Search Result
Results for "
U87
" in MedChemExpress (MCE) Product Catalog:
10
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-12033
-
|
2-ME2; NSC-659853
|
Microtubule/Tubulin
Reactive Oxygen Species (ROS)
Apoptosis
Autophagy
Endogenous Metabolite
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Cancer
|
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2-Methoxyestradiol (2-ME2), an orally active endogenous metabolite of 17β-estradiol (E2), is an apoptosis inducer and an angiogenesis inhibitor with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules. 2-Methoxyestradio, also a potent superoxide dismutase (SOD) inhibitor and a ROS-generating agent, induces autophagy in the transformed cell line HEK293 and the cancer cell lines U87 and HeLa .
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-
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- HY-B1490
-
|
|
Serotonin Transporter
Apoptosis
Autophagy
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Neurological Disease
Inflammation/Immunology
Cancer
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Imipramine hydrochloride is an orally active tertiary amine tricyclic antidepressant. Imipramine hydrochloride is a Fascin1 inhibitor with antitumor activities. Imipramine hydrochloride also inhibits serotonin transporter with an IC50 value of 32 nM. Imipramine hydrochloride stimulates U-87MG glioma cells autophagy and induces HL-60 cell apoptosis. Imipramine hydrochloride shows neuroprotective and immunomodulatory effects .
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- HY-B1490A
-
|
|
Serotonin Transporter
Autophagy
Apoptosis
|
Neurological Disease
Inflammation/Immunology
Cancer
|
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Imipramine is an orally active tertiary amine tricyclic antidepressant. Imipramine is a Fascin1 inhibitor with antitumor activities. Imipramine also inhibits serotonin transporter with an IC50 value of 32 nM. Imipramine stimulates U-87MG glioma cells autophagy and induces HL-60 cell apoptosis. Imipramine shows neuroprotective and immunomodulatory effects .
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-
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- HY-B0754A
-
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Hematoporphyrin IX dihydrochloride
|
Apoptosis
Endogenous Metabolite
|
Cancer
|
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Hematoporphyrin dihydrochloride (Hematoporphyrin IX dihydrochloride), a photosensitizer, is a substrate for affinity chromatography of heme-binding proteins. Hematoporphyrin dihydrochloride can induce apoptosis in U87 glioma cells and decrease tumor growth in vivo when exposed to red light .
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-
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- HY-P99762
-
|
MGD009
|
CD3
|
Cancer
|
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Obrindatamab is a humanized anti-B7-H3/CD3 bispecific antibody. Obrindatamab binds to B7-H3 and CD3, thereby mediating redirected cytotoxic T-lymphocyte (CTL) activity against B7-H3-expressing cancer cells. Obrindatamab can be used in research of cancer .
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-
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- HY-111449
-
BAY-218
2 Publications Verification
AHR antagonist 1
|
Aryl Hydrocarbon Receptor
|
Inflammation/Immunology
Cancer
|
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BAY-218 (AHR antagonist 1) is an aryl hydrocarbon receptor (AHR) antagonist. BAY-218 has AHR inhibitory activity with an IC50 of 39.9 nM in in U87 glioblastoma cells. BAY-218 can be used for the research of cancer or conditions with dysregulated immune responses .
|
-
-
- HY-13768
-
Topotecan
Maximum Cited Publications
38 Publications Verification
SKF 104864A; NSC 609669
|
Topoisomerase
Autophagy
Apoptosis
|
Cancer
|
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Topotecan (SKF 104864A; NSC 609669) is an orally active and potent Topoisomerase I inhibitor. Topotecan induces cell cycle arrest in G0/G1 and S phases and promotes apoptosis. Topotecan shows anticancer activity .
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-
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- HY-B0754
-
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Hematoporphyrin IX
|
Apoptosis
Endogenous Metabolite
|
Cancer
|
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Hematoporphyrin (Hematoporphyrin IX), a photosensitizer, is a substrate for affinity chromatography of heme-binding proteins. Hematoporphyrin can induce apoptosis in U87 glioma cells and decrease tumor growth in vivo when exposed to red light .
|
-
-
- HY-12833
-
AMZ30
1 Publications Verification
|
Phosphatase
Akt
ERK
|
Others
|
|
AMZ30 is selective protein phosphatase methylesterase-1(PME-1) inhibitor with IC50s of 600 nM and 3.5 µM in human cell lysates and in HEK 293T cells, respectively. AMZ30 shows >100-fold selectivity relative to other serine hydrolases. AMZ30 reduces the demethylated form of PP2A in living cells. AMZ30 attenuates muscle cell differentiation. AMZ30 increases the resistance of U87MG and U251MG glioblastoma cells to t-BHP-induced oxidative stress. AMZ30can be used for the study of glioblastoma .
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- HY-108693
-
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Leukotriene Receptor
Apoptosis
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Inflammation/Immunology
|
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β-Tocotrienol is an isomer of vitamin E. β-Tocotrienol is a less potent antioxidant than α-tocotrienol. β-Tocotrienol can be found in the tocotrienol-rich fraction (TRF) of palm oil, which possesses anti-carcinogenic effects in vitro on human colon carcinoma and prostate cancer cells. β-Tocotrienol inhibits the growth of A549 (GI50 = 1.38 μM) and U87MG (GI50 = 2.53 μM) cells. β-Tocotrienol also induces apoptosis in cancer cells. β-Tocotrienol can inhibit PD-L1 expression and mitigates PD-L1-mediated immune suppression in vitro and in vivo .
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-
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- HY-116273
-
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Phospholipase
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Cancer
|
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ML299 is a selective allosteric modulator and a dual inhibitor of phospholipases D1 and D2 (IC50 values are 6 and 12 nM, respectively). ML299 decreases invasive migration in U87-MG glioblastoma cells .
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-
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- HY-168708
-
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Histone Demethylase
Apoptosis
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Cancer
|
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AH2-14c is an inhibitor for DNA demethylase ALKBH2. AH2-14c inhibits the cell viability (IC50 is 4.56 µM) and migration of GBM U87. AH2-14c regulates the expression of apoptosis-related genes, and induces apoptosis in GBM U87 cell .
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-
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- HY-12033S2
-
|
2-ME2-d5; NSC-659853-d5
|
Isotope-Labeled Compounds
Microtubule/Tubulin
Reactive Oxygen Species (ROS)
Apoptosis
Autophagy
Endogenous Metabolite
|
Cancer
|
|
2-Methoxyestradiol-d5 is the deuterium labeled 2-Methoxyestradiol. 2-Methoxyestradiol (2-ME2), an orally active endogenous metabolite of 17β-estradiol (E2), is an apoptosis inducer and an angiogenesis inhibitor with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules. 2-Methoxyestradio, also a potent superoxide dismutase (SOD) inhibitor and a ROS-generating agent, induces autophagy in the transformed cell line HEK293 and the cancer cell lines U87 and HeLa .
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-
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- HY-155439
-
|
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FAK
|
Cancer
|
FAK-IN-14 (compound 8d) is a focal adhesion kinase(FAK) inhibitor with an IC50 value of 0.2438 nM. FAK-IN-14 induces U87-MG cell early apoptosis and arrest the cell at the G2/M phase .
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-
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- HY-149530
-
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EGFR
Apoptosis
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Cancer
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EGFR-IN-86 (compound 4i) is an EGFR inhibitor (IC50: 1.5 nM) with high activity against glioblastoma. EGFR-IN-86 induces apoptosis and arrests the U87 cell cycle in the G2/M phase .
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- HY-106892
-
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348U87
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DNA/RNA Synthesis
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Infection
|
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BW 348U87 is an inhibitor for ribonucleotide reductase, which exhibits synergistic effect with Acyclovir (HY-17422), potentiate the antiviral activity of Acyclovir against herpes simplex virus (HSV) in athymic nude mouse model .
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- HY-173066
-
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PROTACs
Indoleamine 2,3-Dioxygenase (IDO)
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Cancer
|
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NU227326 is a blood-brain barrier penetrant IDO1 PROTAC degrader, with a DC50 of 4.5 nM in HiBiT degradation assays. NU227326 degrades IDO1 in U87 and GBM43 cells, with DC50 values of 7.1 nM and 11.8 nM, respectively (WB assays). NU227326 is applicable to research related to glioblastoma, prostate cancer, triple-negative breast cancer, pancreatic cancer, and ovarian cancer .
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- HY-N3001
-
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STAT
VEGFR
Bcl-2 Family
Survivin
IAP
NF-κB
Apoptosis
Caspase
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Neurological Disease
Inflammation/Immunology
Cancer
|
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Isolinderalactone is a sesquiterpene that exhibits anti-cancer, anti-inflammatory, and neuroprotective effects. Isolinderalactone inhibits VEGF expression and tyrosine phosphorylation of VEGFR2. Isolinderalactone decreases viability and induces apoptosis in U-87 glioblastoma (GBM) cells and colorectal cancer (CRC) cells. Isolinderalactone induces G2/M phase cell cycle arrest, ROS generation, pJNK/p38 MAPK activation, in colorectal cancer (CRC) cells. Isolinderalactone blocks LPS (HY-D1056)-induced NF-κB activation while activating Nrf2-HMOX1 signaling in RAW264.7 macrophages. Isolinderalactone improves cognitive dysfunction in APP/PS1 mice. Isolinderalactone can be used for the study of Glioblastoma multiforme (GBM), colorectal cancer, Alzheimer’s disease and acute lung injury .
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-
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- HY-150401
-
|
|
ADC Payload
Topoisomerase
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Cancer
|
|
Exatecan-amide-cyclopropanol (compound 1) is a anticancer agent. Exatecan-amide-cyclopropanol shows anti-proliferation activity against SK-BR-3 and U87 cells, with IC50 values of 0.12 and 0.23 nM, respectively .
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-
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- HY-15398C
-
|
Epicholecalciferol
|
Hedgehog
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Cancer
|
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3-epi-Vitamin D3 (Epicholecalciferol) (Compound 4), a Vitamin D3 analogue, is a Hedgehog pathway inhibitor with an IC50 of 39.2 μM measured in U87MG cells .
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-
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- HY-124674A
-
|
|
Monoamine Oxidase
EGFR
Akt
TGF-beta/Smad
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Cancer
|
|
CCT365623 hydrochloride is an orally active lysyl oxidase (LOX) inhibitor, with an IC50 of 0.89 μM. CCT365623 hydrochloride suppresses EGFR (pY1068) and AKT phosphorylation driven by EGF. CCT365623 hydrochloride is extremely well tolerated, and has good pharmacokinetic properties .
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-
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- HY-111187
-
|
KX-02
|
Src
Microtubule/Tubulin
Apoptosis
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Cancer
|
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KX2-361 (KX-02) is a Src-kinase and tubulin polymerization inhibitor. KX2-361 shows good oral bioavailability and readily crosses the BBB in mice. KX2-361 shows anti-tumor activity and induces apoptosis of Glioblastoma (GBM) cell .
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- HY-176537
-
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Microtubule/Tubulin
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Cancer
|
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RGN6024 is a brain-penetrant, orally active and reversible small molecule tubulin destabilizer. RGN6024 inhibits microtubule polymerization both in biochemical and cellular assays, binds to the colchicine binding pocket of β-tubulin (SPR: Kd = 6.7 μM; tryptophan assay: Kd = 7.4 μM), and triggers G2/M arrest in glioblastoma (GB) cells. RGN6024 retains activity in βIII-tubulin overexpressing cells. RGN6024 inhibits tumor growth in a GB xenograft mouse model. RGN6024 can be used for the study of glioblastoma (GB) .
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-
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- HY-155888
-
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Epigenetic Reader Domain
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Cancer
|
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IV-255 is a selective small molecule inhibitor of the BRG1 bromodomain. IV-255 increases the extent of DNA damage induced by Temozolomide (HY-17364) and Bleomycin (HY-108345). IV-255 inhibits the invasiveness of GBM cells. IV-255 enhances Temozolomide-induced cell death and the apoptosis-inducing activity of Temozolomide .
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-
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- HY-116165
-
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Phospholipase
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Cancer
|
|
ML298 is a potent and selective inhibitor of Phospholipase D2 (PLD2) with an IC50 of 355 nM. ML298 decreases invasive migration in U87-MG glioblastoma cells .
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-
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- HY-13768S1
-
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Isotope-Labeled Compounds
Topoisomerase
Autophagy
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Cancer
|
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Topotecan-d6 is the deuterium labeled Topotecan. Topotecan (SKF 104864A; NSC 609669) is a Topoisomerase I inhibitor. The IC50 values of Topotecan at 24 h are 2.73±0.25 μM of U251 cells, 2.95±0.23 μM of U87 cells, 5.46±0.41 μM of GSCs-U251 and 5.95 μM of GSCs-U87 .
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- HY-B1490R
-
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Reference Standards
Serotonin Transporter
Apoptosis
Autophagy
|
Neurological Disease
Inflammation/Immunology
Cancer
|
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Imipramine (hydrochloride) (Standard) is the analytical standard of Imipramine (hydrochloride). This product is intended for research and analytical applications. Imipramine hydrochloride is an orally active tertiary amine tricyclic antidepressant. Imipramine hydrochloride is a Fascin1 inhibitor with antitumor activities. Imipramine hydrochloride also inhibits serotonin transporter with an IC50 value of 32 nM. Imipramine hydrochloride stimulates U-87MG glioma cells autophagy and induces HL-60 cell apoptosis. Imipramine hydrochloride shows neuroprotective and immunomodulatory effects .
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- HY-136479
-
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Sirtuin
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Cancer
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F0911-7667 is a SIRT1 activator that induces autophagic cell death in U87MG and T98G cells by activating the AMPK-mTOR-ULK complex. CWR tripeptide was also identified as a SIRT1 activator that reduced p53 acetylation in IMR32 neuroblastoma cells and protected cells from cell death induced by Aβ fragments .
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- HY-170405
-
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PROTACs
mTOR
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Cancer
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YB-3-17 is a bifunctional molecule, that inhibits mTOR (IC50=0.22 nM) or degrades G1 to S phase transition 1 gene (GSPT1, DC50=5 nM) in a PROTAC mechanism. YB-3-17 exhibits antiproliferative activity in multi glioblastoma cell lines with IC50 of nanomolare levels. YB-3-17 exhibits antitumor efficacy in mouse models . (Pink: ligand for target protein (HY-170407); Black: linker (HY-A0102); Blue: ligand for E3 ligase Cereblon (HY-14658))
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- HY-125964
-
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Survivin
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Cancer
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LLP-3 is a potent Survivin inhibitor that disrupts the Survivin-Ran interaction in cancer cells. LLP-3 can be used in the research of Glioblastoma multiforme (GBM) .
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-
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- HY-175291
-
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MMP
Cadherin
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Cancer
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Cystatin B agonist 1 is an orally active MMP-2/9 inhibitor. Cystatin B agonist 1 exhibits inhibitory effects with IC50 values of 3.95 and 3.43 μM against U87 and T98G cells, respectively. Cystatin B agonist 1 induces the cell-cycle arrest at S phase, inhibits angiogenesis, and suppresses migration and invasion of MG cells. Cystatin B agonist 1 inhibits tumor growth in U87 MG xenograft model. Cystatin B agonist 1 can be used for the study of malignant glioma (MG) .
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- HY-156349
-
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Apoptosis
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Others
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Sec61-IN-4 (Compound 16b) is a Sec61 inhibitor (IC50: 0.04 nM in U87-MG cells) .
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-
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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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-
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- HY-19130
-
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Adenosine Receptor
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Neurological Disease
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BW-534U87 is an orally active adenosine A1 receptor agonist and competitive adenosine deaminase (ADA) inhibitor (Ki=7 μM). BW-534U87 elevates brain adenosine levels and suppresses epileptiform activity. BW-534U87 demonstrate anticonvulsant efficacy in animal seizure models. BW-534U87 is promising for research of epilepsy and adenosine-related neuropsychiatric disorders .
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- HY-175213
-
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Isocitrate Dehydrogenase (IDH)
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Cancer
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Mutant IDH1-IN-7 is a highly selective Isocitrate Dehydrogenase 1 (IDH1) R132H (IC50 = 0.26 μM, Kd = 2.1 μM)/R132C (IC50 = 1.1 μM) inhibitor. Mutant IDH1-IN-7 has no inhibitory effect on wild-type IDH1, IDH2-wt, and IDH2 R140Q. Mutant IDH1-IN-7 inhibits 2-Hydroxyglutarate (2-HG) production in U87-MG R132H cells (EC50 = 0.55 μM). Mutant IDH1-IN-7 exhibits moderate antiproliferative effects on U87-MG R132H and HT-1080 cells .
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-
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- HY-129094
-
|
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CXCR
|
Cancer
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ICT5040 is a small molecule CXCR4 antagonist (IC50=3.8 μM). ICT5040 inhibits CXCL12-mediated proliferation and migration, and suppresses CXCL12-induced intracellular calcium mobilisation in U87 glioma cells .
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-
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- HY-175530
-
|
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OLIG2
|
Cancer
|
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OLIG2-IN-1 is a potent and selective oligodendrocyte transcription factor 2 (OLIG2) inhibitor. OLIG2-IN-1 directly and dose-dependently downregulates nuclear OLIG2 levels with an IC50 value of 0.88 μM. OLIG2-IN-1 exhibits strong anti-proliferative activity in U87 and U251 cells with IC50 values of 7.02 μM and 6.43 μM, respectively. OLIG2-IN-1 can be used for the research of cancer, such as glioblastoma multiforme .
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-
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- HY-155684
-
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PROTACs
VEGFR
PDGFR
Ephrin Receptor
|
Cancer
|
|
SA-PA is an intracellular self-assembled PROTAC based on azide and alkyne. SA-PA is able to selectively degrade VEGFR-2, PDGFR-β and EphB4 proteins in U87 cells. SA-PA can be converted to PROTAC in situ by click reaction with the help of endogenous copper in tumor tissues .
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-
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- HY-168338
-
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Cannabinoid Receptor
Caspase
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Cancer
|
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CB2 receptor agonist 8 (Compound 17) is an agonist for cannabinoid receptor 2 (CB2 receptor). CB2 receptor agonist 8 exhibits cytotoxicity in cells U87, RPMI 8226, HL-60, and L929 with IC50s of 91.03, 16.29, 23.51 and 564.6 μM, respectively. CB2 receptor agonist 8 activates caspase 3/7, increases the expressions of pro-apoptotic genes BAX, BAD, BIM and tumor suppressor genes p53, and induces apoptosis in U87. CB2 receptor agonist 8 inhibits the migration of U87 .
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- HY-12033S1
-
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2-ME2-13C6; NSC-659853-13C6
|
Isotope-Labeled Compounds
Microtubule/Tubulin
Reactive Oxygen Species (ROS)
Apoptosis
Autophagy
Endogenous Metabolite
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Cancer
|
|
2-Methoxyestradiol- 13C6 is the 13C-labeled 2-Methoxyestradiol. 2-Methoxyestradiol (2-ME2), an orally active endogenous metabolite of 17β-estradiol (E2), is an apoptosis inducer and an angiogenesis inhibitor with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules. 2-Methoxyestradio, also a potent superoxide dismutase (SOD) inhibitor and a ROS-generating agent, induces autophagy in the transformed cell line HEK293 and the cancer cell lines U87 and HeLa .
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-
-
- HY-12033S
-
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|
Isotope-Labeled Compounds
Microtubule/Tubulin
Reactive Oxygen Species (ROS)
Apoptosis
Autophagy
Endogenous Metabolite
|
Cancer
|
|
2-Methoxyestradiol- 13C,d3 is the 13C- and deuterium labeled 2-Methoxyestradiol. 2-Methoxyestradiol (2-ME2), an orally active endogenous metabolite of 17β-estradiol (E2), is an apoptosis inducer and an angiogenesis inhibitor with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules. 2-Methoxyestradio, also a potent superoxide dismutase (SOD) inhibitor and a ROS-generating agent, induces autophagy in the transformed cell line HEK293 and the cancer cell lines U87 and HeLa .
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-
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- HY-168279
-
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VEGFR
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Cancer
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VEGF-IN-1 (compound 6) can reduce the release of VEGF in U87-MG cells and inhibit angiogenesis in vitro. VEGF-IN-1 can inhibit cell proliferation by inducing autophagy in tumor cells, with an IC50 value of 28.35 μM for U87-MG cells .
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- HY-N12834
-
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Others
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Inflammation/Immunology
Cancer
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Ecdysoside B (compound 6b) is a pregnanoside compound isolated from the plant Ecdysanthera rosea. Ecdysoside B and its derivatives and isomers shows anticancer, immunosuppressive and anti-inflammatory activities. Ecdysoside B shows cytotoxicity to a variety of human tumor cell lines, including PANC-1 (human pancreatic cancer cells), A375 (human melanoma cells) and U87 (brain glioma U87 cells). Ecdysoside B can be used for research in the areas of cancer, immunomodulation and anti-inflammato .
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- HY-168899
-
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FAK
Apoptosis
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Cancer
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FAK-IN-24 (Compound 9f) is a FAK inhibitor (IC50: 0.815 nM). FAK-IN-24 induces DNA damage and apoptosis. FAK-IN-24 has anti-glioblastoma activity. FAK-IN-24 inhibits proliferation of glioblastoma cell lines U87-MG (IC50 = 15 nM) and U251 (IC50 = 20 nM). FAK-IN-24 inhibits tumor growth in U87-MG xenograft model .
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- HY-149427
-
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PI3K
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Cancer
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PI3Kα-IN-12 (compound 13) is a highly selective PI3Kα inhibitor (IC50: 1.2 nM). PI3Kα-IN-12 inhibits HCT-116 and U87-MG with IC50s values of 0.83 and 1.25 μM, respectively. PI3Kα-IN-12 (40 mg/kg; IP) causes tumor regression in a U87-MG cell line xenograft mouse model .
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- HY-112666
-
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FTS amide; Salirasib amide
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Ras
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Cancer
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Farnesyl thiosalicylic acid amide (FTS-A) is an orally active derivative of farnesyl thiosalicylic acid (HY-14754). Farnesyl thiosalicylic acid amide reduces Ras-GTP levels and inhibits cell growth with IC50s of 20 and 10 μM for Panc-1 and U87 cells, respectively. Farnesyl thiosalicylic acid amide can be used for the research of cancer .
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- HY-147682
-
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NF-κB
Apoptosis
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Cancer
|
|
NF-κB-IN-5 (compound 4d) is an orally active and potent NF-κB inhibitor by interacting directly with NF-κB. NF-κB-IN-5 shows antitumor activity against human cancer cell lines (HCT116, U87-MG, HepG2, BGC823, PC9), with IC50 values of 5.35, 2.81, 2.83, 2.02 and 3.90 μM, respectively. NF-κB-IN-5 induces apoptosis in U87-MG tumor cell and cell cycle arrest in G0/G1 phase .
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-
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- HY-13768S
-
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SKF 104864A-d5; NSC 609669-d5
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Isotope-Labeled Compounds
Topoisomerase
Autophagy
|
Cancer
|
|
Topotecan-d5 is the deuterium labeled Topotecan. Topotecan (SKF 104864A; NSC 609669) is a Topoisomerase I inhibitor. The IC50 values of Topotecan at 24 h are 2.73±0.25 μM of U251 cells, 2.95±0.23 μM of U87 cells, 5.46±0.41 μM of GSCs-U251 and 5.95±0.24 μM of GSCs-U87 .
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-
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- HY-155440
-
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FAK
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Cancer
|
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FAK-IN-15 (Compound 9b) is a focal adhesion kinase (FAK) inhibitor with an IC50 value of 0.2691 nM. FAK-IN-15 has anti-tumor activity with an IC50 value of 1.033 μM against U87-MG cells .
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-
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- HY-157125
-
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PI3K
Apoptosis
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Cancer
|
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PI3Kα-IN-14 (compound F8) is a selective PI3Kα inhibitor with an IC50 of 0.14 nM. PI3Kα-IN-14 induces a great decrease in mitochondrial membrane which caused cell cycle arrest at G1 phase and apoptosis in U87-MG cells. PI3Kα-IN-14 shows significant anti-proliferative activities against three tumor-derived cell lines (PC-3: IC50 of 0.28 μM; HCT-116: IC50 of 0.57 μM; and U87-MG: IC50 of 1.37 μM) .
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- HY-178140
-
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STAT
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Cancer
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STAT3-IN-47 is an orally active STAT3 inhibitor. STAT3-IN-47 exhibits broad-spectrum anti-tumor activity against HeLa, HepG2, U87, and LN229 cells. STAT3-IN-47 suppresses STAT3 activation in vitro. STAT3-IN-47 can be used for the study of solid tumors, especially central nervous system (CNS) malignancies and hepatocellular carcinoma .
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- HY-149376
-
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Microtubule/Tubulin
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Cancer
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Tubulin inhibitor 38 (compound 14) is a tetrazole-based Tubulin inhibitor with antiproliferative potencies. Tubulin inhibitor 38 (100 nM,24 h) mediates mitotic arrest,blocks cell cycle at G2/M phase and induces apoptosis. Tubulin inhibitor 38 exhibits high cytotoxicity with high selectivity index among HeLa,MCF7,and U87 MG cells .
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- HY-144808
-
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Microtubule/Tubulin
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Cancer
|
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Anticancer agent 40 (compound 3e) is a potent anticancer agent. Anticancer agent 40 shows anticancer activities with IC50s of 0.94, 0.98, 0.96, 0.95, 2.13 nM for SKBR-3, SKOV-3, PC-3, U-87, HDF cells, respectively .
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- HY-117991
-
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VEGFR
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Cancer
|
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DW10075 is a highly selective and orally active VEGFR inhibitor targeting the VEGF/VEGFR pathway. DW10075 selectively inhibits VEGFR-1, VEGFR-2, and VEGFR-3, but has no effect on FGFR and PDGFR. DW10075 inhibits VEGF-induced HUVEC proliferation, migration, and tube formation. And DW10075 inhibits angiogenesis in both the rat aortic ring model and the chick chorionic membrane model. DW10075 also exhibits antiproliferative activity against human cancer cell lines, with IC50s of 2.2 μM and 22.2 μM against U87-MG human glioblastoma cells and A375 melanoma cells, respectively. In the nude mouse U87-MG xenograft tumor model, DW10075 (po) significantly inhibits tumor growth and reduces the expression of CD31 and Ki67 in tumor tissues.
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- HY-N12887
-
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Mitochondrial Metabolism
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Others
Cancer
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Mycothiazole is an inhibitor for mitochondrial electron transport chain (ETC) complex I. Mycothiazole exhibits cytotoxicity in cancer cells Huh7 (IC50 is 55.8 μM), U87 and MCF7. Mycothiazole induces apoptosis in Huh7. Mycothiazole utilizes the unfolded protein response (UPR) and heat shock response (HSR) pathway involved transcription factors ATFS-1 and HSF1, to extend the lifespan of C. elegans .
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- HY-161256
-
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Microtubule/Tubulin
Apoptosis
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Cancer
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Tubulin inhibitor 41 (Compd D19), a promising anti-GBM (glioblastoma) lead compound and tublin inhibitor with BBB permeability, induces G2/M phase arrest, resulted in cell apoptosis and inhibits the migration of U87 cells .
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- HY-B1490AS
-
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Isotope-Labeled Compounds
Serotonin Transporter
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Neurological Disease
Inflammation/Immunology
Cancer
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Imipramine-d6 is the deuterium labeled Imipramine hydrochloride. Imipramine is an orally active tertiary amine tricyclic antidepressant. Imipramine is a Fascin1 inhibitor with antitumor activities. Imipramine also inhibits serotonin transporter with an IC50 value of 32 nM. Imipramine stimulates U-87MG glioma cells autophagy and induces HL-60 cell apoptosis. Imipramine shows neuroprotective and immunomodulatory effects .
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-
- HY-B1490S1
-
-
- HY-162078
-
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Casein Kinase
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Cancer
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Antiproliferative agent-46 (compound 5e) is an inhibitor of the casein kinase-2 enzyme (CK2) receptor. Antiproliferative agent-46 has a potent antiproliferative activity with an IC50 value of 5.75 μM on the U87 cell line .
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- HY-B1490AR
-
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Serotonin Transporter
Autophagy
Apoptosis
Reference Standards
|
Neurological Disease
Inflammation/Immunology
Cancer
|
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Imipramine (Standard) is the analytical standard of Imipramine. This product is intended for research and analytical applications. Imipramine is an orally active tertiary amine tricyclic antidepressant. Imipramine is a Fascin1 inhibitor with antitumor activities. Imipramine also inhibits serotonin transporter with an IC50 value of 32 nM. Imipramine stimulates U-87MG glioma cells autophagy and induces HL-60 cell apoptosis. Imipramine shows neuroprotective and immunomodulatory effects .
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-
- HY-157168
-
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Trk Receptor
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Neurological Disease
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TrkA-IN-6 (compound R48) is a hydrazone-like, selective inhibitor of tropomyosin kinase type A receptor kinase (TrkA). TrkA-IN-6 exhibited a higher cytotoxic effect on U87 GBM cells than Temozolomide (HY-17364), with an IC50 of 68.99 μM .
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- HY-17662
-
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AK-918/41759663
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Bcl-2 Family
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Cancer
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Mol4 (AK-918/41759663) is a highly selective BCL-2 protein inhibitor (IC50=153.3 μM). Mol4 induces mitochondrial outer membrane permeabilization (MOMP) and cytochrome c release, showing significant antiproliferative activity against glioblastoma (U87-MG) cell lines. Mol4 is promising for research of BCL-2-dependent tumors (e.g., chronic lymphocytic leukemia) .
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-
- HY-162090
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TRP Channel
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Cancer
|
|
TRPC antagonist 1 (compound 15g) is a potent TRP channel (TRPC) antagonist with IC50s of 2.4 μM, 12.2 μM, 7.6 μM, 2.9 μM, and 3.4 μM for TRPC3, TRPC4, TRPC5, TPRC6, and TRPC7, respectively. TRPC antagonist 1 displays noteworthy anti-glioblastoma efficacy in vitro against U87 cell lines .
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- HY-169002
-
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Phosphatase
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Cancer
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|
PP5-IN-2 is an orally active and selective protein phosphatase 5 (PP5) inhibitor with an IC50 value of 0.9 μM. PP5-IN-2 activates p53 and downregulates cyclin D1 and MGMT, which shows potency in cell cycle arrest and reverses Temozolomide (TMZ) (HY-17364) resistance in the U87 MG cell line. PP5-IN-2 effectively inhibits tumor growth in the xenograft mouse model .
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-
- HY-114459
-
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Isocitrate Dehydrogenase (IDH)
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Cancer
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|
Mutant IDH1-IN-4 (compound 434) is an inhibitor of mutant Isocitrate dehydrogenase 1 (IDH 1), with IC50 values of ≤ 0.5 μM for mutant IDH1 in R132H, HT1080 and U87R132H cells .
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- HY-155685
-
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PROTACs
VEGFR
Ephrin Receptor
Apoptosis
|
Cancer
|
|
SA-VA is an intracellular self-assembled PROTAC based on azide and alkyne. SA-VA is able to selectively degrade VEGFR-2 and EphB4 proteins in U87 cells. SA-VA can be converted to PROTAC in situ by click reaction with the help of endogenous copper in tumor tissues. SA-VA promotes apoptosis and blocks cells in S phase .
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-
- HY-146275
-
|
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LXR
|
Cancer
|
|
LXRβ agonist-3 (compound 4-13) is a potent and selective LXRβ (liver X receptor β) agonist, with an EC50 of 0.095 μM. LXRβ agonist-3 efficiently inhibits U87EGFRvIII cell, with an IC50 of 3.75 μM. LXRβ agonist-3 shows antitumor activity, and can inhibit glioblastoma .
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-
- HY-172159
-
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HDAC
Apoptosis
|
Cancer
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FF2039 (compound 1j) is a specific HDAC1, HDAC6, and HDAC isoforms of class I, IIa and IIb PROTAC degrader. FF2039 demonstrates s significant antiproliferative activity against both hematological and solid cancer cell lines, driven by cell cycle arrest and Apoptosis induction. FF2039 inhibits HDAC isoform of HDAC1, HDAC2, HDAC4 and HDAC6 with IC50s of 1.03, 2.15, 12.4 and 0.053 μM, respectively. FF2039 shows antiproliferative activity against different tumor entities of MM.1S, MDA-MB-231 and U-87MG with EC50s of 2.8, 28 and 30 μM, respectively. (Pink: PRMT5 ligand (HY-168864); Blue: E3 ligase ligand HY-W957284); Black: linker (HY-W881439); E3+linker (HY-172185 )) .
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-
- HY-178034
-
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PROTACs
Oxysterol-binding Protein-related Protein (ORP)
|
Cancer
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PROTAC OSBP Degrader-1 (Compound 5) is a Oxysterol-binding protein (OSBP) PROTAC degrader with a DC50 of 322 nM (24 h). PROTAC OSBP Degrader-1 can rapidly penetrate into cells and induce massive recruitment of OSBP at the Trans-Golgi network. PROTAC OSBP Degrader-1 has potent anticancer activity with potent cytotoxicity against U-87 MG, A549, MCF7, HeLa and MDA-MB-231 cells . Pink: OSBP ligand (HY-178035); Blue: CRBN ligase ligand (HY-10984); Black: linker
|
-
- HY-170577
-
|
|
Pyruvate Kinase
Apoptosis
|
Cancer
|
|
PKM2-IN-8 (Compound 9b) is a pyruvate kinase M2 (PKM2) inhibitor (IC50 = 0.31 μM). PKM2-IN-8 has potent antiproliferative activity against U87MG glioma cells. PKM2-IN-8 can induce early apoptosis and reduce lactate levels. PKM2-IN-8 can be used for the research of glioblastoma .
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-
- HY-173431
-
|
|
Dopamine Receptor
Reactive Oxygen Species (ROS)
|
Cancer
|
|
Dopamine D4 receptor ligand 3 (Compound 16) is a dopamine D4 receptor (D4R) antagonist (pKi: 8.86). Dopamine D4 receptor ligand 3 has pIC50 values of 5.78, 5.55, and 6.17 for Go, Gi, and βArr2 sensors in HEK-293T cells, respectively. Dopamine D4 receptor ligand 3 inhibits the viability of three human glioma cell lines, U87 MG, T98G, and U251 MG. Dopamine D4 receptor ligand 3 induces ROS production and mitochondrial dysfunction in glioma cells .
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-
- HY-173116
-
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Carbonic Anhydrase
|
Cancer
|
|
DOTA-XYIMSR-01 is a molecular probe targeting CAIX that can be labeled with 177Lu for the inhibition and localization of malignant gliomas. The uptake of [177Lu] Lu-XYIMSR-01 in U87MG tumors is 6.19 % of the injected dose per gram (% ID/g), and the tumor-to-muscle uptake ratio is 20.14. In the orthotopic glioma model, combined injection with Temozolomide (HY-17364) can significantly improve the survival rate of mice and inhibit tumor growth. DOTA-XYIMSR-01 shows promise for research in the field of anti-cancer therapy .
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-
- HY-146715
-
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Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
IDO/Tubulin-IN-2 (HT2) is a potent TDO and tubulin inhibitor. IDO/Tubulin-IN-2 also shows potent activity against U87, HepG2, A549, HCT-116, and LO2 cancer cell lines, with IC50 values of 0.43, 0.036, 0.041, 0.095 and 1.04 μM, respectively. IDO/Tubulin-IN-2 remarkably promotes the antitumor activity .
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-
- HY-178178
-
|
|
PARP
Reactive Oxygen Species (ROS)
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
PARP1-IN-46 is a potent PARP-1 inhibitor with an IC50 of 2.4 nM. PARP1-IN-46 demonstrates remarkable anti-proliferative activity in both rat (C6) and human (U87MG) glioma cells. PARP1-IN-46 promotes PARP cleavage, triggers DNA damage, and increases ROS. PARP1-IN-46 effectively inhibits the migration, invasion and colony formation of glioma cells, and ultimately induces cell apoptosis. PARP1-IN-46 can be used to the study of glioma .
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-
- HY-173013
-
|
|
Cyclophilin
HIV
HCV
|
Infection
|
|
TWH106 is an inhibitor for Cyclophilin (Cyp) that exhibits good affinity to CypA and CypB with KD of 53 nM and 139 nM. TWH106 inhibits the replication of HIV and HCV, exhibiting antiviral activity .
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-
- HY-N12135
-
|
|
Others
|
Cancer
|
|
15α-Hydroxy-20-oxo-6,7-seco-ent-kaur-16-en-1,7α(6,11α)-diolide (compound 2) is an enantio-kaurene diterpenoid (ent -kaurene diterpenoid), which can be isolated from Rubescens rubescens. 15α-Hydroxy-20-oxo-6,7-seco-ent-kaur-16-en-1,7α(6,11α)-diolide has cellular activity against EC-1, U87, A549, MCF-7 and HeLa cell lines Toxicity, IC50s are 37.69 μM, 79.362 μM, 80.07 μM, 197.35 μM, 462.13 μM, and 180.09 μM respectively .
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-
- HY-148228
-
|
|
ROS Kinase
|
Cancer
|
|
ROS kinases-IN-1 (pag 98) is a ROS tyrosine kinase inhibitor with IC50 value of 1.22 μM. ROS kinases-IN-1 shows anti-tumor activity .
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-
- HY-12033R
-
|
2-ME2 (Standard); NSC-659853 (Standard)
|
Microtubule/Tubulin
Reactive Oxygen Species (ROS)
Apoptosis
Autophagy
Endogenous Metabolite
Reference Standards
|
Cancer
|
|
2-Methoxyestradiol (Standard) is the analytical standard of 2-Methoxyestradiol. This product is intended for research and analytical applications. 2-Methoxyestradiol (2-ME2), an orally active endogenous metabolite of 17β-estradiol (E2), is an apoptosis inducer and an angiogenesis inhibitor with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules. 2-Methoxyestradio, also a potent superoxide dismutase (SOD) inhibitor and a ROS-generating agent, induces autophagy in the transformed cell line HEK293 and the cancer cell lines U87 and HeLa .
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-
- HY-B2085
-
|
Arsthinol; Balarsen
|
Drug Intermediate
|
Cancer
|
|
Arsthinenol is an orally active antitumor agent, that exhibits cytotoxicity in U87MG cells with an IC50 of 31.6 μM. Arsthinenol forms complex with cyclodextrin, inhibits the tumor growth and improves the survival rates of U87MG xenograft mice .
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-
- HY-176162
-
|
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Reactive Oxygen Species (ROS)
Apoptosis
|
Cancer
|
|
BJ-13 is a reactive oxygen species (ROS) inducer that can lead to mitochondrial membrane potential collapse and caspase-dependent apoptosis. BJ-13 inhibits the proliferation of SGC-7901, U-87MG, and HepG-2 cancer cells (IC50 values of 15.33, 27.18, and 20.44 nM, respectively). BJ-13 can be used in the study of gastric cancer .
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-
- HY-B1490S
-
|
|
Serotonin Transporter
Apoptosis
Autophagy
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Imipramine-d4 (hydrochloride) is the deuterium labeled Imipramine hydrochloride. Imipramine hydrochloride is an orally active tertiary amine tricyclic antidepressant. Imipramine hydrochloride is a Fascin1 inhibitor with antitumor activities. Imipramine hydrochloride also inhibits serotonin transporter with an IC50 value of 32 nM. Imipramine hydrochloride stimulates U-87MG glioma cells autophagy and induces HL-60 cell apoptosis. Imipramine hydrochloride shows neuroprotective and immunomodulatory effects .
|
-
- HY-B1490AS1
-
|
|
Serotonin Transporter
Isotope-Labeled Compounds
Apoptosis
Autophagy
|
Others
|
|
Imipramine-d4 is deuterium labeled Imipramine. Imipramine is an orally active tertiary amine tricyclic antidepressant. Imipramine is a Fascin1 inhibitor with antitumor activities. Imipramine also inhibits serotonin transporter with an IC50 value of 32 nM. Imipramine stimulates U-87MG glioma cells autophagy and induces HL-60 cell apoptosis. Imipramine shows neuroprotective and immunomodulatory effects .
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-
- HY-B1490AS3
-
-
- HY-119780
-
-
- HY-181517
-
|
|
Bacterial
|
Infection
Cancer
|
|
Antitumor agent-212 is a α-exo-methylene-selenolactone derivative with prominent selective antitumor activity. Antitumor agent-212 exhibits an MIC value of 128 μg/mL against Gram-positive bacteria. Antitumor agent-212 exhibits significant antitumor effects in the U87 human glioma xenograft model. Antitumor agent-212 can be used for the study of glioma, breast cancer and non-small cell lung cancer, and antibacterial study .
|
-
- HY-158251
-
|
|
PARP
|
Cancer
|
|
BIBD-300 is a PARP-1 imaging agent with high affinity for PARP-1. BIBD-300 can accurately localize C6 and U87MG tumors, which can be used for research in the diagnosis of breast cancer, prostate cancer, glioma, and liver cancer .
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-
- HY-136765
-
|
|
PI3K
|
Cancer
|
|
PI3K-IN-11 (compound 13) is a PI3K inhibitor, which selectively inhibits PI3Kα, PI3Kβ, PI3K, and PI3Kδ (IC50s=6.4, 13, 8, and 11 nM, respectively) over mTOR (IC50=2.9 μM). PX-13-17OH is greater than 420-fold selective for PI3K in a panel of 20 lipid and protein kinases. PX-13-17OH inhibits phosphorylation of Akt and S6 kinase (S6K) in PTEN-negative U87MG cells when used at concentrations ranging from 0.03 to 1 μg/mL. It inhibits tumor growth in a U87MG mouse xenograft model when administered at doses ranging from 2.5 to 10 mg/kg.
|
-
- HY-121916
-
|
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
|
|
ML309 is a highly selective and potent inhibitor of the R132H mutant isocitrate dehydrogenase 1 (IDH1 R132H), with an IC50 of 96 nM. ML309 is a competitive inhibitor of α-KG, with a Ki value of 156 nM, and its inhibitory activity against the wild-type IDH1 is greater than 35 μM. ML309 effectively reduces the production of the tumor metabolite 2-HG in U87MG cells. ML309 can be used as a chemical probe to study the role of the mutant IDH1 in cancer .
|
-
- HY-156124
-
|
|
Sigma Receptor
|
Cancer
|
|
Sigma-2 Radioligand 1 (compound 1) is a Sigma-2 selective ligand. Sigma-2 Radioligand 1 has good biodistribution in mice and good in vivo activity in rats. [18F] Modified Sigma-2 Radioligand 1 for visualization of tumors in micro-PET/CT imaging, exhibiting high tumor uptake and tumor-to-background ratio. Experiments show that Sigma-2 Radioligand 1 binds highly specifically in U87MG glioma xenografts .
|
-
- HY-144450
-
|
|
PI3K
Akt
|
Cancer
|
|
PI3K-IN-29 is a potent PI3K inhibitor. PI3K-IN-29 displays good inhibition potencies against U87MG, HeLa and HL60 cells with IC50 values of 0.264, 2.04 and 1.14 µM, respectively. PI3K-IN-29 inhibits PI3K/Akt pathway by inhibiting phosphorylation of Akt that is catalyzed by PI3K .
|
-
- HY-143234
-
|
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
|
|
mIDH1-IN-1 (compound 43) is a potent and selective mIDH1 (mutant isocitrate dehydrogenases 1) inhibitor, with an IC50 of 961.5 nM. mIDH1-IN-1 potently inhibits intracellular 2-HG (2-hydroxyglutarate) production in HT1080 cells, with an EC50 of 208.6 ± 8.0 nM. mIDH1-IN-1 shows a significant anti-proliferation activity on IDH1 mutant-U-87 cells, with an IC50 of 41.8 nM. mIDH1-IN-1 is an antitumor agent, and can be used for IDH1 mutated solid tumors research .
|
-
- HY-163691
-
|
|
Carbonic Anhydrase
|
Cancer
|
|
Antitumor agent-163 (Compound 3) is a photosensitizer used in Molecular-Targeted Photodynamic Therapy (MT-PDT) targeting carbonic anhydrase IX (CAIX). Antitumor agent-163 inactivates CAIX protein via singlet oxygen under 540 nm wavelength light, without affecting internal standard proteins such as α-tubulin, β-actin, and proliferating cell nuclear antigen (PCNA). Antitumor agent-163 induces cell membrane damage, inhibits cell viability (IC50 is 0.2 and 0.05 μM for A549 and U87MG). Antitumor agent-163 exhibits antitumor efficacy in mouse model .
|
-
- HY-172180
-
-
- HY-13768C
-
|
SKF 104864A hydrochloride hydrate; NSC 609669 hydrochloride hydrate
|
Topoisomerase
Apoptosis
Autophagy
|
Cancer
|
|
Topotecan hydrochloride hydrate is an orally active and potent Topoisomerase I inhibitor. Topotecan hydrochloride hydrate induces cell cycle arrest in G0/G1 and S phases and promotes apoptosis. Topotecan hydrochloride hydrate shows anticancer activity .
|
-
- HY-168915
-
|
|
Akt
PKA
|
Cancer
|
|
ML-B01 is the orally active inhibitor for Akt and PKA with the IC50 of 2 nM and 136 nM. ML-B01 exhibits good ability to penetrate the blood-brain barrier (BBB) in the mouse brain .
|
-
- HY-108693R
-
|
|
Leukotriene Receptor
Reference Standards
Apoptosis
|
Inflammation/Immunology
|
|
β-Tocotrienol (Standard) is the analytical standard of β-Tocotrienol. This product is intended for research and analytical applications. β-Tocotrienol is an isomer of vitamin E. β-Tocotrienol is a less potent antioxidant than α-tocotrienol. β-Tocotrienol can be found in the tocotrienol-rich fraction (TRF) of palm oil, which possesses anti-carcinogenic effects in vitro on human colon carcinoma and prostate cancer cells. β-Tocotrienol inhibits the growth of A549 (GI50 = 1.38 μM) and U87MG (GI50 = 2.53 μM) cells. β-Tocotrienol also induces apoptosis in cancer cells. β-Tocotrienol can inhibit PD-L1 expression and mitigates PD-L1-mediated immune suppression in vitro and in vivo .
|
-
- HY-155889
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
IV-275 is an inhibitor of both BRG1 and BRM bromodomains. IV-275 increases the extent of DNA damage induced by Temozolomide (HY-17364) and Bleomycin (HY-108345). IV-275 inhibits the invasiveness of GBM cells. IV-275 enhances Temozolomide-induced cell death and the apoptosis-inducing activity of Temozolomide .
|
-
- HY-144783
-
|
|
CXCR
|
Inflammation/Immunology
Cancer
|
|
CXCR2 antagonist 6 (compound 35c) is a potent CXCR2 antagonist. CXCR2 antagonist 6 shows potent CXCR2 binding affinity (IC50=0.044 µM) and calcium mobilization (IC50=0.66 µM) [ 1].
|
-
- HY-144781
-
|
|
CXCR
|
Inflammation/Immunology
Cancer
|
|
CXCR2 antagonist 5 (compound 25) is a potent CXCR2 antagonist. CXCR2 antagonist 5 shows potent CXCR2 binding affinity (IC50=0.013 µM) and calcium mobilization (IC50=0.1 µM) [ 1].
|
-
- HY-181580
-
|
|
FAP
|
Cancer
|
|
FAP Ligand 3 (compound 54) is a reagent that binds to FAP, with a Ki value of 0.092 nM against human targets. FAP Ligand 3 acts as a tumor-retaining agent and serves as a FAP-targeted positron emission tomography (PET) tracer for tumor imaging. FAP Ligand 3 is applicable to studies related to U87MG glioma .
|
-
- HY-144784
-
|
|
CXCR
|
Inflammation/Immunology
Cancer
|
|
CXCR2 antagonist 7 (compound 19) is a potent CXCR2 antagonist. CXCR2 antagonist 7 shows potent CXCR2 binding affinity (IC50=0.044 µM) and calcium mobilization (IC50=0.66 µM) [ 1].
|
-
- HY-168883
-
|
|
Apoptosis
Pyruvate Kinase
|
Cancer
|
|
PKM2 modulator 2 (compound C599) is a potent PKM2 inhibitor. PKM2 modulator 2 shows antiproliferative activity. PKM2 modulator 2 induces apoptosis. PKM2 modulator 2 has the potential for the research of glioblastoma .
|
-
- HY-19747
-
HPOB
3 Publications Verification
|
HDAC
Apoptosis
|
Cancer
|
|
HPOB is a highly potent and selective inhibitor of HDAC6 with an IC50 of 56 nM. HPOB displays >30 fold less potent against other HDACs. HPOB enhances the effectiveness of DNA-damaging anticancer agents in transformed cells but not normal cells. HPOB does not block the ubiquitin-binding activity of HDAC6 .
|
-
- HY-168882
-
|
|
Apoptosis
Pyruvate Kinase
|
Cancer
|
|
PKM2 modulator 1 (compound C998) is a potent PKM2 inhibitor. PKM2 modulator 1 shows antiproliferative activity. PKM2 modulator 1 induces apoptosis. PKM2 modulator 1 has the potential for the research of glioblastoma .
|
-
- HY-173044
-
|
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
|
5-HT1AR/5-HT6R ligand-1 (Compound PP13) is the ligand for 5-HT receptor that exhibits good affinity to 5-HT1AR, 5-HT6R and 5-HT7R (Ki of 19, 69 and 198 nM, respectively), thereby inhibiting the cAMP production in HEK293 cell with EC50 of 1535, 488 and 53 nM, respectively. 5-HT1AR/5-HT6R ligand-1 exhibits anti-proliferative activity against a variety of cancer cells (IC50 for 1321N1, U87MG, MCF7, and AsPC-1 is 9.6, 13.6, 19.3 and 14.6 μM, respectively). 5-HT1AR/5-HT6R ligand-1 also exhibits antagonist activity for dopamine receptor D2R with Ki of 1903 nM .
|
-
- HY-123927
-
|
|
VEGFR
Ephrin Receptor
|
Inflammation/Immunology
Cancer
|
|
UniPR1331 is an orally active 3β-hydroxy-Δ5-choline acid derivative that inhibits Eph-ephrin interactions. UniPR1331 blocks the interaction of VEGFR2 with its natural ligand vascular endothelial growth factor and inhibits subsequent autophosphorylation, signaling, and pro-angiogenic activation of endothelial cells. UniPR1331 exhibits anti-angiogenesis, anti-cancer and anti-inflammation effects. UniPR1331 can be used for the researches of cancer and inflammation, such as glioma and colitis .
|
-
- HY-149696
-
|
|
NF-κB
|
Cancer
|
|
IR-Crizotinib is a NF-κB-inducing kinase (NIK) inhibitor that crosses the blood-brain barrier and fluorescently localizes intracranial glioblastoma (GBM) in mice (IC50=3.381 μM). IR-Crizotinib is conjugated from the near-infrared dye IR-786 and the NF-κB-inducing kinase (NIK) inhibitor Crizotinib. IR-Crizotinib can effectively inhibit the growth and invasion of glioma in vitro and in vivo and can be used in cancer research .
|
-
- HY-120115
-
|
Olaparib-bodipy FL
|
PARP
Fluorescent Dye
|
Cancer
|
|
PARPi-FL (Olaparib-bodipy FL) is a small-molecule fluorescent inhibitor of PARP1 that can specifically bind to PARP1. PARPi-FL can be used as a fluorescent imaging agent for tumor detection, diagnosis, and surgical guidance .
|
-
- HY-P11326
-
-
- HY-181982
-
-
- HY-151985
-
|
|
Apoptosis
|
Cancer
|
|
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 .
|
-
- HY-170778
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin polymerization-IN-77 (Compound 15c) is a tubulin polymerization inhibitor that exerts anti-glioblastoma activity by inhibiting tubulin polymerization. Tubulin polymerization-IN-77 demonstrates significant blood-brain barrier permeability, effectively inducing G2/M phase arrest and triggering apoptosis in GBM cells, while also significantly inhibiting tumor cell migration .
|
-
- HY-183258
-
|
|
TGF-β Receptor
|
Neurological Disease
Cancer
|
|
TGFβ1-IN-5 is a TGF-β1 inhibitor with blood-brain barrier permeability. TGFβ1-IN-5 reduces extracellular TGF-β1 levels in glioblastoma cells. TGFβ1-IN-5 exerts antiproliferative, antimigratory and clonogenic inhibitory effects in glioblastoma cells while maintaining the viability of non-cancerous cells. TGFβ1-IN-5 can be used for the research of glioblastoma .
|
-
- HY-N1992
-
|
TF-3; ZP10
|
Virus Protease
HSV
HIV
Flavivirus
|
Infection
Cancer
|
|
Theaflavin 3,3'-digallate (TF-3) is a potent Zika virus (ZIKV) protease inhibitor with an IC50 of 2.3 μM. Theaflavin 3,3'-digallat directly binds to ZIKVpro (Kd=8.86 μM) and inhibits ZIKV replication. Theaflavin 3,3'-digallat inhibits the activity of gp41 and NS2B-3 protease and has antiviral activity against HSV and HIV-1 . Theaflavin 3,3'-digallate, the typical pigment in black tea, is a potent antitumor agent .
|
-
- HY-182809
-
|
|
Hsp-targeting Chimeras
Androgen Receptor
HSP
|
Neurological Disease
Cancer
|
|
Androgen receptor degrader-6 is a blood-brain barrier-permeable AR degrader. Androgen receptor degrader-6 inhibits the chaperone activity of HSP27 and disrupts the HSP27-AR complex. Androgen receptor degrader-6 promotes the degradation of wild-type and mutant AR, reduces AR protein levels, and inhibits the growth of glioblastoma cells. Androgen receptor degrader-6 can be used in glioblastoma research .
|
-
- HY-185208
-
|
|
Antibody-Drug Conjugates (ADCs)
VEGFR
Apoptosis
|
Cancer
|
|
Bevacizumab vedotin is an antibody-drug conjugate (ADC). Bevacizumab vedotin blocks the VEGF/VEGFR pathway to exert anti-angiogenic effects. Bevacizumab vedotin exhibits anti-proliferative effects on cancer cells, promotes cancer cell apoptosis (Apoptosis), induces cancer cell cycle arrest, and possesses anti-migratory activity against breast cancer cells. Bevacizumab vedotin can be used in research related to glioma, hepatocellular carcinoma, and breast cancer .
|
-
- HY-N1992R
-
|
TF-3 (Standard); ZP10 (Standard)
|
Reference Standards
Virus Protease
HSV
HIV
Flavivirus
|
Infection
Cancer
|
|
Theaflavin 3,3'-digallate (Standard) is the analytical standard of Theaflavin 3,3'-digallate. This product is intended for research and analytical applications. Theaflavin 3,3'-digallate (TF-3) is a potent Zika virus (ZIKV) protease inhibitor with an IC50 of 2.3 μM. Theaflavin 3,3'-digallat directly binds to ZIKVpro (Kd=8.86 μM) and inhibits ZIKV replication. Theaflavin 3,3'-digallat inhibits the activity of gp41 and NS2B-3 protease and has antiviral activity against HSV and HIV-1 . Theaflavin 3,3'-digallate, the typical pigment in black tea, is a potent antitumor agent .
|
-
- HY-146756
-
|
|
Bacterial
|
Infection
|
|
22-((4-Methoxyphenyl)urea-1-yl)-22-deoxypleuromutilin (compound 6n) is an antibacterial pleuromutilin derivative against Gram-positive pathogens (GPPs) and Mycoplasma pneumoniae .
|
-
- HY-N17369
-
|
|
Others
|
Others
|
|
Neogenkwanine H is a daphnane-type diterpene that can be found in Daphne genkwa .
|
-
- HY-W006886
-
|
|
Amino Acid Derivatives
|
Others
|
Fmoc-(R)-2-(7-octenyl) Ala-OH is an unnatural Fmoc-protected amino acid and modification module. Fmoc-(R)-2-(7-octenyl) Ala-OH serves as a key building block for all-hydrocarbon cross-linking modification of antimicrobial peptides, and facilitates the generation of stapled peptide derivatives. When introduced into specific sites of the parent peptide, Fmoc-(R)-2-(7-octenyl) Ala-OH effectively increases the α-helix content of the peptide chain, thereby significantly enhancing its antimicrobial activity and proteolytic stability. Fmoc-(R)-2-(7-octenyl) Ala-OH is widely used in research on bacterial infections and the development of related antimicrobial agents . Stapled peptide is a specially chemically modified polypeptide. It locks the peptide chain into a stable α-helical structure by introducing a "staple"-like chemical bridge (usually an all-carbon backbone) at specific positions of the peptide chain.
|
-
- HY-12624
-
|
ON123300
|
CDK
AMPK
PDGFR
|
Cancer
|
|
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 .
|
-
- HY-N0826
-
-
- HY-124171
-
|
|
Fluorescent Dye
Drug Derivative
|
Others
|
|
Zinquin ethyl ester is a cell-permeable and lipophilic fluorescent derivative of Zinquin (HY-D0982). Zinquin ethyl ester reacts with protein-bound Zn 2+ in cells and forms fluorescent ternary adducts. Zinquin ethyl ester undergoes hydrolysis by intracellular esterases impeding its efflux across the plasma membrane (Ex/Em = 370/470 nm) .
|
-
- HY-P11099
-
|
|
Transferrin Receptor
|
Neurological Disease
Cancer
|
|
Cys-LT7 is a transferrin receptor (TfR)-targeting peptide ligand. Cys-LT7 binds to a TfR site distinct from endogenous transferrin, mediates conjugated Doxorubicin (HY-15142A) delivery to TfR-overexpressed tumor cells, and exhibits low toxicity to TfR-low-expressed normal cells. Cys-LT7 is an L-configuration peptide susceptible to proteolytic enzymes, leading to poor biostability in peptide-drug conjugates. Cys-LT7 can be used for the research of glioblastoma, hepatocellular carcinoma, lung carcinoma .
|
-
- HY-12970B
-
|
|
Histone Methyltransferase
Reactive Oxygen Species (ROS)
Apoptosis
|
Neurological Disease
Cancer
|
|
EPZ020411 dihydrochloride is a selective, blood-brain barrier-permeable PRMT6 inhibitor with an IC50 of 0.010 μM. EPZ020411 dihydrochloride blocks PRMT6-mediated histone H3R2 methylation, reduces ROS production, and inhibits Apoptosis. EPZ020411 dihydrochloride is applicable to research related to neuropathic pain, colorectal cancer, ototoxicity, hearing loss and glioblastoma .
|
-
- HY-182254
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
AChE/BChE-IN-35, Tacrine (HY-111338) derivative, is a brain-penetrant dual AChE/BChE inhibitor with an Electric Eel AChE IC50 of 123.66 nM, human AChE IC50 of 122.34 nM, and equine BChE IC50 of 488.00 nM. AChE/BChE-IN-35 undergoes LAT1-mediated active transport across cell membranes. AChE/BChE-IN-35 exhibits enhanced brain exposure with slower brain tissue elimination. AChE/BChE-IN-35 can be used for the research of alzheimer's disease .
|
-
- HY-12475
-
|
Agios 135
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
|
|
Mutant IDH1-IN-1 (Agios 135) is a selective mutant IDH1 inhibitor with activity against both IDH1 R132H and IDH1 R132C. Mutant IDH1-IN-1 reduces the level of 2-hydroxyglutarate (2-HG), stabilizes mutant IDH1 protein, and restores blocked monocyte differentiation. Mutant IDH1-IN-1 can be used in tumor-related research .
|
-
- HY-N12531
-
-
- HY-177482
-
|
|
Drug Intermediate
|
Cancer
|
|
Pro-PTX is a Pd-sensitive Paclitaxel (HY-B0015) prodrug with anticancer activity 200 to 700-fold lower than that of the parent compound. Pro-PTX triggers intramolecular cyclization via Pd-catalyzed depropargylation to release active Paclitaxel (HY-B0015) and a non-toxic byproduct. Pro-PTX diffuses efficiently through porous agarose and alginate hydrogel networks, reacts with embedded Pd nanosheets and gets activated. Pro-PTX exhibits significantly reduced cytotoxicity and antiproliferative activity in cancer cells and non-cancerous human cerebrovascular pericytes. Pro-PTX is applicable for research related to non-small cell lung cancer, glioblastoma and lung cancer .
|
-
- HY-124813
-
|
113B7
|
FAK
EGFR
MMP
NF-κB
SDCBP
|
Cancer
|
|
PDZ1i (113B7) is a inhibitor of MDA-9/Syntenin, with selective binding to the PDZ1 domain. PDZ1i inhibits radiation-induced invasion of glioblastoma (GBM) cells, radiosensitizes GBM cells, and impairs GBM-related signaling pathways (including Src/EphA2, EGFRvIII/FAK, and NF-κB). PDZ1i reduces radiation-induced secretion of invasion-related proteases (MMP-2, MMP-9, ADAM9). PDZ1i shows anti-tumor effects in nude mice bearing intracranial U1242-luc xenografts or GBM xenografts. PDZ1i can be used for the study of glioblastoma (GBM), breast cancer and prostate cancer .
|
-
- HY-185323
-
|
|
Drug Derivative
Apoptosis
DNA/RNA Synthesis
|
Neurological Disease
Cancer
|
|
Gem-C12 is a prodrug of Gemcitabine (HY-17026). Gem-C12 terminates DNA chain elongation, inhibits nucleic acid synthesis and induces Apoptosis. Gem-C12 inhibits the proliferation of glioma cells. Gem-C12 and Honokiol (HY-N0003) exhibit synergistic anti-glioblastoma activity. Gem-C12 can be used in research related to glioblastoma multiforme .
|
-
- HY-155949
-
|
|
|
Neurological Disease
Cancer
|
|
Bt354 is an orally active STAT3 inhibitor with IC50 values of 4.6 μM (DU145), 6.5 μM (MDA-MB-435) and 7.2 μM (MDA-MB-231), respectively. Bt354 induces cell cycle arrest and apoptosis, and downregulates epithelial-mesenchymal transition-related genes. Bt354 exhibits anti-angiogenic and anti-inflammatory activities, attenuates the polarization of M1 microglia and A1 astrocytes, suppresses inflammasome-related signaling pathways, and alleviates mechanical hyperalgesia and thermal hyperalgesia. Bt354 can be used in research related to glioblastoma multiforme, triple-negative breast cancer, prostate cancer and neuropathic pain .
|
-
- HY-147409
-
|
|
CDK
|
Cancer
|
|
Ulecaciclib is an orally activitive inhibitor of cyclin-dependent kinase (CDK), with Ki values of 0.62 μM (CDK2/Cyclin A), 0.2 nM (CDK4/Cyclin D1), 3 nM (CDK6/Cyclin D3), and 0.63 μM (CDK7/Cyclin H), respectively. Ulecaciclib can cross blood brain barrier and has good pharmacokinetic characteristics .
|
-
- HY-181073
-
|
|
Apoptosis
Necroptosis
NF-κB
p38 MAPK
|
Neurological Disease
Cancer
|
|
Apoptosis/necroptosis inducer 1 is an orally active and brain-penetrant apoptosis and necroptosis inducer. Apoptosis/necroptosis inducer 1 induces mitochondria-dependent (intrinsic pathway) apoptosis. Apoptosis/necroptosis inducer 1 induces necroptosis by activating the TNF-α/NF-κB/MAPK signaling pathway. Apoptosis/necroptosis inducer 1 exhibits antiproliferative activity in glioblastoma cell lines and multiple solid tumor types. Apoptosis/necroptosis inducer 1 inhibits growth of orthotopic glioblastoma in animal models and improves survival rate. Apoptosis/necroptosis inducer 1 can be used for the research of glioblastoma .
|
-
- HY-N1983
-
|
|
Apoptosis
Autophagy
Reactive Oxygen Species (ROS)
Mitochondrial Metabolism
PARP
Caspase
Bcl-2 Family
VEGFR
FAK
WDR5
p38 MAPK
JNK
PPAR
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Caudatin is an orally active and brain-penetrant C-21 steroidal found in Cynanchum bungei decne with a variety of biological activities. Caudatin can inhibit cell proliferation, migration, invasion, cause cell phase arrest, induce apoptosis, autophagy, ROS prodution and loss of mitochondrial membrane potential. Caudatin activates PARP, caspase-3, -7, -9, upregulates pro-apoptotic Bad and Bax and downregulates anti-apoptotic Bcl-2 and Bcl-XL. Caudatin suppresses VEGF, FAK phosphorylation, upregulates p21, p27, DR5 protein expression, activates the p38 MAPK, JNK and PPARα/TFEB-mediated autophagy-lysosomal signaling pathways. Caudatin can be used for the research of cancer, inflammation and neurological disease, such as glioma and Alzheimer's disease .
|
-
- HY-134983
-
|
|
E3 Ligase Ligand-Linker Conjugates
Apoptosis
Autophagy
|
Cancer
|
|
Thalidomide-piperazine hydrochloride is a synthetic E3 ligase ligand-linker conjugate, containing a cereblon ligand based on Thalidomide (HY-14658) and one linker. Thalidomide-piperazine hydrochloride can be used in studies related to PROTAC synthesis .
|
-
- HY-N3266
-
|
|
Tyrosinase
Phosphatase
Cholinesterase (ChE)
SARS-CoV
PERK
JNK
p38 MAPK
TGF-beta/Smad
Apoptosis
Reactive Oxygen Species (ROS)
AMPK
MMP
|
Cardiovascular Disease
Infection
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Methyl rosmarinate is an orally active hydroxycinnamic acid. Methyl rosmarinate exhibits an IC50 of 24.70 μM and a Ki of 15.29 μM against PTP1B, an IC50 of 41.46 μg/mL against BChE, a Ki of 0.61 mM against mushroom tyrosinase, and an IC50 of 2.50 μM against SARS-CoV-2 3CLpro. Methyl rosmarinate downregulates the phosphorylation levels of ERK, JNK, p38, Smad2 and Smad3. Methyl rosmarinate activates erythrocyte BPGM and promotes the production of 2,3-BPG. Methyl rosmarinate induces apoptosis of fibroblasts. Methyl rosmarinate prolongs the survival time of hypoxic mice. Methyl rosmarinate improves insulin sensitivity. Methyl rosmarinate binds to SARS-CoV-2 3CLpro and inhibits viral replication. Methyl rosmarinate induces glioblastoma cell death. Methyl rosmarinate activates the TGR5/AMPK axis and reduces the levels of ROS and MDA. Methyl rosmarinate shows inhibitory activity against MMP-1. Methyl rosmarinate can be used in research related to pulmonary fibrosis, hypoxia-induced injury, type 2 diabetes, Alzheimer's disease, hyperpigmentation disorders, COVID-19, glioblastoma and myocardial ischemia-reperfusion injury .
|
-
| Cat. No. |
Product Name |
Type |
-
- HY-124171
-
|
|
Fluorescent Dye
|
|
Zinquin ethyl ester is a cell-permeable and lipophilic fluorescent derivative of Zinquin (HY-D0982). Zinquin ethyl ester reacts with protein-bound Zn 2+ in cells and forms fluorescent ternary adducts. Zinquin ethyl ester undergoes hydrolysis by intracellular esterases impeding its efflux across the plasma membrane (Ex/Em = 370/470 nm) .
|
-
- HY-149696
-
|
|
Fluorescent Dye
|
|
IR-Crizotinib is a NF-κB-inducing kinase (NIK) inhibitor that crosses the blood-brain barrier and fluorescently localizes intracranial glioblastoma (GBM) in mice (IC50=3.381 μM). IR-Crizotinib is conjugated from the near-infrared dye IR-786 and the NF-κB-inducing kinase (NIK) inhibitor Crizotinib. IR-Crizotinib can effectively inhibit the growth and invasion of glioma in vitro and in vivo and can be used in cancer research .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P11099
-
|
|
Transferrin Receptor
|
Neurological Disease
Cancer
|
|
Cys-LT7 is a transferrin receptor (TfR)-targeting peptide ligand. Cys-LT7 binds to a TfR site distinct from endogenous transferrin, mediates conjugated Doxorubicin (HY-15142A) delivery to TfR-overexpressed tumor cells, and exhibits low toxicity to TfR-low-expressed normal cells. Cys-LT7 is an L-configuration peptide susceptible to proteolytic enzymes, leading to poor biostability in peptide-drug conjugates. Cys-LT7 can be used for the research of glioblastoma, hepatocellular carcinoma, lung carcinoma .
|
-
- HY-W006886
-
|
|
Amino Acid Derivatives
|
Others
|
Fmoc-(R)-2-(7-octenyl) Ala-OH is an unnatural Fmoc-protected amino acid and modification module. Fmoc-(R)-2-(7-octenyl) Ala-OH serves as a key building block for all-hydrocarbon cross-linking modification of antimicrobial peptides, and facilitates the generation of stapled peptide derivatives. When introduced into specific sites of the parent peptide, Fmoc-(R)-2-(7-octenyl) Ala-OH effectively increases the α-helix content of the peptide chain, thereby significantly enhancing its antimicrobial activity and proteolytic stability. Fmoc-(R)-2-(7-octenyl) Ala-OH is widely used in research on bacterial infections and the development of related antimicrobial agents . Stapled peptide is a specially chemically modified polypeptide. It locks the peptide chain into a stable α-helical structure by introducing a "staple"-like chemical bridge (usually an all-carbon backbone) at specific positions of the peptide chain.
|
-
- HY-P11326
-
-
- HY-P11029
-
|
|
Peptides
|
Cancer
|
|
CES (CESPLLSEC) is a homing peptide targeting Synaptosomal associated protein 25 (SNAP25). CES specifically homes in intracranial U87MG and the WT-glioblastoma (GBM) model. CES can be used as a targeting peptide for drug delivery for cancers research .
|
| Cat. No. |
Product Name |
Target |
Research Area |
Image |
-
- HY-P99762
-
|
MGD009
|
CD3
|
Cancer
|
|
Obrindatamab is a humanized anti-B7-H3/CD3 bispecific antibody. Obrindatamab binds to B7-H3 and CD3, thereby mediating redirected cytotoxic T-lymphocyte (CTL) activity against B7-H3-expressing cancer cells. Obrindatamab can be used in research of cancer .
|
-
(5)
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-12033
-
-
-
- HY-B0754A
-
-
-
- HY-N1992
-
-
-
- HY-N0826
-
-
-
- HY-B0754
-
-
-
- HY-N1983
-
|
|
Structural Classification
Classification of Application Fields
Asclepiadaceae
Cynanchum otophyllum Schneid.
Cynanchum auriculatum Royle ex Wight
Plants
Disease Research Fields
Steroids
Source Classification
Cancer
|
Apoptosis
Autophagy
Reactive Oxygen Species (ROS)
Mitochondrial Metabolism
PARP
Caspase
Bcl-2 Family
VEGFR
FAK
WDR5
p38 MAPK
JNK
PPAR
|
|
Caudatin is an orally active and brain-penetrant C-21 steroidal found in Cynanchum bungei decne with a variety of biological activities. Caudatin can inhibit cell proliferation, migration, invasion, cause cell phase arrest, induce apoptosis, autophagy, ROS prodution and loss of mitochondrial membrane potential. Caudatin activates PARP, caspase-3, -7, -9, upregulates pro-apoptotic Bad and Bax and downregulates anti-apoptotic Bcl-2 and Bcl-XL. Caudatin suppresses VEGF, FAK phosphorylation, upregulates p21, p27, DR5 protein expression, activates the p38 MAPK, JNK and PPARα/TFEB-mediated autophagy-lysosomal signaling pathways. Caudatin can be used for the research of cancer, inflammation and neurological disease, such as glioma and Alzheimer's disease .
|
-
-
- HY-N3266
-
|
|
Structural Classification
Classification of Application Fields
Simple Phenylpropanols
Adenocarpus cincinnatus (Ball) Maire
Labiatae
Phenols
Polyphenols
Phenylpropanoids
Plants
Disease Research Fields
Source Classification
Cancer
|
Tyrosinase
Phosphatase
Cholinesterase (ChE)
SARS-CoV
PERK
JNK
p38 MAPK
TGF-beta/Smad
Apoptosis
Reactive Oxygen Species (ROS)
AMPK
MMP
|
|
Methyl rosmarinate is an orally active hydroxycinnamic acid. Methyl rosmarinate exhibits an IC50 of 24.70 μM and a Ki of 15.29 μM against PTP1B, an IC50 of 41.46 μg/mL against BChE, a Ki of 0.61 mM against mushroom tyrosinase, and an IC50 of 2.50 μM against SARS-CoV-2 3CLpro. Methyl rosmarinate downregulates the phosphorylation levels of ERK, JNK, p38, Smad2 and Smad3. Methyl rosmarinate activates erythrocyte BPGM and promotes the production of 2,3-BPG. Methyl rosmarinate induces apoptosis of fibroblasts. Methyl rosmarinate prolongs the survival time of hypoxic mice. Methyl rosmarinate improves insulin sensitivity. Methyl rosmarinate binds to SARS-CoV-2 3CLpro and inhibits viral replication. Methyl rosmarinate induces glioblastoma cell death. Methyl rosmarinate activates the TGR5/AMPK axis and reduces the levels of ROS and MDA. Methyl rosmarinate shows inhibitory activity against MMP-1. Methyl rosmarinate can be used in research related to pulmonary fibrosis, hypoxia-induced injury, type 2 diabetes, Alzheimer's disease, hyperpigmentation disorders, COVID-19, glioblastoma and myocardial ischemia-reperfusion injury .
|
-
-
- HY-N3001
-
-
-
- HY-N12834
-
|
|
Apocynaceae
Structural Classification
Plants
Urceola rosea (Hook. & Arn.) D. J. Middleton
Steroids
Source Classification
|
Others
|
|
Ecdysoside B (compound 6b) is a pregnanoside compound isolated from the plant Ecdysanthera rosea. Ecdysoside B and its derivatives and isomers shows anticancer, immunosuppressive and anti-inflammatory activities. Ecdysoside B shows cytotoxicity to a variety of human tumor cell lines, including PANC-1 (human pancreatic cancer cells), A375 (human melanoma cells) and U87 (brain glioma U87 cells). Ecdysoside B can be used for research in the areas of cancer, immunomodulation and anti-inflammato .
|
-
-
- HY-N12887
-
|
|
Natural Products
Marine natural products
Sponge
Source Classification
|
Mitochondrial Metabolism
|
|
Mycothiazole is an inhibitor for mitochondrial electron transport chain (ETC) complex I. Mycothiazole exhibits cytotoxicity in cancer cells Huh7 (IC50 is 55.8 μM), U87 and MCF7. Mycothiazole induces apoptosis in Huh7. Mycothiazole utilizes the unfolded protein response (UPR) and heat shock response (HSR) pathway involved transcription factors ATFS-1 and HSF1, to extend the lifespan of C. elegans .
|
-
-
- HY-N12135
-
|
|
Senegalia pennata (L.) Maslin
Terpenoids
Labiatae
Diterpenoids
Plants
Source Classification
|
Others
|
|
15α-Hydroxy-20-oxo-6,7-seco-ent-kaur-16-en-1,7α(6,11α)-diolide (compound 2) is an enantio-kaurene diterpenoid (ent -kaurene diterpenoid), which can be isolated from Rubescens rubescens. 15α-Hydroxy-20-oxo-6,7-seco-ent-kaur-16-en-1,7α(6,11α)-diolide has cellular activity against EC-1, U87, A549, MCF-7 and HeLa cell lines Toxicity, IC50s are 37.69 μM, 79.362 μM, 80.07 μM, 197.35 μM, 462.13 μM, and 180.09 μM respectively .
|
-
-
- HY-12033R
-
-
-
- HY-N1992R
-
-
-
- HY-N17369
-
-
-
- HY-N12531
-
-
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-12033S2
-
|
|
|
2-Methoxyestradiol-d5 is the deuterium labeled 2-Methoxyestradiol. 2-Methoxyestradiol (2-ME2), an orally active endogenous metabolite of 17β-estradiol (E2), is an apoptosis inducer and an angiogenesis inhibitor with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules. 2-Methoxyestradio, also a potent superoxide dismutase (SOD) inhibitor and a ROS-generating agent, induces autophagy in the transformed cell line HEK293 and the cancer cell lines U87 and HeLa .
|
-
-
- HY-13768S1
-
|
|
|
Topotecan-d6 is the deuterium labeled Topotecan. Topotecan (SKF 104864A; NSC 609669) is a Topoisomerase I inhibitor. The IC50 values of Topotecan at 24 h are 2.73±0.25 μM of U251 cells, 2.95±0.23 μM of U87 cells, 5.46±0.41 μM of GSCs-U251 and 5.95 μM of GSCs-U87 .
|
-
-
- HY-12033S1
-
|
|
|
2-Methoxyestradiol- 13C6 is the 13C-labeled 2-Methoxyestradiol. 2-Methoxyestradiol (2-ME2), an orally active endogenous metabolite of 17β-estradiol (E2), is an apoptosis inducer and an angiogenesis inhibitor with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules. 2-Methoxyestradio, also a potent superoxide dismutase (SOD) inhibitor and a ROS-generating agent, induces autophagy in the transformed cell line HEK293 and the cancer cell lines U87 and HeLa .
|
-
-
- HY-12033S
-
|
|
|
2-Methoxyestradiol- 13C,d3 is the 13C- and deuterium labeled 2-Methoxyestradiol. 2-Methoxyestradiol (2-ME2), an orally active endogenous metabolite of 17β-estradiol (E2), is an apoptosis inducer and an angiogenesis inhibitor with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules. 2-Methoxyestradio, also a potent superoxide dismutase (SOD) inhibitor and a ROS-generating agent, induces autophagy in the transformed cell line HEK293 and the cancer cell lines U87 and HeLa .
|
-
-
- HY-13768S
-
|
|
|
Topotecan-d5 is the deuterium labeled Topotecan. Topotecan (SKF 104864A; NSC 609669) is a Topoisomerase I inhibitor. The IC50 values of Topotecan at 24 h are 2.73±0.25 μM of U251 cells, 2.95±0.23 μM of U87 cells, 5.46±0.41 μM of GSCs-U251 and 5.95±0.24 μM of GSCs-U87 .
|
-
-
- HY-B1490AS
-
|
|
|
Imipramine-d6 is the deuterium labeled Imipramine hydrochloride. Imipramine is an orally active tertiary amine tricyclic antidepressant. Imipramine is a Fascin1 inhibitor with antitumor activities. Imipramine also inhibits serotonin transporter with an IC50 value of 32 nM. Imipramine stimulates U-87MG glioma cells autophagy and induces HL-60 cell apoptosis. Imipramine shows neuroprotective and immunomodulatory effects .
|
-
-
- HY-B1490S1
-
|
|
|
Imipramine-d3 (hydrochloride) is deuterium labeled Imipramine (hydrochloride). Imipramine is an orally active tertiary amine tricyclic antidepressant. Imipramine is a Fascin1 inhibitor with antitumor activities. Imipramine also inhibits serotonin transporter with an IC50 value of 32 nM. Imipramine stimulates U-87MG glioma cells autophagy and induces HL-60 cell apoptosis. Imipramine shows neuroprotective and immunomodulatory effects .
|
-
-
- HY-B1490S
-
|
|
|
Imipramine-d4 (hydrochloride) is the deuterium labeled Imipramine hydrochloride. Imipramine hydrochloride is an orally active tertiary amine tricyclic antidepressant. Imipramine hydrochloride is a Fascin1 inhibitor with antitumor activities. Imipramine hydrochloride also inhibits serotonin transporter with an IC50 value of 32 nM. Imipramine hydrochloride stimulates U-87MG glioma cells autophagy and induces HL-60 cell apoptosis. Imipramine hydrochloride shows neuroprotective and immunomodulatory effects .
|
-
-
- HY-B1490AS1
-
|
|
|
Imipramine-d4 is deuterium labeled Imipramine. Imipramine is an orally active tertiary amine tricyclic antidepressant. Imipramine is a Fascin1 inhibitor with antitumor activities. Imipramine also inhibits serotonin transporter with an IC50 value of 32 nM. Imipramine stimulates U-87MG glioma cells autophagy and induces HL-60 cell apoptosis. Imipramine shows neuroprotective and immunomodulatory effects .
|
-
-
- HY-B1490AS3
-
|
|
|
Imipramine-d4-1 is the deuterium labeled Imipramine (HY-W010179). Imipramine is an orally active tertiary amine tricyclic antidepressant. Imipramine is a Fascin1 inhibitor with antitumor activities. Imipramine also inhibits serotonin transporter with an IC50 value of 32 nM. Imipramine stimulates U-87MG glioma cells autophagy and induces HL-60 cell apoptosis. Imipramine shows neuroprotective and immunomodulatory effects .
|
-
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