Cat. No.: HY-128582

PI3K/HDAC-IN-1

PI3K/HDAC-IN-1 is a potent dual inhibitor of PI3K/HDAC, potently inhibits PI3Kδ and HDAC1 with IC₅₀s of 8.1 nM and 1.4 nM, respectively.

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

CAS No.: 2361418-52-0
Formula: C₂₂H₂₅FN₄O₄
Molecular Weight:428.46

Storage:

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

Data Sheet (268 KB)

PI3K/HDAC-IN-1 Chemical Structure

CAS No.: 2361418-52-0

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Use of MCE Products

Fluorescent Dye

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

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

Biological Activity

Description

PI3K/HDAC-IN-1 is a potent dual inhibitor of PI3K/HDAC, potently inhibits PI3Kδ and HDAC1 with IC₅₀s of 8.1 nM and 1.4 nM, respectively^[1].

IC₅₀ & Target

PI3Kα

42 nM (IC₅₀)

PI3Kβ

101 nM (IC₅₀)

PI3Kγ

67 nM (IC₅₀)

PI3Kδ

8.1 nM (IC₅₀)

HDAC1

1.4 nM (IC₅₀)

HDAC2

3.0 nM (IC₅₀)

HDAC6

6.6 nM (IC₅₀)

HDAC8

18 nM (IC₅₀)

All PI3K Isoforms :

All HDAC Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A20	IC₅₀	23 nM Compound: 34	Antiproliferative activity against mouse A20 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against mouse A20 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 37875056]
BaF3	IC₅₀	23 nM Compound: 34	Antiproliferative activity against mouse BaF3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against mouse BaF3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 37875056]
Bel-7402	IC₅₀	5.2 μM Compound: 23	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	0.43 μM Compound: 23	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: 23	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]
DU-145	IC₅₀	0.54 μM Compound: 23	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]
EL4	IC₅₀	23 nM Compound: 34	Antiproliferative activity against mouse EL4 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against mouse EL4 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 37875056]
HCT-116	IC₅₀	0.15 μM Compound: 23	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-8	IC₅₀	0.32 μM Compound: 23	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	1.1 μM Compound: 23	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	0.11 μM Compound: 23	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]
HL-60	IC₅₀	23 nM Compound: 34	Antiproliferative activity against human HL-60 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against human HL-60 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 37875056]
Huh-7	IC₅₀	2.5 μM Compound: 23	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]
Jurkat	IC₅₀	23 nM Compound: 34	Antiproliferative activity against human Jurkat cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against human Jurkat cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 37875056]
K562	IC₅₀	6.8 μM Compound: 23	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]
K562	IC₅₀	23 nM Compound: 34	Antiproliferative activity against human K562 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against human K562 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 37875056]
L1210	IC₅₀	23 nM Compound: 34	Antiproliferative activity against mouse L1210 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against mouse L1210 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 37875056]
MCF7	IC₅₀	2 μM Compound: 23	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	0.3 μM Compound: 23	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]
MV4-11	IC₅₀	0.25 μM Compound: 17	Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 38048697]
NB-4	IC₅₀	23 nM Compound: 34	Antiproliferative activity against human NB4 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against human NB4 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 37875056]
NCI-H1299	IC₅₀	1 μM Compound: 23	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	3 μM Compound: 23	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]
Ramos	IC₅₀	23 nM Compound: 34	Antiproliferative activity against human Ramos cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against human Ramos cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 37875056]
Sf9	IC₅₀	>1000 nM Compound: 23	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	1.4 nM Compound: 23	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	18 nM Compound: 23	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 nM Compound: 23	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	>1000 nM Compound: 23	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]
SW1990	IC₅₀	0.9 μM Compound: 23	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	5.4 μM Compound: 23	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]
U-87MG ATCC	IC₅₀	3.2 μM Compound: 23	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]
U-937	IC₅₀	23 nM Compound: 34	Antiproliferative activity against human U-937 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against human U-937 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 37875056]
YAC-1	IC₅₀	23 nM Compound: 34	Antiproliferative activity against mouse YAC-1 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against mouse YAC-1 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 37875056]

Chemical Information

CAS No. 2361418-52-0
Molecular Weight 428.46
Formula C₂₂H₂₅FN₄O₄
SMILES

CC1=C2C(C(OCCCCCCC(NO)=O)=CC(C3=CC(F)=C(OC)N=C3)=C2)=NC=N1
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 (268 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]. Zhang K, et al. Design, Synthesis, and Biological Evaluation of 4-Methyl Quinazoline Derivatives as Anticancer Agents Simultaneously Targeting Phosphoinositide 3-Kinases and Histone Deacetylases. J Med Chem. 2019 May 29. [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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PI3K/HDAC-IN-1

All PI3K Isoforms

All HDAC Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

PI3K/HDAC-IN-1 Related Classifications

HY-128582 Related Classifications