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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
5209 Results for "
phytotoxic effect
" in MedChemExpress (MCE) Product Catalog:
Products (5209)
5209 Results for "phytotoxic effect" in MCE Product Catalog:
Cat. No.: HY-109056R
CAS No.: 868046-19-9
Synonyms: R-1206 (Standard)
Elsulfavirine (Standard) is the analytical standard of Elsulfavirine (HY-109056). This product is intended for research and analytical applications. Elsulfavirine (R-1206) is an orally active human carbonic anhydrase (carbonic anhydrase, CA) inhibitor and an allosteric inhibitor of HIV-1 non-nucleoside reverse transcriptase (NNRT). Elsulfavirine also targets and blocks the interaction between adenylosuccinate lyase (ADSL) and insulin-induced gene proteins INSIG1/2, blocks SREBP-1-mediated de novo lipid synthesis, and inhibits the proliferation of liver cancer cells. The combination of Elsulfavirine and Lenvatinib (HY-10981) produces a synergistic anti-tumor effect. Elsulfavirine is converted into the active metabolite VM1500A in vivo, blocks the DNA polymerase activity of reverse transcriptase, and inhibits HIV-1 replication. Elsulfavirine exhibits a Ki of 1960 nM-52400 nM against human carbonic anhydrase isoforms including I, VII, VI, VA, VB, IX, XIII, XIV. Elsulfavirine is used in studies related to HIV-1 infection and liver cancer .
Cat. No.: HY-111527R
CAS No.: 896203-18-2
Target:
Research Areas:
PPZ2 (Standard) is the analytical standard of PPZ2 (HY-111527). This product is intended for research and analytical applications. PPZ2 is a diacylglycerol (DAG)-activated TRPC3/TRPC6/TRPC7 channel activator with activity in promoting neuronal development and survival. PPZ2 activates recombinant TRPC3/TRPC6/TRPC7 channels in a dose-dependent manner without affecting other TRPC channels. PPZ2 elicits cation currents and calcium ion (Ca(2+)) influx in cultured central neurons. PPZ2 is able to induce BDNF-like neurite outgrowth and neuroprotection, an effect that disappears after TRPC3/TRPC6/TRPC7 knocKdown or inhibition. PPZ2 also increases the activation of the calcium-dependent transcription factor cAMP response element binding protein. The effects of PPZ2 suggest that calcium signaling mediated by activation of DAG-activated TRPC channels plays an important role in its neurotrophic effects .
Cat. No.: HY-112624B
CAS No.: 9004-54-0
Synonyms: Dextran 70; Dextran D70; Dextran T70(MW 64000-76000)
Cat. No.: HY-125535
CAS No.: 1290069-19-0
Research Areas:
OSU-53 is an orally active AMPK activator and mTOR inhibitor, with an IC50 of 0.3 μM for AMPK, an EC50 of 2-5 μM for AMPK, and an IC50 of 8.23 μM for mTOR. OSU-53 inhibits the Akt signaling pathway, directly activates AMPK by binding to its autoinhibitory domain, reduces IKKβ-mediated phosphorylation of Foxo3a, blocks Akt-mediated phosphorylation of MDM2, and promotes the nuclear localization and stabilization of Foxo3a, while directly inhibiting mTOR. OSU-53 inhibits epithelial-mesenchymal transition (EMT), induces epithelial phenotype, suppresses invasion and metastasis, induces autophagy, inhibits the activation of ERK and Akt, reduces the secretion of nitric oxide and proinflammatory cytokines, and inhibits the migration of MDSC; at high doses, it induces MDSC apoptosis, attenuates the immunosuppressive effect of MDSC, reduces MDSC levels, and blocks incision-induced mechanical hyperalgesia. OSU-53 can be used in studies related to breast cancer, prostate cancer, thyroid cancer, melanoma and postoperative pain .
Cat. No.: HY-130046R
CAS No.: 547-81-9
Synonyms: 16-epi-Estriol (Standard); 16β,17β-Estriol (Standard)
Research Areas:
16-Epiestriol (Standard) is the analytical standard of 16-Epiestriol (HY-130046). This product is intended for research and analytical applications. 16-Epiestriol (16-epi-Estriol; 16β,17β-Estriol) is a natural stereoisomer of estriol and an anti-inflammatory agent that targets UGT. The Ki values of 16-Epiestriol against human UGT1A10 and UGT2B7 are 98.1 μM and 162 μM, respectively. As a glucuronidation substrate, 16-Epiestriol can be modified at the 3-OH, 16-OH and 17-OH sites by various UGT enzymes; in liver microsomes, the modification mainly occurs at the 16-OH and 17-OH sites, while reactions take place at all three sites in intestinal microsomes. 16-Epiestriol acts on the phase II inflammatory process by blocking edema mediated by prostaglandins and leukocyte infiltration. It lacks glycogenic activity or any effect on blood glucose levels, and serves as an important candidate molecule in the research of inflammatory diseases .
Cat. No.: HY-164919
CAS No.: 2847102-44-5
Synonyms: XMT-2056
Research Areas:
Calotatug ginistinag (XMT-2056) is an antibody-drug conjugate (ADC) targeting HER2, linked to a payload composed of XMT-1519 conjugate-1 (HY-148067) and STING agonist-20 (HY-148068). Calotatug ginistinag activates the STING signaling pathway in tumor cells and tumor-resident immune cells, induces the production of type I interferons and cytokines (CXCL10, IFN-β, IL-6, TNF-α, triggers innate anti-tumor immune responses, and exerts a bystander effect. Calotatug ginistinag exhibits efficacy against HER2-expressing cancer cells in co-culture with PBMCs. Calotatug ginistinag induces tumor regression and reduces systemic inflammation in various tumor models. Combination treatment with Calotatug ginistinag, Trastuzumab (HY-P9907) and T-DXd (HY-138298) yields benefits. Calotatug ginistinag can be used in studies related to HER2-expressing solid tumors such as breast cancer, gastric cancer and ovarian cancer .
Cat. No.: HY-177578
Research Areas:
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].
Cat. No.: HY-178858
Research Areas:
PROTAC FLT3/CHK1 Degrader-1 is a PROTAC FLT3/CHK1 degrader, with DC50 values of 5.88 nM (FLT3) and 4.17 nM (CHK1), respectively. PROTAC FLT3/CHK1 Degrader-1 can inhibit the phosphorylation of FLT3 downstream signaling effectors STAT5 (Tyr694), AKT (Ser473), and ERK (Tyr204), downregulate the protein level of c-Myc and maintain the expression of p53 protein. PROTAC FLT3/CHK1 Degrader-1 induces Apoptosis in cells. PROTAC FLT3/CHK1 Degrader-1 shows significant anti-tumor efficacy in mice bearing MV-4-11 subcutaneous xenografts. PROTAC FLT3/CHK1 Degrader-1 can be used for the study of acute myeloid leukemia (AML) .
Cat. No.: HY-188129
CAS No.: 2889348-10-9
Target:
Research Areas:
GLP-1R modulator-2 is a GLP-1R positive allosteric modulator with an EC50 of 106 nM. GLP-1R modulator-2 simultaneously binds to the extracellular pocket of GLP-1R and the peptide ligand GLP-1 (9-36) through a molecular glue-like allosteric effect, and selectively enhances GLP-1 (9-36)-induced G protein-dependent cAMP signaling. When used in combination with GLP-1 (9-36) under high-glucose conditions, GLP-1R modulator-2 enhances glucose-dependent insulin secretion in wild-type rat pancreatic islets. GLP-1R modulator-2 exhibits strong probe dependence and significantly potentiates the activity of GLP-1 (9-36). GLP-1R modulator-2 can be used for research on type 2 diabetes and obesity .
Cat. No.: HY-N0442R
CAS No.: 84272-85-5
Synonyms: 4'-O-β-D-Glucosyl-5-O-methylvisamminol (Standard)
Cat. No.: HY-P1341
CAS No.: 343268-91-7
Synonyms: Orexin A (17-33) (human, mouse, rat, bovine)
Research Areas:
Category:
Umbelliferae Extract Rudbeckia laciniata L. Ketones, Aldehydes, Acids Plants Endogenous metabolite
Target:
Cat. No.: HY-L174
276 compounds
Macrophages are effector cells of the innate immune system, engulfing bacteria and secreting pro-inflammatory and antibacterial mediators. They are an important component of the first line defense against pathogens and tumor cells. In addition, macrophages play an important role in eliminating damaged cells through programmed cell death. Like all immune cells, macrophages originate from pluripotent hematopoietic stem cells in the bone marrow. Macrophages play key functions in many physiological processes beyond homeostasis and innate immunity, including metabolic function, cell debris clearance, tissue repair, and remodeling. In order to fulfill their different functional roles, macrophages can polarize into a series of phenotypes, including classic (pro inflammatory, M1) and alternative (anti-inflammatory, healing promoting, M2) activation states, as well as a wide range of regulatory phenotypes and subtypes. Macrophages exist in all vertebrate tissues and have a dual function in host protection and tissue damage, maintaining a good balance.
MCE designs a unique collection of 276 macrophage related compounds. It is a good tool to be used for research on Inflammation, cancer and other diseases.
Cat. No.: HY-L136
1,525 compounds
Coagulation, also known as clotting, is the process in which blood changes from a liquid to a solid gel to form a blood clot. Thrombin, which is accurately and evenly generated in the injured part of blood vessels, is a key effector enzyme of the blood coagulation system and participates in many important biological processes, such as platelet activation, fibrinogen conversion to fibrin network, coagulation feedback amplification, etc. At the same time, to avoid the accidental formation of thrombus in the body, there is also an anticoagulant mechanism that inhibits blood coagulation.
Normal coagulation mechanism represents a balance between the pro-coagulant pathway in the injured site and anti-coagulant pathway beyond it. The blood coagulation system may be out of balance during the perioperative period or critical illness, which may lead to thrombosis or excessive bleeding. Therefore, the physiological study of coagulation balance is an important basis for clinical diagnosis and treatment of the abnormal coagulation process.
MCE supplies a unique collection of 1,525 compounds targeting key proteins in coagulation and anti-coagulation system. MCE Coagulation and Anti-coagulation Compound Library is a useful tool for study the mechanism of coagulation and anticoagulation.
Cat. No.: HY-L170
258 compounds
An emerging drug design method is based on the secondary binding site effect, where small molecule drugs are designed to bind to secondary binding sites on target biomolecules rather than primary orthomorphic sites. Successful potential drugs (known as allosteric modulators) will be able to bind to allosteric sites and remotely alter (or modify) the conformation of the main orthosteric binding sites of biological targets. Allosteric modulators (AMs) are ligands of proteins that act through binding sites different from natural (orthosteric) ligand sites. AMs are relatively small, more lipophilic, and more rigid compounds. The binding efficacy of AMs with their targets is often slightly lower. AMs are divided into positive AMs (PAMs) and negative AMs (NAMs). AMs are ideal drug targets because they can fine-tune receptor activity while preserving the spatial and temporal signal transduction characteristics of endogenous ligands, resulting in fewer targeted side effects, improved subtype selectivity, and better promotion of biased signal transduction than normal ligands.
MCE designs a unique collection of 258 small allosteric modulators. It is a good tool to be used for research on metabolize, cancer and other diseases.
Cat. No.: HY-L065
3,276 compounds
Chinese herbal therapy is an important part of Traditional Chinese Medicine (TCM). It has been used for centuries in China, where herbs are considered fundamental therapy for many acute and chronic conditions. Many studies indicated TCM exerted an overall regulatory effect via multi-component and multi-target network. Active components from Traditional Chinese Medicine possess many medicinal properties such as antioxidant, anti-cancer, and anti-bacterial effects, which makes it an important source of new drugs. Nearly 200 modern medicines have been developed either directly or indirectly from the plants used as medicines in China. For example, artemisinin, used in multidrug resistant malaria, was first isolated from the Chinese herb Artemisia annua L. Today, scientists continue to identify compounds in Chinese herbal remedies that may be useful in the development of new therapeutic agents applicable in Western medicine.
MCE designs a unique collection of 3,276 active compounds of Chinese Herbal Medicines. MCE Traditional Chinese Medicine Active Compound Library is a useful tool for discovery new drugs from TCM.
Cat. No.: HY-112817A
Synonyms: 8-Oxo-Deoxyguanosine triphosphate trisodium
8-Oxo-dGTP (8-Oxo-Deoxyguanosine triphosphate) trisodium solution (100mM) is an oxidized guanine nucleotide formed by ROS-mediated oxidative modification of dGTP, and it also serves as a key substrate for 8-oxo-dGTP pyrophosphohydrolases (such as hMTH1 and E. coli MutT). 8-Oxo-dGTP trisodium solution (100mM) acts as a DNA mutagen, inserts into nascent DNA and pairs with adenine and cytosine, inducing A:T to C:G transversion mutations. Furthermore, 8-Oxo-dGTP trisodium solution (100mM) causes oxidative DNA base modification, strand breakage and S-phase arrest, and ultimately triggers AIF-mediated apoptosis and promotes spontaneous carcinogenesis in mth1-deficient mice. Accumulation of 8-Oxo-dGTP trisodium solution (100mM) in cells induces genomic instability, but it exhibits a tumor-suppressive effect that reduces tumor incidence in mouse models instead. 8-Oxo-dGTP trisodium solution (100mM) is widely used in studies related to spontaneous carcinogenesis, Parkinson's disease, Alzheimer's disease, heart failure and tumor mechanisms .
Cat. No.: HY-173309
Research Areas:
P53/TLR2 modulator-1 (Compound Z9) is a modulator that targets both the P53 pathway and TLR2 simultaneously, exhibiting anti-radiation activity. P53/TLR2 modulator-1 reduces apoptosis by inhibiting the radiation-induced expression of P53 and Bax. At the same time, it activates the TLR2 pathway, upregulates the expression of downstream proteins MyD88 and P65, and promotes the secretion of cytokines such as IL-6, thus exerting an anti-radiation effect. P53/TLR2 modulator-1 shows significant anti-radiation activity against both AHH-1 cells and HUVECs. It can also increase the survival rate of C57BL/6J mice irradiated with a lethal dose of radiation and reduce the damage to their hematopoietic system, the villous structure of the small intestine, and the spleen caused by radiation. P53/TLR2 modulator-1 can be used in the research of radiation injury-related diseases .
Cat. No.: HY-179041
CAS No.: 924851-91-2
Target:
PGE synthase Prostaglandin Receptor MDM-2/p53 Amino acid Transporter Glutathione Peroxidase Ferroptosis
Research Areas:
SZ0232 is a selective mPGES-2 inhibitor. SZ0232 binds to the active site of mPGES-2 via hydrogen bonds and π-π stacking, reduces the production of prostaglandin E2 (PGE2) and blocks the PGE2-EP3 pathway. SZ0232 regulates Ferroptosis by activating the heme-dependent p53/SLC7A11/GPX4 axis, inhibits lipid peroxidation, and protects renal tubules. SZ0232 enhances glucose-stimulated insulin secretion, inhibits β-cell senescence, and improves glucose homeostasis. SZ0232 reduces renal lipid accumulation, alleviates fibrosis, and ameliorates renal dysfunction in diabetic mice. SZ0232 inhibits renal cyst growth in polycystic kidney disease models. SZ0232 exhibits an insulinotropic effect that strengthens with the increase of animal age. SZ0232 can be used in studies related to type 2 diabetes, acute kidney injury, diabetic kidney disease, and autosomal dominant polycystic kidney disease .
Cat. No.: HY-181906
Target:
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ZnPc-PEG2-VH032 is a VHL-pathway-dependent photodegradation targeting chimera (PDTAC) and cytotoxic agent. ZnPc-PEG2-VH032 (HY-120217) binds to the VHL ligand domain, and then specifically degrades VHL under light irradiation, a process independent of non-specific ROS-mediated protein damage. ZnPc-PEG2-VH032 uses Zinc phthalocyanine (HY-19204) as a photosensitizer, and generates ROS via type I and type II photodynamic pathways under 680 nm LED irradiation. On one hand, it targets and degrades the bound VHL protein through ROS; on the other hand, it exerts direct photodynamic cytotoxicity. Meanwhile, the degradation of VHL downregulates the phosphorylation level of CDK2/4, induces cell cycle arrest in tumor cells, further enhances the sensitivity of tumor cells to oxidative damage caused by ROS, and achieves a synergistic anti-tumor effect. ZnPc-PEG2-VH032 exerts significant in vivo efficacy in an orthotopic mouse model of non-muscle invasive bladder cancer (NMIBC) .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
