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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
1443 Results for "
weak
" in MedChemExpress (MCE) Product Catalog:
Products (1443)
1443 Results for "weak" in MCE Product Catalog:
Cat. No.: HY-170846
Target:
Research Areas:
FGFRs-IN-1 (Compound A16) is the orally active inhibitor for FGFR, that inhibits FGFR1/2/3/4 with IC50s of 2.3, 7, 11, and 163 nM, respectively. FGFRs-IN-1 also inhibits VEGFR1/2/3, Abl, and Flt3 with IC50s of 61, 176, 112, 26, and 353 nM, respectively. FGFRs-IN-1 exhibits weak inhibitory efficacy against CYP enzymes. FGFRs-IN-1 reduces the expression of α-SMA and collagen I, and inhibits epithelial-mesenchymal transition (EMT) in TGF-β1 stimulated A549 cell. FGFRs-IN-1 exhibits anti-inflammatory activity in Bleomycin (HY-17565)-induced mouse pulmonary fibrosis model and CCl4 (HY-Y0298)-induced mouse liver fibrosis model .
Cat. No.: HY-171807
CAS No.: 189274-78-0
Research Areas:
TC-2559 free base is a α4β2 nicotinic acetylcholine receptor (nAChR) agonists with an EC50 of 0.18 μM. TC-2559 free base shows much weaker potencies on the group of b4-containing nAChR subtypes, α2β4, α4β4 and α3β4 receptors, with EC50s in the range of 10-30 µM. TC-2559 free base can increase the discharge of dopamine cells in the ventral tegmental area (VTA) of rats in vitro, enhancing the excitability and aggressive behavior of VTA dopamine neurons. TC-2559 free base inhibits STAT3 to exert anti-inflammatory properties and relieves mice mechanical allodynia and improve rats cognitive deficits. TC-2559 free base can be used for the study of nerve pain .
Cat. No.: HY-181086
CAS No.: 2864394-30-7
Research Areas:
FLT3/HDAC-IN-3 is a dual inhibitor of FLT3 and HDAC. FLT3/HDAC-IN-3 potently inhibits FLT3 (IC50 = 14 nM), HDAC1 (IC50 = 27 nM), HDAC6 (IC50 = 20 nM), and FLT3 D853Y (IC50 = 55 nM), exhibits weak activity against HDAC8, and shows no activity against HDAC4. FLT3/HDAC-IN-3 possesses kinase selectivity, plasma stability, and stability in human liver microsomes. FLT3/HDAC-IN-3 demonstrates anti-proliferative effects in a variety of hematological malignancy cell lines. FLT3/HDAC-IN-3 shows efficacy in the Jeko-1 xenograft model without observed significant toxicity. FLT3/HDAC-IN-3 can be used in the study of hematological malignancies .
Cat. No.: HY-184656
CAS No.: 3099422-14-4
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VEGFR/PDGFR/CA II-IN-1 is a VEGFR/PDGFR/CA II inhibitor. VEGFR/PDGFR/CA II-IN-1 potently inhibits VEGFR2 (IC50 = 62.66 nM), PDGFRα (IC50 = 18.65 nM), PDGFRβ (IC50 = 5.23 nM), and hCA II (Ki = 19.4 nM), with weaker activity against hCA I (Ki = 154.2 nM) and hCA IX (Ki = 121.0 nM). VEGFR/PDGFR/CA II-IN-1 exhibits potent antiproliferative activity in VEGFR2-BAF3 cells and robust inhibition of angiogenesis in human umbilical vein endothelial cells (HUVECs). VEGFR/PDGFR/CA II-IN-1 inhibits the formation of corneal neovascularization in rabbits through multiple signaling pathways, and significantly reduced intraocular pressure (IOP) in both acute and chronic glaucoma models. VEGFR/PDGFR/CA II-IN-1 can be used to study neovascular glaucoma (NVG) .
Cat. No.: HY-B0383R
CAS No.: 181183-52-8
Synonyms: PNU180638 (Standard)
Target:
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Almotriptan malate (Standard) is the analytical standard of Almotriptan malate (HY-B0383). This product is intended for research and analytical applications. Almotriptan malate (PNU180638) is an orally active, highly selective agonist of the 5-HT1B/1D receptor (5-HT1B/1D receptor), with EC50 values of 1.6 nM and 3.1 nM, respectively. Almotriptan malate shows moderate affinity for the 5-HT1F receptor, and weak affinity for the 5-HT1A, 5-HT6 and 5-HT7 receptors. Almotriptan malate induces intracranial vasoconstriction, inhibits nociceptive neurotransmission in the trigeminocervical complex, and suppresses the release of vasoactive peptides from trigeminal nerve endings. Almotriptan malate can be used in research related to migraine.
Research Areas:
Dihydroergotamine (DFN-19) is a blood-brain barrier-permeable semi-synthetic ergot alkaloid, acting as a full agonist of 5-HT1B/1D receptors (Ki values of 0.3 nM and 2.5 nM, respectively; functional IC50 values of 2 nM and 2.2 nM, respectively). Dihydroergotamine inhibits Forskolin (HY-15371)-stimulated cAMP accumulation, possesses α-adrenergic receptor antagonistic activity and weak dopaminergic agonistic activity. It mediates intracranial cerebrovascular contraction, inhibits the release of neuropeptides such as CGRP/substance P, and suppresses neurogenic inflammation by activating 5-HT1B/1D receptors in the trigeminovascular system. Dihydroergotamine binds to the catalytic site of Trypanosoma cruzi trypanothione reductase and exhibits trypanocidal activity in vitro. Dihydroergotamine can be used in studies related to migraine and trypanosome infections .
Cat. No.: HY-B0871R
CAS No.: 84087-01-4
Research Areas:
Quinclorac (Standard) is the analytical standard of Quinclorac (HY-B0871). This product is intended for research and analytical applications. Quinclorac is a highly selective quinoline carboxylic acid synthetic auxin herbicide. Quinclorac weakly inhibits HPPD, accompanied by a transient decrease in carotenoids. Quinclorac upregulates ACC synthase (ACS), leading to the co-accumulation of ethylene and cyanide, while increasing the ABA/IAA ratio, which induces ROS burst, membrane lipid peroxidation (MDA) and lethal growth inhibition. Residual Quinclorac in soil can cause abnormal growth of subsequent tobacco crops. In calli of Phaseolus vulgaris, Quinclorac induces oxidative stress (increased MDA and decreased RGR), but cells after stepwise pressurized acclimation acquire a constitutive antioxidant state, which remains stable after de-acclimation and tolerates oxidative damage caused by Quinclorac. Quinclorac can be used in studies related to herbicide action mechanisms, bioremediation of soil residues, and adaptive responses of plant cells to oxidative stress .
Cat. No.: HY-B0871S
Research Areas:
Quinclorac- 13C is the 13C-labeled Quinclorac (HY-B0871). Quinclorac is a highly selective quinoline carboxylic acid synthetic auxin herbicide. Quinclorac weakly inhibits HPPD, accompanied by a transient decrease in carotenoids. Quinclorac upregulates ACC synthase (ACS), leading to the co-accumulation of ethylene and cyanide, while increasing the ABA/IAA ratio, which induces ROS burst, membrane lipid peroxidation (MDA) and lethal growth inhibition. Residual Quinclorac in soil can cause abnormal growth of subsequent tobacco crops. In calli of Phaseolus vulgaris, Quinclorac induces oxidative stress (increased MDA and decreased RGR), but cells after stepwise pressurized acclimation acquire a constitutive antioxidant state, which remains stable after de-acclimation and tolerates oxidative damage caused by Quinclorac. Quinclorac can be used in studies related to herbicide action mechanisms, bioremediation of soil residues, and adaptive responses of plant cells to oxidative stress .
Cat. No.: HY-D3119
CAS No.: 2246946-49-4
Research Areas:
MitoAIE1 is a Fluorescent probe for mitochondrial viscosity detection. MitoAIE1 contains a pyridinium structural unit, which endows it with mitochondria-targeting specificity. The detection mechanism of this probe is based on aggregation-induced emission (AIE): in low-viscosity media such as PBS buffer, intramolecular rotation leads to non-radiative energy dissipation, resulting in only weak fluorescence; however, in high-viscosity environments such as the mitochondrial matrix or the vicinity of the inner mitochondrial membrane, such intramolecular motion is restricted, thereby significantly enhancing its fluorescent signal; in addition, this probe is not interfered by changes in microenvironment polarity and pH. Its emission wavelength is 625 nm, with absorption peaks at 325 nm and 450 nm; when transferred from low-viscosity PBS to high-viscosity 99% glycerol, its fluorescence intensity at 625 nm can be increased by 38-fold. It can be used to monitor changes in mitochondrial viscosity during processes such as Stauroporine (HY-15141)-induced apoptosis and starvation-induced mitophagy in live cells, and has good biocompatibility .
Cat. No.: HY-P5142
CAS No.: 193981-10-1
Synonyms: ω-ACTX-Hv1; ω-Atracotoxin-HV1
Research Areas:
Cardiovascular Disease Neurological Disease Inflammation/Immunology
Cat. No.: HY-P5142A
Synonyms: ω-ACTX-Hv1 TFA; ω-Atracotoxin-HV1 TFA
Research Areas:
Cardiovascular Disease Neurological Disease Inflammation/Immunology
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-187629
CAS No.: 2202678-04-2
Research Areas:
HH2853 is an orally active EZH1/EZH2 inhibitor, with an IC50 of 9.26 nM for EZH1 and IC50 values ranging from 2.21 to 3.75 nM for both wild-type and mutant EZH2 . HH2853 simultaneously inhibits the methyltransferase activities of EZH1 and EZH2, blocks the compensatory pathway that arises following EZH2 inhibition, and reduces H3K27me3 levels. HH2853 upregulates the expression of c-Myc and TfR-1 to induce intracellular iron accumulation, and stabilizes GPX4 via HSPA5 to suppress ferroptosis. HH2853 combined with Erastin (HY-15763) synergistically inhibits EZH2 wild-type DLBCL cell proliferation. HH2853 alone shows weak activity against EZH2 wild-type DLBCL and is well tolerated. HH2853 is applicable for research related to diffuse large B-cell lymphoma, non-Hodgkin's lymphoma, epithelioid sarcoma, and follicular lymphoma .
Cat. No.: HY-B0670S
Dihydroergotamine-d3 is the d3-labeled Dihydroergotamine (HY-B0670). Dihydroergotamine (DFN-19) is a blood-brain barrier-permeable semi-synthetic ergot alkaloid, acting as a full agonist of 5-HT1B/1D receptors (Ki values of 0.3 nM and 2.5 nM, respectively; functional IC50 values of 2 nM and 2.2 nM, respectively). Dihydroergotamine inhibits Forskolin (HY-15371)-stimulated cAMP accumulation, possesses α-adrenergic receptor antagonistic activity and weak dopaminergic agonistic activity. It mediates intracranial cerebrovascular contraction, inhibits the release of neuropeptides such as CGRP/substance P, and suppresses neurogenic inflammation by activating 5-HT1B/1D receptors in the trigeminovascular system. Dihydroergotamine binds to the catalytic site of Trypanosoma cruzi trypanothione reductase and exhibits trypanocidal activity in vitro. Dihydroergotamine can be used in studies related to migraine and trypanosome infections .
Cat. No.: HY-D3120
CAS No.: 2246946-53-0
Target:
Research Areas:
LysoAIE2 is a Fluorescent probe for lysosomal viscosity detection and live-cell imaging. Its detection mechanism relies on the aggregation-induced emission effect: it exhibits only weak fluorescence in non-viscous media; in viscous environments, restricted intramolecular motion inhibits non-radiative energy dissipation pathways, thereby significantly enhancing fluorescence intensity. It achieves specific targeting of lysosomes through the proton acceptor property of its indole ring structure, while its hydroxyl group endows it with excellent water solubility. This probe is basically unaffected by microenvironmental polarity and pH within the range of pH 4.0 to pH 8.0, which avoids interference from these factors in viscosity measurement. LysoAIE2 has an emission wavelength of 570 nm. It can be used to monitor lysosomal viscosity changes during processes such as Dexamethasone (HY-14648)-induced lysosomal migration and starvation-induced mitophagy in live cells; at concentrations up to 40 μM, cell viability remains above 80%, demonstrating excellent biocompatibility .
Cat. No.: HY-L942
1,626 compounds
Unlike highly conserved orthosteric sites, allosteric sites exhibit low conservation, high hydrophobicity, weak polarity, confined geometry, and dynamic cryptic properties. Rather than rigid keyhole-like cavities, they typically appear as flexible grooves, subunit interface clefts, or shallow depressions formed by protein conformational changes.
Based on the dynamic, hydrophobic, and elongated nature of allosteric pockets, MCE has carried out targeted fragment modification and screening under strict physicochemical criteria: MW 120–280 Da, HBD ≤ 2, HBA ≤ 3, PSA 30–80 Ų, rotatable bonds ≤ 2, cLogP 1–3.5. High 3D diversity was further ensured by PMI analysis, yielding fragments with excellent shape complementarity to allosteric pockets.
This library contains 1,800 structurally diverse, drug-like fragments, this library supports allosteric drug development and pocket optimization. It significantly improves screening hit rates and enables efficient, precise early-stage R&D of allosteric drugs.
Cat. No.: HY-L941
4,236 compounds
Orthosteric sites are highly conserved, leading to poor subtype selectivity, off-target toxicity and drug resistance in traditional drugs. By contrast, allosteric sites show low conservation, high hydrophobicity, weak polarity, confined geometry and dynamic cryptic properties, granting modulators high selectivity, functional tunability and safety. Thus, allosteric therapy has become a major focus in drug discovery.
MCE curated nearly 1,000 clinical-stage allosteric modulators, analyzed PDB complex structures to identify key pharmacophores and privileged scaffolds, then designed and filtered compounds using rational “scaffold derivation + physicochemical screening” with strict property criteria. The resulting compounds show high rigidity and shape complementarity to shallow, dynamic, hydrophobic allosteric pockets.
This library comprises 4,315 diverse, lead-like compounds ideal for allosteric drug discovery and target screening, covering kinases, GPCRs and more. All are analogs of clinical-stage molecules with similarity > 0.6, combining high druggability and allosteric binding potential to support efficient early-stage R&D.
Cat. No.: HY-188044
Target:
Research Areas:
DC-98-LC74 is a selective modulator of adult skeletal muscle-type nicotinic acetylcholine receptor (α1β1δε), with an EC50 value of 6.5 µM for the human receptor and an IC50 of 13.45 µM for the human α3β4 nicotinic acetylcholine receptor. DC-98-LC74 increases the ligand-free opening probability of the receptor via the ε subunit M2-M3 loop, and prolongs the burst duration and opening probability of wild-type and fast-channel mutant AChR. DC-98-LC74 exerts weak effects on neuronal AChR subtypes and has no agonist activity. DC-98-LC74 prolongs the mouse diaphragm endplate current and improves muscle contractility in isolated neuromuscular preparations from sarcopenic mice. DC-98-LC74 can be used for studies on neuromuscular junction function and myasthenia-related diseases .
Cat. No.: HY-D3084
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C-TPA is a fluorescent probe used for hypochlorite detection and bioimaging of lipid droplet polarity in cancer cells. For hypochlorite detection, when its derivative C-TPA-S is exposed to hypochlorite, an oxidative desulfurization reaction converts the thiocarbonyl group of C-TPA-S to the carbonyl group of C-TPA, thus restoring bright fluorescence from the almost non-fluorescent C-TPA-S. For bioimaging of lipid droplet polarity, the intramolecular charge transfer process between its Triphenylamine (HY-W011998) donor group and Coumarin (HY-N0709) acceptor group endows C-TPA with solvatochromism-it exhibits stronger fluorescence in less polar environments (such as lipid droplets in cancer cells) and weaker fluorescence in more polar environments (such as lipid droplets in normal cells), enabling the differentiation of cancer cells and cancer tissues from normal cells and normal tissues. The excitation wavelength of C-TPA is 405 nm, and the emission wavelengths used for cell and tissue imaging cover 425-475 nm and 500-550 nm; in solvents, its emission peak shifts from 494 nm in non-polar toluene to 528 nm in polar water .
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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
