HI5
HI5 is a potent tublin and IDO inhibitor, with an IC50 value of 70 nM in HeLa cells. HI5 inhibit IDO expression and decrease kynurenine production, leading to stimulating T cells activation and proliferation. HI5 can inhibit tubulin polymerization and cell migration, cause G2/M phase arrest, and induce apoptosis via the mitochondrial dependent apoptosis pathway and cause reactive oxidative stress generation in HeLa cells. HI5 can be used for researching anticancer.
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- CAS No.: 2411548-90-6
- Formule: C42H43N5O8
- Masse moléculaire:745.82
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
IC50: 70 nM in HeLa[1]
In Vitro
HI5 (0-10 μM; 72 hours) exhibits potent antiproliferative activity in HeLa, PC-3, A549 and HUVEC[1].
HI5 (0.1 and 0.5 μM; 24 hours) exhibits markedly disruption of microtubule organization in a concentration-dependent manner[1].
HI5 (0.5 μM; 24 hours) significantly up-regulates the expression level of Bax protein, while down-regulates the protein of Bcl-2, furthermore, markedly up-regulates the protein expressions of caspase-3 and PARP[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HeLa, PC-3, A549 and HUVEC[1]
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Concentration:0-10 μM
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Incubation Time:72 hours
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Result:Exhibited potent antiproliferative activity in HeLa, PC-3, A549 and HUVEC with IC50s of 0.07 ± 0.005 μM, 0.46 ± 0.06 μM, 0.22 ± 0.10 μM, 1.52 ± 0.09 μM, respectively.
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Cell Line:HeLa[1]
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Concentration:0.1 and 0.5 μM
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Incubation Time:24 hours
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Result:Exhibited markedly disruption of microtubule organization in a concentration-dependent manner.
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Cell Line:HeLa[1]
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Concentration:0.5 μM
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Incubation Time:24 hours
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Result:Significantly up-regulated the expression level of Bax protein, while down-regulated the protein of Bcl-2, furthermore, markedly up-regulated the protein expressions of caspase-3 and PARP.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude mice (18-22 g, 5 week-old, injected with HeLa cells)[1]
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Dosage:15 and 30 mg/kg
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Administration:IV; daily, for 21 days
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Result:Significantly inhibited tumor growth at a dose-dependent manner with inhibitory rates of 50.73% and 65.76% at doses of 15 and 30 mg/kg, respectively.
Chemical Information
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CAS No. 2411548-90-6
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Masse moléculaire 745.82
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Formule C42H43N5O8
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SMILES
NC(CC1=CN(C)C2=CC=CC=C12)C(OCCC3=CN(CC4=CC=CC(C(OC5=CC(/C=C\C6=CC(OC)=C(OC)C(OC)=C6)=CC=C5OC)=O)=C4)N=N3)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
HI5 Related Classifications
HY-146261 Related Classifications
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