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Cat. No.: HY-144299

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Tubulin polymerization-IN-5

Tubulin polymerization-IN-5 (compound 20q) is a potent tubulin inhibitor with potential anticancer activities. Tubulin polymerization-IN-5 can arrest ESCC cells at G2/M phase and cause cells apoptosis.

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

CAS No.: 3033213-12-3
Formula: C₂₉H₃₉N₃O₈S₂
Molecular Weight:621.77

Storage:

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

Data Sheet (272 KB)

Tubulin polymerization-IN-5 Chemical Structure

CAS No.: 3033213-12-3

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Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

Tubulin

Cellular Effect

Cell Line	Type	Value	Description	References
HCT-116	IC₅₀	0.128 μM Compound: 20q	Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay	[PMID: 34971875]
HCT-116	IC₅₀	0.22 μM Compound: I-13	Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 36940611]
KYSE-30	IC₅₀	0.069 μM Compound: 20q	Antiproliferative activity against human KYSE-30 cells assessed as cell viability measured after 48 hrs by CCK8 assay Antiproliferative activity against human KYSE-30 cells assessed as cell viability measured after 48 hrs by CCK8 assay	[PMID: 34971875]
KYSE-450	IC₅₀	0.076 μM Compound: 20q	Antiproliferative activity against human KYSE-450 cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay Antiproliferative activity against human KYSE-450 cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay	[PMID: 34971875]
KYSE-450	IC₅₀	0.076 μM Compound: 20q	Antiproliferative activity against human KYSE-450 cells assessed as cell viability measured after 48 hrs by CCK8 assay Antiproliferative activity against human KYSE-450 cells assessed as cell viability measured after 48 hrs by CCK8 assay	[PMID: 34971875]
KYSE-450	IC₅₀	0.078 μM Compound: I-13	Antiproliferative activity against human KYSE-450 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human KYSE-450 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 36940611]
MGC-803	IC₅₀	0.082 μM Compound: 20q	Antiproliferative activity against human MGC-803 cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay Antiproliferative activity against human MGC-803 cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay	[PMID: 34971875]
MGC-803	IC₅₀	0.084 μM Compound: I-13	Antiproliferative activity against human MGC-803 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human MGC-803 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 36940611]

In Vitro

Tubulin polymerization-IN-5 (compound 20q) (0-100 nM, 48 h) exhibits potent antiproliferative activity against Kyse30, Kyse450, MGC-803, and HCT-116 cells^[1].
Tubulin polymerization-IN-5 (0-60 nM, 7 d) obviously inhibits the cellular colony formation ability of the Kyse30 and Kyse450 cells^[1].
Tubulin polymerization-IN-5 (0-100 nM, 48 h) inhibits microtubule assembly and disrupts cytoskeleton^[1].
Tubulin polymerization-IN-5 (0-300 nM, 24 h) causes a significant weakening of the β-tubulin adduct band in Kyse30 and Kyse450 cells, competitively bind the colchicine binding site of β-tubulin^[1].
Tubulin polymerization-IN-5 (0-100 nM, 48 h) effectively arrests cells at the G2/M phase, and induces cell apoptosis in Kyse30 and Kyse450 cells by regulating the expression of related proteins^[1].
Tubulin polymerization-IN-5 (0-100 nM, 48 h) induces cell mitochondrial apoptosis in ESCC cells, leads to a significant depolarization of mitochondria membrane potential in Kyse30 and Kyse450 cells^[1].

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

Cell Proliferation Assay

Cell Line:

Kyse30, Kyse450, MGC-803, and HCT-116 cells^[1]
Concentration:

0, 80, 100 nM
Incubation Time:

48 h
Result:

Exhibited potent antiproliferative activity against Kyse30, Kyse450, MGC-803, and HCT-116 cells, with IC₅₀ values of 0.069, 0.078, 0.084, and 0.227 μM, respectively.

Cell Cycle Analysis

Cell Line:

Kyse30 and Kyse450 cells^[1]
Concentration:

0, 80, 100 nM
Incubation Time:

48 h
Result:

Effectively arrested 2 ESCC cells at the G2/M phase, significantly increased of percentages of cells at the G2/M phase from 19.38 to 76.9767 in Kyse30 cells, and 7.04333 to 80.8933 in Kyse450 cells.

Apoptosis Analysis

Cell Line:

Kyse30 and Kyse450 cells^[1]
Concentration:

0, 80, 100 nM
Incubation Time:

48 h
Result:

Dose-dependently induced cell apoptosis in Kyse30 and Kyse450 cells, significantly increased the percentages of total apoptotic cells from 8.1667% (0 nM) to 23.8% (80 nM, Kyse30 cells), 34.0333% (80 nM, Kyse450 cells), 38.633% (100 nM, Kyse30 cells), and 57.3667% (100 nM, Kyse450 cells), respectively.

Western Blot Analysis

Cell Line:

Kyse30 and Kyse450 cells^[1]
Concentration:

0, 80, 100 nM
Incubation Time:

48 h
Result:

Dose-dependently down-regulated the expression of the G2 phase related proteins CDK1, CDC25c and p-Wee 1, up-regulated the level of the M phase marker protein p-Histone H3; up-regulated the activity of the executors of apoptosis caspase-3, up-regulated the pro-apoptotic proteins Bax and Noxa, and down-regulated the anti-apoptotic protein Bcl-2, decreased the levels of IAP (Inhibitor of Apoptosis Proteins) family protein XIAP.

Chemical Information

CAS No. 3033213-12-3
Molecular Weight 621.77
Formula C₂₉H₃₉N₃O₈S₂
SMILES

COC1=CC(N(C(CSC(N2CCN(CC2)C(OC(C)(C)C)=O)=S)=O)CC3=CC(O)=C(C=C3)OC)=CC(OC)=C1OC
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Sun YX, et al. Design, synthesis and evaluation of novel bis-substituted aromatic amide dithiocarbamate derivatives as colchicine site tubulin polymerization inhibitors with potent anticancer activities. Eur J Med Chem. 2022;229:114069. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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