493 is an orally active liver-targeted mitochondrial uncoupling agent. OPC-163493 reduces Δψ and mitochondrial ROS production. OPC-163493 has antidiabetic and cardiovascular beneficial effects. OPC-163493 lowers blood pressure, extends survival, and improves renal function in the rat model of stroke/hypertension .
Mirvetuximab soravtansine (IMGN853) is an antibody drug-conjugate (ADC) consisting of the cytotoxic maytansinoid, DM4, covalently linked to the humanized monoclonal antibody M9346A. Mirvetuximab soravtansine selectively binds to folate receptor 1 (FOLR1). Mirvetuximab soravtansine has an anti-proliferative effect via growth arrest and augmented DNA damage .
Mirvetuximab soravtansine (IMGN853) solution is an antibody drug-conjugate (ADC) consisting of the cytotoxic maytansinoid, DM4, covalently linked to the humanized monoclonal antibody M9346A. Mirvetuximab soravtansine selectively binds to folate receptor 1 (FOLR1). Mirvetuximab soravtansine has an anti-proliferative effect via growth arrest and augmented DNA damage .
α-Glucosidase-IN-55 (Compound 8g) is an orally active and competitive alpha-glucosidase inhibitor, with IC50 and Ki values of 12.1 and 9.66 µM, respectively. α-Glucosidase-IN-55 can be used for the research into type 2 diabetes mellitus (T2DM) to improve blood sugar control and metabolic health .
LY2922470 is a potent, selective and orally available agonist of the G protein-coupled receptor 40 (GPR40), with EC50s of 7 nM, 1 nM and 3 nM for human GPR40, mouse GPR40 and rat GPR40, respectively. LY2922470 reduces glucose levels along with significant increases in insulin and GLP-1, is potential for the treatment of type 2 diabetes mellitus (T2DM) .
OM-153 is a potent and orally active tankyrase inhibitor with IC50s of 13 nM and 2 nM for tankyrase 1 and tankyrase 2 (TNKS1/2), respectively. OM-153 inhibits luciferase-based Wnt/β-catenin signaling reporter activity with an IC50 value of 0.63 nM. OM-153 shows inhibition of Wnt/β-catenin signaling and proliferation in COLO 320DM .
DS45500853 is an estrogen-related receptor α (ERRα) agonist. DS45500853 inhibits the binding between receptor-interacting protein 140 (RIP140) corepressor peptide (10 nM) and GST-ERRα ligand-binding domain (LBD; 1.2 μM) with an IC50 value of 0.80 μM. DS45500853 can be used for the research of metabolic disorders, including type 2 diabetes mellitus (T2DM) .
DS20362725 is an estrogen-related receptor α (ERRα) agonist. DS20362725 inhibits the binding between receptor-interacting protein 140 (RIP140) corepressor peptide (10 nM) and GST-ERRα ligand-binding domain (LBD; 1.2 μM) with an IC50 value of 0.6 μM. DS20362725 can be used for the research of metabolic disorders, including type 2 diabetes mellitus (T2DM) .
Vincamine is a monoterpenoid indole alkaloid extracted from the Madagascar periwinkle. Vincamine is a peripheral vasodilator and exerts a selective vasoregulator action on the brain microcapilar circulation . Vincamine is a GPR40 agonist and acts as a β-cell protector by ameliorating β-cell dysfunction and promoting glucose-stimulated insulin secretion (GSIS). Vincamine improves glucose homeostasis in vivo, and has the potential for the type 2 diabetes mellitus (T2DM) research .
INCB13739 is an orally active, potent, selective and tissue-specific11β-HSD1 (11β-hydroxysteroid dehydrogenase 1) inhibitor, with IC50 values of 3.2 nM (11β-HSD1 enzymatic) and 1.1 nM (11β-HSD1 PBMC), respectively. INCB13739 can be used for type 2 diabetes mellitus (T2DM) and obesity research .
GSK256073 is a potent, selective and orally active GPR109A agonist and a long-lasting and non-flushing HCA2 full agonist with a pEC50 of 7.5 (human HCA2). GSK256073 acutely improves glucose homeostasis via inhibition of lipolysis and has the potential for the study of type 2 diabetes mellitus (T2DM)and dyslipidemia . GPR109A: G-protein coupled receptor 109A; HCA2: hydroxy-carboxylic acid receptor 2
Dapagliflozin ((2S)-1,2-propanediol, hydrate) is the S-enantiomer of Dapagliflozin 1,2-propanediol, hydrate. Dapagliflozin ((2S)-1,2-propanediol, hydrate), a new type of agent used to treat diabetes mellitus (DM), is a competitive sodium/glucose cotransporter 2 (SGLT2) inhibitor, which results in excretion of glucose into the urine . Dapagliflozin ((2S)-1,2-propanediol, hydrate) induces HIF1 expression and attenuates renal IR injury .
α-Glucosidase-IN-36 (compound 5g) is a potent α-glucosidase inhibitor, with an IC50 of 6.69 ± 0.18 μM, Ki and Kis of 1.65 μM and 4.54 μM, respectively. α-Glucosidase-IN-36 may inhibit α-glucosidase activity by binding with its active site as well as changing the secondary structure of α-glucosidase. α-Glucosidase-IN-36 can be used for type 2 diabetes mellitus (T2DM) research .
PF-07238025 is a BCKDC kinase (BDK) inhibitor (EC50=19 nM). PF-07238025 stabilizes the interaction between BDK and BCKDH core subunit E2 and prevents phosphorylation of E1. While BDK mediates branched-chain ketoacid dehydrogenase (BCKDH) phosphorylation, and inhibition of BCKDH is involved in controlling the rate-limiting step of branched-chain amino acid (BCAA) degradation. Impaired BCAA catabolism has been associated with several diseases, particularly cardiometabolic diseases, including heart failure (HF), type 2 diabetes mellitus (T2DM), non-alcoholic fatty liver disease (NAFLD), and obesity. PF-07238025 improved cardiometabolic endpoints and improves glucose tolerance in mice .
PF-07247685 is a BCKDC kinase (BDK) inhibitor (EC50=2.2 nM). PF-07247685 stabilizes the interaction between BDK and BCKDH core subunit E2 and prevents phosphorylation of E1. While BDK mediates branched-chain ketoacid dehydrogenase (BCKDH) phosphorylation, and inhibition of BCKDH is involved in controlling the rate-limiting step of branched-chain amino acid (BCAA) degradation. Impaired BCAA catabolism has been associated with several diseases, particularly cardiometabolic diseases, including heart failure (HF), type 2 diabetes mellitus (T2DM), non-alcoholic fatty liver disease (NAFLD), and obesity. PF-07247685 improved cardiometabolic endpoints and improves glucose tolerance in mice .
PTP1B/AKR1B1-IN-2 (Compound 7f) is a dual PTP1B/AKR1B1 inhibitor (IC50s: 3.2 and 2.1 μM, Kis: 4.0 and 0.9μM). PTP1B/AKR1B1-IN-2 is an insulin-mimetic agent. PTP1B/AKR1B1-IN-2 improves glucose uptake in murine C2C12 myoblasts. PTP1B/AKR1B1-IN-2 can be used for research of Type 2 diabetes mellitus (T2DM) .
PTP1B/AKR1B1-IN-1 is a dual inhibitor of protein tyrosine phosphatase 1B (PTP1B) and aldose reductase (AKR1B1), with IC50s of 0.06 μM and 4.3 μM, respectively. PTP1B/AKR1B1-IN-1 also inhibits TC-PTP with an IC50 value of 9 μM. PTP1B/AKR1B1-IN-1 serves as an insulin-mimetic agent in murine myoblasts, and reduces AKR1B1-dependent sorbitol accumulation. PTP1B/AKR1B1-IN-1 inhibits development of type 2 diabetes mellitus (T2DM) to control blood glucose levels .
LDN193189 (DM-3189) (GMP) is LDN193189 (HY-12071) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. LDN193189 is selective BMP type I receptor inhibitor .
DM-β-CD (2,6-Di-O-methyl-β-cyclodextrin) is a cyclic molecule consisting of seven glucose units modified with two methyl groups at the 2- and 6-positions. It is usually used as a solubilizer and carrier for poorly soluble drugs in pharmaceutical preparations. Furthermore, it has applications in analytical chemistry, food science, and environmental remediation due to its ability to form clathrates with various guest molecules, such as aromatic compounds, pesticides, and heavy metals.
LDN193189 (DM-3189) (GMP) is LDN193189 (HY-12071) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. LDN193189 is selective BMP type I receptor inhibitor .
3-Hydroxypalmitoylcarnitine (3-Hydroxyhexadecanoylcarnitine) is an acylcarnitine. Elevated levels of 3-Hydroxypalmitoylcarnitine are associated with cardiovascular disease (CVD) in type 2 diabetes mellitus (T2DM) .
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 >) .
Ecnoglutide (XW003) is a long-acting, cAMP-biased glucagon-like peptide 1 (GLP-1) receptor agonist. Ecnoglutide can be used for research of T2DM and obesity .
Cantuzumab ravtansine (IMGN242; huC242-DM4), an ADC, is a humanized monoclonal antibody, huC242, covalently linked via a disulfide bond to DM4 (DM4 (HY-12454)). Cantuzumab ravtansine has broad antitumor efficacy against a range of CanAg-positive human tumor xenografts .
Tusamitamab ravtansine (SAR-408701) is a targeted ADC against tumor cells expressing CEACAM5, composed of a humanized anti-CEACAM5 monoclonal antibody covalently linked to the potent cytotoxic agent, maytansinoid DM4 (HY-12454), via a cleavable linker. Tusamitamab ravtansine has an average drug-to-antibody ratio (DAR) of 3.8 .
Izeltabart is a high-affinity humanized antibody targeting ADAM9. Izeltabart can be used as ADC Antibody for site-specific conjugation with Maytansinoid-based DM21-C (a Drug-Linker Conjugates for ADC), to synthesize IMGC936 (Antibody-Drug Conjugates (ADCs)) with strong anti-cancer activity. DM21-C is composed of Maytansinoid (microtubule inhibitor) and a stable tripeptide linker. IMGC936 exhibits cytotoxicity against ADAM9-positive human tumor cell lines and potent antitumor activity in xenograft tumor models .
Tusamitamab is an IgG1 monoclonal antibody that targets CEACAM5. Tusamitamab can be used to synthesize Tusamitamab ravtansine (SAR408701), which is a first-in-class humanized antibody-drug conjugate (ADC) that combines Tusamitamab and DM4 (a potent maytansine derivative) .
Cantuzumab mertansine (SB-408075; huC242-DM1), an ADC, is an immunoconjugate of the potent maytansine derivative (DM1; HY-19792) and the humanized monoclonal antibody (huC242) directed to CanAg. Cantuzumab mertansine has cytotoxic toward colon cancer cells and has broad antitumor efficacy against a range of CanAg-positive human tumor xenografts .
Fazpilodemab (BFKB8488A) is a humanized, agonistic, bispecific antibody targeting fibroblast growth factor receptor 1c (FGFR1c) and Klothoβ. Fazpilodemab can be used for the research of type 2 diabetes mellitus (T2DM) or nonalcoholic fatty liver disease (NAFLD) .
Ganoderic acid DM, a natural triterpenoid isolated from Ganoderma lucidum, induces DNA damage, G1 cell cycle arrest and apoptosis in human breast cancer cells. Ganoderic acid DM as a specific inhibitor of osteoclastogenesis .
Beta-Sitosterol (purity>75%) is a phytosterol with oral activity. Beta-Sitosterol (purity>75%) interferes with a variety of cell signaling pathways, including the cell cycle, apoptosis and cell proliferation. Beta-Sitosterol (purity>75%) has anti-inflammatory, antioxidant, and antitumor activities .
Vincamine is a monoterpenoid indole alkaloid extracted from the Madagascar periwinkle. Vincamine is a peripheral vasodilator and exerts a selective vasoregulator action on the brain microcapilar circulation . Vincamine is a GPR40 agonist and acts as a β-cell protector by ameliorating β-cell dysfunction and promoting glucose-stimulated insulin secretion (GSIS). Vincamine improves glucose homeostasis in vivo, and has the potential for the type 2 diabetes mellitus (T2DM) research .
Anticancer agent 149 (compound 3) is an anticancer agent isolated from the rhizome of Dioscorea dioscorea (DM). Anticancer agent 149 exhibits selective cytotoxic activity against MCF-7 cells (IC50=31.41 μM) .
PF-07238025 is a BCKDC kinase (BDK) inhibitor (EC50=19 nM). PF-07238025 stabilizes the interaction between BDK and BCKDH core subunit E2 and prevents phosphorylation of E1. While BDK mediates branched-chain ketoacid dehydrogenase (BCKDH) phosphorylation, and inhibition of BCKDH is involved in controlling the rate-limiting step of branched-chain amino acid (BCAA) degradation. Impaired BCAA catabolism has been associated with several diseases, particularly cardiometabolic diseases, including heart failure (HF), type 2 diabetes mellitus (T2DM), non-alcoholic fatty liver disease (NAFLD), and obesity. PF-07238025 improved cardiometabolic endpoints and improves glucose tolerance in mice .
DMPK is a non-receptor serine/threonine protein kinase that is critical for skeletal muscle integrity, affecting myocyte differentiation, nuclear membrane integrity, and muscle-specific gene expression. It may inhibit myosin phosphatase (PPP1R12A), regulate myosin phosphorylation and affect cardiac contractility and conduction. DMPK Protein, Human (Sf9) is the recombinant human-derived DMPK protein, expressed by Sf9 insect cells , with tag free. The total length of DMPK Protein, Human (Sf9) is 629 a.a., .
DMPK is a non-receptor serine/threonine protein kinase that is critical for skeletal muscle integrity, affecting myocyte differentiation, nuclear membrane integrity, and muscle-specific gene expression. It may inhibit myosin phosphatase (PPP1R12A), regulate myosin phosphorylation and affect cardiac contractility and conduction. DMPK Protein, Human (Sf9, His) is the recombinant human-derived DMPK protein, expressed by Sf9 insect cells , with N-6*His labeled tag. The total length of DMPK Protein, Human (Sf9, His) is 629 a.a., .
CYP51 Proteinas is a sterol 14α-demethylase that acts with an unknown physiological substrate and accepts electrons from the iron-sulfur ferredoxin Fdx. In vitro, it catalyzes the C14-demethylation of lanosterol, 24,25-dihydrolanosterol, and obtanyol, showing stereoselectivity in producing 8,14-diene. CYP51 Protein, Mycobacterium tuberculosis (Baculovirus, His-Myc) is the recombinant CYP51 protein, expressed by Sf9 insect cells , with N-10*His, C-Myc labeled tag. The total length of CYP51 Protein, Mycobacterium tuberculosis (Baculovirus, His-Myc) is 451 a.a., with molecular weight of ~54.8 kDa.
ERG11 Proteinas is a sterol 14α-demethylase, a key enzyme in the ergosterol biosynthetic pathway, particularly in the late pathway that occurs in the endoplasmic reticulum membrane. ERG11 catalyzes the three-step removal of the 14α-methyl group from lanosterol, releasing it as a formate, resulting in the conversion of the sterol into a key intermediate in ergosterol biosynthesis. ERG11 Protein, Saccharomyces cerevisiae (GST) is the recombinant ERG11 protein, expressed by E. coli , with N-GST labeled tag. The total length of ERG11 Protein, Saccharomyces cerevisiae (GST) is 20 a.a., with molecular weight of ~29.1 kDa.
DM4-d6 is deuterium labeled DM4. DM4 is is an antitubulin agent that inhibit cell division. DM4 can be used in the preparation of antibody agent conjugate.
Brexpiprazole S-oxide-d8 is a deuterium labeled Brexpiprazole S-oxide. Brexpiprazole S-oxide is a main metabolite of Brexpiprazole and is metabolized by cytochrome P450 3A4 (CYP3A4). Brexpiprazole is an atypical antipsychotic agent and a partial agonist of human 5-HT1A and dopamine receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM[1][2][3].
Dehydroaripiprazole-d8 is deuterium labeled Dehydroaripiprazole. Dehydroaripiprazole (OPC-14857) is an active metabolite of Aripiprazole. Aripiprazole is an antipsychotic agent and is metabolized by CYP3A4 and CYP2D6 forming mainly Dehydroaripiprazole. Dehydroaripiprazole has with antipsychotic activity equivalent to Aripiprazole[1][2][3].
Ravtansine (DM4) is a maytansinoid, a chemical derivative of maytansine being investigated as the cytotoxic payload of a number of antibody-drug conjugates (ADCs). Microtubules are dynamic cytoskeletal polymers that switch stochastically between states of growing and shortening, called “dynamic instability”. They function in the precise segregation of chromosomes during cell division, transport of cellular cargos, and positioning and movement of intracellular organelles. Inhibition of microtubule function leads to cell cycle arrest and cell death. Microtubule-targeted drugs including the Vinca alkaloids, taxanes, and epothilones suppress the dynamic instability of microtubules, induce mitotic arrest, inhibit cell proliferation and induce apoptosis. The anticancer properties of maytansinoids have been attributed to their ability to disrupt microtubule function. The maytansinoid emtansine (DM1), for example, binds at the ends of microtubules and thereby suppress their dynamic instability. It is synthesized in order to link maytansinoids to antibodies via disulfide bonds. Maytansinoids inhibit tubulin polymerization and microtubule assembly and enhance microtubule destabilization, so there is potent suppression of microtubule dynamics resulting in a mitotic block and subsequent apoptotic cell death. DM4 can be used in the preparation of antibody drug conjugate. Although S-methyl DM1 and S-methyl DM4 inhibited microtubule assembly more weakly than maytansine, they suppressed dynamic instability more strongly than maytansine. Like vinblastine, the maytansinoids potently suppress microtubule dynamic instability by binding to a small number of high affinity sites, most likely at microtubule ends. Thus, the maytansine derivatives that result from cellular metabolism of the antibody conjugates are themselves potent microtubule poisons, interacting with microtubules as effectively as or more effectively than the parent molecule.
DM1 Antibody (YA898) is an unconjugated, mouse-derived, anti-DM1 (YA898) monoclonal antibody. DM1 Antibody (YA898) can be used for: ELISA, Sandwich ELISA, Competitive ELISA expriments in background without labeling.
Human(predicted: Mouse, Rat, Chicken, Dog, Pig, Cow, Horse, Rabbit)
CD166 Antibody is an unconjugated, approximately 62 kDa, rabbit-derived, anti-CD166 polyclonal antibody. CD166 Antibody can be used for: WB, ELISA, IHC-F, Flow-Cyt, IF expriments in human, and predicted: mouse, rat, chicken, dog, pig, cow, horse, rabbit background without labeling.
DM1-(PEG)4-DBCO is a agent-linker conjugate composed of a potent microtubulin inhibitor DM1 and a linker DBCO-PEG4-Ahx to make antibody agent conjugate (ADC). Mertansine (DM1) is a microtubulin inhibitor and is an antibody-conjugatable maytansinoid that is developed to overcome systemic toxicity associated with maytansine and to enhance tumor-specific delivery. DM1-PEG4-DBCO is a click chemistry reagent, it contains a DBCO group that can undergo strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing Azide groups.
DBCO-PEG4-Ahx-DM1 is a agent-linker conjugate composed of a potent microtubulin inhibitor DM1 and a linker DBCO-PEG4-Ahx to make antibody agent conjugate (ADC). Mertansine (DM1) is a microtubulin inhibitor and is an antibody-conjugatable maytansinoid that is developed to overcome systemic toxicity associated with maytansine and to enhance tumor-specific delivery. DBCO-PEG4-Ahx-DM1 is a click chemistry reagent, it contains a DBCO group that can undergo strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing Azide groups.
Inquiry Online
Your information is safe with us. * Required Fields.