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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
875 Results for "
binding affinity
" in MedChemExpress (MCE) Product Catalog:
Products (875)
875 Results for "binding affinity" in MCE Product Catalog:
Cat. No.: HY-P990778
CAS No.: 2756879-35-1
Synonyms: ATG-101
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Cat. No.: HY-P991930
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Cat. No.: HY-182354
CAS No.: 861877-12-5
VEGFR2-IN-84 is an orally active, multi-targeted tyrosine kinase inhibitor based on a naphthalene ring scaffold. VEGFR2-IN-84 inhibits VEGFR2 with sub-nanomolar affinity and broadly targets kinases including Kit, FGFR, PDGFR, and Ret. By competitively binding to the ATP-binding pocket, VEGFR2-IN-84 blocks the phosphorylation of VEGFR2 and its downstream AKT/ERK signaling pathway, thereby significantly inhibiting endothelial cell proliferation, migration, and tumor angiogenesis. VEGFR2-IN-84 exhibits broad-spectrum antiproliferative activity against various solid tumors such as liver cancer, lung cancer, and renal cancer, shows weak toxicity to normal cells, and has superior potency to Lenvatinib (HY-10981). VEGFR2-IN-84 possesses favorable pharmacokinetic properties and high safety (LD50>2000 mg/kg), and can be used in related studies of various malignant tumors .
Cat. No.: HY-P703986
Purity: ≥ 95%, as determined by Bis-Tris PAGE.
Synonyms: FCER2; Immunoglobulin E-binding Factor; Prev. CD23A; Lymphocyte IgE Receptor; Prev. FCE2; Fc-Epsilon-RII; CLEC4J; BLAST-2; FcepsilonRII; IGEBF; CD23 Antigen; Fc Fragment Of IgE, Low affinity II, Receptor For (CD23A); FCErII; C-Type Lectin Domain Family 4,
Species:
Human
Source:
HEK293
Cat. No.: HY-LD004
14 million compounds
DEL technology enables the simultaneous screening of millions or billions of compounds in a single tube by covalently linking each small molecule with a unique DNA sequence. Traditional DEL screening primarily focuses on identifying non-covalent binding molecules, where interactions with the target are reversible. In contrast, DNA‑encoded covalent library is an ultra‑high‑throughput screening library developed on the basis of conventional DNA‑encoded library technology. It incorporates controllable electrophilic covalent warheads capable of forming irreversible covalent bonds with amino acid residues at the active sites of target proteins, including Cys, Lys, Ser, Tyr, and others. This covalent binding enhances binding affinity, prolongs residence time at the target site, and has the potential to overcome challenges associated with traditional non-covalent inhibitors, such as drug resistance or off-target effects.
Each compound in the library contains both a binding domain and an electrophilic warhead. It first recognizes and binds to the target through non covalent interactions, and then forms a stable covalent bond with key amino acid residues to achieve irreversible inhibition. This library is specifically designed for the discovery of potent, long lasting, and highly selective covalent inhibitors, particularly for undruggable targets such as kinases, GPCRs, proteases, and mutant oncoproteins. Each molecule is uniquely labeled with a DNA barcode for molecular identification and sequencing decoding.
This library is an advanced and highly diverse collection, consists of 35 independent sub-libraries with a total scaleof 14 million compounds, It incorporates over 14 experimentally validated covalent warheads capable of targeting cysteine, lysine, arginine, aspartic acid and glutamic acid. This library is constructed with diverse drug like core scaffolds and integrated controllable covalent warheads, it features structural diversity, reaction spec
Cat. No.: HY-101390D
CAS No.: 120054-86-6
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(R)-Niguldipine, a R-epimer of Niguldipine (HY-101390B), is a calcium channel antagonist. (R)-Niguldipine exerts a vasodilatory effect by blocking calcium channels and reducing the transmembrane influx of calcium ions. (R)-Niguldipine can inhibit U-46619 (HY-108566)-induced coronary artery contraction in guinea pig Langendorff hearts (pID50 of 9.93), has high affinity for calcium channel binding sites on guinea pig skeletal muscle membranes (Ki of 8.10), and lowers blood pressure in spontaneously hypertensive rats (pED30 of 5.55). (R)-Niguldipine can improve cardiovascular diseases such as hypertension, angina pectoris, and arrhythmias .
Cat. No.: HY-106095
CAS No.: 102253-70-3
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DQ 2556 is a semi-synthetic cephalosporin antibiotic. DQ-2556 exhibits significant activity against both Gram-positive and Gram-negative bacteria, particularly Gram-positive bacteria and Enterobacteriaceae infections. DQ 2556 exerts its bactericidal effect by interfering with cell division. DQ-2556 has a strong affinity for the penicillin-binding proteins (PBPs) of Escherichia coli: PBP1A/1B (IC₅₀ = 0.57-0.73 μg/mL) and PBP3 (IC₅₀ = 0.088 μg/mL). DQ-2556 demonstrates significant in vivo protective effects. DQ-2556 can be used in the development of injectable cephalosporins .
Cat. No.: HY-124399
CAS No.: 925891-74-3
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Peroxisome proliferator-activated receptors (PPARs) play an important role in regulating lipid and glucose metabolism, and oleoylethanolamide (OEA) is a natural ligand for PPARα. N-Octadecyl-N'-propyl-sulfamide is an analog of OEA and a potent activator of PPARα, with selective binding affinity for PPARα (EC50=100 nM, compared to 120 nM for OEA). N-Octadecyl-N'-propyl-sulfamide (10 mg/kg; ip) inhibits food intake and reduces body weight gain in rats. At a dose of 1 mg/kg, N-Octadecyl-N'-propyl-sulfamide induces satiety, thereby reducing food intake, body weight, and plasma triglyceride concentrations in free-feeding Wistar rats and obese Zucker (fa/fa) rats.
Cat. No.: HY-12497R
CAS No.: 219766-25-3
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ANA-12 (Standard) is an analytical standard of ANA-12 (HY-12479). This product is intended for research and analytical applications. ANA-12 is a brain-penetrant, selective TrkB antagonist with IC50 values of 45.6 nM and 41.1 μM, and Kd values of 10 nM and 12 μM, for high- and low-affinity sites, respectively. ANA-12 specifically inhibits BDNF-induced TrkB receptor activation and its downstream signaling cascades by directly and non-competitively binding to the TrkB receptor, without affecting the functions of TrkA and TrkC. ANA-12 is used in research concerning neuropsychiatric disorders (such as depression and anxiety), acute and chronic pain, neuroimmune inflammation, and the mechanisms of learning and memory.
Cat. No.: HY-134058S
Synonyms: Butylethylcarbinol-d4
Cat. No.: HY-15080
CAS No.: 143691-37-6
Synonyms: LY 293606
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GYKI 53405 (LY 293606) is a non-competitive, orally active AMPA receptor antagonist. GYKI 53405 shows no significant binding affinity for GABAA, GABAB or benzodiazepine receptors. GYKI 53405 increases self-grooming behavior, induces wet dog-like shakes, reduces spontaneous activity, produces anxiolytic-like behavior, reverses the anxiogenic effect induced by mCPP, inhibits locomotor activity, suppresses sound-induced and maximal electroshock-induced seizures, prolongs survival in global cerebral ischemia models, and exhibits sustained anticonvulsant effects at doses below the sedation threshold. GYKI 53405 can be used in research related to absence epilepsy, anxiety disorders and global cerebral ischemia .
Cat. No.: HY-15210
CAS No.: 54870-28-9
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Meglitinide is an ATP-sensitive potassium (KATP) channel inhibitor. Meglitinide exhibits IC50 values of 0.26 μM, 0.53 μM and 1.6 μM against KATP channels containing SUR1, SUR2A and SUR2B, respectively, with a Kd value of 7 μM for both SUR1 and SUR2A, and a Kd value of 8 μM for SUR2B. Meglitinide binds to the SUR1, SUR2A and SUR2B subunits with high affinity to close KATP channels, acting on a binding site shared by all SUR subtypes, and its interaction with SUR1 carrying the S1237Y mutation remains unchanged. Meglitinide is applicable to research related to type 2 diabetes .
Cat. No.: HY-169056
CAS No.: 14668-59-8
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SLC7A11-IN-2 (Compound 1) is an SLC7A11/xCT inhibitor. SLC7A11-IN-2 induces cell death in HeLa cells by lowering intracellular glutathione levels and increasing oxidative stress, thereby disrupting the oxidative balance within the cells, with an IC50 value of 10.23 μM. Molecular dynamics simulation analysis indicates that SLC7A11-IN-2 has a stronger binding affinity to SLC7A11 compared to Erastin (HY-15763). SLC7A11-IN-2 can be utilized in research within the field of cervical cancer .
Cat. No.: HY-180557
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4A-BFA-11 is a folate-targeted PEG-MMAE conjugate that exhibits specific binding affinity for the folate receptor α (FR-α) (KD = 106.7 nM). 4A-BFA-11 achieves tumor enrichment by combining PEG-mediated long circulation (EPR effect) and folate receptor targeting. 4A-BFA-11 undergoes enzymatic cleavage at the tumor site to release the active payload, enabling precise action. 4A-BFA-11 sefficiently carries, targets, and controls the release of MMAE in tumor tissues in a HeLa mouse model. 4A-BFA-11 can be used for cervical cancer, ovarian cancer, and lung cancer research .
Cat. No.: HY-182603
CAS No.: 157360-23-1
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BO-653 is an orally active anti-atherosclerotic antioxidant that exhibits high binding affinity for LDL. BO-653 scavenges linoleic acid peroxyl radicals, inhibits lipid peroxidation during the auto-oxidation of linoleic acid, and potently suppresses LDL oxidation. BO-653 inhibits Hepatitis C Virus (HCV) replication in a concentration-dependent manner, with an IC50 of 36.0 μM against the HCV subgenomic replicon in FLR3-1 cells. BO-653 demonstrates significant anti-atherosclerotic effects in various animal models, including the Watanabe heritable hyperlipidemic rabbit. BO-653 is suitable for use in research related to atherosclerosis and Hepatitis C Virus infection .
Cat. No.: HY-187185
CAS No.: 3050643-44-9
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Sigma-1 receptor antagonist 7 is a selective sigma-1 receptor antagonist capable of crossing the blood-brain barrier, with an IC50 of 12.7 nM against guinea pig σ1R. Sigma-1 receptor antagonist 7 binds to σ1R, and its binding affinity decreases in the presence of Phenytoin (HY-B0448). Sigma-1 receptor antagonist 7 alleviates mechanical and thermal hyperalgesia induced by acute inflammation in rats. Sigma-1 receptor antagonist 7 can be used for research related to hyperalgesia .
Cat. No.: HY-P990742
CAS No.: 2762499-30-7
Synonyms: TJ-CD4B; ABL111; TJ033721
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Cat. No.: HY-P992389
Cat. No.: HY-P992434
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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
