| NCI-H82 |
Apoptosis Assay |
0.3/1/3 μM |
48 h |
increases the level of cleaved-Caspase 3 |
24158701 |
| GLC4 |
Apoptosis Assay |
0.3/1/3 μM |
48 h |
increases the level of cleaved-Caspase 3 |
24158701 |
| NCI-N592 |
Apoptosis Assay |
0.3/1/3 μM |
48 h |
increases the level of cleaved-Caspase 3 |
24158701 |
| NCI-H82 |
Function Assay |
0.3/1/3 μM |
24 h |
induces G2/M cell cycle arrest |
24158701 |
| GLC4 |
Function Assay |
0.3/1/3 μM |
24 h |
induces G2/M cell cycle arrest |
24158701 |
| NCI-N592 |
Function Assay |
0.3/1/3 μM |
24 h |
induces G2/M cell cycle arrest |
24158701 |
| CWR22Rv1 |
Function Assay |
800 nM |
72 h |
suppresses IL-6-induced migratory |
24577942 |
| DU145 |
Function Assay |
800 nM |
72 h |
suppresses IL-6-induced migratory |
24577942 |
| DU145 |
Function Assay |
0-200 nM |
1 h |
suppresses IL-6-activated Stat3 and ERK1/2 signaling |
24577942 |
| MO4 |
Function Assay |
0.5/1/5 μM |
6 h |
inhibits P-STAT3 expression |
25149535 |
| OVCAR-8 |
Apoptosis Assay |
0.5/1/5 μM |
48 h |
induces significant apoptosis at high concerntration |
25646015 |
| OVCAR-5 |
Apoptosis Assay |
0.5/1/5 μM |
48 h |
induces significant apoptosis at high concerntration |
25646015 |
| OVCAR-8 |
Cell Viability Assay |
0.05-10 μM |
72 h |
reduces cell viability at the concerntration of 5 μM |
25646015 |
| OVCAR-5 |
Cell Viability Assay |
0.05-10 μM |
72 h |
reduces cell viability at the concerntration of 5 μM |
25646015 |
| A1847 |
Cell Viability Assay |
0.05-10 μM |
72 h |
reduces cell viability at the concerntration of 5 μM |
25646015 |
| MOVCAR-5009 |
Function Assay |
0.05-10 μM |
24 h |
reduces phosphorylated STAT3 levels |
25646015 |
| MOVCAR-5447 |
Function Assay |
0.05-10 μM |
24 h |
reduces phosphorylated STAT3 levels |
25646015 |
| OVCAR-8 |
Function Assay |
0.05-10 μM |
24 h |
reduces phosphorylated STAT3 levels |
25646015 |
| OVCAR-5 |
Function Assay |
0.05-10 μM |
24 h |
reduces phosphorylated STAT3 levels |
25646015 |
| A1847 |
Function Assay |
0.05-10 μM |
24 h |
reduces phosphorylated STAT3 levels |
25646015 |
| UM-22A |
Function Assay |
0.0005-1.6 μM |
24 h |
abrogates IL-6–induced up-regulation of pSTAT3Tyr705 in a dose-dependent manner |
25810010 |
| HH5 |
Function Assay |
0.0005-3.8 μM |
24 h |
abrogates IL-6–induced up-regulation of pSTAT3Tyr705 in a dose-dependent manner |
25810010 |
| Cal33 |
Function Assay |
0.0005-3.8 μM |
24 h |
abrogates IL-6–induced up-regulation of pSTAT3Tyr705 in a dose-dependent manner |
25810010 |
| UMSCC-1 |
Function Assay |
0.0005-1.6 μM |
24 h |
abrogates IL-6–induced up-regulation of pSTAT3Tyr705 in a dose-dependent manner |
25810010 |
| LoVo |
Function Assay |
5 μM |
48 h |
blocks JAK2/STAT3 signaling |
25954974 |
| SW620 |
Function Assay |
5 μM |
48 h |
blocks JAK2/STAT3 signaling |
25954974 |
| KCNR |
Apoptosis Assay |
0.5/1.0/2.5 μM |
24 h |
induces an increase in caspase 3/7 activity |
23531921 |
| SY5Y |
Apoptosis Assay |
0.5/1.0/2.5 μM |
24 h |
induces an increase in caspase 3/7 activity |
23531921 |
| Rh18 |
Apoptosis Assay |
0.5/1.0/2.5 μM |
24 h |
induces an increase in caspase 3/7 activity |
23531921 |
| TC32 |
Apoptosis Assay |
0.5/1.0/2.5 μM |
24 h |
induces an increase in caspase 3/7 activity |
23531921 |
| KCNR |
Function Assay |
0.5/1.0/2.5/5 μM |
24 h |
inhibits both endogenous constitutive and IL-6-induced STAT3 activation |
23531921 |
| SY5Y |
Function Assay |
0.5/1.0/2.5/5 μM |
24 h |
inhibits both endogenous constitutive and IL-6-induced STAT3 activation |
23531921 |
| Rh18 |
Function Assay |
0.5/1.0/2.5/5 μM |
24 h |
inhibits both endogenous constitutive and IL-6-induced STAT3 activation |
23531921 |
| TC32 |
Function Assay |
0.5/1.0/2.5/5 μM |
24 h |
inhibits both endogenous constitutive and IL-6-induced STAT3 activation |
23531921 |
| TPC-1 |
Growth Inhibition Assay |
1 µM |
0-4 d |
inhibits cell growth after 2 d treatment |
23056499 |
| MZ-CRC1 |
Growth Inhibition Assay |
1 µM |
0-5 d |
inhibits cell growth after 1 d treatment |
23056499 |
| TT |
Growth Inhibition Assay |
1 µM |
0-4 d |
inhibits cell growth after 1 d treatment |
23056499 |
| TPC-1 |
Function Assay |
1 µM |
72 h |
induces G1 blockage |
23056499 |
| MZ-CRC1 |
Function Assay |
1 µM |
72 h |
induces G1 blockage |
23056499 |
| TT |
Function Assay |
1 µM |
72 h |
induces G1 blockage |
23056499 |
| MZ-CRC1 |
Apoptosis Assay |
1 µM |
48 h |
induces apoptosis |
23056499 |
| TT |
Apoptosis Assay |
1 µM |
48 h |
induces apoptosis |
23056499 |
| HD-LM2 |
Function Assay |
0.1/0.5/1/5 μM |
72 h |
inhibits STAT3, STAT5 and STAT6 phosphorylation |
22829094 |
| L-428 |
Function Assay |
0.1/0.5/1/5 μM |
72 h |
inhibits STAT3, STAT5 and STAT6 phosphorylation |
22829094 |
| KM-H2 |
Function Assay |
0.1/0.5/1/5 μM |
72 h |
inhibits STAT3, STAT5 and STAT6 phosphorylation |
22829094 |
| L-540 |
Function Assay |
0.1/0.5/1/5 μM |
72 h |
inhibits STAT3, STAT5 and STAT6 phosphorylation |
22829094 |
| HD-LM2 |
Apoptosis Assay |
1/5 μM |
72 h |
induces apoptosis |
22829094 |
| L-428 |
Apoptosis Assay |
1/5 μM |
72 h |
induces apoptosis |
22829094 |
| KM-H2 |
Apoptosis Assay |
1/5 μM |
72 h |
induces apoptosis |
22829094 |
| L-540 |
Apoptosis Assay |
1/5 μM |
72 h |
induces apoptosis |
22829094 |
| U251-MG |
Function Assay |
1 µM |
0-16 h |
inhibits constitutive STAT-3 and JAK2 activation |
22027691 |
| U87-MG |
Function Assay |
1 µM |
0-16 h |
inhibits constitutive STAT-3 and JAK2 activation |
22027691 |
| 4C8 |
Function Assay |
1 µM |
0-16 h |
inhibits constitutive STAT-3 and JAK2 activation |
22027691 |
| U251-MG |
Growth Inhibition Assay |
1/10 µM |
24/48/72 h |
inhibits cell proliferation at a concentration of 10 µM |
22027691 |
| U87-MG |
Growth Inhibition Assay |
1/10 µM |
24/48/72 h |
inhibits cell proliferation at a concentration of 10 µM |
22027691 |
| 4C8 |
Growth Inhibition Assay |
1/10 µM |
24/48/72 h |
inhibits cell proliferation at a concentration of 10 µM |
22027691 |
| U266 |
Apoptosis Assay |
0.5-2 μM |
48/72 h |
induces apoptosis dose dependently |
21164517 |
| Kms.11 |
Apoptosis Assay |
0.5-2 μM |
48/72 h |
induces apoptosis dose dependently |
21164517 |
| 8226 |
Apoptosis Assay |
0.5-2 μM |
48/72 h |
induces apoptosis dose dependently |
21164517 |
| SW620 |
Cell cycle assay |
3.3 uM |
24 hrs |
Cell cycle arrest in human SW620 cells assessed as accumulation at G2/M phase at 3.3 uM after 24 hrs by flow cytometry |
21138246 |
| HEL |
Function assay |
0.3 uM |
5 mins |
Inhibition of Stat5 phosphorylation in human HEL cells at 0.3 uM after 5 mins by Western blotting |
21138246 |
| HEL |
Function assay |
0.3 uM |
30 to 60 mins |
Inhibition of Stat5 phosphorylation in human HEL cells at 0.3 uM after 30 to 60 mins by Western blotting |
21138246 |
| BA/F3 |
Antitumor assay |
30 mg/kg |
12 hrs |
Antitumor activity against mouse BA/F3 cells expressing Tel-JAK2 xenografted in NCr mouse assessed as reduction of phosphorylated Stat5 level in spleen at 30 mg/kg, po after 12 hrs by Western blotting |
21138246 |
| HEL |
Function assay |
0.3 uM |
5 mins |
Inhibition of Stat3 phosphorylation in human HEL cells at 0.3 uM after 5 mins by Western blotting |
21138246 |
| HEL |
Function assay |
0.3 uM |
30 to 60 mins |
Inhibition of Stat3 phosphorylation in human HEL cells at 0.3 uM after 30 to 60 mins by Western blotting |
21138246 |
| Hs578T |
Function assay |
1 uM |
24 hrs |
Inhibition of STAT3C-mediated transcription in human Hs578T cells at 1 uM after 24 hrs by luciferase reporter gene assay |
24978112 |
| NCI-H1975 |
Function assay |
0.003 to 3 uM |
2 hrs |
Inhibition of JAK1 in human NCI-H1975 cells assessed as reduction in STAT3 phosphorylation at 0.003 to 3 uM after 2 hrs by Western blot analysis |
26614408 |
| PALJDL |
Cell Viability Assay |
|
72 h |
IC50=2.4 μM |
25504635 |
| AKRSL |
Cell Viability Assay |
|
72 h |
IC50>10 μM |
25504635 |
| PCI-15B |
Growth Inhibition Assay |
|
72 h |
EC50=0.99 ± 1.74 μM |
25810010 |
| PCI-52 |
Growth Inhibition Assay |
|
72 h |
EC50=1.00 ± 0.09 μM |
25810010 |
| OSC19 |
Growth Inhibition Assay |
|
72 h |
EC50=1.26 ± 0.20 μM |
25810010 |
| UM-22A |
Growth Inhibition Assay |
|
72 h |
EC50=1.32 ± 0.39 μM |
25810010 |
| UM SCC-1 |
Growth Inhibition Assay |
|
72 h |
EC50=1.67 ± 0.42 μM |
25810010 |
| 686LN |
Growth Inhibition Assay |
|
72 h |
EC50=2.05 ± 1.33 μM |
25810010 |
| UM-22B |
Growth Inhibition Assay |
|
72 h |
EC50=2.66 ± 0.24 μM |
25810010 |
| Cal33 |
Growth Inhibition Assay |
|
72 h |
EC50=3.37 ± 0.75 μM |
25810010 |
| HN5 |
Growth Inhibition Assay |
|
72 h |
EC50=3.81 ± 1.99 μM |
25810010 |
| HD-LM2 |
Growth Inhibition Assay |
|
72 h |
IC50=7.844 μM |
22829094 |
| L-428 |
Growth Inhibition Assay |
|
72 h |
IC50=7.947 μM |
22829094 |
| KM-H2 |
Growth Inhibition Assay |
|
72 h |
IC50=1.308 μM |
22829094 |
| L-540 |
Growth Inhibition Assay |
|
72 h |
IC50=8.216 μM |
22829094 |
| SET2 |
Growth inhibition assay |
|
48 hrs |
Growth inhibition of human SET2 cells expressing Jak2 V617F mutant after 48 hrs by MTS assay, GI50 = 0.016 μM. |
21138246 |
| SET2 |
Function assay |
|
1 hr |
Inhibition of Stat3 phosphorylation in human SET2 cells after 1 hr by Western blotting, IC50 = 0.023 μM. |
21138246 |
| SET2 |
Function assay |
|
1 hr |
Inhibition of Stat5 phosphorylation in human SET2 cells after 1 hr by Western blotting, IC50 = 0.025 μM. |
21138246 |
| HEL |
Function assay |
|
1 hr |
Inhibition of Stat5 phosphorylation in human HEL cells after 1 hr by Western blotting, IC50 = 0.041 μM. |
21138246 |
| UKE1 |
Growth inhibition assay |
|
48 hrs |
Growth inhibition of human UKE1 cells expressing Jak2 V617F mutant after 48 hrs by MTS assay, GI50 = 0.054 μM. |
21138246 |
| BA/F3 |
Growth inhibition assay |
|
48 hrs |
Growth inhibition of mouse BA/F3 cells expressing Tel-JAK2 kinase after 48 hrs by MTS assay, GI50 = 0.06 μM. |
21138246 |
| HEL |
Function assay |
|
1 hr |
Inhibition of Stat3 phosphorylation in human HEL cells after 1 hr by Western blotting, IC50 = 0.08 μM. |
21138246 |
| HEL |
Growth inhibition assay |
|
48 hrs |
Growth inhibition of human HEL cells expressing Jak2 V617F mutant after 48 hrs by MTS assay, GI50 = 0.39 μM. |
21138246 |
| BA/F3 |
Growth inhibition assay |
|
48 hrs |
Growth inhibition of mouse BA/F3 cells expressing Tel-JAK1 kinase after 48 hrs by MTS assay, GI50 = 0.7 μM. |
21138246 |
| BA/F3 |
Growth inhibition assay |
|
48 hrs |
Growth inhibition of mouse BA/F3 cells expressing Tel-Tyk2 kinase after 48 hrs by MTS assay, GI50 = 2 μM. |
21138246 |
| BA/F3 |
Growth inhibition assay |
|
48 hrs |
Growth inhibition of mouse BA/F3 cells expressing Tel-JAK3 kinase after 48 hrs by MTS assay, GI50 = 2.1 μM. |
21138246 |
| UKE1 |
Function assay |
|
1 hr |
Inhibition of Stat5 phosphorylation in human UKE1 cells after 1 hr by Western blotting |
21138246 |
| HEL 92.1.7 |
Function assay |
|
2 hrs |
Inhibition of JAK2 in human HEL 92.1.7 cells assessed as reduction in STAT5 phosphorylation after 2 hrs by Western blot analysis |
26614408 |
| IMR32 |
Growth Inhibition Assay |
|
|
IC50=0.66 μM |
23531921 |
| NGP |
Growth Inhibition Assay |
|
|
IC50=0.56 μM |
23531921 |
| AS |
Growth Inhibition Assay |
|
|
IC50=1.53 μM |
23531921 |
| BE2 |
Growth Inhibition Assay |
|
|
IC50=0.71 μM |
23531921 |
| SY5Y |
Growth Inhibition Assay |
|
|
IC50=0.36 μM |
23531921 |
| KCNR |
Growth Inhibition Assay |
|
|
IC50=0.46 μM |
23531921 |
| HEK293 |
Growth Inhibition Assay |
|
|
IC50=8.67 μM |
23531921 |
| ARPE19 |
Growth Inhibition Assay |
|
|
IC50=24.38 μM |
23531921 |
| RC165N |
Apoptosis Assay |
|
|
IC50=2.083 μM |
23942095 |
| DU145 |
Apoptosis Assay |
|
|
IC50=3.517 μM |
23942095 |
| PC-3 |
Apoptosis Assay |
|
|
IC50=1.755 μM |
23942095 |
| CWR22Pc |
Apoptosis Assay |
|
|
IC50=0.438 μM |
23942095 |
| CWR22Rv1 |
Apoptosis Assay |
|
|
IC50=0.482 μM |
23942095 |
| DMS114 |
Growth Inhibition Assay |
|
|
IC50=0.73 μM |
24158701 |
| H1173 |
Growth Inhibition Assay |
|
|
IC50=2.39 μM |
24158701 |
| H526 |
Growth Inhibition Assay |
|
|
IC50=3.08 μM |
24158701 |
| GLC4 |
Growth Inhibition Assay |
|
|
IC50=1.79 μM |
24158701 |
| H82 |
Growth Inhibition Assay |
|
|
IC50=1.37 μM |
24158701 |
| N592 |
Growth Inhibition Assay |
|
|
IC50=0.84 μM |
24158701 |
| LAN5 |
Growth Inhibition Assay |
|
|
IC50=1.04 μM |
23531921 |
| RH18 |
Growth Inhibition Assay |
|
|
IC50=1.42 μM |
23531921 |
| RH30 |
Growth Inhibition Assay |
|
|
IC50=1.25 μM |
23531921 |
| RH17 |
Growth Inhibition Assay |
|
|
IC50=2.51 μM |
23531921 |
| RH28 |
Growth Inhibition Assay |
|
|
IC50=4.28 μM |
23531921 |
| RH36 |
Growth Inhibition Assay |
|
|
IC50=5.37 μM |
23531921 |
| RH41 |
Growth Inhibition Assay |
|
|
IC50=0.48 μM |
23531921 |
| RD |
Growth Inhibition Assay |
|
|
IC50=4.32 μM |
23531921 |
| TC32 |
Growth Inhibition Assay |
|
|
IC50=3.85 μM |
23531921 |
| TC71 |
Growth Inhibition Assay |
|
|
IC50=4.33 μM |
23531921 |
| Ba/F3 |
Function assay |
|
|
Inhibition of Stat5 phosphorylation in mouse Ba/F3 cells expressing TEL-Jak2, IC50 = 0.046 μM. |
21138246 |
| DAOY |
qHTS assay |
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells |
29435139 |
| SJ-GBM2 |
qHTS assay |
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells |
29435139 |
| A673 |
qHTS assay |
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells |
29435139 |
| SK-N-MC |
qHTS assay |
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells |
29435139 |
| BT-37 |
qHTS assay |
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells |
29435139 |
| NB-EBc1 |
qHTS assay |
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells |
29435139 |
| Saos-2 |
qHTS assay |
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells |
29435139 |
| SK-N-SH |
qHTS assay |
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells |
29435139 |
| NB1643 |
qHTS assay |
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells |
29435139 |
| BT-12 |
qHTS assay |
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells |
29435139 |
| OHS-50 |
qHTS assay |
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells |
29435139 |
| RD |
qHTS assay |
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells |
29435139 |
| MG 63 (6-TG R) |
qHTS assay |
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells |
29435139 |
| Rh41 |
qHTS assay |
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells |
29435139 |