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Cat. No.: HY-151985

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TACC3 inhibitor 1

TACC3 inhibitor 1 is a potent and cross the blood-brain barrier TACC3 inhibitor. TACC3 inhibitor 1 induces Apoptosis and cell cycle arrest at G2/M phase. TACC3 inhibitor 1 induces the generation of intracellular ROS. TACC3 inhibitor 1 shows antiproliferative and anti-tumor activity.

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

CAS No.: 3033646-06-6
Formula: C₂₀H₂₁N₅OS
Molecular Weight:379.48

Storage:

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

Data Sheet (270 KB)

TACC3 inhibitor 1 Chemical Structure

CAS No.: 3033646-06-6

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

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

Biological Activity

Description

Cellular Effect

Cell Line	Type	Value	Description	References
JIMT-1	IC₅₀	4.84 μM Compound: 7g	Antiproliferative activity against human JIMT-1 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay Antiproliferative activity against human JIMT-1 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay	[PMID: 36332551]
MDA-MB-231	IC₅₀	6.46 μM Compound: 7g	Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay	[PMID: 36332551]
SK-OV-3	IC₅₀	8.21 μM Compound: 7g	Antiproliferative activity against human SK-OV-3 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay Antiproliferative activity against human SK-OV-3 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay	[PMID: 36332551]
U-251	IC₅₀	5.61 μM Compound: 7g	Cytotoxicity against human U251 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay Cytotoxicity against human U251 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay	[PMID: 36332551]
U-87MG ATCC	IC₅₀	27.54 μM Compound: 7g	Cytotoxicity against human U87 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay Cytotoxicity against human U87 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay	[PMID: 36332551]
U-87MG ATCC	IC₅₀	3.29 μM Compound: 7g	Antiproliferative activity against human U87 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human U87 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 36332551]

In Vitro

TACC3 inhibitor 1 (compound 7g) (1, 2, 4 µM; 36 h) induces apoptosis and cell cycle arrest at G2/M phase^[1].
TACC3 inhibitor 1 (1, 2, 4 µM; 36 h) decreases the mitochondrial membrane potential and induces the generation of intracellular ROS^[1].
TACC3 inhibitor 1 (1, 2, 4 µM; 24 h) inhibits cell migration and invasion in U87 cells^[1].

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

Cell Proliferation Assay^[1]

Cell Line:

U251, U87, MDA-MB-231, JIMT-1, SKOV-3, HLF-1 cells
Concentration:

0-100 µM
Incubation Time:

24 h
Result:

Showed antiproliferative activities with IC₅₀s of 5.61, 3.29, 6.46, 4.84, 8.21, 23.11 µM for U251, U87, MDA-MB-231, JIMT-1, SKOV-3, HLF-1 cells, respectively.

Cell Cycle Analysis^[1]

Cell Line:

U87 cells
Concentration:

1, 2, 4 µM
Incubation Time:

36 h
Result:

Induced cell cycle arrest at G2/M phase with the 41.2% cells at G2/M phase at 4 µM.

Apoptosis Analysis^[1]

Cell Line:

U87 cells
Concentration:

1, 2, 4 µM
Incubation Time:

36 h
Result:

Induced apoptosis in a dose-dependent manner with the percentage of early apoptotic cells increased from 4.49% in control group to 21.42%, late apoptotic cells increased from 0.52% to 26.72% at 4 µM.

In Vivo

TACC3 inhibitor 1 (20 mg/kg; i.p.; daily for 20 days) shows anti-tumor activity in mouse^[1].

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

Animal Model:

Six-week-old BALB/c nude mice (U87 xenograft model)^[1]
Dosage:

20 mg/kg
Administration:

I.p.; daily for 20 days
Result:

Exhibited a significant tumor growth regression and no observable toxicity during the administration period and had no effects on the body weight.

Chemical Information

CAS No. 3033646-06-6
Molecular Weight 379.48
Formula C₂₀H₂₁N₅OS
SMILES

OC1CC2CC1CN2C3=CC=NC(NCC4=CSC(C5=CC=CC=C5)=N4)=N3
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 (270 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]. Zhao W, et al. Discovery of novel analogs of KHS101 as transforming acidic coiled coil containing protein 3 (TACC3) inhibitors for the treatment of glioblastoma. Eur J Med Chem. 2022 Dec 15;244:114874. [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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