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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
169 Results for "
allosteric binding
" in MedChemExpress (MCE) Product Catalog:
Products (169)
169 Results for "allosteric binding" in MCE Product Catalog:
Cat. No.: HY-178714
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JNJ627 is a small molecule allosteric inhibitor of IL-17A with a KD of 92 nM. JNJ627 effectively inhibits the binding of IL-17A and IL-17RA, with an IC50 value of 16 nM. JNJ627 is capable of inhibiting the secretion of G-CSF (granulocyte colony-stimulating factor) caused by IL-17A stimulation. JNJ627 can be used for the study of autoimmune diseases (such as psoriasis) .
Cat. No.: HY-110208R
CAS No.: 32703-82-5
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BRD9876 (Standard) is the analytical standard of BRD9876 (HY-110208). This product is intended for research and analytical applications. BRD9876 is the "rigor" inhibitor that locks Kinesin-5 (Eg5) in a state with enhanced microtubules (MTs) binding, leading to bundling and stabilization of MTs. BRD9876 interacts with the tyrosine 104 residue that is part of the α4-α6 allosteric binding pocket. BRD9876 specifically targets microtubule-bound Eg5 and selectively inhibits myeloma over CD34 cells. BRD9876 has the potential for multiple myeloma (MM) research .
Cat. No.: HY-160426
CAS No.: 2270984-21-7
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Gcase activator 3 is a β-glucocerebrosidase (GCase) activator with an EC50 of 1.49 μM. By binding to the allosteric site of GCase, Gcase activator 3 partially stabilizes GCase and enhances its activity. Gcase activator 3 can be conjugated with fluorophores to form fluorescent probes, which are used for high-throughput screening of GCase. Gcase activator 3 is applicable to research related to Gaucher's disease, Parkinson's disease, dementia with Lewy bodies, and multiple system atrophy .
Cat. No.: HY-180554
CAS No.: 300587-89-7
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UCB1244283 is a synaptic vesicle glycoprotein 2A (SV2A) allosteric modulator. UCB1244283 binds to a secondary ligand-binding site in SV2A and enhances orthosteric ligand engagement when the orthosteric site is occupied, by stabilizing the occluded state and slowing ligand dissociation. UCB1244283 shows a clear protective effect against both tonic and clonic convulsions in sound-sensitive mice. UCB1244283 can be used for epilepsy research .
Cat. No.: HY-153701S
CAS No.: 2417135-66-9
Synonyms: Envudeucitinib; ESK-001
Cat. No.: HY-175594
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DNMT2-IN-2 is a selective DNA methyltransferase 2 (DNMT2) inhibitor with a KD value of 3.04 μM. DNMT2-IN-2 targets to a cryptic allosteric binding site of DNMT2. DNMT2-IN-2 reduces m5C levels in MOLM-13 tRNA and synergizes with Doxorubicin (HY-15142A) to impair cell viability. DNMT2-IN-2 can be used for cancer research, such as cervical cancer and leukemia .
Cat. No.: HY-188141
CAS No.: 3057557-03-3
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Allopole-A is a Plk1 inhibitor with an IC50 of 1.4-2.5 μM against human Plk1 PBD1. Allopole-A binds to the allosteric W-F pocket in Plk1 PBD1, displacing the L2 loop, thereby disrupting water-mediated phospho-ligand binding interactions and promoting inhibitory interactions between the kinase domain and PBD to suppress Plk1 kinase activity. Allopole-A can be used in studies of human cancers with plk1 overexpression .
Cat. No.: HY-W066579
CAS No.: 2305-79-5
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4,5,6,7-Tetrahydroindazole acts as an Antimicrobial agent, an interleukin-2-induced T-cell kinase inhibitor, a positive allosteric modulator of AMPA receptors, and a ligand for CYP2E1, with a Kd1 value of 0.023 μM for its binding to rabbit-derived CYP2E1. 4,5,6,7-Tetrahydroindazole scavenges DPPH free radicals. It exhibits anti-tumor, anti-tuberculosis, and anti-inflammatory activities .
Cat. No.: HY-179607
CAS No.: 2954281-30-0
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LUF8100 is a dual-target antagonist of CCR2/CCR5 with pKi values for CCR2 and CCR5 of 5.23 and 4.97 respectively. LUF8100 can be used for research on immune homeostasis and cancer .
Cat. No.: HY-103565R
CAS No.: 97075-46-2
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AMN082 (Standard) is the analytical standard of AMN082. This product is intended for research and analytical applications. AMN082, a selective, orally active, and brain penetrant mGluR7 agonist, directly activates receptor signaling via an allosteric site in the transmembrane domain. AMN082 potently inhibits cAMP accumulation and stimulates GTPγS binding (EC50 values, 64-290 nM) at transfected mammalian cells expressing mGluR7. AMN082 shows selectivity over other mGluR subtypes and selected ionotropic glutamate receptors. Antidepressant effects .
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BDM-2 is an IN-LEDGF allosteric inhibitor (INLAI) of HIV-1 integrase (IN refers to integrase) (IC50=47 nM) with potent anti-Retroviral (ARV) activity. BDM-2 shows IN multimerization activation effect with an AC50 value of 20 nM. BDM-2 blocks the interaction between the catalytic core domain of IN (IN-CCD) and the Integrase binding domain of LEDGF/p75 (IBD), with an IC50 value of 0.15 μM. BDM-2 exhibits highly selective and favorable cytotoxicity .
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YL-365 is a potent and selective GPR34 antagonist with an IC50 of 17 nM. YL-365 binds to a portion of the orthosteric binding pocket of GPR34 and induces allosteric changes that stabilize the receptor in an inactive conformation. YL-365 down-regulates expression of the proinflammatory gene iNOS in M1 microglia and suppresses proinflammatory responses. YL-365 reduces mechanical allodynia in a dose-dependent manner in a mouse model of neuropathic pain. YL-365 can be used for the research of neuropathic pain .
Cat. No.: HY-161928
CAS No.: 1030098-18-0
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GPX4 activator 1 is an allosteric activator of glutathione peroxidase 4 (GPX4) with a Kd value of 5.86 μM. GPX4 activator 1 binds to a specific region of GPX4 to alter protein binding kinetics and counteract ferroptosis (EC50 = 19.19 μM). GPX4 activator 1 inhibits lipid peroxidation, rescues ferroptotic cell death and maintains cell viability. GPX4 activator 1 can be used in studies related to Doxorubicin (HY-15142A)-induced myocardial injury .
Cat. No.: HY-171450
CAS No.: 1802770-18-8
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VMD-928 is an orally active, allosteric, irreversible and selective tropomyosin receptor kinase A (TrkA) inhibitor. VMD-928 blocks the downstream signaling pathways triggered by the binding of nerve growth factor (NGF) to TrkA, thereby inhibiting cell proliferation, invasion, and promoting cancer cell death. VMD-928 is promising for research of various cancers, including prostate cancer, thymic carcinoma, mesothelioma, squamous cell carcinoma of the head and neck, squamous cell carcinoma of the lung, ovarian cancer, hepatocellular carcinoma .
Cat. No.: HY-182751
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ACLY-IN-4 is an ATP-citrate lyase (ACLY) inhibitor with an IC50 of 0.022 μM and a Kd of 0.19 μM. ACLY-IN-4 binds to the allosteric binding site of ACLY. ACLY-IN-4 exhibits hypolipidemic, anti-steatotic, insulin sensitivity-improving, anti-oxidative stress, anti-inflammatory and anti-fibrotic activities. ACLY-IN-4 alleviates hepatic steatosis, systemic insulin resistance, oxidative stress, hepatic inflammation and fibrosis. ACLY-IN-4 can be used for the research of metabolic dysfunction-associated steatohepatitis .
Cat. No.: HY-184423
SOS1-IN-27 is a potent, selective allosteric SOS1 inhibitor with a KD of 14 nM and SOS1-KRAS binding IC50 of 1.6 nM. SOS1-IN-27 disrupts SOS1-KRAS interaction, inhibits MAPK/PI3K signaling, induces G1 arrest and tumor cell apoptosis. SOS1-IN-27 serves as a valuable tool compound for pan-KRAS-driven colorectal cancer studies .
Cat. No.: HY-W751808S
CAS No.: 2726226-14-6
Synonyms: 2,3-DPG-13C3
Cat. No.: HY-179634
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ASF-006 sodium, a tetrapodal tryptophan derivative, is a potent viral invasion inhibitor. ASF-006 sodium shows potent antiviral activity against different SARS-CoV-2 Omicron variants but not against the ancestral SARS-CoV.2 strain (Wuhan-Hu-1). ASF-006 sodium competitively inhibits receptor-binding domain (RBD)-ACE2 binding via an allosteric mechanism. ASF-006 sodium inhibits Omicron BA.1, Omicron XBB.1.5, respiratory syncytial virus (RSV) and Ebola virus infection with IC50s of 0.02 μM, 0.3 μM, 1.52 μM and 0.2 μM, respectively. ASF-006 sodium inhibits cell entry of both HIV and enterovirus A71[1].
Cat. No.: HY-185978
CAS No.: 2133456-91-2
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GL-II-73 is a selective, orally active and blood-brain barrier permeable positive allosteric modulator of α5GABAA receptor, acting on the benzodiazepine-binding site of GABAA receptors. The binding selectivity of GL-II-73 for the α5 subtype is 6-, 11- and 12.5-fold higher than that for the α2, α1 and α3 subtypes, respectively . GL-II-73 reverses pilocarpine-induced hyperactivation of dopamine neurons in the ventral tegmental area, improves working memory and pyramidal neuron dendritic morphology in 5xFAD mice, but does not reduce β-amyloid load . GL-II-73 can be used in research related to Alzheimer's disease and temporal lobe epilepsy with comorbid psychosis .
Cat. No.: HY-P5542
CAS No.: 1251838-01-3
Synonyms: SB-01; Peniel 2000
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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
