1. Cell Cycle/DNA Damage Cytoskeleton Apoptosis
  2. Microtubule/Tubulin Apoptosis
  3. IDO/Tubulin-IN-2

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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IDO/Tubulin-IN-2 Chemical Structure

IDO/Tubulin-IN-2 Chemical Structure

CAS No. : 2409479-24-7

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Description

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[1].

IC50 & Target

TDO, Tubulin[1]

In Vitro

IDO/Tubulin-IN-2 (HT2) (0-50 μM, 4 h) shows potent cytotoxicity with IC50 values between 0.036 and 0.43 μM against cancer cell lines[1].
IDO/Tubulin-IN-2 (0.1 μM, 24 h) arrests the HepG2 cells cycle mainly at the G2 phase[1].
IDO/Tubulin-IN-2 (0.1 μM, 24 h) can effectively cause cell apoptosis[1].
IDO/Tubulin-IN-2 (0.1 μM, 24 h) has strongly effects on inducing the proteolytic cleavage of PARP and up-regulating the expression level of caspase-3[1].
IDO/Tubulin-IN-2 (0.05 μM, 24, 48 and 72 h) markedly decreases mRNA expression level of TDO at a time-dependent manner[1].
IDO/Tubulin-IN-2 (2 days) can improve T-cell activation and proliferation and enhance immune response[1].

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

Cell Proliferation Assay

Cell Line: Human cancer cell lines and non-tumoral cell line[1]
Concentration: 0-50 μM
Incubation Time: 4 h
Result: Displayed potent cytotoxicity with IC50 values of 0.43 μM (U87), 0.036 μM (HepG2), 0.041 μM (A549), 0.095 μM (HCT-116), and 1.04 μM (LO2).

Cell Cycle Analysis

Cell Line: HepG2 cells[1]
Concentration: 0.1 μM
Incubation Time: 24 h
Result: Arrested the HepG2 cells cycle mainly at the G2 phase.

Apoptosis Analysis

Cell Line: HepG2 cells[1]
Concentration: 0.1 μM
Incubation Time: 24 h
Result: Effectively caused cell apoptosis, the percentage of apoptosis cells increased to 54%

Western Blot Analysis

Cell Line: HepG2 cells[1]
Concentration: 0.1 μM
Incubation Time: 24 h
Result: Showed strongly effects on inducing the proteolytic cleavage of PARP and up-regulating the expression level of caspase-3, which could lead to cell death at last.

RT-PCR

Cell Line: HepG2 cells[1]
Concentration: 0.05 μM
Incubation Time: 24, 48 and 72 h
Result: Markedly decreased mRNA expression level of TDO at a time-dependent manner.
In Vivo

IDO/Tubulin-IN-2 (HT2) (30 mg/kg; IV; daily, for 21 days) significantly inhibits tumor growth[1].
IDO/Tubulin-IN-2 (30 mg/kg; IV; 29 days) has effective antitumor immunity ability to promote the tumor therapeutic efficacy[1].

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

Animal Model: ICR mice (mouse liver cancer xenograft models, established by subcutaneous inoculation of H22 cells)[1]
Dosage: 30 mg/kg
Administration: Intravenously injected via a tail vein; daily, for 21 days
Result: Significantly inhibited tumor growth.
Animal Model: Male A549 tumor xenograft BALB/c nude mice (5 weeks, 18-22 g)[1]
Dosage: 30 mg/kg
Administration: IV, daily, for 29 days
Result: Had effective antitumor immunity ability to promote the tumor therapeutic efficacy.
Molecular Weight

860.87

Formula

C48H40N6O10

CAS No.
SMILES

COC1=CC=C(C=C1OC(C2=CC=CC(CN3C=C(N=N3)CCOC(C4=CC=CC(CN5N=NC6=C5C(C7=CC=CC=C7C6=O)=O)=C4)=O)=C2)=O)/C=C\C8=CC(OC)=C(C(OC)=C8)OC

Shipping

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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IDO/Tubulin-IN-2 Related Classifications

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Help & FAQs
  • 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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IDO/Tubulin-IN-2
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