|
Screening of Various CDK and NFkB/IKK Inhibitors and Related Molecules for HTLV-1 Cell Killing |
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| 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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Agbottah et al. AIDS Research and Therapy 2008 5:12 doi:10.1186/1742-6405-5-12 |
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