1. Cell Cycle/DNA Damage Cytoskeleton Metabolic Enzyme/Protease Apoptosis
  2. Microtubule/Tubulin Indoleamine 2,3-Dioxygenase (IDO) Apoptosis
  3. 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.

For research use only. We do not sell to patients.

HI5 Chemical Structure

HI5 Chemical Structure

CAS No. : 2411548-90-6

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Description

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[1].

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.

Cell Proliferation Assay

Cell Line: HeLa, PC-3, A549 and HUVEC[1]
Concentration: 0-10 μM
Incubation Time: 72 hours
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.

Immunofluorescence

Cell Line: HeLa[1]
Concentration: 0.1 and 0.5 μM
Incubation Time: 24 hours
Result: Exhibited markedly disruption of microtubule organization in a concentration-dependent manner.

Western Blot Analysis

Cell Line: HeLa[1]
Concentration: 0.5 μM
Incubation Time: 24 hours
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

HI5 (15 and 30 mg/kg; IV; daily, for 21 days) significantly inhibits tumor growth at a dose-dependent manner[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/c nude mice (18-22 g, 5 week-old, injected with HeLa cells)[1]
Dosage: 15 and 30 mg/kg
Administration: IV; daily, for 21 days
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.
Molecular Weight

745.82

Formula

C42H43N5O8

CAS No.
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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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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HI5
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HY-146261
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