Search Result
Results for "
brain tumor
" in MedChemExpress (MCE) Product Catalog:
6
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-13459
-
|
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Smo
|
Cancer
|
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PF-5274857 is a potent, selective, orally active and brain-penetrant antagonist of Smo, with an IC50 of 5.8 nM and Ki of 4.6 nM. PF-5274857 has potential for research of tumor types including brain tumors and brain metastasis driven by an activated Hh pathway .
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- HY-153432
-
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Cholinesterase (ChE)
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Neurological Disease
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TRV-7019 is a BBB-penetrable radioligand for brain imaging that target butyrylcholinesterase. TRV-7019 can be used for the diagnosis of an amyloid disease, multiple sclerosis, a brain tumor, or butyrylcholinesterase activity .
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-
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- HY-105155
-
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RMP 7
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Bradykinin Receptor
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Cancer
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Lobradimil (RMP 7), a synthetic bradykinin analog, is a potent and selective bradykinin B2 receptor agonist (Ki: 0.54 nM). Lobradimil increases the permeability of the BBB. Lobradimil can be used in the research of brain tumors .
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-
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- HY-139662
-
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E1/E2/E3 Enzyme
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Cancer
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HB007 is a small ubiquitin-related modifier 1 (SUMO1) degrader. HB007 induces ubiquitination and degradation of SUMO1, resulting in reduced tumor growth in vivo. HB007 can be used for the research of brain, breast, colon, and lung cancers .
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-
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- HY-13459A
-
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Smo
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Cancer
|
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PF-5274857 hydrochloride is a potent, selective, orally active and brain-penetrant antagonist of Smo, with an IC50 of 5.8 nM and Ki of 4.6 nM. PF-5274857 hydrochloride has potential for research of tumor types including brain tumors and brain metastasis driven by an activated Hh pathway .
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-
-
- HY-12624
-
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ON123300
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CDK
AMPK
PDGFR
|
Cancer
|
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Narazaciclib (ON123300), a strong and brain-penetrant multi-kinase inhibitor, inhibits CDK4 (IC50=3.9 nM), Ark5 (IC50=5 nM), PDGFRβ (IC50=26 nM), FGFR1 (IC50=26 nM), RET (IC50=9.2 nM), and FYN (IC50=11 nM). Single agent Narazaciclib causes a dose-dependent suppression of phosphorylation of Akt as well as activation of Erk in brain tumors . Narazaciclib inhibits CDK6 with an IC50 of 9.82 nM .
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- HY-133016
-
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MetAP
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Cardiovascular Disease
Cancer
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M8891 is an orally active, reversible and brain penetrant Methionine Aminopeptidase-2 (MetAP-2) inhibitor with an IC50 of 54 nM and a Ki of 4.33 nM. M8891 does not inhibit MetAP-1 (IC50>10 µM) . M8891 inhibits growth of primary endothelial cells as well as tumor cells and demonstrates antiangiogenic and antitumoral activity .
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-
-
- HY-124813
-
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113B7
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FAK
EGFR
MMP
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Cancer
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PDZ1i is a potent, BBB-penetrated and specific MDA-9/Syntenin inhibitor. PDZ1i inhibits crucial GBM (glioblastoma multiforme) signaling involving FAK and EGFRvIII. PDZ1i reduces MMP secretion. PDZ1i can improve survival of brain tumor-bearing mice and reduce tumor invasion .
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- HY-153863
-
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MEK
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Cancer
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MS934 is a novel improved VHL-recruiting MEK 1/2 degrader. MS934 has anti-proliferation potency at inhibiting the growth of HT-29 cells with a GI50 value of 0.023 μM. MS934 can be used for the research of variety of human cancers, such as melanoma, nonsmall cell lung cancer (NSCLC), colorectal cancer, primary brain tumors, and hepatocellular carcinoma .
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-
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- HY-136201
-
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Others
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Cancer
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Sodium Glucoheptonate is used as a kit for radio-labeling with Tc-99m. Tc-99m glucoheptonate is kidney- and brain-imaging agent, and can be used in brain-tumor detection .
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-
-
- HY-137442
-
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EOS-850
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Adenosine Receptor
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Cancer
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Inupadenant is an orally active, highly selective A2A receptor antagonist. Inupadenant is not brain-penetrant. Inupadenant has potent anti-tumor activity .
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-
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- HY-142118A
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AP 12009 sodium
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TGF-beta/Smad
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Cancer
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Trabedersen sodium is an antisense oligodeoxynucleotide that specifically inhibits TGF-β2 (TGF-beta/Smad). Trabedersen sodium can be used for the study of malignant brain tumors and other solid tumors overexpressing TGF-β2, such as those of the skin, pancreas and colon .
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- HY-W011522
-
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Bacterial
Apoptosis
Antibiotic
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Infection
Cancer
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Taurolidine is a broad-spectrum antimicrobial for the prevention of central venous catheter-related infections. Taurolidine has a direct and selective antineoplastic effect on brain tumor cells by the induction of apoptosis .
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- HY-137442A
-
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EOS-850 hydrochloride
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Adenosine Receptor
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Cancer
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Inupadenant (EOS-850) hydrochloride is an orally active, highly selective A2A receptor antagonist. Inupadenant hydrochloride is not brain-penetrant. Inupadenant hydrochloride has potent anti-tumor activity .
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- HY-142118
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AP 12009
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TGF-beta/Smad
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Cancer
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Trabedersen (AP 12009) is an antisense oligodeoxynucleotide that specifically inhibits TGF-β2 (TGF-beta/Smad). Trabedersen can be used for the study of malignant brain tumors and other solid tumors overexpressing TGF-β2, such as those of the skin, pancreas and colon .
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- HY-113303
-
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Endogenous Metabolite
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Neurological Disease
Cancer
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FAPy-adenine is an oxidized DNA base. Fapy-adenine shows an increased trend levels in the Alzheimer's disease brain. Oxidized nucleosides are biochemical markers for tumors, aging, and neurodegenerative diseases .
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- HY-D0022
-
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5-AF
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Fluorescent Dye
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Others
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5-Aminofluorescein (5-AF) is a fluorescence marker, covalently bound to human serum albumin. The excitation wavelength is 495 nm and the emission wavelength is 535 nm .
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- HY-15649
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UNC1215
3 Publications Verification
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Histone Methyltransferase
Apoptosis
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Cancer
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UNC1215 is a potent and selective inhibitor for the methyllysine (Kme) reading domain function of L3MBTL3 with a Kd value of 120 nM and an IC50 of 40 nM. UNC1215 has the potential to treat malignant brain tumor.
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- HY-P99849
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ABT-806
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EGFR
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Cancer
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Depatuxizumab is a brain-penetrant and humanized tumor-specific anti EGFR monoclonal antibody. Depatuxizumab inhibits the growth of xenograft models of mutant EGFRvIII and wild-type EGFR. Depatuxizumab can be used for research on cancer .
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- HY-12768B
-
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BLZ945 dihydrochloride
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c-Fms
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Neurological Disease
Cancer
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Sotuletinib (BLZ945) dihydrochloride is an orally active and blood-brain barrier-permeable CSF1-R-specific inhibitor (IC50=1 nM). Sotuletinib (BLZ945) dihydrochloride induces tumor cell apoptosis and effectively inhibits tumor growth in mouse models. Sotuletinib dihydrochloride can be used in cancer and amyotrophic lateral sclerosis (ALS) research .
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- HY-E70228
-
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Others
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Cancer
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Cathepsin H, human liver is an aminopeptidase and an endopeptidase. Involved in the catabolism of proteins in the lysosomal system. Cathepsin H, human liver has a key role in the regulation of the biological behavior of tumor cells and the pathological processes of brain diseases .
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- HY-N0123
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Aloin-A; Barbaloin-A
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Others
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Cancer
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Aloin (Aloin-A; Barbaloin-A) is a natural anti-tumor anthraquinone glycoside with iron chelating activity. Aloin induces the differentiation of MC3T3-E1 cells into osteoblasts through MAPK-mediated Wnt and Bmp signaling pathways. Alkaline phosphatase (ALP) is an early marker of osteoblast differentiation, and the activity of ALP is also enhanced by Aloin. Aloin also reduces brain edema, reduces blood-brain barrier disruption and improves cortical impact injuries. Aloin is used in research into osteoporosis and traumatic brain injury (TBI) .
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- HY-123410
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Cannabinoid Receptor
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Cancer
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KM-233 is a classical cannabinoid with good blood brain barrier penetration. KM-233 possesses a selective affinity for the CB2 receptors relative to THC. KM-233 is effective at reducing U87 glioma tumor burden, and can be used for glioma research .
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- HY-134990
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Apoptosis
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Cancer
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Hematoporphyrin monomethyl ether, second generation of porphyrin-related photosensitizer, is characterized by its single form, high yield of singlet oxygen, high selectivity, and low toxicity, which has been widely used in the diagnosis and research of various tumors, including lung cancer, bladder cancer, and nevus flammeus and brain glioma .
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- HY-119696S
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Isotope-Labeled Compounds
Drug Metabolite
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Neurological Disease
Cancer
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MTIC-d3 is deuterium labeled MTIC. MTIC is the active metabolite of Temozolomide (TMZ). MITC has lower bioavailability in the brain compared with TMZ, because the agent’s permeability through biological barriers and tumor cell membranes affects bioavailability. MITC exhibits low affinity to biological membrane[1].
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- HY-B1334A
-
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Mitochondrial Metabolism
Apoptosis
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Cardiovascular Disease
Cancer
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Perhexiline maleate is an orally active CPT1 and CPT2 inhibitor that reduces fatty acid metabolism. Perhexiline maleate induces mitochondrial dysfunction and apoptosis in hepatic cells. Perhexiline maleate can cross the blood brain barrier (BBB) and shows anti-tumor activity. Perhexiline maleate can be used in the research of cancers, and cardiovascular disease like angina .
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- HY-104044
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BGB-290
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PARP
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Cancer
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Pamiparib (BGB-290) is an orally active, potent, highly selective PARP inhibitor, with IC50 values of 0.9 nM and 0.5 nM for PARP1 and PARP2, respectively. Pamiparib has potent PARP trapping, and capability to penetrate the brain, and can be used for the research of various cancers including the solid tumor .
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- HY-120574
-
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ADC Cytotoxin
Topoisomerase
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Cancer
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TH1338 (compound 3b), an orally active camptothecin derivative and a potent chemotherapeutic agent for cancer, demonstrates excellent cytotoxic potency against human tumor cell lines in vitro. TH1338 (compound 3b) possesses significant brain penetration, favorable efflux pump properties, and hematological toxicity profile .
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- HY-B1334
-
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Mitochondrial Metabolism
Apoptosis
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Cardiovascular Disease
Cancer
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Perhexiline is an orally active CPT1 and CPT2 inhibitor that reduces fatty acid metabolism. Perhexiline induces mitochondrial dysfunction and apoptosis in hepatic cells. Perhexiline can cross the blood brain barrier (BBB) and shows anti-tumor activity. Perhexiline can be used in the research of cancers, and cardiovascular disease like angina .
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- HY-112037
-
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IACS-10759
|
Oxidative Phosphorylation
Mitochondrial Metabolism
Apoptosis
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Cancer
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IACS-010759 is an orally active, potent mitochondrial complex I of oxidative phosphorylation (OXPHOS) inhibitor. IACS-010759 inhibits proliferation and induces apoptosis in models of brain cancer and acute myeloid leukemia (AML) reliant on OXPHOS. IACS-010759 has the potential for relapsed/refractory AML and solid tumors research .
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- HY-112037A
-
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IACS-10759 hydrochloride
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Oxidative Phosphorylation
Mitochondrial Metabolism
Apoptosis
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Cancer
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IACS-010759 hydrochlorideis an orally active, potent mitochondrial complex I of oxidative phosphorylation (OXPHOS) inhibitor. IACS-010759 hydrochlorideinhibits proliferation and induces apoptosis in models of brain cancer and acute myeloid leukemia (AML) reliant on OXPHOS. IACS-010759 hydrochloride has the potential for relapsed/refractory AML and solid tumors research .
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- HY-17364
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Temozolomide
Maximum Cited Publications
109 Publications Verification
NSC 362856; CCRG 81045; TMZ
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DNA Alkylator/Crosslinker
Autophagy
Apoptosis
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Cancer
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Temozolomide (NSC 362856) is an oral active DNA alkylating agent that crosses the blood-brain barrier. Temozolomide is also a proautophagic and proapoptotic agent. Temozolomide is effective against tumor cells that are characterized by low levels of O6-alkylguanine DNA alkyltransferase (OGAT) and a functional mismatch repair system. Temozolomide has antitumor and antiangiogenic effects .
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- HY-151985
-
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Apoptosis
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Cancer
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TACC3 inhibitor 1 is a potent and cross the blood-brain barrier TACC3 inhibitor. TACC3 inhibitor 1 induces Apoptosis and cell cycle arrest at G2/M phase. TACC3 inhibitor 1 induces the generation of intracellular ROS. TACC3 inhibitor 1 shows antiproliferative and anti-tumor activity .
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- HY-161117
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Others
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Cancer
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AD-8007 is an acetyl CoA synthase 2 (ACSS2) inhibitor that can cross the blood-brain barrier. AD-8007 can significantly reduce lipid storage and cell colony formation in vitro models, and increase tumor cell death. AD-8007 has anti-cancer activity and can be used in the research of breast cancer .
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- HY-122607
-
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Others
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Inflammation/Immunology
Cancer
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DPA-714 is a high affinity translocator protein (TSPO) ligand (Ki=7 nM), which is designed with a fluorine atom in its structure, allowing labelling with fluorine -18 and in vivo imaging using positron emission tomography. 18FDPA-714 successfully evaluates for the specific imaging of inflammation in various models of neuroinflammation and in a brain tumor model .
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- HY-104077S
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GS-5734-d5
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DNA/RNA Synthesis
SARS-CoV
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Infection
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Remdesivir-d5 is a deuterium labeled Remdesivir. Remdesivir (GS-5734) is a nucleoside analogue, with effective antiviral activity, with EC50s of 74 nM for SARS-CoV and MERS-CoV in HAE cells, and 30 nM for murine hepatitis virus in delayed brain tumor cells. Remdesivir is highly effective in the control of 2019-nCoV (COVID-19) infection in vitro[1][2].
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- HY-145949
-
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Drug Metabolite
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Infection
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Remdesivir de(ethylbutyl 2-aminopropanoate) is an impurity of Remdesivir. Remdesivir, a nucleoside analogue with effective antiviral activity, has EC50s of 74 nM for SARS-CoV and MERS-CoV in HAE cells, and 30 nM for murine hepatitis virus in delayed brain tumor cells. Remdesivir is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro .
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- HY-B0568
-
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Ferroptosis
HCV
Apoptosis
COX
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Infection
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
Endocrinology
Cancer
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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 has antianemic, neuroprotective, anti-inflammatory, antioxidant, and antidotal activity. Deferiprone can be used in cancer, cardiovascular disease, infection, inflammation, and neurological disease study .
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- HY-104077S1
-
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GS-5734-d4
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DNA/RNA Synthesis
SARS-CoV
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Infection
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Remdesivir-d4 is deuterium labeled Remdesivir. Remdesivir (GS-5734), a nucleoside analogue with effective antiviral activity, has EC50s of 74 nM for SARS-CoV and MERS-CoV in HAE cells, and 30 nM for murine hepatitis virus in delayed brain tumor cells. Remdesivir is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro[1][2].
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- HY-148114
-
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Others
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Cancer
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MOPIPP is a novel indolebased chalcone, and vacuolin-1, is a non-lethal vacuoleinducing 2-propyl analog of MOMIPP (HY-148114). MOPIPP induces cellular vacuolization and increases autophagosomes numbers. MOPIPP also triggers methuosis, and interrupts glucose uptake and glycolytic metabolism. MOPIPP can cross the blood-brain barrier and shows efficacy in suppressing tumor progression agaisnt glioblastoma cells .
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- HY-17364S
-
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DNA Alkylator/Crosslinker
Autophagy
Apoptosis
|
Cancer
|
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Temozolomide-d3 is the deuterium labeled Temozolomide. Temozolomide (NSC 362856) is an oral active DNA alkylating agent that crosses the blood-brain barrier. Temozolomide is also a proautophagic and proapoptotic agent. Temozolomide is effective against tumor cells that are characterized by low levels of O6-alkylguanine DNA alkyltransferase (OGAT) and a functional mismatch repair system. Temozolomide has antitumor and antiangiogenic effects[1][2].
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- HY-155532
-
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Biochemical Assay Reagents
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Cancer
|
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10m/ZS44 is a blood-brain barrier-permeable Glioblastoma (GBM) inhibitor. 10m/ZS44 significantly inhibits GBM tumor growth in a mouse xenograft model. 10m/ZS44 also activates the SIRT1/p53-mediated apoptosis pathway, thereby inhibiting the proliferation of U251 cells .
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- HY-107758
-
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Prolyl Endopeptidase (PREP)
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Cancer
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Y-29794 oxalate is a selective, orally active and blood-brain barrier permeable non-peptide prolyl endopeptidase inhibitor. Y-29794 oxalate blocks the IRS1-AKT-mTORC1 pathway and inhibits tumor growth. Y-29794 oxalate is also effective in inhibiting the progression of Aβ-like deposition in the hippocampus of aging-accelerated mice (SAM) .
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- HY-103441
-
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EGFR
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Cancer
|
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JNJ28871063 hydrochloride is an orally active, highly selective and ATP competitive pan-ErbB kinase inhibitor with IC50 values of 22 nM, 38 nM, and 21 nM for ErbB1, ErbB2, and ErbB4, respectively. JNJ28871063 hydrochloride inhibits phosphorylation of functionally important tyrosine residues in both EGFR and ErbB2. JNJ28871063 hydrochloride crosses the blood-brain barrier and has antitumor activity in human tumor xenograft models that overexpress EGFR and ErbB2 .
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-
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- HY-144825
-
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Apoptosis
Reactive Oxygen Species
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Cancer
|
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Chol-CTPP is a ligand with dual targeting effect on blood-brain barrier (BBB) and glioma cells. Lip-CTPP can be gained by Chol-CTPP and another mitochondria targeting ligand (Chol-TPP). Lip-CTPP is a promising potential carrier to exert the anti-glioma effect of doxorubicin (DOX) and lonidamine (LND) collaboratively. Lip-CTPP elevates the inhibition rate of tumor cell proliferation, migration and invasion, promote apoptosis and necrosis, and interfere with mitochondrial function .
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- HY-104077S2
-
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DNA/RNA Synthesis
SARS-CoV
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Infection
|
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Remdesivir impurity 9-d4 is deuterium labeled Remdesivir. Remdesivir (GS-5734), a nucleoside analogue with effective antiviral activity, has EC50s of 74 nM for SARS-CoV and MERS-CoV in HAE cells, and 30 nM for murine hepatitis virus in delayed brain tumor cells. Remdesivir is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro[1][2].
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- HY-149556
-
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EGFR
PI3K
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Cancer
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MTX-241F is a selective small molecule inhibitor targeting EGFR and PI3 kinase family members. MTX-241F is able to penetrate the blood-brain barrier and control tumor growth over the long term. MTX-241F exhibits radiosensitizing activity in patient-derived DIPG neurospheres and may be used in the study of diffuse intrinsic pontine glioma (DIPG) .
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- HY-N0784
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- HY-158115
-
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Molecular Glues
Raf
MEK
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Cancer
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NST-628 is a brain-permeable MAPK pathway molecule glue that inhibits RAF phosphorylation and MEK activation. NST-628 also binds RAF and prevents the formation of BRAF-CRAF and BRAF-ARAF heterodimers, effectively inhibiting the RAS-MAPK pathway. NST-628 inhibits RAS- and RAF-driven cancers and demonstrated potent inhibition in mutant KRAS, NRAS, BRAF class II/III, and NF1-mutant tumors .
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- HY-107691
-
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Neurokinin Receptor
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Neurological Disease
Endocrinology
Cancer
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GR 159897 is a highly potent, selective, competitive, brain-penetrated non-peptide neurokinin 2 (NK2) receptor antagonist. GR 159897 has little or no affinity for NK1 and NK3 receptors. GR 159897 inhibits binding of [ 3H]GR100679 to human NK2 (hNK2)-CHO cells and rat colon membranes with pKis of 9.51 and 10, respectively. Antagonizes bronchoconstriction. Anxiolytic-like and anti-tumor effects .
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- HY-121618
-
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GABA Receptor
Reactive Oxygen Species
Parasite
Apoptosis
Autophagy
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Infection
Neurological Disease
Cancer
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α-Thujone is a monoterpene isolated from Thuja occidentalis essential oil with potent anti-tumor activities. α-Thujone is a reversible modulator of the GABA type A receptor and the IC50 for α-Thujone is 21 μM in suppressing the GABA-induced currents. α-Thujone induces ROS accumulation-dependent cytotoxicity, also induces cell apoptosis and autophagy. α-Thujone has antinociceptive, insecticidal, and anthelmintic activity, and easily penetrates the blood-brain barrier .
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- HY-115925
-
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SHP2
Phosphatase
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Cancer
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SHP2-IN-9 is a specific SHP2 inhibitor (IC50 =1.174 μM) with enhanced blood–brain barrier penetration. SHP2-IN-9 shows 85-fold more selective for SHP2 than SHP1. SHP2-IN-9 inhibits SHP2-mediated cell signal transduction and cancer cell proliferation, and inhibits the growth of cervix cancer tumors and glioblastoma growth in vivo .
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- HY-149695
-
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EGFR
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Cancer
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EGFR-IN-91 (compound 9) is an orally available EGFR inhibitor with blood-brain barrier penetrability. EGFR-IN-91 inhibits EGFR L858R/C797S and EGFR exon 19del/C797S, inducing tumor regression in xenograft (PDX) mouse models. EGFR-IN-91 has the potential to inhibit localized and metastatic non-small cell lung cancer (NSCLC) driven by EGFR mutants .
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- HY-155577
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Monoamine Oxidase
HSP
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Cancer
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MAO A/HSP90-IN-1 (4-b) is a MAO A/HSP90 dual inhibitor with IC50 value of 1.77 μM and 0.019 μM in Glioblastoma (GBM) GL26 cells and HSP90α, respectively. MAO A/HSP90-IN-1 (4-b) can inhibit MAO A activity, HSP90 binding and the expression of HER2 and phospho-Akt to inhibit the growth of GBM, they also reduce PD-L1 expression, which inhibits T cell activation. MAO A/HSP90-IN-1 (4-b) have potential to inhibit tumor immune escape. MAO A/HSP90-IN-1 (4-b) can be used for brain tumor-related diseases research .
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- HY-N2038
-
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Phosphodiesterase (PDE)
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Neurological Disease
Cancer
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3,5,6,7,8,3',4'-Heptemthoxyflavone, a flavonoid from satsuma peel, is an orally available CREB activator with anti-tumor and anti-neuroinflammatory activity. 3,5,6,7,8,3',4'-Heptemthoxyflavone inhibits collagenase activity and increases the content of type I procollagen in human dermal fibroblast neoblast (HDFn) cells. 3,5,6,7,8,3',4'-Heptemthoxyflavone induces brain-derived neurotrophic factor (BDNF) expression through the cAMP/ERK/CREB signaling pathway and reduces phosphodiesterase activity in C6 glioma .
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- HY-12678S1
-
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NMS-E628-d8; RXDX-101-d8
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Isotope-Labeled Compounds
Autophagy
Anaplastic lymphoma kinase (ALK)
Trk Receptor
ROS Kinase
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Cancer
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Entrectinib-d8 (NMS-E628-d8; RXDX-101-d8) is a deuterated version of Entrectinib (HY-12678). Entrectinib (NMS-E628) is an orally available, blood-brain barrier permeable, central nervous system active TrkA/B/C, ROS1 and ALK inhibitor with IC50 values of 1, 3, 5, 12 and 12, respectively. 7 nM. Entrectinib induces apoptosis and cycle arrest in cancer cells, has anti-tumor activity, and also alleviates bleomycin-induced pulmonary fibrosis in mice .
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- HY-143877
-
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HDAC
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Cancer
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NN-390 is a potent and selective HDAC6 inhibitor, with an IC50 of 9.8 nM. NN-390 penetrates the blood-brain barrier (BBB). NN-390 shows study potential in metastatic Group 3 MB (medulloblastoma) .
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- HY-153321
-
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BTK-IN-24
|
Btk
PROTACs
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Inflammation/Immunology
Cancer
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NX-5948 (BTK-IN-24) is an orally active chimeric targeting molecule (CTM) that induces specific BTK protein degradation by the cereblon E3 ligase (CRBN) complex without degradation of other cereblon neo-substrates. NX-5948 mediates potent anti-inflammatory activity via BTK degradation with resultant inhibition of B cell activation. NX-5948 exhibits potent tumor growth inhibition in TMD8 xenograft models that contain either wild-type BTK or BTKi-resistant mutations. NX-5948 is efficacious in a mouse collageninduced arthritis (CIA) model. NX-5948 can cross the blood brain barrier (BBB). NX-5948 is a PROTAC composed of the ligand for target protein, a linker, and a cereblon E3 ligase (CRBN) complex (Red: ligand for target protein; Blue: CRBN; Black: linker) .
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HY-L028
-
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856 compounds
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The blood-brain barrier (BBB) is the complex network of brain microvessels. It protects the brain from the external bloodstream environment and supplies the brain with the required nutrients for normal function. However, blood-brain barrier is also the obstacle to deliver beneficial drugs to treat CNS (central nervous system) diseases or brain tumors, as it has the least permeable capillaries in the entire body due to physical barriers (tight junctions). Therefore, it is crucial to discover drugs which can cross this barrier for the treatment of brain-based diseases, such as Alzheimer’s disease (AD), Parkinson’s disease (PD) and epilepsy.
MCE offers a unique collection of 856 compounds with confirmed CNS-Penetrant property. It’s a useful tool for the discovery of drugs used for brain diseases, such as brain tumors, mental disorders, and neurodegenerative diseases.
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| Cat. No. |
Product Name |
Type |
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- HY-D0022
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5-AF
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Fluorescent Dyes/Probes
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5-Aminofluorescein (5-AF) is a fluorescence marker, covalently bound to human serum albumin. The excitation wavelength is 495 nm and the emission wavelength is 535 nm .
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| Cat. No. |
Product Name |
Target |
Research Area |
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- HY-105155
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RMP 7
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Bradykinin Receptor
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Cancer
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Lobradimil (RMP 7), a synthetic bradykinin analog, is a potent and selective bradykinin B2 receptor agonist (Ki: 0.54 nM). Lobradimil increases the permeability of the BBB. Lobradimil can be used in the research of brain tumors .
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| Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P99849
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ABT-806
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EGFR
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Cancer
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Depatuxizumab is a brain-penetrant and humanized tumor-specific anti EGFR monoclonal antibody. Depatuxizumab inhibits the growth of xenograft models of mutant EGFRvIII and wild-type EGFR. Depatuxizumab can be used for research on cancer .
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| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
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- HY-113303
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- HY-N0123
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- HY-N0784
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- HY-121618
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- HY-N2038
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Structural Classification
Flavonols
Flavonoids
Rutaceae
Plants
Citrus reticulata Blanco
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Phosphodiesterase (PDE)
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3,5,6,7,8,3',4'-Heptemthoxyflavone, a flavonoid from satsuma peel, is an orally available CREB activator with anti-tumor and anti-neuroinflammatory activity. 3,5,6,7,8,3',4'-Heptemthoxyflavone inhibits collagenase activity and increases the content of type I procollagen in human dermal fibroblast neoblast (HDFn) cells. 3,5,6,7,8,3',4'-Heptemthoxyflavone induces brain-derived neurotrophic factor (BDNF) expression through the cAMP/ERK/CREB signaling pathway and reduces phosphodiesterase activity in C6 glioma .
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| Cat. No. |
Product Name |
Chemical Structure |
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- HY-104077S
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2 Publications Verification
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Remdesivir-d5 is a deuterium labeled Remdesivir. Remdesivir (GS-5734) is a nucleoside analogue, with effective antiviral activity, with EC50s of 74 nM for SARS-CoV and MERS-CoV in HAE cells, and 30 nM for murine hepatitis virus in delayed brain tumor cells. Remdesivir is highly effective in the control of 2019-nCoV (COVID-19) infection in vitro[1][2].
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- HY-17364S
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Temozolomide-d3 is the deuterium labeled Temozolomide. Temozolomide (NSC 362856) is an oral active DNA alkylating agent that crosses the blood-brain barrier. Temozolomide is also a proautophagic and proapoptotic agent. Temozolomide is effective against tumor cells that are characterized by low levels of O6-alkylguanine DNA alkyltransferase (OGAT) and a functional mismatch repair system. Temozolomide has antitumor and antiangiogenic effects[1][2].
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- HY-119696S
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MTIC-d3 is deuterium labeled MTIC. MTIC is the active metabolite of Temozolomide (TMZ). MITC has lower bioavailability in the brain compared with TMZ, because the agent’s permeability through biological barriers and tumor cell membranes affects bioavailability. MITC exhibits low affinity to biological membrane[1].
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- HY-104077S1
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Remdesivir-d4 is deuterium labeled Remdesivir. Remdesivir (GS-5734), a nucleoside analogue with effective antiviral activity, has EC50s of 74 nM for SARS-CoV and MERS-CoV in HAE cells, and 30 nM for murine hepatitis virus in delayed brain tumor cells. Remdesivir is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro[1][2].
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- HY-104077S2
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Remdesivir impurity 9-d4 is deuterium labeled Remdesivir. Remdesivir (GS-5734), a nucleoside analogue with effective antiviral activity, has EC50s of 74 nM for SARS-CoV and MERS-CoV in HAE cells, and 30 nM for murine hepatitis virus in delayed brain tumor cells. Remdesivir is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro[1][2].
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- HY-12678S1
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Entrectinib-d8 (NMS-E628-d8; RXDX-101-d8) is a deuterated version of Entrectinib (HY-12678). Entrectinib (NMS-E628) is an orally available, blood-brain barrier permeable, central nervous system active TrkA/B/C, ROS1 and ALK inhibitor with IC50 values of 1, 3, 5, 12 and 12, respectively. 7 nM. Entrectinib induces apoptosis and cycle arrest in cancer cells, has anti-tumor activity, and also alleviates bleomycin-induced pulmonary fibrosis in mice .
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