Top/HDAC-IN-2

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Top/HDAC-IN-2 (45b), a Top and HDAC dual inhibitor, exhibits potent antitumor activities and induces apoptosis.

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Top/HDAC-IN-2 Chemical Structure

CAS No. : 2775446-64-3

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•Related Small Molecules:

•Related Proteins:

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HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

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Topoisomerase Topo I Topo II

Biological Activity
Purity & Documentation
References
Customer Review

Description

Top/HDAC-IN-2 (45b), a Top and HDAC dual inhibitor, exhibits potent antitumor activities and induces apoptosis^[1].

IC₅₀ & Target

HDAC1

0.004 μM (IC₅₀)

HDAC2

0.005 μM (IC₅₀)

HDAC6

0.15 μM (IC₅₀)

HDAC3

1.10 μM (IC₅₀)

HDAC8

4.5 μM (IC₅₀)

Top1

Topoisomerase II

In Vitro

Top/HDAC-IN-2 (45b) shows antitumor activities against the HCT116 (IC₅₀ = 0.23 µM), MCF-7 and A549 cells^[1].
Top/HDAC-IN-2 (45b) (0-5 µM, 24h) arrests the HCT116 cell cycle at the G2 phase in a concentration-dependent manner^[1].
Top/HDAC-IN-2 (45b) (0-2.5 µM, 24h) induces the apoptosis in HCT116 cell line in a concentration-dependent manner^[1].
Top/HDAC-IN-2 (45b) (0-5 μM, 24h) inhibits HDAC in living cells^[1].

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

Cell Cycle Analysis^[1]

Cell Line:	HCT116
Concentration:	0.1, 2.5 and 5 μM
Incubation Time:	24 h
Result:	Arrested the HCT116 cell cycle at the G2 phase in a concentration-dependent manner.

Apoptosis Analysis^[1]

Cell Line:	HCT116
Concentration:	0.1, 0.5 and 2.5 μM
Incubation Time:	24 h
Result:	Effectively induced the apoptosis in HCT116 cell line in a concentration-dependent manner.

Western Blot Analysis^[1]

Cell Line:	HCT116
Concentration:	1 μM and 5 μM
Incubation Time:	24 h
Result:	Concentration-dependently increased the level of acetyl-H3 and acetyl-H4 in HCT116 cells.

Molecular Weight

568.63

Formula

C₃₀H₃₂N₈O₄

CAS No.

2775446-64-3

SMILES

CN1C2=C(C(N3CCC4=C(C13)NC5=CC=C(C=C54)O)=O)C=C(C=C2)NCC6CCN(CC6)C7=NC=C(C=N7)C(NO)=O

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

Handling Instructions (2659 KB)

References

[1]. Fugui Zhu, et al. Design, Synthesis, and Structure-Activity relationships of Evodiamine-Based topoisomerase (Top)/Histone deacetylase (HDAC) dual inhibitors. Bioorg Chem. 2022 May;122:105702. [Content Brief]

Top/HDAC-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.

Keywords:

Top/HDAC-IN-22775446-64-3HDACTopoisomeraseApoptosisHistone deacetylasesHCT116metabolic stabilitiesantitumorInhibitorinhibitorinhibit

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