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

PI3K/HDAC-IN-2 是一种有效的双重 PI3K/HDAC 抑制剂，对 PI3Kα、PI3Kβ、PI3Kγ、PI3Kδ的 IC50 分别为 226 nM、279 nM、467 nM、29 nM，对于 HDAC1、HDAC2、HDC4、HDAC6、HDAC8，IC50 分别为 1.3 nM、3.4 nM、972 nM、17 nM、12 nM。PI3K/HDAC-IN-2 表现出 PI3Kδ 和 I 类和 IIb 类 HDAC 选择性。PI3K/HDAC-IN-2具有显着的抗癌作用。

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PI3K/HDAC-IN-2 Chemical Structure

PI3K/HDAC-IN-2 Chemical Structure

CAS No. : 2361418-65-5

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PI3K/HDAC-IN-2 相关抗体

Top Publications Citing Use of Products

查看 PI3K 亚型特异性产品:

查看所有亚型
PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

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

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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)

细胞效力
(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-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]
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]
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
> 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]
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]
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]
体外研究
(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].

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

PI3K/HDAC-IN-2 相关抗体:
体内研究
(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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

461.47

Formula

C23H23N7O4
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

PI3K/HDAC-IN-2 相关分类

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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:

PI3K/HDAC-IN-22361418-65-5PI3KHDACPhosphoinositide 3-kinaseHistone deacetylasesPI3KαPI3KβPI3KγPI3δKHDAC1HDAC2HDC4HDAC6HDAC8anticancer effectInhibitorinhibitorinhibit

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