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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
21 Results for "
balanced inhibitor
" in MedChemExpress (MCE) Product Catalog:
Products (21)
21 Results for "balanced inhibitor" in MCE Product Catalog:
2
2 Cited Publications
Cat. No.: HY-50862
CAS No.: 893422-47-4
Akt1/Akt2-IN-1 (Compound 17) is an allosteric inhibitor of Akt1 (IC50=3.5 nM) and Akt2 (IC50=42 nM), with potent and balanced activity .
Synonyms: ATI-2042 tartrate
Research Areas:
Budiodarone (ATI-2042) tartrate is a chemical analogue of Amiodarone (HY-14187) with balanced, multiple cardiac ion channel (potassium, sodium and calcium channels) inhibiting activity. Budiodarone tartrate is an antiarrhythmic agent .
Cat. No.: HY-142696
CAS No.: 2677026-14-9
CDK6/PIM1-IN-1 is a potent and balanced dual CDK6/PIM1 inhibitor with IC50 values of 39 and 88 nM, respectively. CDK6/PIM1-IN-1 inhibits CDK4 (IC50=3.6 nM). CDK6/PIM1-IN-1 significantly inhibits acute myeloid leukemia (AML) cell proliferation, arrest cell cycle at the G1 phase, and promote cell apoptosis. CDK6/PIM1-IN-1 exhibits potent anti-AML activity .
Cat. No.: HY-146260
CAS No.: 1453082-52-4
NVP-CLR457 (compound 40) is an orally active, potent and balanced pan-class I PI3K inhibitor. NVP-CLR457 shows a clear dose-dependent PK/PD/efficacy relationship. NVP-CLR457 has antitumor activity .
Cat. No.: HY-176287
Target:
Research Areas:
ARN25657 is a dual-acting D3R/GSK-3β modulator. ARN25657 has both partial D3R agonist activity (EC50 = 15.2 nM, Ki =1.5 nM) and potent GSK-3β inhibitor activity (IC50 = 19.3 nM). ARN25657 exhibits excellent GSK-3β selectivity over FYN, PKA, and CDK5/p35. ARN25657 inhibits P-glycoprotein (P-gP)-mediated acetoxymethyl calcein efflux and improves in vitro ADME properties while maintaining a balanced dual-target profile. ARN25657 is useful for studying bipolar disorder and related neuropsychiatric disorders .
Cat. No.: HY-106605
CAS No.: 61325-80-2
Synonyms: LY 120363
Target:
Research Areas:
Flumezapine (LY 120363) is a potent and balanced antagonist of the dopamine D2 receptor and the 5-hydroxytryptamine receptor (5-HT receptor). Flumezapine does not alter the increase in serum cortisol caused by κ-opioid receptor agonists. Flumezapine inhibits the conditioned avoidance response in rats and has a low risk of extrapyramidal side effects. Flumezapine can be used in antipsychotic research .
Cat. No.: HY-114284
CAS No.: 168473-51-6
Target:
Research Areas:
L-163958 is an efficient, orally active, balanced angiotensin II receptor (AII receptor) antagonist. L-163958 has balanced high affinity for AT1 and AT2, with its IC50 values being 0.16, 0.12, 0.50, and 0.64 nM in rabbit aorta (AT1), rat midbrain (AT2), human adrenal gland (AT1), and human adrenal gland (AT2), respectively. L-163958 has a strong inhibitory effect on the pressor activity in rats. L-163958 can be used for the study of hypertension and related cardiovascular diseases .
Cat. No.: HY-143324
CAS No.: 2767560-51-8
Target:
Research Areas:
A2AAR/HDAC-IN-1 (compound 14c) is an orally active, potent and balanced A2AAR/HDAC dual inhibitor, with a Ki of 163.5 nM for A2AAR and an IC50 of 145.3 nM for HDAC1. A2AAR/HDAC-IN-1 shows anticancer activity .
Cat. No.: HY-161341
Target:
Research Areas:
β-Glucuronidase responsive conjugate 1 (compound 3) is a well-balanced photosensitizer which has photodynamic activity. β-Glucuronidase responsive conjugate 1 inhibits T-24 cell viability and growth with an IC50 of 0.2 μM. β-Glucuronidase responsive conjugate 1 can used to study bladder cancers .
Cat. No.: HY-106605S
Synonyms: LY 120363-d8 hydrochloride
Cat. No.: HY-175658
Target:
Research Areas:
AChE/BChE-IN-29 is an AChE/BChE inhibitor. AChE/BChE-IN-29 exhibits balanced dual cholinesterase inhibitory activity with IC50 values of 2.1 μM for Electrophorus electricus AChE (eeAChE) and 6.3 μM for equine serum butyrylcholinesterase (eqBChE). AChE/BChE-IN-29 effectively inhibits amyloid-β (Aβ42) aggregation and tau protein aggregation in E. coli cell models. AChE/BChE-IN-29 can be used for the study of Alzheimer’s disease (AD) .
Cat. No.: HY-157527
CAS No.: 2978613-03-3
Target:
Research Areas:
hAChE-IN-7 (compound 5s) is a mixed inhibitor affecting both the catalytic active site (CAS) and peripheral anionic site (PAS) of hAChE. hAChE-IN-7 displays the balanced inhibitory effect on hAChE (IC50=69.8 nM) and hBuChE (IC50=68.0 nM), and exhibits inhibitory activity against β-secretase-1 (BACE-1) (IC50=3.6 μM). hAChE-IN-7 has the potential for Alzheimer's disease (AD) research .
Cat. No.: HY-162585
CAS No.: 3048071-20-8
Target:
Research Areas:
5-HT1AR agonist 1 (Compound A3) emerges as a relatively balanced multi-target activity profile, including 5-HT1AR agonist with an EC50 value of 34 nM, SERT reuptake ihibitor (IC50 =12 nM), NET reuptake inhibitor (IC50 =78 nM) and DAT reuptake inhibitor (IC50 =135 nM). 5-HT1AR agonist 1 performs significant antidepressant effects and exhibits excellent bioavailability and low clearance in mice, which is promising for research in the field of antidepressant drugs .
Cat. No.: HY-P11275
Target:
Research Areas:
Cat. No.: HY-136737
CAS No.: 307548-94-3
Target:
Research Areas:
MAO-A/B-IN-1 (Compound 21) is a balanced MAO-A/B inhibitor, with an IC50 of 235 nM against hMAO-A and an IC50 of 165 nM against hMAO-B. MAO-A/B-IN-1 can be used in the research of depression, Parkinson's disease and Alzheimer's disease .
Cat. No.: HY-14834AS
Synonyms: ATI-2042-d10 tartrate
Cat. No.: HY-184422
SOS1-IN-26 is a potent, orally active selective allosteric SOS1 inhibitor with a KD of 33 nM and SOS1-KRAS binding IC50 of 4.0 nM. SOS1-IN-26 disrupts SOS1-KRAS interaction, inhibits MAPK/PI3K signaling, induces G1 phase arrest and tumor cell apoptosis. SOS1-IN-26 serves as a balanced lead therapeutic candidate for pan-KRAS-driven colorectal cancer studies .
Cat. No.: HY-19091
CAS No.: 123297-52-9
Research Areas:
ICI-170777 is an orally active cardiotonic agent and type III Phosphodiesterase inhibitor, with an IC50 of 2.5 μM against cyclic AMP phosphodiesterase type III from canine cardiac fractions. ICI-170777 inhibits Aldrin epoxidase and pentobarbital metabolism. It enhances β-adrenergic receptor-mediated positive inotropic effects without causing chronotropic effects, while also exerting balanced arteriolar/venular vasodilator, platelet aggregation inhibitor and smooth muscle relaxant activities. ICI-170777 restores cardiac function in an acute canine heart failure model, exhibits additive effects when combined with Ouabain (HY-B1457), and shows no significant activity against multiple receptor classes or non-cardiac systems. ICI-170777 can be used in research related to congestive heart failure .
Cat. No.: HY-L110
97 compounds
Cyclic peptides are polypeptide chains taking cyclic ring structure, which exhibit diverse biological activities, such as antibacterial activity, immunosuppressive activity and anti-tumor activity. Cyclic peptides, with the features of good binding affinity, target selectivity and low toxicity, show great success as therapeutics. Multiple cyclic peptides are currently in clinical use, for examples, gramicidin and tyrocidine with bactericidal activity, cyclosporin A with immunosuppressive activity, and vancomycin with antibacterial activity. Furthermore, cyclic peptides usually have the sufficient size and a balanced conformational flexibility/rigidity for binding to flat protein-protein interaction (PPI) interfaces, which have potential to develop PPI drugs.
MCE offers a unique collection of 97 cyclic peptides, all of which have good bioactivities. MCE Cyclic Peptide Library is a powerful tool for drug discovery and PPI inhibitor screening.
Cat. No.: HY-L945
72 compounds
Sulfonyl fluoride (-SO₂F) overcomes the poor target selectivity of traditional covalent warheads that rely heavily on cysteine. With high stability and tunable electrophilicity under physiological conditions, it targets multiple nucleophilic residues including Lys, Tyr, Ser and His, offering expanded druggable space, lower off-target risks and prolonged efficacy. It is widely used in covalent inhibitors, molecular glues, PROTACs and chemical probes.
MCE has built a highly diverse sulfonyl fluoride fragment library with 1,162 structurally diverse, drug-like fragments. Designed for balanced reactivity, stability and compatibility, these molecules feature tunable electrophilicity, simple scaffolds and high derivatization potential. Combined with SuFEx click chemistry, the library enables efficient modular modification and rapid structure optimization.
Ideal for targeting non-cysteine residues, this library improves covalent screening and probe development efficiency, serving as a precise tool for early-stage covalent drug discovery and chemical biology research.
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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
