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Table 1 Screening of Various CDK and NFkB/IKK Inhibitors and Related Molecules for HTLV-1 Cell Killing

From: Two specific drugs, BMS-345541 and purvalanol A induce apoptosis of HTLV-1 infected cells through inhibition of the NF-kappaB and cell cycle pathways

Selectivity

Name

MT-2

MT-4

C8166

C10/MJ

CEM

Jurkat

Reported activities of molecules (IC50 in nM)

   

Infected

Uninfected

 

High

BMS-345541

(10 uM)

++++*

+++

+++

+

- **

-

IKK-1(4), IKK-2(0.3)

 

Purvalanol A

(10 uM)

++++

++

++

-

-

-

CDK1(4), CDK2(70), CDK5(75)

 

Indirubin-3'-monoxime

(10 uM)

+++

+++

+++

+++

++

++

CDK1(180), CDK2(250), CDK4(3330), CDK5(100)

 

Indirubin-3'-monoxime-5'-Iodo

(10 uM)

+++

+++

+++

+++

++

++

CDK1(25), CDK5(20)

 

9-Cyanopaullone

(10 uM)

++++

+

-

-

-

-

CDK1(24), CDK5(44)

 

Aloisine A

(10 uM)

+++

+

-

-

-

-

CDK1(150), CDK2(120), CDK5(200)

 

Compound 52

(10 uM)

+++

+

-

-

-

-

CDK1(340)

 

Flavopiridol

(0.1 uM)

++

+

-

-

-

-

CDK9(50)

Moderate

r-Roscovitine

(10 uM)

++

-

-

-

-

-

CDK1(650), CDK2(700), CDK5(160), CDK7(500)

 

Bohemine

(10 uM)

++

-

-

-

-

-

CDK1(1000)

 

s-Roscovitine

(10 uM)

+

-

-

-

-

-

CDK1(650), CDK2(700), CDK5(160), CDK7(500)

 

WHI-P180

(10 uM)

+

N/A

N/A

-

N/A

N/A

CDK2(1000)

 

Kenpaullone

(10 uM)

+

-

-

-

-

-

CDK1(400), CDK2(680), CDK5(850)

 

2,6-Diaminopurine

(10 uM)

-

+

-

-

-

-

 
 

Flavone

(10 uM)

+

-

-

-

-

-

CDK1(300), CDK2(100), CDK4(400), CDK7(300)

 

Alsterpaullone

(10 uM)

++++

++

+++

+

++

++

CDK1(35), CDK2(15), CDK5(40)

 

CGP 74514A

(10 uM)

++++

++

+++

+

++

++

CDK1(25)

 

BAY 11-7085

(10 uM)

+

++++

+++

N/A

++++

++++

 
 

BAY 11-7082

(10 uM)

+

++++

+++

N/A

++++

++++

IkBa(10000)

 

CAPE

(10 uM)

+

+++

-

N/A

++++

++++

 
 

Diethylmaleate

(10 uM)

+

+++

-

N/A

++++

++++

 
 

Parthenolide

(10 uM)

+

+++

+++

N/A

++++

++++

 
 

Pyrrolidinedithiocarbamic acid

(10 uM)

-

+++

+++

N/A

++++

++++

 
 

Wedelolactone

(10 uM)

+

++

-

N/A

++

++

 

Poor

6-Benzyloxypurine

(10 uM)

-

-

-

-

-

-

 
 

5-amino alicylic acid

(10 uM)

-

-

-

N/A

-

-

 
 

2,6-Dichloropurine

(10 uM)

-

-

-

-

-

-

 
 

6-Dimethylaminopurine

(10 uM)

-

-

-

-

-

-

CDC

 

Indirubin-3'-monoxime-5'-sulphonic acid

(10 uM)

-

-

-

-

-

-

CDK1(5), CDK5(7)

 

Iso-olomoucine

(10 uM)

-

-

-

-

-

-

CDK1(>500,000), CDK4,5(>1,000,000)

 

N-6-(Δ2-Isopentyl)-adenine

(10 uM)

-

-

-

-

-

-

CDK1,2,5(>50,000)

 

Olomoucine

(10 uM)

-

-

-

-

-

-

CDK1,2(7000), CDK5(3000)

 

Olomoucine, N9-isopropyl

(10 uM)

-

-

-

-

-

-

CDK1(2000)

 

SC-514

(10 uM)

-

-

-

-

-

-

IKK-1(>200), IKK-2(11.2)

 

QNZ

(10 uM)

-

-

-

N/A

++

+

 
 

* positive sign indicates level of cell inhibition

 

Inhibition

Percentage

     
 

** negative sign indicates no cell inhibition

 

-

1–5%

     
   

+

25%

     
   

++

50%

     
   

+++

75%

     
   

++++

90%

     
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AIDS Research and Therapy

ISSN: 1742-6405

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