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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
358 Results for "
PKA
" in MedChemExpress (MCE) Product Catalog:
Products (358)
358 Results for "PKA" in MCE Product Catalog:
Cat. No.: HY-D0077
CAS No.: 195136-58-4
Synonyms: Oregon green 488
Target:
Research Areas:
2',7'-Difluorofluorescein (Oregon green 488) is a fluorescein derivative and a pH-sensitive fluorescent probe (pKa ~4.7). Upon excitation at 488 nm, 2',7'-Difluorofluorescein exhibits pH-sensitive fluorescence intensity through the formation of dianions, while its pH sensitivity decreases under excitation at 450 nm, allowing its use in ratiometric pH analysis. 2',7'-Difluorofluorescein can be used for the quantitative analysis of pH values in the range of 2-7 in submicron aerosol particles. 2',7'-Difluorofluorescein undergoes buffer-mediated and buffer-free excited-state proton transfer between different protonated forms, and its cationic form undergoes rapid excited-state deprotonation. 2',7'-Difluorofluorescein is resistant to photodegradation, maintains stable absorption and fluorescence properties within the physiological pH range, and serves as a fluorescent protein label, a component of Ca 2+ indicators, a fluorescent imaging agent, and an anisotropy probe .
Cat. No.: HY-N0378S3
CAS No.: 287100-69-0
Synonyms: Mannitol-2-13C; Mannite-2-13C
Cat. No.: HY-N0378S6
CAS No.: 1217463-58-5
Synonyms: Mannitol-13C,d2; Mannite-13C,d2
Cat. No.: HY-N0688R
CAS No.: 13476-25-0
Cat. No.: HY-N20708
CAS No.: 89353-99-1
Target:
Cat. No.: HY-W049881
CAS No.: 2521-07-5
Target:
Research Areas:
9-Methyl-β-carboline is a monoamine oxidase inhibitor and dopaminergic modulator, with an IC50 of 1 μM against human MAO-A and an IC50 of 15.5 μM against human MAO-B. 9-Methyl-β-carboline possesses cognitive enhancement potential and can cross the blood-brain barrier. 9-Methyl-β-carboline increases dopamine levels by inhibiting monoamine oxidase activity and microglial proliferation. 9-Methyl-β-carboline activates PKA/PKC and mitochondrial respiratory chain complex I, promotes neurotrophic factor expression and reduces α-synuclein (α-synuclein) levels, thereby reversing neurotoxin-induced dopaminergic neuron damage. 9-Methyl-β-carboline also regulates the PI3K pathway and exerts an anti-proliferative effect on astrocytes. 9-Methyl-β-carboline is widely used in Parkinson's disease-related studies .
Cat. No.: HY-189218
Target:
Aryl Hydrocarbon Receptor Phosphodiesterase (PDE) Cytochrome P450 Interleukin Related Epigenetic Reader Domain
Research Areas:
AhR/PDE4 modulator-1 is a AhR/PDE4D dual-target modulator, with an AhR agonistic EC50 of 0.11 μM and a PDE4D inhibitory IC50 of 2.12 μM. AhR/PDE4 modulator-1 activates the AhR-CYP1A1 signaling pathway, promotes AhR nuclear translocation, and upregulates downstream CYP1A1; it inhibits PDE4D activity, elevates intracellular cAMP levels, and activates the downstream cAMP-PKA-CREB signaling pathway. Topical administration of AhR/PDE4 modulator-1 exerts anti-inflammatory effects in the Imiquimod (HY-B0180)-induced psoriasis-like mouse model, alleviates epidermal hyperplasia and inflammatory infiltration, and suppresses the expression of IL-17A/F. AhR/PDE4 modulator-1 can be used in research related to psoriasis .
Cat. No.: HY-P6292
CAS No.: 2724212-01-3
Research Areas:
Cat. No.: HY-107543R
CAS No.: 634207-53-7
Synonyms: 8-CPT-2'-O-Me-cAMP sodium (Standard)
Target:
Research Areas:
8-pCPT-2′-O-Me-cAMP sodium (Standard) is the analytical standard of 8-pCPT-2′-O-Me-cAMP (sodium) (HY-107543). This product is intended for research and analytical applications. 8-pCPT-2′-O-Me-cAMP (8-CPT-2'-O-Me-cAMP) sodium, an analog of cAMP, is an activator of exchange proteins activated by cAMP (Epac). 8-pCPT-2′-O-Me-cAMP sodium activates Epac1 (EC50 = 2.2 μM), but not PKA (EC50 >10 μM). 8-pCPT-2′-O-Me-cAMP sodium stimulates Epac-mediated Ca2+ release in pancreatic β-cells in vitro. 8-pCPT-2′-O-Me-cAMP sodium is a Rap1 activator. 8-pCPT-2′-O-Me-cAMP sodium enhances the retinal pigment epithelium barrier against the pathological choroidal endothelial cell invasion that occurs in macular degeneration .
Cat. No.: HY-P3075
CAS No.: 112540-82-6
Synonyms: pTHrP (1-34)
Target:
PTHR PKA PKC PI3K Akt ERK NADPH Oxidase Reactive Oxygen Species (ROS) TGF-beta/Smad Caspase Apoptosis NO Synthase
Research Areas:
pTH-Related Protein (1-34) (human,mouse,rat) (pTHrP (1-34)) is a parathyroid hormone-related protein fragment. Binding of pTH-Related Protein (1-34) (human,mouse,rat) to PTH1R triggers cAMP/PKA and PKC signaling, PI3K-mediated Akt and ERK1/2 phosphorylation, NADPH oxidase-dependent ROS generation, and TGF-beta1 and p47phox expression. pTH-Related Protein (1-34) (human,mouse,rat) induces fibronectin upregulation, osteoblast differentiation, osteoclastic bone resorption, bone formation, eNOS/NO-mediated vasodilation, and sensitization of type II pneumocytes to ultraviolet-induced apoptosis (apoptosis) via caspase 3. pTH-Related Protein (1-34) (human,mouse,rat) can be used in research on diabetic nephropathy, breast cancer, acute lung injury, humoral hypercalcemia of malignancy, osteoporosis, and cartilage degeneration .
Research Areas:
Neurological Disease Metabolic Disease Inflammation/Immunology
NYX-2925 is an orally active, blood-brain barrier-permeable NMDAR modulator, with EC50 values of 55 pM, 28 fM, 11 pM and 55 pM against NR2A, NR2B, NR2C and NR2D, respectively . NYX-2925 enhances synaptic plasticity, long-term potentiation, metaplasticity, structural plasticity, learning ability, memory capacity and circadian rhythm amplitude. NYX-2925 regulates the signaling pathways of Src kinase, EIF2, mTOR, CDK5 and protein kinase A (PKA). NYX-2925 increases the levels of PSD-95, GluA1, activated Src and synaptic GluN2B . NYX-2925 is used in the research of neuropathic pain, fibromyalgia, painful diabetic peripheral neuropathy, post-traumatic stress disorder, cognitive impairment, depression, age-related cognitive decline and NMDAR-mediated central nervous system diseases .
Target:
TSPO TRP Channel Microphthalmia Associated Transcription Factor (MITF) PKC PKA p38 MAPK PERK Interleukin Related
Research Areas:
FGIN-1-27 is a blood-brain barrier-penetrant TSPO ligand with a Ki value of 5 nM. FGIN 1-27 inhibits PKC-β, PKA/CREB, p38/ERK MAPK, MITF, tyrosinase, TRP-1, and TRP-2, thereby inhibiting melanogenesis and pigmentation. FGIN-1-27 alleviates X-ray radiation-induced astrocyte mitochondrial hyperfunction, reduces ROS and superoxide production, inhibits excessive activation of A1-type astrocytes, downregulates GFAP and C3 protein expression, and restores astrocyte proliferative capacity. FGIN-1-27 produces anticonvulsant effects in normal mice; in diazepam-withdrawn mice, the brain MDR pathway becomes subsensitive, and the anticonvulsant activity disappears. FGIN-1-27 attenuates pigmentation in zebrafish embryos and ameliorates UVB-induced skin pigmentation in guinea pigs. FGIN-1-27 directly stimulates testicular Leydig cells while upregulating luteinizing hormone levels, causing an acute increase in serum testosterone in male rats. FGIN 1-27 can be used for research related to hyperpigmentation, epilepsy, brain injury, and other diseases .
Cat. No.: HY-L165
282 compounds
Dopamine receptor (DAR), widely distributed in the brain, plays a key role in regulating motor function, motivation, driving force and cognition. The role of DA is mediated by D1-type (D1, D5) and D2-type receptors (D2S, D2L, D3, D4), which are distributed in presynaptic, postsynaptic and extrasynaptic, projection neurons and interneurons. Each receptor has a different function. D1 and D5 receptors couple with G stimulation sites and activate Adenylyl cyclase. The activation of Adenylyl cyclase leads to the production of the second messenger cAMP, which leads to the production of protein kinase A (PKA), which leads to further transcription in the nucleus. D2 to D4 receptors are coupled to G inhibitory sites to inhibit adenylyl cyclase and activate potassium Ion channel. These receptors utilize phosphorylation cascades or direct membrane interactions to affect the functions of voltage-gated and neurotransmitter-gated channels, cytoplasmic enzymes, and transcription factors. Dopamine receptor plays an important role in daily life.
MCE designs a unique collection of 282 small molecules related to dopamine receptor. It is a good tool for screening drugs from nervous system disease.
Cat. No.: HY-L950
2,787 compounds
Seven-membered rings are privileged medium-sized scaffolds with distinct twist-chair conformations and greater 3D diversity than five- and six-membered rings. Their flexible conformations allow induced-fit protein binding and precise pharmacophore positioning. They also modulate Fsp³, pKa and logP to enhance solubility and permeability. Azepanes, oxepanes and benzodiazepines serve as bioisosteres for hit discovery against GPCRs, ion channels and kinases.
Widely found in plant and microbial alkaloids, seven-membered heterocycles show excellent biocompatibility and target affinity. They underpin many approved drugs for CNS, cancer and infectious diseases, including diazepam, imipramine and carbamazepine. Clinical candidates further highlight their unique value. However, high transannular strain and synthetic difficulty limit their availability, leaving them rare in standard screening libraries.
MCE 7 Membered Scaffold Library contains 2,792 structurally diverse, lead-like molecules covering azepanes, oxepanes, benzodiazepines and dibenzazepines. With varied substitutions, chiral centers and synthetic accessibility, it fills the shortage of medium-ring scaffolds. Ideal for HTS, virtual screening and SAR studies, these novel, patent-clear compounds offer a distinctive starting point for drug discovery in CNS disorders, oncology, antivirals and challenging targets such as PPIs.
Cat. No.: HY-101059R
CAS No.: 142720-24-9
FGIN 1-27 (Standard) is the analytical standard of FGIN 1-27 (HY-101059). This product is intended for research and analytical applications. FGIN-1-27 is a blood-brain barrier-penetrant TSPO ligand with a Ki value of 5 nM. FGIN 1-27 inhibits PKC-β, PKA/CREB, p38/ERK MAPK, MITF, tyrosinase, TRP-1, and TRP-2, thereby inhibiting melanogenesis and pigmentation. FGIN-1-27 alleviates X-ray radiation-induced astrocyte mitochondrial hyperfunction, reduces ROS and superoxide production, inhibits excessive activation of A1-type astrocytes, downregulates GFAP and C3 protein expression, and restores astrocyte proliferative capacity. FGIN-1-27 produces anticonvulsant effects in normal mice; in diazepam-withdrawn mice, the brain MDR pathway becomes subsensitive, and the anticonvulsant activity disappears. FGIN-1-27 attenuates pigmentation in zebrafish embryos and ameliorates UVB-induced skin pigmentation in guinea pigs. FGIN-1-27 directly stimulates testicular Leydig cells while upregulating luteinizing hormone levels, causing an acute increase in serum testosterone in male rats. FGIN 1-27 can be used for research related to hyperpigmentation, epilepsy, brain injury, and other diseases .
Cat. No.: HY-L913
105 compounds
Recently, significant advancements in tyrosine-targeting electrophiles have primarily occurred in the field of protein-protein interactions (PPIs), where cysteine residues are often underrepresented and novel chemistries are needed to address these interfaces. In this context, tyrosines are frequently more accessible compared to more buried binding sites. Moreover, they are commonly found at "hot spots," which are functional epitopes of PPIs, with 12.3% of the residues consisting of tyrosines. This prevalence is likely due to the hydrophobic nature of tyrosine, its ability to participate in aromatic π-interactions, and its capacity for hydrogen bonding. Beyond PPIs, some progress has also been made in covalent tyrosine targeting in other areas where more commonly addressed side chains are lacking. Even though tyrosine has a slightly lower pKa value compared to the protonated lysine side chain (approximately 10 vs. 10.5 for the unprotected amino acid side chains), significantly less progress has been made in the development of tyrosine-targeted covalent ligands compared to lysine. This is likely due to the reduced flexibility of the tyrosine side chain and the greater steric hindrance of its hydroxy group, which makes it more challenging to adopt suitable reaction geometries.
Through careful selection, we constructed a structural filter containing over 110 electrophilic groups. By analyzing the electrophilic fragments selected by the structural filter, we removed any molecules with trivial or undesirable structural features. Ultimately, we obtained 124 fragment molecules which can target tyrosine residue and can be used for fragment-based covalent 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
