- 阻害剤
- 研究分野別
- PI3K/Akt/mTOR
- Epigenetics
- Methylation
- Immunology & Inflammation
- Protein Tyrosine Kinase
- Angiogenesis
- Apoptosis
- Autophagy
- ER stress & UPR
- JAK/STAT
- MAPK
- Cytoskeletal Signaling
- Cell Cycle
- TGF-beta/Smad
- 化合物ライブラリー
- 抗体
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Akti-1/2
別名：Akt Inhibitor VIII
Akti-1/2 (Akt Inhibitor VIII) is a highly selective Akt1/Akt2 inhibitor with IC50 of 58 nM/210 nM, respectively, about 36-fold selectivity for Akt1 over Akt3. Akti-1/2 induces apoptosis.
CAS No. 612847-09-3
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製品安全説明書
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純度：
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Akti-1/2関連製品
| 関連ターゲット | Akt1 Akt2 Akt3 | もっと見る |
|---|---|---|
| 関連化合物ライブラリー | Kinase Inhibitor Library PI3K/Akt Inhibitor Library Apoptosis Compound Library Cell Cycle compound library NF-κB Signaling Compound Library | もっと見る |
シグナル伝達経路
Akt阻害剤の選択性比較
Cell Data
| Cell Lines | Assay Type | Concentration | Incubation Time | 活性情報 | PMID |
|---|---|---|---|---|---|
| MDA-MB-468 cells | Cytotoxicity assay | 10 μM | Cytotoxicity against human MDA-MB-468 cells in presence of 10 uM chloroquine by SRB assay, GI50=2.66 μM | 18691894 | |
| MDA-MB-231 cells | Cytotoxicity assay | 10 μM | Cytotoxicity against human MDA-MB-231 cells in presence of 10 uM chloroquine by SRB assay, GI50=4.55 μM | 18691894 | |
| MCF7 cells | Cytotoxicity assay | 10 μM | Cytotoxicity against human MCF7 cells in presence of 10 uM chloroquine by SRB assay, GI50=0.41 μM | 18691894 | |
| 184B5 cells | Cytotoxicity assay | 20 μM | Cytotoxicity against human 184B5 cells at 20 uM chloroquine by SRB assay, GI50=25.76 μM | 18691894 | |
| NCI-H526 cells | Growth inhibition assay | Inhibition of Akt-mediated antiapoptotic activity in human NCI-H526 cells assessed as disruption of protein-Apaf-1 complex at 50 uM after 24 hrs by Western blot analysis | 17603540 | ||
| NCI-H1563 cell | Growth inhibition assay | Inhibition of human NCI-H1563 cell growth in a cell viability assay, IC50=0.54246 μM | SANGER | ||
| NCI-H1618 cel | Growth inhibition assay | Inhibition of human NCI-H1618 cell growth in a cell viability assay, IC50=21.9982 μM | SANGER | ||
| NCI-H1623 cell | Growth inhibition assay | Inhibition of human NCI-H1623 cell growth in a cell viability assay, IC50=15.0596 μM | SANGER | ||
| NCI-H1648 cell | Growth inhibition assay | Inhibition of human NCI-H1648 cell growth in a cell viability assay, IC50=5.7551 μM | SANGER | ||
| NCI-H1650 cell | Growth inhibition assay | Inhibition of human NCI-H1650 cell growth in a cell viability assay, IC50=11.5134 μM | SANGER | ||
| NCI-H1651 cell | Growth inhibition assay | Inhibition of human NCI-H1651 cell growth in a cell viability assay, IC50=16.4338 μM | SANGER | ||
| NCI-H1703 cell | Growth inhibition assay | Inhibition of human NCI-H1703 cell growth in a cell viability assay, IC50=15.577 μM | SANGER | ||
| NCI-H1734 cell | Growth inhibition assay | Inhibition of human NCI-H1734 cell growth in a cell viability assay, IC50=10.7788 μM | SANGER | ||
| NCI-H1755 cell | Growth inhibition assay | Inhibition of human NCI-H1755 cell growth in a cell viability assay, IC50=1.05531 μM | SANGER | ||
| NCI-H1770 cell | Growth inhibition assay | Inhibition of human NCI-H1770 cell growth in a cell viability assay, IC50=34.1793 μM | SANGER | ||
| NCI-H1792 cell | Growth inhibition assay | Inhibition of human NCI-H1792 cell growth in a cell viability assay, IC50=29.8379 μM | SANGER | ||
| NCI-H1963 cell | Growth inhibition assay | Inhibition of human NCI-H1963 cell growth in a cell viability assay, IC50=19.7494 μM | SANGER | ||
| NCI-H1993 cell | Growth inhibition assay | Inhibition of human NCI-H1993 cell growth in a cell viability assay, IC50=22.615 μM | SANGER | ||
| NCI-H2009 cell | Growth inhibition assay | Inhibition of human NCI-H2009 cell growth in a cell viability assay, IC50=7.39019 μM | SANGER | ||
| NCI-H2030 cell | Growth inhibition assay | Inhibition of human NCI-H2030 cell growth in a cell viability assay, IC50=1.94483 μM | SANGER | ||
| NCI-H2122 cell | Growth inhibition assay | Inhibition of human NCI-H2122 cell growth in a cell viability assay, IC50=10.1385 μM | SANGER | ||
| NCI-H2126 cell | Growth inhibition assay | Inhibition of human NCI-H2126 cell growth in a cell viability assay, IC50=12.3371 μM | SANGER | ||
| NCI-H2170 cell | Growth inhibition assay | Inhibition of human NCI-H2170 cell growth in a cell viability assay, IC50=18.1028 μM | SANGER | ||
| NCI-H2196 cell | Growth inhibition assay | Inhibition of human NCI-H2196 cell growth in a cell viability assay, IC50=24.8003 μM | SANGER | ||
| NCI-H2228 cell | Growth inhibition assay | Inhibition of human NCI-H2228 cell growth in a cell viability assay, IC50=2.28604 μM | SANGER | ||
| NCI-H2342 cell | Growth inhibition assay | Inhibition of human NCI-H2342 cell growth in a cell viability assay, IC50=0.93779 μM | SANGER | ||
| NCI-H2347 cell | Growth inhibition assay | Inhibition of human NCI-H2347 cell growth in a cell viability assay, IC50=16.1581 μM | SANGER | ||
| NCI-H2405 cell | Growth inhibition assay | Inhibition of human NCI-H2405 cell growth in a cell viability assay, IC50=10.4212 μM | SANGER | ||
| NCI-H2452 cell | Growth inhibition assay | Inhibition of human NCI-H2452 cell growth in a cell viability assay, IC50=26.6594 μM | SANGER | ||
| NCI-H292 cell | Growth inhibition assay | Inhibition of human NCI-H292 cell growth in a cell viability assay, IC50=6.04837 μM | SANGER | ||
| NCI-H345 cell | Growth inhibition assay | Inhibition of human NCI-H345 cell growth in a cell viability assay, IC50=16.2706 μM | SANGER | ||
| NCI-H358 cell | Growth inhibition assay | Inhibition of human NCI-H358 cell growth in a cell viability assay, IC50=19.7233 μM | SANGER | ||
| NCI-H460 cell | Growth inhibition assay | Inhibition of human NCI-H460 cell growth in a cell viability assay, IC50=4.62993 μM | SANGER | ||
| NCI-H520 cell | Growth inhibition assay | Inhibition of human NCI-H520 cell growth in a cell viability assay, IC50=1.13303 μM | SANGER | ||
| NCI-H522 cell | Growth inhibition assay | Inhibition of human NCI-H522 cell growth in a cell viability assay, IC50=11.0874 μM | SANGER | ||
| NCI-H526 cell | Growth inhibition assay | Inhibition of human NCI-H526 cell growth in a cell viability assay, IC50=22.8873μM | SANGER | ||
| NCI-H596 | Growth inhibition assay | Inhibition of human NCI-H596 cell growth in a cell viability assay, IC50=17.5708 μM | SANGER | ||
| NCI-H630 cell | Growth inhibition assay | Inhibition of human NCI-H630 cell growth in a cell viability assay, IC50=5.51055 μM | SANGER | ||
| NCI-H64 cell | Growth inhibition assay | Inhibition of human NCI-H64 cell growth in a cell viability assay, IC50=12.5431 μM | SANGER | ||
| NCI-H650 cell | Growth inhibition assay | Inhibition of human NCI-H650 cell growth in a cell viability assay, IC50=7.59877 μM | SANGER | ||
| NCI-H661 cell | Growth inhibition assay | Inhibition of human NCI-H661 cell growth in a cell viability assay, IC50=5.42326 μM | SANGER | ||
| NCI-H747 cell | Growth inhibition assay | Inhibition of human NCI-H747 cell growth in a cell viability assay, IC50=7.62799 μM | SANGER | ||
| NCI-H838 cell | Growth inhibition assay | Inhibition of human NCI-H838 cell growth in a cell viability assay, IC50=31.4118 μM | SANGER | ||
| NCI-N87 cell | Growth inhibition assay | Inhibition of human NCI-N87 cell growth in a cell viability assay, IC50=29.3042 μM | SANGER | ||
| NH-12 cell | Growth inhibition assay | Inhibition of human NH-12 cell growth in a cell viability assay, IC50=0.60864 μM | SANGER | ||
| NKM-1 cell | Growth inhibition assay | Inhibition of human NKM-1 cell growth in a cell viability assay, IC50=2.75923 μM | SANGER | ||
| NMC-G1 cell | Growth inhibition assay | Inhibition of human NMC-G1 cell growth in a cell viability assay, IC50=42.6693 μM | SANGER | ||
| NOS-1 cell | Growth inhibition assay | Inhibition of human NOS-1 cell growth in a cell viability assay, IC50=1.36953 μM | SANGER | ||
| NUGC-3 cell | Growth inhibition assay | Inhibition of human NUGC-3 cell growth in a cell viability assay, IC50=16.5906 μM | SANGER | ||
| NY cell | Growth inhibition assay | Inhibition of human NY cell growth in a cell viability assay, IC50=31.1864 μM | SANGER | ||
| OAW-42 cell | Growth inhibition assay | Inhibition of human OAW-42 cell growth in a cell viability assay, IC50=7.31565 μM | SANGER | ||
| OCI-AML2 cell | Growth inhibition assay | Inhibition of human OCI-AML2 cell growth in a cell viability assay, IC50=33.2531 μM | SANGER | ||
| OCUB-M cell | Growth inhibition assay | Inhibition of human OCUB-M cell growth in a cell viability assay, IC50=7.72152 μM | SANGER | ||
| OE19 cell | Growth inhibition assay | Inhibition of human OE19 cell growth in a cell viability assay, IC50=7.76684 μM | SANGER | ||
| OE33 cell | Growth inhibition assay | Inhibition of human OE33 cell growth in a cell viability assay, IC50=1.88926 μM | SANGER | ||
| OMC-1 cell | Growth inhibition assay | Inhibition of human OMC-1 cell growth in a cell viability assay, IC50=9.25098 μM | SANGER | ||
| OS-RC-2 cell | Growth inhibition assay | Inhibition of human OS-RC-2 cell growth in a cell viability assay, IC50=8.52307 μM | SANGER | ||
| OVCAR-3 cell | Growth inhibition assay | Inhibition of human OVCAR-3 cell growth in a cell viability assay, IC50=1.84415 μM | SANGER | ||
| OVCAR-4 cell | Growth inhibition assay | Inhibition of human OVCAR-4 cell growth in a cell viability assay, IC50=30.466 μM | SANGER | ||
| P12-ICHIKAWA cell | Growth inhibition assay | Inhibition of human P12-ICHIKAWA cell growth in a cell viability assay, IC50=14.7683 μM | SANGER | ||
| P30-OHK cell | Growth inhibition assay | Inhibition of human P30-OHK cell growth in a cell viability assay, IC50=4.536 μM | SANGER | ||
| PA-1 cell | Growth inhibition assay | Inhibition of human PA-1 cell growth in a cell viability assay, IC50=9.07615 μM | SANGER | ||
| PANC-03-27 cell | Growth inhibition assay | Inhibition of human PANC-03-27 cell growth in a cell viability assay, IC50=8.71082 μM | SANGER | ||
| PANC-10-05 cell | Growth inhibition assay | Inhibition of human PANC-10-05 cell growth in a cell viability assay, IC50=14.9959 μM | SANGER | ||
| PC-3 cell | Growth inhibition assay | Inhibition of human PC-3 cell growth in a cell viability assay, IC50=10.5135 μM | SANGER | ||
| PF-382 cell | Growth inhibition assay | Inhibition of human PF-382 cell growth in a cell viability assay, IC50=11.6828 μM | SANGER | ||
| RCC10RGB cell | Growth inhibition assay | Inhibition of human RCC10RGB cell growth in a cell viability assay, IC50=8.6567 μM | SANGER | ||
| RD cell | Growth inhibition assay | Inhibition of human RD cell growth in a cell viability assay, IC50=20.6036 μM | SANGER | ||
| REH cell | Growth inhibition assay | Inhibition of human REH cell growth in a cell viability assay, IC50=11.4883 μM | SANGER | ||
| RERF-LC-MS cell | Growth inhibition assay | Inhibition of human RERF-LC-MS cell growth in a cell viability assay, IC50=26.1347 μM | SANGER | ||
| RKO cell | Growth inhibition assay | Inhibition of human RKO cell growth in a cell viability assay, IC50=19.4439 μM | SANGER | ||
| RO82-W-1 cell | Growth inhibition assay | Inhibition of human RO82-W-1 cell growth in a cell viability assay, IC50=47.2783 μM | SANGER | ||
| RPMI-2650 cell | Growth inhibition assay | Inhibition of human RPMI-2650 cell growth in a cell viability assay, IC50=5.77947 μM | SANGER | ||
| RPMI-8402 cell | Growth inhibition assay | Inhibition of human RPMI-8402 cell growth in a cell viability assay, IC50=16.343 μM | SANGER | ||
| RS4-11 cell | Growth inhibition assay | Inhibition of human RS4-11 cell growth in a cell viability assay, IC50=6.68645 μM | SANGER | ||
| RT-112 cell | Growth inhibition assay | Inhibition of human RT-112 cell growth in a cell viability assay, IC50=6.71952 μM | SANGER | ||
| RVH-421 cell | Growth inhibition assay | Inhibition of human RVH-421 cell growth in a cell viability assay, IC50=32.3606 μM | SANGER | ||
| RXF393 cell | Growth inhibition assay | Inhibition of human RXF393 cell growth in a cell viability assay, IC50=20.5863 μM | SANGER | ||
| SBC-5 cell | Growth inhibition assay | Inhibition of human SBC-5 cell growth in a cell viability assay, IC50=20.8325 μM | SANGER | ||
| SCC-25 cell | Growth inhibition assay | Inhibition of human SCC-25 cell growth in a cell viability assay, IC50=15.8179 μM | SANGER | ||
| SCC-4 cell | Growth inhibition assay | Inhibition of human SCC-4 cell growth in a cell viability assay, IC50=9.59283 μM | SANGER | ||
| SCC-9 cell | Growth inhibition assay | Inhibition of human SCC-9 cell growth in a cell viability assay, IC50=3.08536 μM | SANGER | ||
| SF126 cell | Growth inhibition assay | Inhibition of human SF126 cell growth in a cell viability assay, IC50=10.6746 μM | SANGER | ||
| SF268 cell | Growth inhibition assay | Inhibition of human SF268 cell growth in a cell viability assay, IC50=15.1387 μM | SANGER | ||
| SF295 cell | Growth inhibition assay | Inhibition of human SF295 cell growth in a cell viability assay, IC50=13.6183 μM | SANGER | ||
| SIG-M5 cell | Growth inhibition assay | Inhibition of human SIG-M5 cell growth in a cell viability assay, IC50=12.6604 μM | SANGER | ||
| SJSA-1 cell | Growth inhibition assay | Inhibition of human SJSA-1 cell growth in a cell viability assay, IC50=36.9072 μM | SANGER | ||
| SK-CO-1 cell | Growth inhibition assay | Inhibition of human SK-CO-1 cell growth in a cell viability assay, IC50=10.6394 μM | SANGER | ||
| SK-LMS-1 cell | Growth inhibition assay | Inhibition of human SK-LMS-1 cell growth in a cell viability assay, IC50=8.76452 μM | SANGER | ||
| SK-LU-1 cell | Growth inhibition assay | Inhibition of human SK-LU-1 cell growth in a cell viability assay, IC50=42.043 μM | SANGER | ||
| SK-MEL-24 cell | Growth inhibition assay | Inhibition of human SK-MEL-24 cell growth in a cell viability assay, IC50=13.1675 μM | SANGER | ||
| SK-MEL-3 cell | Growth inhibition assay | Inhibition of human SK-MEL-3 cell growth in a cell viability assay, IC50=21.4696 μM | SANGER | ||
| SK-MES-1 cell | Growth inhibition assay | Inhibition of human SK-MES-1 cell growth in a cell viability assay, IC50=2.10096 μM | SANGER | ||
| human SN12C cell | Growth inhibition assay | Inhibition of human SN12C cell growth in a cell viability assay, IC50=17.1967 μM | SANGER | ||
| SNB75 cell | Growth inhibition assay | Inhibition of human SNB75 cell growth in a cell viability assay, IC50=7.8297 μM | SANGER | ||
| SNU-387 cell | Growth inhibition assay | Inhibition of human SNU-387 cell growth in a cell viability assay, IC50=4.19544 μM | SANGER | ||
| SNU-423 cell | Growth inhibition assay | Inhibition of human SNU-423 cell growth in a cell viability assay, IC50=5.94933 μM | SANGER | ||
| SNU-C1 cell | Growth inhibition assay | Inhibition of human SNU-C1 cell growth in a cell viability assay, IC50=2.00948 μM | SANGER | ||
| SNU-C2B cell | Growth inhibition assay | Inhibition of human SNU-C2B cell growth in a cell viability assay, IC50=22.2673 μM | SANGER | ||
| SR cell | Growth inhibition assay | Inhibition of human SR cell growth in a cell viability assay, IC50=13.0746 μM | SANGER | ||
| SU-DHL-1 cell | Growth inhibition assay | Inhibition of human SU-DHL-1 cell growth in a cell viability assay, IC50=6.81543 μM | SANGER | ||
| SW1710 cell | Growth inhibition assay | Inhibition of human SW1710 cell growth in a cell viability assay, IC50=1.38892 μM | SANGER | ||
| SW780 cell | Growth inhibition assay | Inhibition of human SW780 cell growth in a cell viability assay, IC50=4.89358 μM | SANGER | ||
| SW872 cell | Growth inhibition assay | Inhibition of human SW872 cell growth in a cell viability assay, IC50=14.1435 μM | SANGER | ||
| SW954 cell | Growth inhibition assay | Inhibition of human SW954 cell growth in a cell viability assay, IC50=5.85783 μM | SANGER | ||
| T47D cell | Growth inhibition assay | Inhibition of human T47D cell growth in a cell viability assay, IC50=0.5162 μM | SANGER | ||
| 22RV1 cell | Growth inhibition assay | Inhibition of human 22RV1 cell growth in a cell viability assay, IC50=6.61424 μM | SANGER | ||
| 23132-87 cell | Growth inhibition assay | Inhibition of human 23132-87 cell growth in a cell viability assay, IC50=0.75938 μM | SANGER | ||
| 639-V cell | Growth inhibition assay | Inhibition of human 639-V cell growth in a cell viability assay, IC50=5.8773 μM | SANGER | ||
| 697 cell | Growth inhibition assay | Inhibition of human 697 cell growth in a cell viability assay, IC50=7.17746 μM | SANGER | ||
| 769-P cell | Growth inhibition assay | Inhibition of human 769-P cell growth in a cell viability assay, IC50=1.10483 μM | SANGER | ||
| 8-MG-BA cell | Growth inhibition assay | Inhibition of human 8-MG-BA cell growth in a cell viability assay, IC50=8.63401 μM | SANGER | ||
| A4-Fuk cell | Growth inhibition assay | Inhibition of human A4-Fuk cell growth in a cell viability assay, IC50=1.8583 μM | SANGER | ||
| A427 cell | Growth inhibition assay | Inhibition of human A427 cell growth in a cell viability assay, IC50=3.07693 μM | SANGER | ||
| A498 cell | Growth inhibition assay | Inhibition of human A498 cell growth in a cell viability assay, IC50=1.08134 μM | SANGER | ||
| AN3-CA cell | Growth inhibition assay | Inhibition of human AN3-CA cell growth in a cell viability assay, IC50=1.65611 μM | SANGER | ||
| AU565 cell | Growth inhibition assay | Inhibition of human AU565 cell growth in a cell viability assay, IC50=1.23917 μM | SANGER | ||
| BB30-HNC cell | Growth inhibition assay | Inhibition of human BB30-HNC cell growth in a cell viability assay, IC50=2.86449 μM | SANGER | ||
| BxPC-3 cell | Growth inhibition assay | Inhibition of human BxPC-3 cell growth in a cell viability assay, IC50=2.22442 μM | SANGER | ||
| C-33-A cell | Growth inhibition assay | Inhibition of human C-33-A cell growth in a cell viability assay, IC50=12.4783 μM | SANGER | ||
| C2BBe1 cell | Growth inhibition assay | Inhibition of human C2BBe1 cell growth in a cell viability assay, IC50=13.6679 μM | SANGER | ||
| C3A cell | Growth inhibition assay | Inhibition of human C3A cell growth in a cell viability assay, IC50=4.42192 μM | SANGER | ||
| CAL-33 cell | Growth inhibition assay | Inhibition of human CAL-33 cell growth in a cell viability assay, IC50=3.43125 μM | SANGER | ||
| CAL-51 cell | Growth inhibition assay | Inhibition of human CAL-51 cell growth in a cell viability assay, IC50=7.62841 Μm | SANGER | ||
| CAL-54 cell | Growth inhibition assay | Inhibition of human CAL-54 cell growth in a cell viability assay, IC50=4.88625 μM | SANGER | ||
| CAL-85-1 cell | Growth inhibition assay | Inhibition of human CAL-85-1 cell growth in a cell viability assay, IC50=5.95309 μM | SANGER | ||
| TE-10 cell | Growth inhibition assay | Inhibition of human TE-10 cell growth in a cell viability assay, IC50=9.04225 μM | SANGER | ||
| TE-15 cell | Growth inhibition assay | Inhibition of human TE-15 cell growth in a cell viability assay, IC50=6.49393 μM | SANGER | ||
| TE-5 cell | Growth inhibition assay | Inhibition of human TE-5 cell growth in a cell viability assay, IC50=4.82452 μM | SANGER | ||
| TE-8 cell | Growth inhibition assay | Inhibition of human TE-8 cell growth in a cell viability assay, IC50=24.5243 μM | SANGER | ||
| TT cell | Growth inhibition assay | Inhibition of human TT cell growth in a cell viability assay, IC50=5.32724 μM | SANGER | ||
| U-118-MG cell | Growth inhibition assay | Inhibition of human U-118-MG cell growth in a cell viability assay, IC50=9.90258 μM | SANGER | ||
| U-698-M cell | Growth inhibition assay | Inhibition of human U-698-M cell growth in a cell viability assay, IC50=39.0015 μM | SANGER | ||
| U251 cell | Growth inhibition assay | Inhibition of human U251 cell growth in a cell viability assay, IC50=19.204 μM | SANGER | ||
| UACC-62 cell | Growth inhibition assay | Inhibition of human UACC-62 cell growth in a cell viability assay, IC50=27.0545 μM | SANGER | ||
| UACC-893 cell | Growth inhibition assay | Inhibition of human UACC-893 cell growth in a cell viability assay, IC50=5.29339 μM | SANGER | ||
| VMRC-RCZ cell | Growth inhibition assay | Inhibition of human VMRC-RCZ cell growth in a cell viability assay, IC50=3.70955 μM | SANGER | ||
| YKG-1 cell | Growth inhibition assay | Inhibition of human YKG-1 cell growth in a cell viability assay, IC50=1.01806 μM | SANGER | ||
| CCF-STTG1 cell | Growth inhibition assay | Inhibition of human CCF-STTG1 cell growth in a cell viability assay, IC50=6.81501 μM | SANGER | ||
| CCRF-CEM cell | Growth inhibition assay | Inhibition of human CCRF-CEM cell growth in a cell viability assay, IC50=4.93541 μM | SANGER | ||
| CESS cell | Growth inhibition assay | Inhibition of human CESS cell growth in a cell viability assay, IC50=2.70089 μM | SANGER | ||
| CHP-212 cell | Growth inhibition assay | Inhibition of human CHP-212 cell growth in a cell viability assay, IC50=4.55867 μM | SANGER | ||
| COLO-205 cell | Growth inhibition assay | Inhibition of human COLO-205 cell growth in a cell viability assay, IC50=1.99706 μM | SANGER | ||
| COR-L279 cell | Growth inhibition assay | Inhibition of human COR-L279 cell growth in a cell viability assay, IC50=1.68064 μM | SANGER | ||
| CTB-1 cell | Growth inhibition assay | Inhibition of human CTB-1 cell growth in a cell viability assay, IC50=7.59751 μM | SANGER | ||
| Ca-Ski cell | Growth inhibition assay | Inhibition of human Ca-Ski cell growth in a cell viability assay, IC50=5.3411 μM | SANGER | ||
| Ca9-22 cell | Growth inhibition assay | Inhibition of human Ca9-22 cell growth in a cell viability assay, IC50=5.97333 μM | SANGER | ||
| Calu-1 cell | Growth inhibition assay | Inhibition of human Calu-1 cell growth in a cell viability assay, IC50=7.25613 μM | SANGER | ||
| Calu-3 cell | Growth inhibition assay | Inhibition of human Calu-3 cell growth in a cell viability assay, IC50=3.65321 μM | SANGER | ||
| DMS-273 cell | Growth inhibition assay | Inhibition of human DMS-273 cell growth in a cell viability assay, IC50=4.15134 μM | SANGER | ||
| DOK cell | Growth inhibition assay | Inhibition of human DOK cell growth in a cell viability assay, IC50=4.15134 μM | SANGER | ||
| DSH1 cell | Growth inhibition assay | Inhibition of human DSH1 cell growth in a cell viability assay, IC50=0.98722 μM | SANGER | ||
| DV-90 cell | Growth inhibition assay | Inhibition of human DV-90 cell growth in a cell viability assay, IC50=6.03122 μM | SANGER | ||
| Detroit562 cell | Growth inhibition assay | Inhibition of human Detroit562 cell growth in a cell viability assay, IC50=4.79465 μM | SANGER | ||
| DoTc2-4510 cell | Growth inhibition assay | Inhibition of human DoTc2-4510 cell growth in a cell viability assay, IC50=3.43202 μM | SANGER | ||
| EB2 cell | Growth inhibition assay | Inhibition of human EB2 cell growth in a cell viability assay, IC50=7.75468 μM | SANGER | ||
| ECC12 cell | Growth inhibition assay | Inhibition of human ECC12 cell growth in a cell viability assay, IC50=8.88569 μM | SANGER | ||
| EFM-19 cell | Growth inhibition assay | Inhibition of human EFM-19 cell growth in a cell viability assay, IC50=0.56408 μM | SANGER | ||
| EFO-21 cell | Growth inhibition assay | Inhibition of human EFO-21 cell growth in a cell viability assay, IC50=4.43468 μM | SANGER | ||
| ES7 cell | Growth inhibition assay | Inhibition of human ES7 cell growth in a cell viability assay, IC50=1.34511 μM | SANGER | ||
| ETK-1 | Growth inhibition assay | Inhibition of human ETK-1 cell growth in a cell viability assay, IC50=4.57383 μM | SANGER | ||
| EW-3 cell | Growth inhibition assay | Inhibition of human EW-3 cell growth in a cell viability assay, IC50=5.64414 μM | SANGER | ||
| HCC70 cell | Growth inhibition assay | Inhibition of human HCC70 cell growth in a cell viability assay, IC50=0.75078 μM | SANGER | ||
| HGC-27 cell | Growth inhibition assay | Inhibition of human HGC-27 cell growth in a cell viability assay, IC50=0.15033 μM | SANGER | ||
| IGROV-1 cell | Growth inhibition assay | Inhibition of human IGROV-1 cell growth in a cell viability assay, IC50=0.72328 Μm | SANGER | ||
| MDA-MB-361 cell | Growth inhibition assay | Inhibition of human MDA-MB-361 cell growth in a cell viability assay, IC50=0.48995 μM | SANGER | ||
| MDA-MB-415 cell | Growth inhibition assay | Inhibition of human MDA-MB-415 cell growth in a cell viability assay, IC50=1.73449 μM | SANGER | ||
| MDA-MB-468 cell | Growth inhibition assay | Inhibition of human MDA-MB-468 cell growth in a cell viability assay, IC50=3.70773 μM | SANGER | ||
| ME-180 cell | Growth inhibition assay | Inhibition of human ME-180 cell growth in a cell viability assay, IC50=3.15011 Μm | SANGER | ||
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生物活性
| 製品説明 | Akti-1/2 (Akt Inhibitor VIII) is a highly selective Akt1/Akt2 inhibitor with IC50 of 58 nM/210 nM, respectively, about 36-fold selectivity for Akt1 over Akt3. Akti-1/2 induces apoptosis. | ||||||
|---|---|---|---|---|---|---|---|
| Targets |
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| In Vitro | ||||
| In vitro |
In a cell-based IPKA (C33A) assay, Akti-1/2 inhibits Akt1 and Akt2 with IC50 of 305 nM and 2086 nM, respectively. In HT29, MCF7, and A2780 cells, Akti-1/2 induces cell apoptosis by dramatically increasing caspase-3 activity. [1] In liver cells, Akti-1/2 blocks insulin regulation of PEPCK, G6Pase expression, and FOXO1 activity. [2] Akti-1/2 also strongly potentiates PAR-1-mediated platelet aggregation by blocking PKB. [3] In HCC827, NCI-H522, NCI-1651, and PC-9 cells, Akti-1/2 inhibits cell growth with IC50 of 4.7 μM, 7.25 μM, and 9.5 μM, when in combination with gefitinib, Akti-1/2 causes enhanced inhibition of cell growth and apoptosis. [4] |
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|---|---|---|---|---|
| Kinase Assay | Kinase screen | |||
| Briefly, all assays (25.5 μl at 21°C for 30 min) are performed using a Biomek 2000 Laboratory Automation Workstation in a 96-well format. Reactions contains 5–20 mU purified kinase along with substrate peptide or protein and are initiated by the addition of 10 mM MgAcetate and 5, 20, or 50 μM ATP ([γ-33P]-ATP, 800 cpm/pmol). | ||||
| 細胞実験 | 細胞株 | HCC827, NCI-H522, NCI-1651, and PC-9 cells | ||
| 濃度 | ~10 μM | |||
| 反応時間 | 96 h | |||
| 実験の流れ | The cell growth inhibitory effect of AKTi-1/2 is studied using the 96 h sulforhodamine B assay (SRB). Drug concentrations that inhibited 50% of cell growth (IC50) are calculated for each compound in GraphPad Prism 6.0 using non-linear regression analysis and sigmoidal dose–response (variable slope) equation. |
|||
| 実験結果図 | Methods | Biomarkers | 結果図 | PMID |
| Western blot | p-AKT / AKT / p-Foxo3a / p-GSK3β / p-p70S6K / p-S6 / p-4EBP1 / Cyclin D1 / Cyclin D2 / Cyclin D3 / p-Rb / p27 |
|
18725974 | |
| Immunofluorescence | MCM2 / H3K9me2 / CD63 |
|
26637368 | |
| In Vivo | ||
| In Vivo |
In mice, Akti-1/2 (50 mg/kg, i.p.) inhibits basal and IGF-stimulated Akt1 and Akt2 phosphorylation in lung. [1] |
|
|---|---|---|
| 動物実験 | 動物モデル | C57BL/6 J mice |
| 投与量 | 50 mg/kg | |
| 投与経路 | i.p. | |
化学情報
| 分子量 | 551.64 | 化学式 | C34H29N7O |
| CAS No. | 612847-09-3 | SDF | Download Akti-1/2 SDFをダウンロードする |
| Smiles | C1CN(CCC1N2C3=CC=CC=C3NC2=O)CC4=CC=C(C=C4)C5=C(N=C6C=C7C(=NC=N7)C=C6N5)C8=CC=CC=C8 | ||
| 保管 | |||
|
In vitro |
DMSO : 22 mg/mL ( (39.88 mM)； 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。) Water : Insoluble Ethanol : Insoluble |
モル濃度計算器 |
|
in vivo Add solvents to the product individually and in order. |
投与溶液組成計算機 | ||||
実験計算
投与溶液組成計算機(クリア溶液)
ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）
mg/kg
g
μL
匹
ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計算結果：
投与溶媒濃度： mg/ml;
DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )
投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH2O，を加え完全に溶解させます。
投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。
注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。
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