PI3K/HDAC-IN-1

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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.

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PI3K/HDAC-IN-1 Chemical Structure

CAS No. : 2361418-52-0

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•Related Small Molecules:

•Related Proteins:

View All PI3K Isoform Specific Products:

View All Isoforms

PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

View All HDAC Isoform Specific Products:

View All Isoforms

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

Biological Activity
Purity & Documentation
References
Customer Review

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)

Cellular Effect

Cell Line	Type	Value	Description	References
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]
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]
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]
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]
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]
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]
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]
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]
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]

Molecular Weight

428.46

Formula

C₂₂H₂₅FN₄O₄

CAS No.

2361418-52-0

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

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]

PI3K/HDAC-IN-1 Related Classifications

Molarity Calculator
Dilution Calculator

The molarity calculator equation

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

Mass		Concentration		Volume		Molecular Weight *
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The dilution calculator equation

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)	×	Volume _(start)	=	Concentration _(final)	×	Volume _(final)
	×		=		×
C1		V1		C2		V2

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:

PI3K/HDAC-IN-12361418-52-0PI3KHDACPhosphoinositide 3-kinaseHistone deacetylasesInhibitorinhibitorinhibit

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