Table 1

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

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%






Agbottah et al. AIDS Research and Therapy 2008 5:12   doi:10.1186/1742-6405-5-12