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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
887 Results for "
penetrant
" in MedChemExpress (MCE) Product Catalog:
Products (887)
887 Results for "penetrant" in MCE Product Catalog:
306
Research Areas:
(+)-JQ-1 (JQ1), a chemical probe, is a potent, specific, CNS-penetrant and reversible BET bromodomain inhibitor, with IC50s of 77 and 33 nM for the first and second bromodomain (BRD4(1/2)) . (+)-JQ-1 also activates autophagy .
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98
98 Cited Publications
Target:
Research Areas:
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 demonstrates desirable PK properties in varies animals. PLX5622 is predominantly administered via ad libitum diets with a dose of 1200 ppm .
98
98 Cited Publications
Cat. No.: HY-114153A
Purity: 99.88%
Target:
Research Areas:
PLX5622 hemifumarate is a highly selective brain penetrant and orally active CSF1R inhibitor (IC50=0.016 μM; Ki=5.9 nM). PLX5622 hemifumarate allows for extended and specific microglial elimination, preceding and during pathology development. PLX5622 hemifumarate demonstrates desirable PK properties in varies animals .
98
98 Cited Publications
Cat. No.: HY-P1061
CAS No.: 867021-83-8
Research Areas:
98
98 Cited Publications
Cat. No.: HY-P1061A
CAS No.: 2803948-60-7
Research Areas:
92
92 Cited Publications
Target:
Research Areas:
MPTP hydrochloride is a brain penetrant dopaminergic neurotoxin. MPTP hydrochloride can be used to induce Parkinson’s Disease model. MPTP hydrochloride, a precusor of MPP +, induces apoptosis . MPTP hydrochloride has been verified by MCE with professional biological experiments.
92
92 Cited Publications
Cat. No.: HY-W114750
CAS No.: 28289-54-5
Target:
Research Areas:
MPTP (1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine) is a brain penetrant dopamine neurotoxin. MPTP can be used to induce Parkinson’s Disease model. MPTP, a precusor of MPP +, induces apoptosis .
90
90 Cited Publications
Synonyms: BKM120 Hydrochloride; NVP-BKM120 Hydrochloride
Research Areas:
Infection Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
Buparlisib Hydrochloride (BKM120 Hydrochloride) is a CNS-penetrant pan-class I PI3K inhibitor, with IC50 of 52 nM/166 nM/116 nM/262 nM for p110α/p110β/p110δ/p110γ, respectively.
78
78 Cited Publications
Synonyms: FTY720 free base
Target:
Research Areas:
Infection Neurological Disease Inflammation/Immunology Cancer
Fingolimod (FTY720 free base) is a brain-penetrant sphingosine 1-phosphate (S1P) antagonist with an IC50 of 0.033 nM in K562 and NK cells. Fingolimod also is a pak1 activator, a immunosuppressant .
64
49
49 Cited Publications
Cat. No.: HY-B0568
CAS No.: 30652-11-0
Target:
Deferiprone is a potent, orally active, brain-penetrant, cell-penetrant, skin-permeable, free iron chelating agent. Deferiprone inhibits the proliferation and migration, and stimulates apoptosis in tumor cell. Deferiprone can inhibit KDM. Deferiprone has antianemic, neuroprotective, anti-inflammatory, antioxidant, and antidotal activity. Deferiprone can be used in cancer, cardiovascular disease, infection, inflammation, and neurological disease study .
42
42 Cited Publications
Synonyms: BLZ945 hydrochloride
Sotuletinib (BLZ945) hydrochloride is a potent, selective, orally active and brain-penetrant CSF-1R (c-Fms) inhibitor with an IC50 of 1 nM, showing more than 1,000-fold selectivity against its closest receptor tyrosine kinase homologs. Sotuletinib hydrochloride can be used for microglia depletion, and for tumor and CNS-related disease research. .
42
Target:
Research Areas:
Sotuletinib (BLZ945) is a potent, selective, orally active and brain-penetrant CSF-1R (c-Fms) inhibitor with an IC50 of 1 nM, showing more than 1,000-fold selectivity against its closest receptor tyrosine kinase homologs. Sotuletinib can be used for microglia depletion, and for tumor and CNS-related disease research .
42
42 Cited Publications
Synonyms: RTA 402; NSC 713200; CDDO Methyl ester
Target:
Research Areas:
Bardoxolone methyl (RTA 402) is an orally active and blood-brain-barrier-penetrant activator of Nrf2 and an inhibitor of SARS-CoV-2 3CL protease. Bardoxolone methyl inhibits SARS-CoV-2 replication in Vero cells with an EC50 value of 0.29 μM. Bardoxolone methyl increases levels of pNrf2 and HO-1, inhibits inflammatory mediators like pNFκB and MCP-1. Bardoxolone methyl activates the Nrf2 pathway to enhance antioxidant and anti-inflammatory responses, inhibits viral replication, and improves mitochondrial function. Bardoxolone methyl can be used in research on chemotherapy-induced neuropathic pain (CINP), COVID-19, and chronic kidney disease (CKD) .
40
40 Cited Publications
Synonyms: LY231514 disodium hemipenta hydrate
Target:
Research Areas:
Infection Neurological Disease Inflammation/Immunology Cancer
Pemetrexed (LY231514) disodium hemipenta hydrate is a CNS-penetrant antifolate, the Ki values of the pentaglutamate of LY231514 are 1.3, 7.2, and 65 nM for inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively.
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Research Areas:
Lorlatinib (PF-06463922) is a selective, orally active, brain-penetrant and ATP-competitive ROS1/ALK inhibitor with anticancer activity. Lorlatinib has Kis of <0.025 nM, <0.07 nM, and 0.7 nM for ROS1, wild type ALK, and ALK L1196M, respectively. Lorlatinib targets to EML4-ALK, and inhibits ALK phosphorylation with IC50s of 15-43 nM (ALK L1196), 14-80 nM (ALK G1269A), 38-50 nM (ALK 1151Tins), 77-113 nM (ALK G1202R), respectively .
35
35 Cited Publications
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33
Research Areas:
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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
