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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
1345 Results for "
High Selectivity
" in MedChemExpress (MCE) Product Catalog:
Products (1345)
1345 Results for "High Selectivity" in MCE Product Catalog:
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CP 339818 hydrochloride is a non-peptide Kv1.3 channel (IC50 = 200 nM) and Kv1.4 channel blocker. CP 339818 hydrochloride inhibits HCN channel with IC50s of 18.9 μM and 43.4 μM against HCN1 and HCN4 (high Cl -). CP 339818 hydrochloride has significantly weaker blocking effects on Kv1.1, Kv1.2, Kv1.5, Kv1.6, Kv3.1-4, and Kv4.2 channels. CP 339818 hydrochloride selectively blocked Kv1.3, thereby inhibiting the activation process of human T cells. CP 339818 hydrochloride can be used to study the physiological functions of HCN and Kv channels .
Cat. No.: HY-114540
CAS No.: 185855-91-8
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CP-339818 is a non-peptide Kv1.3 channel (IC50 = 200 nM) and Kv1.4 channel blocker. CP 339818 inhibits HCN channel with IC50s of 18.9 μM and 43.4 μM against HCN1 and HCN4 (high Cl -). CP-339818 has significantly weaker blocking effects on Kv1.1, Kv1.2, Kv1.5, Kv1.6, Kv3.1-4, and Kv4.2 channels. CP-339818 selectively blocked Kv1.3, thereby inhibiting the activation process of human T cells. CP-339818 can be used to study the physiological functions of HCN and Kv channels .
Synonyms: PF-06372865; CVL-865
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Darigabat (PF-06372865) is an orally active, α2/α3/α5 subtype-selective GABAA positive allosteric modulator (PAM). Darigabat is a high affinity ligand at GABAA receptors containing α1/α2/α3/α5 subunits (Kis of 2.9 nM, 21 nM, 134 nM for α2, α1 PAM, α2 PAM, respectively), with low affinity for α4/α6 subunits. Darigabat can across the blood-brain barrier (BBB). Darigabat has anxiolytic activity and has the potential for epilepsy .
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Apcin-A is a small molecule inhibitor that selectively targets the cell division cycle protein Cdc20 and is a derivative of Apcin (HY-110287). Apcin-A competitively binds to the D-box binding pocket of Cdc20 and inhibits substrate ubiquitination mediated by the anaphase promoting complex APC/C-Cdc20. Apcin-A also blocks the binding of Cdc20 to substrates (such as securin and cyclin B1), inhibiting anaphase initiation and cell cycle exit. Apcin-A can promote or prolong mitotic slippage in coordination with p31 comet under conditions of high spindle assembly checkpoint (SAC) activity. Apcin-A can be used to develop anti-mitotic drugs and overcome tumor chemotherapy resistance. Apcin-A can be used to synthesize PROTAC CP5V (HY-130257)[1][2][3].
Cat. No.: HY-179227
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HDAC6 ligand-7 (Compound 16a) is a positron emission tomography (PET) tracer for the deacetylase 6 (HDAC6) enzyme with a Kd value of 1.66 nM. HDAC6 ligand-7 exhibits excellent HDAC6 inhibitory activity, with IC50 values of 2.7 and 3.7 nM for hHDAC6 and mHDAC6, respectively, and has high selectivity for HDAC1/4/7/8. HDAC6 ligand-7 after being radioactively labeled with fluorine-18, [¹⁸F]HDAC6 ligand-7 shows varying degrees of radioactive uptake in PET, which can reflect the specific binding to HDAC6. HDAC6 ligand-7 can be used for the study of HDAC6 imaging .
Cat. No.: HY-181533
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IAP ligand 9 is an ASX-series, non-peptidic SMAC mimetic and IAP binder with high cell permeability. IAP ligand 9 selectively targets cIAP1-BIR3, XIAP-BIR3, exhibits extremely weak binding affinity for XIAP-BIR2, with a KD of 100 nM for cIAP1-BIR3 and 10 nM for XIAP-BIR2. IAP ligand 9 can be used to synthesize IAP-recruiting protein degraders (IPD), and can calibrate the cell permeability and cellular-level target binding assays of the IPD molecule SNIPER (TEAD)-1 (HY-181607). IAP ligand 9 and its series of degraders can be used in the research of solid tumors such as malignant pleural mesothelioma associated with abnormal activation of the Hippo pathway .
Cat. No.: HY-182243
CAS No.: 2748366-80-3
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HK2-IN-4 is a selective hexokinase 2 (HK2) inhibitor with an IC50 value of 0.79 μM and a Kd value of 0.41 μM. HK2-IN-4 blocks the interaction between HK2 and voltage-dependent anion channel 1 (VDAC1). HK2-IN-4 reduces lactate and ATP levels in cancer cells. HK2-IN-4 induces the production of apoptosis (apoptosis) markers in cancer cells, including increased p-AMPK/AMPK ratio and Bax levels, as well as decreased Bcl2 levels. HK2-IN-4 inhibits the proliferation of cancer cells with high HK2 expression. HK2-IN-4 can be used in research related to colorectal cancer and non-small cell lung cancer .
Cat. No.: HY-184297
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Topoisomerase II-IN-26 is a dual bacterial type II topoisomerase (Top II) inhibitor, with IC50 values of 0.081 μM and 0.093 μM against Staphylococcus aureus DNA gyrase and topoisomerase IV, respectively, and IC50 values of 0.906 μM and 0.103 μM against Escherichia coli DNA gyrase and topoisomerase IV, respectively. Topoisomerase II-IN-26 also shows high selectivity for human topoisomerase IIα. Topoisomerase II-IN-26 inhibits biofilm formation, reduces the metabolic activity of mature biofilms, exhibits activity against Staphylococcus aureus, MRSA strains, Escherichia coli and Acinetobacter baumannii, and possesses a post-antibiotic effect. Topoisomerase II-IN-26 can be used for the research of bacterial infections such as Staphylococcus aureus and MRSA .
Cat. No.: HY-184389
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PROTAC HDAC6 degrader 10 is a highly efficient, safe and selective HDAC6 PROTAC degrader with a pIC50 of 8.75 and a pDC50 of 9.2 in BEAS-2B cells. PROTAC HDAC6 degrader 10 recruits cereblon to form a ternary complex with HDAC6, thereby achieving the degradation of HDAC6. PROTAC HDAC6 degrader 10 significantly induces hyperacetylation of α-tubulin without affecting the acetylation of H3, and achieves sustained HDAC6 knockdown in mouse lung tissues. PROTAC HDAC6 degrader 10 exhibits high bioavailability after subcutaneous administration in mice. PROTAC HDAC6 degrader 10 enables the study of HDAC6 pharmacology via chemical knockdown of HDAC6 in vitro and in vivo, and can be used for research on pulmonary diseases .
Cat. No.: HY-187206
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CYP1B1-IN-15 is a CYP1B1 inhibitor with an IC50 of 1.47 nM, and it exhibits high selectivity against six major CYP subtypes. CYP1B1-IN-15 exerts competitive inhibitory effects by competing with substrates for binding to the active site of CYP1B1. CYP1B1-IN-15 enhances the inhibitory effect of Paclitaxel (HY-B0015) on the proliferation of paclitaxel-resistant cancer cells, and inhibits the migration and invasion of paclitaxel-resistant cancer cells. CYP1B1-IN-15 can be used in studies related to paclitaxel-resistant non-small cell lung cancer .
Cat. No.: HY-B0661CS
CAS No.: 1189923-88-3
Cat. No.: HY-B0696AR
CAS No.: 145821-59-6
Synonyms: NO050328 hydrochloride (Standard); NO328 hydrochloride (Standard); TGB hydrochloride (Standard)
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Tiagabine (hydrochloride) (Standard) is the analytical standard of Tiagabine (hydrochloride). This product is intended for research and analytical applications. Tiagabine hydrochloride (NO050328; NO328; TGB) is an orally active, highly selective, and reversible GAT-1 inhibitor and anticonvulsant that crosses the blood-brain barrier. By blocking the reuptake of GABA in neurons and glial cells, tiagabine increases extracellular GABA levels to enhance inhibitory signal transduction, thereby exerting multiple activities such as anticonvulsant, neuroprotective, and antioxidant effects. Tiagabine hydrochloride exhibits linear pharmacokinetic properties. Although it is metabolized by CYP3A and has a high protein binding rate, it carries a low risk of cognitive impairment. Tiagabine hydrochloride is widely used in research on related diseases including epilepsy (including refractory partial seizures), alcohol withdrawal symptoms, and Huntington's disease .
Cat. No.: HY-B0696AS
Synonyms: NO050328-d4 hydrochloride; NO328-d4 hydrochloride; TGB-d4 hydrochloride
Cat. No.: HY-B0696S
CAS No.: 1217672-34-8
Synonyms: NO050328-d6; NO328-d6; TGB-d6
Cat. No.: HY-B0696S1
Synonyms: NO050328-d4; NO328-d4; TGB-d4
Cat. No.: HY-P11291A
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Cat. No.: HY-P11899
Synonyms: Cyclo(VVIaWG)
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Cyclo (Val-Val-Ile-d-Ala-Trp-Gly) (Cyclo(VVIaWG)) is a six-membered cyclic peptide designed based on the C-terminal region of Aβ1-42. Cyclo (Val-Val-Ile-d-Ala-Trp-Gly) binds selectively to Aβ15-36 (Kd = 0.6 μM), regulates the aggregation of Aβ1-42 at high concentrations, weakly inhibits fibrillation at a 10-fold excess, and inhibits oligomerization at equimolar concentrations. Cyclo (Val-Val-Ile-d-Ala-Trp-Gly) does not interfere with the aggregation of IAPP. Cyclo (Val-Val-Ile-d-Ala-Trp-Gly) can serve as a targeting ligand for fluorescent probes of Aβ prefibrillar aggregates, and is applicable to research related to Alzheimer's disease .
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α-Glucosidase, rice is a GH31 glycoside hydrolase in rice seeds, with high selectivity for α-1,4-glycosidic bonds. α-Glucosidase, rice can be inhibited by rice husk extracts (IC50 = 1.25 μg/mL) and steroidal components (IC50 = 1.83 μg/mL). α-Glucosidase, rice exists in two major isoforms, among which isoform II is more sensitive to inhibitors. α-Glucosidase, rice can directly bind to and degrade starch granules in rice seeds. α-Glucosidase, rice can form ONG2-I and ONG2-II via post-translational proteolysis. α-Glucosidase, rice can be used in type 2 diabetes research .
Cat. No.: HY-L180
655 compounds
Mitochondrial autophagy refers to the selective encapsulation and degradation of damaged mitochondria by cells through the autophagy mechanism, thereby maintaining mitochondrial and cellular homeostasis. The concept of mitochondrial autophagy has received extensive attention since it was proposed. Current studies have shown that the mechanisms of mitochondrial autophagy can generally be divided into two categories: Ubiquitin-dependent pathways and Ub-independent pathways. In addition, mitochondrial autophagy is a research hotspot related to the pathogenesis of neurodegenerative diseases, cardiovascular diseases, cancer, metabolic diseases and other clinical diseases. Therefore, high-throughput screening based on mitochondrial autophagy can effectively screen out compounds that are closely related to the occurrence of diseases and analyze their mechanisms.
MCE can provide a library of 655 mitophagy compounds, which can be used for drug development and mechanism research in cancer, immunity, infection and other hot research fields.
Cat. No.: HY-L033
370 compounds
Peptidomimetics are compounds whose essential elements (pharmacophore) mimic a natural peptide or protein in 3D space and which retain the ability to interact with the biological target and produce the same biological effect. Peptidomimetics are designed to circumvent some of the problems associated with a natural peptide: e.g. stability against proteolysis (duration of activity) and poor bioavailability. Certain other properties, such as receptor selectivity or potency, often can be substantially improved. The design and synthesis of peptidomimetics are most important because of the dominant position peptide and protein-protein interactions play in molecular recognition and signaling, especially in living systems. Hence mimics have great potential in drug discovery.
MCE Peptidomimetic Library contains 370 compounds including peptoid, α-helix mimetics, β-turn/sheets mimetics, etc. This library is an indispensable tool of structure-activity relationships in drug discovery.
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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
