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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
162 Results for "
cell penetrant
" in MedChemExpress (MCE) Product Catalog:
Products (162)
162 Results for "cell penetrant" in MCE Product Catalog:
172
172 Publications Verification
Synonyms: trans-Resveratrol; SRT501
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 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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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:
Research Areas:
Cardiovascular Disease Infection Neurological Disease Cancer
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: 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) .
26
26 Cited Publications
Synonyms: VE-822; VX-970; M6620
Berzosertib (VE-822) is an orally active, CNS-penetrant, and selective ATR kinase inhibitor. Berzosertib blocks ATR kinase activity, abrogates G2/M cell cycle checkpoint, impairs DNA damage repair. Berzosertib induces apoptosis, inhibnits conlony migration, inhibits cell proliferation, and activates cGAS-STING axes in cancer cells. Berzosertib can be used for the research of cancers, such as head and neck squamous cell carcinoma, and colorectal cancer .
26
26 Cited Publications
Cat. No.: HY-13902A
CAS No.: 1428935-04-9
Synonyms: VE-822 hydrochloride; VX-970 hydrochloride; M6620 hydrochloride
Berzosertib (VE-822) hydrochloride is an orally active, CNS-penetrant, and selective ATR kinase inhibitor. Berzosertib hydrochloride blocks ATR kinase activity, abrogates G2/M cell cycle checkpoint, impairs DNA damage repair. Berzosertib hydrochloride induces apoptosis, inhibnits conlony migration, inhibits cell proliferation, and activates cGAS-STING axes in cancer cells. Berzosertib hydrochloride can be used for the research of cancers, such as head and neck squamous cell carcinoma, and colorectal cancer .
14
Lonafarnib (Sch66336) is an orally active, blood-brain barrier penetrant farnesyltransferase (FPTase) inhibitor. Lonafarnib increases the phosphorylation levels of Akt, CaMKII and CREB, upregulates BDNF expression in the hippocampus, elevates the content of α7nAChR on cell membranes, and blocks the isoprenylation of H-Ras. Lonafarnib repairs synapses and reverses spatial memory deficits in Aβ1-42 model mice. Lonafarnib inhibits RSV fusion and replication, and alleviates virus-induced lung injury. Lonafarnib activates the lysosomal and autophagic pathways, and reduces the phosphorylation and aggregation of tau. Lonafarnib acts synergistically with Sorafenib (HY-10201) to promote apoptosis, and inhibits the proliferation and invasion of melanoma cells. Lonafarnib inhibits the farnesylation of progerin, repairs nuclear membrane defects, and activates the cGAS-STING-STAT1 signaling pathway. Lonafarnib can be used in research related to diseases including Alzheimer's disease, viral infections, melanoma, and progeria .
12
12 Cited Publications
Synonyms: 2,3,5-Triphenyltetrazolium chloride; TPTZ; TTC
11
Target:
Research Areas:
Elrelesertib (AZD1390) is an orally active, brain-penetrant ATM kinase inhibitor with IC50 values of 0.78 nM. Elrelesertib blocks ATM-dependent DNA damage response, inhibits ATM autophosphorylation and downstream Chk2, Rad50 phosphorylation, and accumulates at DNA breaks. Elrelesertib acts as a radiosensitizer, induces apoptosis, genomic instability, G2-M cell cycle arrest, ROS elevation, and mitochondrial membrane potential alteration. Elrelesertib has low efflux liability against P-gp and BCRP. Elrelesertib can be used for the research of central nervous system malignancies, glioblastoma multiforme, glioma, lung cancer brain metastases, and breast cancer .
7
Research Areas:
Infection Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
Zorifertinib (AZD3759) is a potent, orally active, BBB-penetrant, EGFR inhibitor. At Km ATP concentrations, the IC50s are 0.3, 0.2, and 0.2 nM for EGFR wt, EGFR L858R, and EGFR exon 19Del, respectively. Zorifertinib induces cancer cell apoptosis. Zorifertinib has antitumor activity, and can be used for NSCLC, HCC etc. research .
6
6 Cited Publications
Synonyms: Alflutinib; Furmonertinib; AST2818
Firmonertinib (Alflutinib; Furmonertinib) is an orally active, mutant-selective, and highly brain penetrant EGFR inhibitor. Firmonertinib inhibits EGFR active mutations as well as the T790M acquired resistant mutation. Firmonertinib has the potential for the research of cancer diseases, especially advanced non-small cell lung cancer (NSCLC) with EGFR ex20ins mutation .
6
6 Cited Publications
Synonyms: Alflutinib mesylate; Furmonertinib mesylate; AST2818 mesylate
Target:
Research Areas:
Firmonertinib (Alflutinib; Furmonertinib) mesylate is is an orally active, mutant-selective, and blood-brain barrier penetrant EGFR inhibitor. Firmonertinib mesylate inhibits EGFR active mutations as well as the T790M acquired resistant mutation. Firmonertinib mesylate has the potential for the research of cancer diseases, especially advanced non-small cell lung cancer (NSCLC) with EGFR ex20ins mutation .
6
6 Cited Publications
Synonyms: Methylglyoxal-bis(guanylhydrazone); MGBG; Methyl-GAG
Mitoguazone (Methylglyoxal-bis(guanylhydrazone)) is a synthetic polycarbonyl derivative with potent antineoplastic activity. Mitoguazone is a brain-penetrant and competitive S-adenosyl-methionine decarboxylase (SAMDC) inhibitor that disrupts polyamine biosynthesis. Mitoguazone induces cell apoptosis. Mitoguazone inhibits HIV DNA integration into the cellular DNA in both monocytes and macrophages. Mitoguazone has the potential for acute leukemia, Hodgkin's and non-Hodgkin's lymphoma treatment .
5
5 Cited Publications
Target:
Research Areas:
GSK805 is an orally active and CNS penetrant RORγt inhibitor. GSK805 inhibits RORγ and Th17 cells differentiation with pIC50 values of 8.4 and >8.2. GSK805 inhibits the function of Th17 cells. GSK805 can be used for the research of immunity .
5
5 Cited Publications
Target:
Research Areas:
GSK467 is a cell penetrant and selective KDM5B (JARID1B or PLU1) inhibitor with a Ki of 10 nM and an IC50 of 26 nM. GSK467 shows 180-fold selectivity for KDM4C and no measurable inhibitory effects toward KDM6 or other Jumonji family members .
5
5 Cited Publications
Cat. No.: HY-N0430A
CAS No.: 1198398-71-8
4
4 Cited Publications
Cat. No.: HY-W015309
CAS No.: 334-48-5
4
4 Cited Publications
Synonyms: 4,4′-Diaminodiphenyl sulfone; DDS
Research Areas:
Dapsone (4,4′-Diaminodiphenyl sulfone) is an orally active and blood-brain penetrant sulfonamide antibiotic with bacteriostatic, antimycobacterial and antiprotozoal activities . Dapsone?exerts effective antileprosy activity?and inhibits folate synthesis in cell extracts of?M. leprae. Dapsone is used for dermatologic disorder research, including leprosy, dermatitis herpetiformis, acne vulgaris et al .
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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
