Cat. No.: HY-146159

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.

CAS No.: 2361418-65-5
Formula: C₂₃H₂₃N₇O₄
Molecular Weight:461.47

Storage:

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

Data Sheet (271 KB)

PI3K/HDAC-IN-2 Chemical Structure

CAS No.: 2361418-65-5

Size

Price

Stock

Quantity

Amount: USD 0.00

* Please select Quantity before adding items.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

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

Biological Activity

Description

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)

All PI3K Isoforms :

All HDAC Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
Bel-7402	IC₅₀	1.6 μM Compound: 36	Antiproliferative activity against human Bel7402 cells after 96 hrs by MTT assay Antiproliferative activity against human Bel7402 cells after 96 hrs by MTT assay	[PMID: 31117517]
Capan-2	IC₅₀	0.27 μM Compound: 36	Antiproliferative activity against human Capan2 cells after 96 hrs by MTT assay Antiproliferative activity against human Capan2 cells after 96 hrs by MTT assay	[PMID: 31117517]
CHO	IC₅₀	>30 μM Compound: 36	Inhibition of human ERG stably expressed in CHO cells by whole cell patch clamp method Inhibition of human ERG stably expressed in CHO cells by whole cell patch clamp method	[PMID: 31117517]
DOHH-2	IC₅₀	0.0077 μM Compound: 8	Antiproliferative activity against human DOHH-2 cells measured after 4 days by Cell Titer Glo Luminescent Cell Viability Assay Antiproliferative activity against human DOHH-2 cells measured after 4 days by Cell Titer Glo Luminescent Cell Viability Assay	[PMID: 35644299]
DU-145	IC₅₀	0.066 μM Compound: 36	Antiproliferative activity against human DU145 cells after 96 hrs by MTT assay Antiproliferative activity against human DU145 cells after 96 hrs by MTT assay	[PMID: 31117517]
HBL1	IC₅₀	0.0079 μM Compound: 8	Antiproliferative activity against human HBL1 cells measured after 4 days by Cell Titer Glo Luminescent Cell Viability Assay Antiproliferative activity against human HBL1 cells measured after 4 days by Cell Titer Glo Luminescent Cell Viability Assay	[PMID: 35644299]
HCT-116	IC₅₀	0.007 μM Compound: 36	Antiproliferative activity against human HCT116 cells after 96 hrs by MTT assay Antiproliferative activity against human HCT116 cells after 96 hrs by MTT assay	[PMID: 31117517]
HCT-116	IC₅₀	7 nM Compound: 8	Growth inhibition of human HCT-116 cells Growth inhibition of human HCT-116 cells	[PMID: 35644299]
HCT-8	IC₅₀	0.059 μM Compound: 36	Antiproliferative activity against human HCT8 cells after 96 hrs by MTT assay Antiproliferative activity against human HCT8 cells after 96 hrs by MTT assay	[PMID: 31117517]
HepG2	IC₅₀	0.076 μM Compound: 36	Antiproliferative activity against human HepG2 cells after 96 hrs by MTT assay Antiproliferative activity against human HepG2 cells after 96 hrs by MTT assay	[PMID: 31117517]
HGC-27	IC₅₀	0.014 μM Compound: 36	Antiproliferative activity against human HGC27 cells after 96 hrs by MTT assay Antiproliferative activity against human HGC27 cells after 96 hrs by MTT assay	[PMID: 31117517]
HGC-27	IC₅₀	14 nM Compound: 8	Growth inhibition of human HGC-27 cells Growth inhibition of human HGC-27 cells	[PMID: 35644299]
Huh-7	IC₅₀	0.24 μM Compound: 36	Antiproliferative activity against human HuH7 cells after 96 hrs by MTT assay Antiproliferative activity against human HuH7 cells after 96 hrs by MTT assay	[PMID: 31117517]
K562	IC₅₀	1.2 μM Compound: 36	Antiproliferative activity against human K562 cells after 96 hrs by MTT assay Antiproliferative activity against human K562 cells after 96 hrs by MTT assay	[PMID: 31117517]
KARPAS-422	IC₅₀	0.021 μM Compound: 8	Antiproliferative activity against human KARPAS-422 cells measured after 4 days by Cell Titer Glo Luminescent Cell Viability Assay Antiproliferative activity against human KARPAS-422 cells measured after 4 days by Cell Titer Glo Luminescent Cell Viability Assay	[PMID: 35644299]
MCF7	IC₅₀	1.1 μM Compound: 36	Antiproliferative activity against human MCF7 cells after 96 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 96 hrs by MTT assay	[PMID: 31117517]
MDA-MB-453	IC₅₀	0.004 μM Compound: 36	Antiproliferative activity against human MDA-MB-453 cells after 96 hrs by MTT assay Antiproliferative activity against human MDA-MB-453 cells after 96 hrs by MTT assay	[PMID: 31117517]
MDA-MB-453	IC₅₀	4 nM Compound: 8	Growth inhibition of human MDA-MB-453 cells Growth inhibition of human MDA-MB-453 cells	[PMID: 35644299]
NCI-H1299	IC₅₀	0.18 μM Compound: 36	Antiproliferative activity against human NCI-H1299 cells after 96 hrs by MTT assay Antiproliferative activity against human NCI-H1299 cells after 96 hrs by MTT assay	[PMID: 31117517]
NCI-H460	IC₅₀	2.7 μM Compound: 36	Antiproliferative activity against human NCI-H460 cells after 96 hrs by MTT assay Antiproliferative activity against human NCI-H460 cells after 96 hrs by MTT assay	[PMID: 31117517]
OCI-LY19	IC₅₀	0.0192 μM Compound: 8	Antiproliferative activity against human OCILY19 cells measured after 4 days by Cell Titer Glo Luminescent Cell Viability Assay Antiproliferative activity against human OCILY19 cells measured after 4 days by Cell Titer Glo Luminescent Cell Viability Assay	[PMID: 35644299]
OCI-Ly3	IC₅₀	0.0036 μM Compound: 8	Antiproliferative activity against human OCILY3 cells measured after 4 days by Cell Titer Glo Luminescent Cell Viability Assay Antiproliferative activity against human OCILY3 cells measured after 4 days by Cell Titer Glo Luminescent Cell Viability Assay	[PMID: 35644299]
OCI-Ly7	IC₅₀	0.0056 μM Compound: 8	Antiproliferative activity against human OCILY7 cells measured after 4 days by Cell Titer Glo Luminescent Cell Viability Assay Antiproliferative activity against human OCILY7 cells measured after 4 days by Cell Titer Glo Luminescent Cell Viability Assay	[PMID: 35644299]
Pfeiffer	IC₅₀	0.0053 μM Compound: 8	Antiproliferative activity against human Pfeiffer cells measured after 4 days by Cell Titer Glo Luminescent Cell Viability Assay Antiproliferative activity against human Pfeiffer cells measured after 4 days by Cell Titer Glo Luminescent Cell Viability Assay	[PMID: 35644299]
Sf9	IC₅₀	1.3 nM Compound: 36	Inhibition of recombinant C-terminal His/FLAG-tagged HDAC1 (unknown origin) expressed in baculovirus infected Sf9 insect cells using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr Inhibition of recombinant C-terminal His/FLAG-tagged HDAC1 (unknown origin) expressed in baculovirus infected Sf9 insect cells using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr	[PMID: 31117517]
Sf9	IC₅₀	12 nM Compound: 36	Inhibition of recombinant human full length C-terminal His-tagged HDAC8 expressed in baculovirus infected Sf9 insect cells using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr Inhibition of recombinant human full length C-terminal His-tagged HDAC8 expressed in baculovirus infected Sf9 insect cells using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr	[PMID: 31117517]
Sf9	IC₅₀	3.4 nM Compound: 36	Inhibition of recombinant human full length HDAC2 expressed in baculovirus infected Sf9 insect cells using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr Inhibition of recombinant human full length HDAC2 expressed in baculovirus infected Sf9 insect cells using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr	[PMID: 31117517]
Sf9	IC₅₀	972 nM Compound: 36	Inhibition of recombinant human full length HDAC4 expressed in baculovirus infected Sf9 insect cells using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr Inhibition of recombinant human full length HDAC4 expressed in baculovirus infected Sf9 insect cells using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr	[PMID: 31117517]
Sf9	IC₅₀	>1000 nM Compound: 36	Inhibition of recombinant human full length HDAC11 expressed in baculovirus infected Sf9 insect cells using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr Inhibition of recombinant human full length HDAC11 expressed in baculovirus infected Sf9 insect cells using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr	[PMID: 31117517]
SUD4	IC₅₀	0.0076 μM Compound: 8	Antiproliferative activity against human SU-DHL-4 cells measured after 4 days by Cell Titer Glo Luminescent Cell Viability Assay Antiproliferative activity against human SU-DHL-4 cells measured after 4 days by Cell Titer Glo Luminescent Cell Viability Assay	[PMID: 35644299]
SU-DHL10	IC₅₀	0.0097 μM Compound: 8	Antiproliferative activity against human SU-DHL-10 cells measured after 4 days by Cell Titer Glo Luminescent Cell Viability Assay Antiproliferative activity against human SU-DHL-10 cells measured after 4 days by Cell Titer Glo Luminescent Cell Viability Assay	[PMID: 35644299]
SU-DHL-5	IC₅₀	0.0036 μM Compound: 8	Antiproliferative activity against human SU-DHL-5 cells measured after 4 days by Cell Titer Glo Luminescent Cell Viability Assay Antiproliferative activity against human SU-DHL-5 cells measured after 4 days by Cell Titer Glo Luminescent Cell Viability Assay	[PMID: 35644299]
SU-DHL-6	IC₅₀	0.0065 μM Compound: 8	Antiproliferative activity against human SU-DHL-6 cells measured after 4 days by Cell Titer Glo Luminescent Cell Viability Assay Antiproliferative activity against human SU-DHL-6 cells measured after 4 days by Cell Titer Glo Luminescent Cell Viability Assay	[PMID: 35644299]
SU-DHL-8	IC₅₀	0.0064 μM Compound: 8	Antiproliferative activity against human SU-DHL-8 cells measured after 4 days by Cell Titer Glo Luminescent Cell Viability Assay Antiproliferative activity against human SU-DHL-8 cells measured after 4 days by Cell Titer Glo Luminescent Cell Viability Assay	[PMID: 35644299]
SW1990	IC₅₀	0.23 μM Compound: 36	Antiproliferative activity against human SW1990 cells after 96 hrs by MTT assay Antiproliferative activity against human SW1990 cells after 96 hrs by MTT assay	[PMID: 31117517]
THP-1	IC₅₀	0.91 μM Compound: 36	Antiproliferative activity against human THP1 cells after 96 hrs by MTT assay Antiproliferative activity against human THP1 cells after 96 hrs by MTT assay	[PMID: 31117517]
Toledo	IC₅₀	0.0056 μM Compound: 8	Antiproliferative activity against human Toledo cells measured after 4 days by Cell Titer Glo Luminescent Cell Viability Assay Antiproliferative activity against human Toledo cells measured after 4 days by Cell Titer Glo Luminescent Cell Viability Assay	[PMID: 35644299]
U2932	IC₅₀	0.0177 μM Compound: 8	Antiproliferative activity against human U2932 cells measured after 4 days by Cell Titer Glo Luminescent Cell Viability Assay Antiproliferative activity against human U2932 cells measured after 4 days by Cell Titer Glo Luminescent Cell Viability Assay	[PMID: 35644299]
U-87MG ATCC	IC₅₀	0.34 μM Compound: 36	Antiproliferative activity against human U87 cells after 96 hrs by MTT assay Antiproliferative activity against human U87 cells after 96 hrs by MTT assay	[PMID: 31117517]
WSUDLCL2	IC₅₀	0.016 μM Compound: 8	Antiproliferative activity against human WSUDLCL2 cells measured after 4 days by Cell Titer Glo Luminescent Cell Viability Assay Antiproliferative activity against human WSUDLCL2 cells measured after 4 days by Cell Titer Glo Luminescent Cell Viability Assay	[PMID: 35644299]
WSU-NHL	IC₅₀	0.0052 μM Compound: 8	Antiproliferative activity against human WSU-NHL cells measured after 4 days by Cell Titer Glo Luminescent Cell Viability Assay Antiproliferative activity against human WSU-NHL cells measured after 4 days by Cell Titer Glo Luminescent Cell Viability Assay	[PMID: 35644299]

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.

Chemical Information

CAS No. 2361418-65-5
Molecular Weight 461.47
Formula C₂₃H₂₃N₇O₄
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
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 (271 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]. Kehui Zhang, et al. Bioevaluation of a dual PI3K/HDAC inhibitor for the treatment of diffuse large B-cell lymphoma. Bioorg Med Chem Lett. 2022 Sep 1;71:128825. [Content Brief]

Calculators

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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.

Keywords

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent:

Product Name:
CAS No.:
Species:
Purity:
Quantity:

PI3K/HDAC-IN-2

All PI3K Isoforms

All HDAC Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

PI3K/HDAC-IN-2 Related Classifications

HY-146159 Related Classifications