1. PI3K/Akt/mTOR Epigenetics Cell Cycle/DNA Damage
  2. PI3K HDAC
  3. PI3K/HDAC-IN-2

PI3K/HDAC-IN-2 is a potent dual PI3K/HDAC inhibitor with IC50s of 226 nM, 279 nM, 467 nM, 29 nM for PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ, respectively, and IC50s of 1.3 nM, 3.4 nM, 972 nM, 17 nM, 12 nM for HDAC1, HDAC2, HDC4, HDAC6, HDAC8, respectively. PI3K/HDAC-IN-2 exhibits PI3Kδ and class I and IIb HDAC selectivity. PI3K/HDAC-IN-2 has remarkable anticancer effects.

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

PI3K/HDAC-IN-2 Chemical Structure

PI3K/HDAC-IN-2 Chemical Structure

CAS No. : 2361418-65-5

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Description

PI3K/HDAC-IN-2 is a potent dual PI3K/HDAC inhibitor with IC50s of 226 nM, 279 nM, 467 nM, 29 nM for PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ, respectively, and IC50s of 1.3 nM, 3.4 nM, 972 nM, 17 nM, 12 nM for HDAC1, HDAC2, HDC4, HDAC6, HDAC8, respectively. PI3K/HDAC-IN-2 exhibits PI3Kδ and class I and IIb HDAC selectivity. PI3K/HDAC-IN-2 has remarkable anticancer effects[1].

IC50 & Target[1]

PI3Kα

226 nM (IC50)

PI3Kβ

279 nM (IC50)

PI3Kγ

467 nM (IC50)

PI3Kδ

29 nM (IC50)

HDAC1

1.3 nM (IC50)

HDAC2

3.4 nM (IC50)

HDAC4

972 nM (IC50)

HDAC6

17 nM (IC50)

HDAC8

12 nM (IC50)

In Vitro

For PI3K/HDAC-IN-2 (Compound 8), the IC50 values in the growth inhibition assay against MDA-MB-453, HCT116 and HGC-27 cells are as low as namomolar level, which are 4 nM, 7 nM and 14 nM respectively[1].
PI3K/HDAC-IN-2 (Compound 8) shows antiproliferative activities against 16 DLBCL cell lines with IC50s of 3.6-21 nM[1].

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

In Vivo

In the zebrafish xenograft model of SU-DHL-4 cells, PI3K/HDAC-IN-2 (Compound 8) exhibits in vivo growth inhibitory activity at 3 μM[1].

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

Molecular Weight

461.47

Formula

C23H23N7O4

CAS No.
SMILES

O=C(C1=CN=C(N(CCOC2=CC(C3=CC=C(OC)N=C3)=CC4=C(C)N=CN=C24)C)N=C1)NO

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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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Product Name:
PI3K/HDAC-IN-2
Cat. No.:
HY-146159
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