2. Epigenetics Cell Cycle/DNA Damage Apoptosis
  3. HDAC CDK Apoptosis
  4. CDK/HDAC-IN-2

CDK/HDAC-IN-2 is a potent HDAC/CDK dual inhibitor with IC50 of 6.4, 0.25, 45, >1000, 8.63, 0.30, >1000 nM for HDAC1, HDAC2, HDAC3, HDAC6,8, CDK1, CDK2, CDK4,6,7, respectively. CDK/HDAC-IN-2 shows excellent antiproliferative activities. CDK/HDAC-IN-2 induces apoptosis and cell cycle arrest at G2/M phase. CDK/HDAC-IN-2 shows potent antitumor efficacy.

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CDK/HDAC-IN-2 Chemical Structure

CDK/HDAC-IN-2 Chemical Structure

CAS No. : 2580938-58-3

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CDK/HDAC-IN-2 Related Antibodies

Top Publications Citing Use of Products

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

View All CDK Isoform Specific Products:

View All Isoforms
CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

  • Biological Activity

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Description

CDK/HDAC-IN-2 is a potent HDAC/CDK dual inhibitor with IC50 of 6.4, 0.25, 45, >1000, 8.63, 0.30, >1000 nM for HDAC1, HDAC2, HDAC3, HDAC6,8, CDK1, CDK2, CDK4,6,7, respectively. CDK/HDAC-IN-2 shows excellent antiproliferative activities. CDK/HDAC-IN-2 induces apoptosis and cell cycle arrest at G2/M phase. CDK/HDAC-IN-2 shows potent antitumor efficacy[1].

IC50 & Target[1]

HDAC1

6.4 nM (IC50)

HDAC2

0.25 nM (IC50)

HDAC3

45 nM (IC50)

HDAC6

>1000 nM (IC50)

HDAC8

>1000 nM (IC50)

CDK1

8.63 nM (IC50)

CDK2

0.30 μM (IC50)

CDK4

>1000 nM (IC50)

CDK6

>1000 nM (IC50)

CDK7

>1000 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
A-375 IC50
1.2 μM
Compound: 7c
Antiproliferative activity against human A375 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human A375 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
[PMID: 31991336]
HCT-116 IC50
0.71 μM
Compound: 7c
Antiproliferative activity against human HCT116 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human HCT116 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
[PMID: 31991336]
HeLa IC50
1.83 μM
Compound: 7c
Antiproliferative activity against human Hela cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human Hela cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
[PMID: 31991336]
NCI-H460 IC50
4.19 μM
Compound: 7c
Antiproliferative activity against human H460 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human H460 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
[PMID: 31991336]
SMMC-7721 IC50
7.76 μM
Compound: 7c
Antiproliferative activity against human SMMC7721 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human SMMC7721 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
[PMID: 31991336]
In Vitro

CDK/HDAC-IN-2 (compound 7c) shows antiproliferative activity with IC50s of 0.71, 1.20, 1.83, 4.19, 7.76, 4.47 µM for HCT116, A375, Hela, H460, SMMC7721, NIH 3T3 cells, respectively[1].
CDK/HDAC-IN-2 (24 h) shows anti-migration ability in A375 and H460 cells[1].
CDK/HDAC-IN-2 (0.5, 1, 2 µM) induces apoptosis and cell cycle arrest at G2/M phase[1].
CDK/HDAC-IN-2 accelerates intracellular ROS accumulation, leading to cancer cell death[1].

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

CDK/HDAC-IN-2 Related Antibodies

Cell Cycle Analysis[1]

Cell Line: A375, HCT116, H460, Hela cells
Concentration: 0.5, 1, 2 µM
Incubation Time: 24 h
Result: Induced cell cycle arrest at G2/M phase.

Apoptosis Analysis[1]

Cell Line: A375, HCT116, H460, Hela cells
Concentration: 0.5, 1, 2 µM
Incubation Time: 48 h
Result: Induced cell apoptosis with the apoptosis rates of A375, HCT116 cells of 97.22%, 60.6%, respectively.
In Vivo

CDK/HDAC-IN-2 (12.5, 25 mg/kg; IP; once daily for 21 days) shows antitumor efficacy in the HCT116 xenograft model (TGI= 51.0%)[1].
Pharmacokinetic Parameters of CDK/HDAC-IN-2 in ICR male mice[1].

compound 7c
Dose (mg/kg) 20
administration i.p.
t1/2 (h) 2.61
Tmax (h) 2.00
Cmax (h) 7570
AUC0-∞ (ng h/mL) 30700
MRT0-∞ (ng h/mL) 3.31
F (%) 63.6
ICR male mice; 20 mg/kg, i.p.[1].

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

Animal Model: ICR male mice[1]
Dosage: 20 mg/kg
Administration: IP
Result: Showed good Pharmacokinetic parameters with bioavailability of F= 63.6%.
Animal Model: 5-6 weeks, BALB/c female mice (HCT116 xenograft nude mice models)[1]
Dosage: 12.5, 25 mg/kg
Administration: IP, once daily for 21 days
Result: Effectively inhibited the growth of HCT116 xenograft tumors tumor growth inhibitions (TGI) at 12.5 and 25 mg/kg of 37.0% and 51.0%, respectively.
Molecular Weight

523.37

Formula

C25H20Cl2N6O3
CAS No.
SMILES

NC1=CC=CC=C1NC(C2=CC=C(C=C2)CNC(C3=NNC=C3NC(C4=C(C=CC=C4Cl)Cl)=O)=O)=O
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
References
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CDK/HDAC-IN-2 Related Classifications

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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:

CDK/HDAC-IN-22580938-58-3HDACCDKApoptosisHistone deacetylasesCyclin dependent kinaseantiproliferativeantitumorG2/M phaseapoptosisHCT116 xenograft modelA375HCT116H460Hela cellsInhibitorinhibitorinhibit

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