solo per uso di ricerca
N. Cat.: S2310
Struttura chimica
| Target correlati | PI3K Akt mTOR GSK-3 ATM/ATR DNA-PK AMPK PDPK1 PTEN PP2A |
|---|---|
| Altro Antineoplastic and Immunosuppressive Antibiotics Inibitori | Staurosporine (STS) Cyclosporin A Oligomycin A (MCH 32) Puromycin Dihydrochloride Nigericin sodium salt Geldanamycin (NSC 122750) Streptozotocin (STZ) Sodium Monensin (NSC 343257) Hygromycin B Cephalomannine |
| Linee cellulari | Tipo di saggio | Concentrazione | Tempo di incubazione | Formulazione | Descrizione dell'attività | PMID |
|---|---|---|---|---|---|---|
| human UACC-903 cells | Cytotoxicity assay | Cytotoxicity against human UACC-903 cells after 72 hrs by MTS assay, IC50=5.1 μM | ||||
| Vero E6 cells | Function assay | Antiviral activity against SARS coronavirus in Vero E6 cells assessed as inhibition of viral replication by ELISA, EC50=6.5 μM | ||||
| human UACC-903 cells | Cytotoxicity assay | Cytotoxicity against human UACC-903 cells after 24 hrs by MTS assay, IC50=7.45 μM | ||||
| human A549 cells | Cytotoxicity assay | Cytotoxicity against human A549 cells after 72 hrs by MTS assay, IC50=7.75 μM | ||||
| human CEM cells | Cytotoxicity assay | Cytotoxicity against human CEM cells, IC50=10.9 μM | ||||
| HEK293 cells | Function assay | Agonist activity at RXRalpha in HEK293 cells assessed as transcriptional activation after 48 hrs by luciferase reporter gene assay, EC50=11.8 μM | ||||
| human A549 cell | Cytotoxicity assay | 24 h | Cytotoxicity against human A549 cells after 24 hrs by MTS assay, IC50=12.51 μM | |||
| human HT-29 cells | Cytotoxicity assay | 72 h | Cytotoxicity against human HT-29 cells after 72 hrs by MTS assay, IC50=13.24 μM | |||
| human PBM cells | Cytotoxicity assay | Cytotoxicity against human PBM cells, IC50=16.1 μM | ||||
| Hep-G2 cells | Cytotoxicity assay | Cytotoxicity of compound against human liver tumor cell line (Hep-G2) was determined, IC50=16.5 μM | ||||
| human HepG2 cells | Proliferation assay | 24 h | Antiproliferative activity against human HepG2 cells after 24 hrs by MTT assay, IC50=16.5 μM | |||
| human K562 cells | Proliferation assay | Antiproliferative activity against human K562 cells by MTT assay, IC50=21.1 μM | ||||
| Vero cells | Cytotoxicity assay | Cytotoxicity against Vero cells, IC50=22.5 μM | ||||
| human A2780 cells | Proliferation assay | Antiproliferative activity against cisplatin-sensitive human A2780 cells by MTT assay, IC50=30.5 μM | ||||
| human SPC-A1 cells | Proliferation assay | Antiproliferative activity against human SPC-A1 cells by MTT assay, IC50=36.1 μM | ||||
| HUVEC cells | Function assay | 20 μM | 24 h | Antimigratory activity against human HUVEC cells at 20 uM after 24 hrs by wound-healing assay | ||
| HEK293 cells | Function assay | 24-48 h | Agonist activity at human RXR-alpha expressed in HEK293 cells coexpressing with pCMX-beta-gal after 24 to 48 hrs by luciferase reporter gene assay | |||
| human SH-SY5Y cells | Function assay | 10 μM | 30 mins | Neuroprotective activity in human SH-SY5Y cells assessed as inhibition of CHP and TBHP-induced cell death at 10 uM incubated for 30 mins prior to challenge measured after 3 hrs by MTT assay | ||
| Clicca per visualizzare più dati sperimentali sulle linee cellulari | ||||||
| Peso molecolare | 266.334 | Formula | C18H18O2 |
Conservazione (Dalla data di ricezione) | |
|---|---|---|---|---|---|
| N. CAS | 35354-74-6 | Scarica SDF | Conservazione delle soluzioni stock |
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| Sinonimi | NSC 293100 | Smiles | C=CCC1=CC(=C(C=C1)O)C2=CC(=C(C=C2)O)CC=C | ||
|
In vitro |
DMSO
: 53 mg/mL
(198.99 mM)
Water : Insoluble Ethanol : Insoluble |
|
In vivo |
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Passo 1: Inserire le informazioni di seguito (Consigliato: Un animale aggiuntivo per tenere conto della perdita durante l'esperimento)
Passo 2: Inserire la formulazione in vivo (Questo è solo il calcolatore, non la formulazione. Contattateci prima se non c'è una formulazione in vivo nella sezione Solubilità.)
Risultati del calcolo:
Concentrazione di lavoro: mg/ml;
Metodo per preparare il liquido master di DMSO: mg farmaco predissolto in μL DMSO ( Concentrazione del liquido master mg/mL, Vi preghiamo di contattarci prima se la concentrazione supera la solubilità del DMSO del lotto del farmaco. )
Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungereμL PEG300, mescolare e chiarire, quindi aggiungereμL Tween 80, mescolare e chiarire, quindi aggiungere μL ddH2O, mescolare e chiarire.
Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungere μL Olio di mais, mescolare e chiarire.
Nota: 1. Si prega di assicurarsi che il liquido sia limpido prima di aggiungere il solvente successivo.
2. Assicurarsi di aggiungere il/i solvente/i in ordine. È necessario assicurarsi che la soluzione ottenuta, nell'aggiunta precedente, sia una soluzione limpida prima di procedere all'aggiunta del solvente successivo. Metodi fisici come il vortex, gli ultrasuoni o il bagno d'acqua calda possono essere utilizzati per facilitare la dissoluzione.
| Targets/IC50/Ki |
Akt-phosphorylation
MEK
|
|---|---|
| In vitro |
Honokiol shows pro-apoptotic effects in melanoma, sarcoma, myeloma, leukemia, bladder, lung, prostate, oral squamous cell carcinoma and colon cancer cell lines. This compound is effective on inducing apoptosis in SVR angiosarcoma cells. Treatment of SVR cells with this chemical causes decreased phosphorylation of MAP kinase, akt, and c-src. In addition, it potentiates TRAIL-mediated apoptosis, and its cytotoxicity is partially abrogated by neutralizing antibodies to TRAIL. This compound also has direct antiangiogenic activity, in that it blocks the phosphorylation and rac activation due to VEGF-VEGFR2 interactions. It causes apoptosis in CLL cells through activation of caspase 8, followed by caspase 9 and 3 activation. This chemical prevents interleukin-4-mediated survival of CLL cells, and potentiats the cytotoxicity of CB-1348, FaraA, and 2-CdA. It kills myeloma cells from relapsed patients at doses that does not kill PBMCs. Caspase 3, 7, 8, and 9 are induced by this compound treatment, as well as PARP cleavage. It is found to induce apoptosis in the colon cancer cell lines RKO. This chemical potentiates apoptosis, suppresses osteoclastogenesis, and inhibits invasion through modulation of nuclear factor-kappaB activation pathway. It may act as a potent anti-inflammatory agent with multipotential activities due to an inhibitory effect on the PI3K/Akt pathway. |
| In vivo |
Honokiol is highly effective against SVR angiosarcoma in nude mice. This compound inhibits the growth of RKO cells in murine xenografts. It prevents the growth of MDA-MD-231 breast cancer cells in murine xenografts. |
Riferimenti |
|
| Metodi | Biomarcatori | Immagini | PMID |
|---|---|---|---|
| Western blot | p-EGFR / p-AKT / p-STAT3 / p-ERK / p-GSK3α/β / Bax / p-pRb / p-BAD / IκBα / CDK2 / CDK4 / Cyclin D1 p-Lyn / Lyn / p-PI3K |
|
27458163 |
| Immunofluorescence | Vimentin / Occludin IκBα / NF-κB p65 |
|
24508063 |