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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
105 Results for "
states
" in MedChemExpress (MCE) Product Catalog:
Products (105)
105 Results for "states" in MCE Product Catalog:
98
98 Publications Verification
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PLX5622 is a highly selective brain penetrant and orally active CSF1R inhibitor (IC50=0.016 μM; Ki=5.9 nM). PLX5622 allows for extended and specific microglial cells elimination, preceding and during pathology development. PLX5622 is an ideal choose for microglia function research in healthy or diseased states. PLX5622 has been verified by MedChemExpress, which demonstrates desirable microglia depletion efficiency in mice. PLX5622 is predominantly administered via ad libitum diets with a dose of 1200 ppm .
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58 Cited Publications
MRTX1133 is a noncovalent, potent, and selective alkyne-based KRAS G12D inhibitor. MRTX1133 optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated KD against KRAS G12D of 0.2 pM. MRTX1133 prevents SOS1-catalyzed nucleotide exchange and/or formation of the KRAS G12D/GTP/RAF1 complex, thereby inhibiting mutant KRAS-dependent signal transduction. MRTX1133 selectively inhibits KRAS G12D mutant, but not KRAS wild-type, tumor cells. MRTX1133 has single digit nanomolar activity in cellular assays and marked in vivo efficacy in tumor models harboring KRAS G12D mutations .
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19 Cited Publications
Synonyms: EPZ019997 dihydrochloride
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GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC50=3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8)). GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) produces a shift in arginine methylation states, alters exon usage, and has strong anti-cancer activity .
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GSK3368715 (EPZ019997) is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC50=3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8)). GSK3368715 (EPZ019997) produces a shift in arginine methylation states, alters exon usage, and has strong anti-cancer activity .
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8 Cited Publications
Cat. No.: HY-114153C
CAS No.: 1303420-67-8
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PLX5622 in AIN-76A Diet (1200 ppm) contains 1200 mg of PLX5622 (HY-114153) per Kg of AIN-76 diet and it can be used for microglia clearance. PLX5622 in AIN-76A Diet (1200 ppm) is ideal choose for microglia function research in healthy/diseased states. PLX5622 in AIN-76A Diet (1200 ppm) has been verified by MedChemExpress (MCE).The color of PLX5622 in AIN-76A Diet (1200 ppm) provided by MCE is blue. Meanwhile, MCE will provide an equal amount of PLX5622-Free AIN-76A Diet (no added pigments) as a complimentary offering, which is used for the control group.
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5 Cited Publications
Synonyms: NG,NG-Dimethylarginine
Category:
Cardiovascular Disease Human Gut Microbiota Metabolites Microorganisms Ketones, Aldehydes, Acids Endogenous metabolite Disease Research Fields
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3
3 Cited Publications
Cat. No.: HY-W015239
CAS No.: 605-62-9
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KAT8-IN-1 is a lysine (K) acetyltransferase 8 (KAT8) inhibitor, with IC50s of 141 μM (KAT8), 221 μM (KAT2B), 106 μM (KAT3B), respectively. KAT8 inhibits histone acetyltransferases (HATs), and could result in disease states, such as cancer or inflammatory diseases .
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Category:
Alkaloids Neurological Disease Other Alkaloids Anisodus tanguticus (Maxinowicz) Pascher Plants Solanaceae Disease Research Fields
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1
1 Cited Publications
STX-721 is an orally active, irreversible, covalent EGFR exon 20 insertion (ex20ins) inhibitor that selectively targets ex20ins-mutant dynamic protein states. STX-721 potently inhibits the kinase activity of EGFR ex20ins mutants (NPG, ASV, SVD). STX-721 inhibits phosphorylation of EGFR (pEGFR Y1068) and downstream ERK (pERK Thr202/Tyr204), and suppresses proliferation of ex20ins-mutant Ba/F3 cells and human NSCLC cell lines (NCI-H2073 ASV KI, CUTO-14 ASV). STX-721 induces tumor regression in EGFR ex20ins-mutant PDX/CDX models. STX-721 can be used for the study of non-small cell lung cancer (NSCLC) harboring EGFR or HER2 ex20ins mutations .
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1 Cited Publications
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PERK-IN-4 is a potent and selective PERK (protein kinase R (PKR)-like endoplasmic reticulum kinase) inhibitor with an IC 50 of 0.3 nM. PERK is activated in response to a variety of endoplasmic reticulum stresses implicated in numerous disease states .
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1 Cited Publications
Cat. No.: HY-A0022A
CAS No.: 63302-99-8
Synonyms: Azafen dihydrochloride monohydrate; Pipofezin dihydrochloride monohydrate; Pipofezine dihydrochloride monohydrate; Azaphenonxazine dihydrochloride monohydrate
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Azaphen (Pipofezin) dihydrochloride monohydrate is an orally active serotonin reuptake inhibitor. Azaphen dihydrochloride monohydrate potentiates sympathomimetic compound effects. Azaphen dihydrochloride monohydrate can be used for the research of depressive states .
Cat. No.: HY-159852
CAS No.: 2971769-60-3
BBO-10203 is a potent inhibitor of PI3Kα and KRAS G12C, selectively and covalently binding to Cys242 in the RAS-Binding Domain of PI3Kα, and inhibiting both the GTP-bound and GDP-bound states of KRAS G12C with an IC50 of 0.031 nM and an EC50 of 0.02 nM. BBO-10203 disrupts the interaction between RAS isoforms and PI3Kα, leading to the inhibition of RAS-mediated PI3Kα activation, and reduces pERK expression, cell growth, and induces G1 arrest and apoptosis. BBO-10203 can be used for the research of breast cancer, colorectal cancer, and non-small cell lung cancer .
Synonyms: CXA-10; 10-Nitrooleate
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10-Nitrooleic acid (CXA-10), a nitro fatty acid, has potential effects in disease states in which oxidative stress, inflammation, fibrosis, and/or direct tissue toxicity play significant roles .
Synonyms: NT-814; BAY3427080
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Elinzanetant is an orally active and selective NK-1 and NK-3 receptor antagonist. Elinzanetant alleviates menopause-associated vasomotor symptoms, including hot flashes and night sweats. Elinzanetant reduces estradiol and progesterone levels. Elinzanetant can be used for the research of moderate to severe vasomotor and sleep disorders associated with menopause .
Cat. No.: HY-NP004
Synonyms: CVF
Cat. No.: HY-W116335A
CAS No.: 21645-51-2
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Dried aluminum hydroxide gel, United States Pharmacopeia (USP) Reference Standard is a commonly used antacid with remarkable compound adhesion and release activity. Dried aluminum hydroxide gel, United States Pharmacopeia (USP) Reference Standard can effectively neutralize gastric acid and relieve stomach discomfort. Dried aluminum hydroxide gel, United States Pharmacopeia (USP) Reference Standard is also often used as an adjuvant in vaccines to enhance immune responses. Dried aluminum hydroxide gel, United States Pharmacopeia (USP) Reference Standard can improve the stability and bioavailability of compounds in preparations .
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Pericyazine (Propericiazine) is a first-generation antipsychotic agent that is used as an adjunct to the short-term management of severe anxiety states and psychosis . Pericyazine is a selective D2-dopamine receptor antagonist . Pericyazine has adrenolytic, anticholinergic, and extrapyramidal effects .
Cat. No.: HY-175238
CAS No.: 1309288-83-2
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KI-DX-014 is a DDX21 inhibitor with high RNA-binding inhibitory activity (IC50 of 3.31 μM). KI-DX-014 targets DDX21’s intrinsically disordered C-terminal domain, inhibits DDX21-structured RNA interaction, modulates DDX21’s RNA-dependent ATPase activity, and disrupts DDX21 biomolecular condensate formation. KI-DX-014 attenuates in vitro P-TEFb release from the 7SK snRNP complex, suppresses P-TEFb-dependent RNA polymerase II CTD phosphorylation, and induces developmental defects in zebrafish embryos. KI-DX-014 acts as a chemical probe for dissecting DDX21 functions in normal physiology and disease states. KI-DX-014 can be used for cancers and neurodegenerative disorders research .
Synonyms: D-Trans-Allethrin; Esbiol
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S-Bioallethrin (D-Trans-Allethrin) is a pyrethroid insecticide. S-Bioallethrin disrupts nerve function by modifying the gating kinetics of transitions between the conducting and nonconducting states of voltage-gated sodium channels. S-Bioallethrin also causes inhibition of lymphocyte proliferation and induces histamine release from human basophils .
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Pyruvate carboxylase is a key mitochondrial anaplerotic enzyme that catalyzes the conversion of pyruvate to oxaloacetate. Pyruvate carboxylase not only maintains tricarboxylic acid cycle activity and redox homeostasis, but also drives hepatic gluconeogenesis and fatty acid synthesis. The activity of Pyruvate carboxylase is upregulated in insulin-resistant states, exacerbating hepatic glucose production. Pyruvate carboxylase also shows significantly enhanced expression in early-stage non-small cell lung cancer (NSCLC). Pyruvate carboxylase promotes tumor proliferation by supporting nucleotide and lipid synthesis, and its functional deficiency cannot be compensated by glutaminolysis. Pyruvate carboxylase can be used in the research of prediabetes type 2 and NSCLC .
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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
