Panobinostat (LBH589)
别名: NVP-LBH589 中文名称：帕比司他
Panobinostat (LBH589, NVP-LBH589)是一种新型的，广谱HDAC抑制剂，无细胞试验中IC50为5 nM。Panobinostat (LBH589) 可诱导自噬和凋亡。Panobinostat 可以有效地破坏体内 HIV 的潜伏期。Phase 3。
Panobinostat (LBH589) Chemical Structure
CAS: 404950-80-7
产品质控
批次：
纯度：
99.88%
99.88
Panobinostat (LBH589)相关产品
相关信号通路图
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| SK-N-BE | Apoptosis Assay | 0–40 nM | 48 h | potently induced apoptosis in a dose-dependent fashion | 24098799 |
| SK-N-SH | Apoptosis Assay | 0–40 nM | 48 h | potently induced apoptosis in a dose-dependent fashion | 24098799 |
| SK-N-DZ | Apoptosis Assay | 0–80 nM | 48 h | potently induced apoptosis in a dose-dependent fashion | 24098799 |
| SK-N-AS | Apoptosis Assay | 0–80 nM | 48 h | potently induced apoptosis in a dose-dependent fashion | 24098799 |
| SK-N-BE | Growth Inhibition Assay | 0–80 nM | 48 h | IC50=75.4 nM | 24098799 |
| SK-N-SH | Growth Inhibition Assay | 0–80 nM | 48 h | IC50=72.3 nM | 24098799 |
| SK-N-DZ | Growth Inhibition Assay | 0–80 nM | 48 h | IC50=21.9 nM | 24098799 |
| SK-N-AS | Growth Inhibition Assay | 0–80 nM | 48 h | IC50=27.4 nM | 24098799 |
| OS-RC-2 | Apoptosis Assay | 50 nM | 48 h | induces cell apoptosis | 24144737 |
| OS-RC-2 | Growth Inhibition Assay | 50 nM | 48 h | induces G2/M arrest | 24144737 |
| OS-RC-2 | Cell Viability Assay | 0-1000 nM | 24/48/72 h | decreases cell viability in both time- and dose-dependent manner | 24144737 |
| PC3-AR | Function Assay | 0-100 nM | 24 h | suppresses expression of activated ATM, Akt and Erk1/2 protein | 24163230 |
| PC3 | Function Assay | 0-100 nM | 24 h | suppresses expression of activated ATM, Akt and Erk1/2 protein | 24163230 |
| PC3-AR | Growth Inhibition Assay | 0-100 nM | 24/48 h | induces cell cycle arrest in the G2M phase | 24163230 |
| PC3 | Growth Inhibition Assay | 0-100 nM | 24/48 h | induces accumulation of subG1 population | 24163230 |
| PC3-AR | Apoptosis Assay | 0-100 nM | 24/48 h | induces apoptosis in both time- and dose-dependent manner | 24163230 |
| PC3 | Apoptosis Assay | 0-100 nM | 24/48 h | induces apoptosis in a dose-dependent manner | 24163230 |
| U937 | Apoptosis Assay | 0–40 nM | 48 h | induces apoptosis in a dose-dependent manner | 24244429 |
| OCI-AML3 | Apoptosis Assay | 0–40 nM | 48 h | induces apoptosis in a dose-dependent manner | 24244429 |
| CTS | Apoptosis Assay | 0–40 nM | 48 h | induces apoptosis in a dose-dependent manner | 24244429 |
| MCF-7 | Function Assay | 5-50 nM | 24 h | reduced the level of expression of ERα, PR and FoxA1 | 24366407 |
| MCF-7 | Morphological Crystal Violet (CV) Assay | 10 nM | 3 d | alters cell morphology | 24810497 |
| BT-549 | Morphological Crystal Violet (CV) Assay | 10 nM | 3 d | alters cell morphology | 24810497 |
| MDA-MB-231 | Morphological Crystal Violet (CV) Assay | 10 nM | 3 d | alters cell morphology | 24810497 |
| 769-P | Apoptosis Assay | 50 nM | 48 h | induces cell apoptosis | 25176354 |
| ACHN | Apoptosis Assay | 50 nM | 48 h | induces cell apoptosis | 25176354 |
| Caki-1 | Apoptosis Assay | 50 nM | 48 h | induces cell apoptosis | 25176354 |
| 769-P | Colony Formation Assay | 50 nM | 7-14 d | suppressed colony formation significantly combined with with bortezomib | 25176354 |
| ACHN | Colony Formation Assay | 50 nM | 7-14 d | suppressed colony formation significantly combined with with bortezomib | 25176354 |
| Caki-1 | Colony Formation Assay | 50 nM | 7-14 d | suppressed colony formation significantly combined with with bortezomib | 25176354 |
| 769-P | Growth Inhibition Assay | 25/50 nM | 48 h | inhibits cell growth in a dose dependent manner synergistically with bortezomib | 25176354 |
| ACHN | Growth Inhibition Assay | 25/50 nM | 48 h | inhibits cell growth in a dose dependent manner synergistically with bortezomib | 25176354 |
| Caki-1 | Growth Inhibition Assay | 25/50 nM | 48 h | inhibits cell growth in a dose dependent manner synergistically with bortezomib | 25176354 |
| 786-O | Apoptosis Assay | 50 nM | 48 h | induces cell apoptosis combined ritonavir | 25279191 |
| 769-P | Apoptosis Assay | 50 nM | 48 h | induces cell apoptosis combined ritonavir | 25279191 |
| ACHN | Apoptosis Assay | 50 nM | 48 h | induces cell apoptosis combined ritonavir | 25279191 |
| Caki-1 | Apoptosis Assay | 50 nM | 48 h | induces cell apoptosis combined ritonavir | 25279191 |
| 786-O | Growth Inhibition Assay | 10/25/50 nM | 48 h | inhibits cell growth in a dose dependent manner synergistically with ritonavir | 25279191 |
| 769-P | Growth Inhibition Assay | 10/25/50 nM | 48 h | inhibits cell growth in a dose dependent manner synergistically with ritonavir | 25279191 |
| ACHN | Growth Inhibition Assay | 10/25/50 nM | 48 h | inhibits cell growth in a dose dependent manner synergistically with ritonavir | 25279191 |
| Caki-1 | Growth Inhibition Assay | 10/25/50 nM | 48 h | inhibits cell growth in a dose dependent manner synergistically with ritonavir | 25279191 |
| RPMI-8226vr10 | Function Assay | 1 μM | 24 h | increases caspase-3 activity 2.5-fold | 25612941 |
| ML-1 | Function Assay | 1 μM | 24 h | increases caspase-3 activity 4-fold | 25612941 |
| RPMI-8226vr10 | Function Assay | 0-1 μM | 24 h | induces DNA fragmentation in a dose-dependent manner | 25612941 |
| ML-1 | Function Assay | 0-1 μM | 24 h | induces DNA fragmentation in a dose-dependent manner | 25612941 |
| AML3 | Function Assay | 0-1 μM | 24 h | induces DNA fragmentation in a dose-dependent manner | 25612941 |
| NCI-H23 | Growth Inhibition Assay | 10 nM | 48 h | enhances cisplatin sensitivity | 25944617 |
| HCC827 | Growth Inhibition Assay | 10 nM | 48 h | enhances cisplatin sensitivity | 25944617 |
| RPMI 8226 | Apoptosis Assay | 4 nM | 24/48 h | induces cell apoptosis in a time-dependent manner | 26000292 |
| H929 | Cell Survival Assay | 2/4/6 nM | 48 h | induces a significant decrease in the cell growth | 26000292 |
| U266 | Cell Survival Assay | 2/4/6 nM | 48 h | induces a significant decrease in the cell growth | 26000292 |
| OPM2 | Cell Survival Assay | 2/4/6 nM | 48 h | induces a significant decrease in the cell growth | 26000292 |
| RPMI 8226 | Cell Survival Assay | 2/4/6 nM | 48 h | induces a significant decrease in the cell growth | 26000292 |
| G401 | Function Assay | 50/100 nM | 24 h | induces cell cycle disorder | 26176219 |
| SK-NEP-1 | Function Assay | 50/100 nM | 24 h | induces cell cycle disorder | 26176219 |
| G401 | Function Assay | 50/100 nM | 24 h | shows the induction of DNA fragmentation | 26176219 |
| SK-NEP-1 | Function Assay | 50/100 nM | 24 h | shows the induction of DNA fragmentation | 26176219 |
| G401 | Apoptosis Assay | 50/100 nM | 24 h | induces cell apoptosis in a dose-dependent manner | 26176219 |
| SK-NEP-1 | Apoptosis Assay | 50/100 nM | 24 h | induces cell apoptosis in a dose-dependent manner | 26176219 |
| G401 | Cell Viability Assay | 50 nM | 1–4 d | reduces cell survival in a time dependent manner | 26176219 |
| SK-NEP-1 | Cell Viability Assay | 50 nM | 1–4 d | reduces cell survival in a time dependent manner | 26176219 |
| G401 | Growth Inhibition Assay | 0.01–10.0 μM | 24 h | IC50=143.02 nM | 26176219 |
| SK-NEP-1 | Growth Inhibition Assay | 0.01–10.0 μM | 24 h | IC50=76.34 nM | 26176219 |
| NCI-H460 | Growth Inhibition Assay | 10/20/30 nM | 72 h | enhances the antiproliferative effect of erlotinib | 26675484 |
| A549 | Growth Inhibition Assay | 10/15/20 nM | 72 h | enhances the antiproliferative effect of erlotinib | 26675484 |
| HCC827 | Growth Inhibition Assay | 5/7.5/10 nM | 72 h | enhances the antiproliferative effect of erlotinib | 26675484 |
| HepG2 | Function Assay | 50 nM | 24-72 h | induced activation of caspase 3 after 24 h | 26702784 |
| HT29 | Function Assay | 50 nM | 24-72 h | induced activation of caspase 3 after 48 h | 26702784 |
| HepG2 | Growth Inhibition Assay | 0-10 μM | 0-4 d | inhibits cell growth in both time- and dose-dependent manner | 26702784 |
| HT29 | Growth Inhibition Assay | 0-10 μM | 0-4 d | inhibits cell growth in both time- and dose-dependent manner | 26702784 |
| SK-N-AS | Function Assay | 0–80 nM | 48 h | induces a dose-dependent cleavage of caspase 3 and PARP | 24098799 |
| SK-N-DZ | Function Assay | 0–80 nM | 48 h | induces a dose-dependent cleavage of caspase 3 and PARP | 24098799 |
| SK-N-SH | Function Assay | 0–40 nM | 48 h | induces a dose-dependent cleavage of caspase 3 and PARP | 24098799 |
| SK-N-BE | Function Assay | 0–40 nM | 48 h | induces a dose-dependent cleavage of caspase 3 and PARP | 24098799 |
| HCC-LM3 | Growth Inhibition Assay | 1-1000 nM | 24/48/72 h | inhibits cell growth in both time- and dose-dependent manner | 24093956 |
| HepG2 | Growth Inhibition Assay | 1-1000 nM | 24/48/72 h | inhibits cell growth in both time- and dose-dependent manner | 24093956 |
| SMMC-7721 | Growth Inhibition Assay | 1-1000 nM | 24/48/72 h | inhibits cell growth in both time- and dose-dependent manner | 24093956 |
| HCC-LM3 | Apoptosis Assay | 50 nM | 48 h | induces cell apoptosis significantly in a caspase-dependent manner by cleavage of caspases 3, 8 and 9 | 24093956 |
| HepG2 | Apoptosis Assay | 50 nM | 48 h | induces cell apoptosis significantly in a caspase-dependent manner by cleavage of caspases 3, 8 and 9 | 24093956 |
| SMMC-7721 | Apoptosis Assay | 50 nM | 48 h | induces cell apoptosis significantly in a caspase-dependent manner by cleavage of caspases 3, 8 and 9 | 24093956 |
| HCC-LM3 | Function Assay | 50/100 nM | 24 h | decreases the levels of p-STAT3 and p-Akt | 24093956 |
| HepG2 | Function Assay | 50/100 nM | 24 h | decreases the levels of p-STAT3 and p-Akt | 24093956 |
| SMMC-7721 | Function Assay | 50/100 nM | 24 h | decreases the levels of p-STAT3 and p-Akt | 24093956 |
| HCC-LM3 | Function Assay | 50/100 nM | 24 h | downregulates Bcl-xL expression | 24093956 |
| HepG2 | Function Assay | 50/100 nM | 24 h | downregulates Bcl-xL expression | 24093956 |
| SMMC-7721 | Function Assay | 50/100 nM | 24 h | downregulates Bcl-xL expression | 24093956 |
| FaDu | Growth Inhibition Assay | 100 nM | 8/10/12 h | displayed a significant and prolonged G2/M arrest at 8 and 12 h post release | 24026482 |
| FaDu | Function Assay | 100 nM | 2/4/8/12 h | induced p21Waf1/Cip1 expression | 24026482 |
| PC-3 | Growth Inhibition Assay | 0-10 μM | 24/48/72 h | inhibits cell growth in both time- and dose-dependent manner | 23991216 |
| LNCaP | Growth Inhibition Assay | 0-5 μM | 24/48/72 h | inhibits cell growth in both time- and dose-dependent manner | 23991216 |
| RWPE-1 | Growth Inhibition Assay | 0-20 μM | 24/48/72 h | inhibits cell growth in both time- and dose-dependent manner | 23991216 |
| Capan-1 | Function Assay | 25/50/100 nM | 8/24/48 h | downregulated Ron mRNA and protein expression and downstream signaling | 23922886 |
| L3.6pl | Function Assay | 25/50/100 nM | 8/24/48 h | downregulated Ron mRNA and protein expression and downstream signaling | 23922886 |
| CFPAC-1 | Function Assay | 25/50/100 nM | 8/24/48 h | downregulated Ron mRNA and protein expression and downstream signaling | 23922886 |
| Capan-1 | Growth Inhibition Assay | 25/50/100 nM | 48 h | reduces cell growth in a dose-dependent manner | 23922886 |
| L3.6pl | Growth Inhibition Assay | 25/50/100 nM | 48 h | reduces cell growth in a dose-dependent manner | 23922886 |
| CFPAC-1 | Growth Inhibition Assay | 25/50/100 nM | 48 h | reduces cell growth in a dose-dependent manner | 23922886 |
| Capan-1 | Apoptosis Assay | 25/50/100 nM | 48 h | induces cell growth in a dose-dependent manner | 23922886 |
| L3.6pl | Apoptosis Assay | 25/50/100 nM | 48 h | induces cell growth in a dose-dependent manner | 23922886 |
| CFPAC-1 | Apoptosis Assay | 25/50/100 nM | 48 h | induces cell growth in a dose-dependent manner | 23922886 |
| HN22 | Growth Inhibition Assay | 0-20 nM | 24/48 h | inhibits cell viability in both time- and dose- dependent manner | 23877235 |
| HSC4 | Growth Inhibition Assay | 0-20 nM | 24/48 h | inhibits cell viability in both time- and dose- dependent manner | 23877235 |
| HN22 | Apoptosis Assay | 0-20 nM | 48 h | induces cell apoptosis | 23877235 |
| HSC4 | Apoptosis Assay | 0-20 nM | 48 h | induces cell apoptosis | 23877235 |
| HN22 | Growth Inhibition Assay | 0-20 nM | 48 h | induces G1 phase cell cycle arrest | 23877235 |
| HSC4 | Growth Inhibition Assay | 0-20 nM | 48 h | induces G1 phase cell cycle arrest | 23877235 |
| HN22 | Function Assay | 0-20 nM | 48 h | suppresses Sp1 expression | 23877235 |
| HSC4 | Function Assay | 0-20 nM | 48 h | suppresses Sp1 expression | 23877235 |
| U937 | Function assay | 1 uM | 24 hrs | Inhibition of HDAC6 in human U937 cells assessed as increase of intracellular acetylated alpha-tubulin level at 1 uM after 24 hrs by Western blot analysis | 24694055 |
| U937 | Function assay | 1 uM | 24 hrs | Inhibition of HDAC1 in human U937 cells assessed as increase of intracellular acetylated histone H3 level at 1 uM after 24 hrs by Western blot analysis | 24694055 |
| U937 | Function assay | 1 uM | 24 hrs | Inhibition of HDAC2 in human U937 cells assessed as increase of intracellular acetylated histone H3 level at 1 uM after 24 hrs by Western blot analysis | 24694055 |
| U937 | Function assay | 1 uM | 24 hrs | Inhibition of HDAC3 in human U937 cells assessed as increase of intracellular acetylated histone H4 level at 1 uM after 24 hrs by Western blot analysis | 24694055 |
| MV4-11 | Function assay | 10 to 1000 nM | 6 hrs | Inhibition of HDAC6 in human MV4-11 cells assessed as upregulation of alpha tubulin acetylation at 10 to 1000 nM after 6 hrs by Western blot analysis | 26443078 |
| HCT116 | Function assay | 10 to 1000 nM | 6 hrs | Inhibition of HDAC6 in human HCT116 cells assessed as upregulation of alpha tubulin acetylation at 10 to 1000 nM after 6 hrs by Western blot analysis | 26443078 |
| HCT116 | Function assay | 10 to 1000 nM | 6 hrs | Inhibition of HDAC1/2/3 in human HCT116 cells assessed as upregulation of histone H3 acetylation at 10 to 1000 nM after 6 hrs by Western blot analysis | 26443078 |
| MV4-11 | Function assay | 10 to 1000 nM | 6 hrs | Inhibition of HDAC1/2/3 in human MV4-11 cells assessed as upregulation of histone H3 acetylation at 10 to 1000 nM after 6 hrs by Western blot analysis | 26443078 |
| MV4-11 | Function assay | 50 nM | 24 hrs | Induction of HDAC6 degradation in human MV4-11 cells at 50 nM after 24 hrs by Western blot method | 29589441 |
| MV4-11 | Function assay | 50 nM | 2 to 24 hrs | Inhibition of HDAC6 in human MV4-11 cells assessed as induction of alpha-tubulin hyperacetylation at 50 nM after 2 to 24 hrs by Western blot method | 29589441 |
| MV4-11 | Cell cycle arrest assay | 30 to 50 nM | 24 hrs | Cell cycle arrest in human MV4-11 cells assessed as accumulation at sub-G1 phase at 30 to 50 nM after 24 hrs by propidium iodide staining-based flow cytometric method | 29589441 |
| MV4-11 | Apoptosis assay | 30 nM | 24 to 48 hrs | Induction of apoptosis in human MV4-11 cells at 30 nM after 24 to 48 hrs by Annexin V-PI staining based flow cytometry | 29738953 |
| SK-N-DZ | Growth Inhibition Assay | 24 h | IC50=17.1 ± 0.4 nM | 25308916 | |
| SK-N-AS | Growth Inhibition Assay | 24 h | IC50=37.1 ± 2.4 nM | 25308916 | |
| SK-N-BE (2), MK PAN | Growth Inhibition Assay | 24 h | IC50=382.0 ± 43.2 nM | 25308916 | |
| SK-N-BE (2), PAN MK | Growth Inhibition Assay | 24 h | IC50=104.0 ± 7.8 nM | 25308916 | |
| SK-N-BE (2) | Growth Inhibition Assay | 24 h | IC50=104.0 ± 7.8 nM | 25308916 | |
| HCT8 | Growth Inhibition Assay | 72 h | IC50=12.9 ± 1.9 nM | 23299388 | |
| H630 | Growth Inhibition Assay | 72 h | IC50=12.4 ± 3.1 nM | 23299388 | |
| cH630 5-FU-res | Growth Inhibition Assay | 72 h | IC50=15.5 ± 1.2 nM | 23299388 | |
| HCT116 | Growth Inhibition Assay | 72 h | IC50=10.7 ± 2.2 nM | 23299388 | |
| HCT116 p53−/− | Growth Inhibition Assay | 72 h | IC50=8.6 ± 1.7 nM | 23299388 | |
| dHCT116 p21−/− | Growth Inhibition Assay | 72 h | IC50=5.9 ± 1.3 nM | 23299388 | |
| HT29 | Growth Inhibition Assay | 72 h | IC50=16.3 ± 2.3 nM | 23299388 | |
| LoVo | Growth Inhibition Assay | 72 h | IC50=5.1 ± 0.6 nM | 23299388 | |
| RKO | Growth Inhibition Assay | 72 h | IC50=7.9 ± 2.2 nM | 23299388 | |
| SW480 | Growth Inhibition Assay | 72 h | IC50=17.5 ± 0.8 nM | 23299388 | |
| eSW620 | Growth Inhibition Assay | 72 h | IC50=9.1 ± 2.1 nM | 23299388 | |
| COLO205 | Antiproliferative assay | 96 hrs | Antiproliferative activity against human COLO205 cells after 96 hrs by celltiter 96 assay, IC50 = 0.018 μM. | 21634430 | |
| PC3 | Antiproliferative assay | 96 hrs | Antiproliferative activity against human PC3 cells after 96 hrs by celltiter 96 assay, IC50 = 0.024 μM. | 21634430 | |
| A2780 | Antiproliferative assay | 96 hrs | Antiproliferative activity against human A2780 cells after 96 hrs by celltiter 96 assay, IC50 = 0.035 μM. | 21634430 | |
| HCT116 | Antiproliferative assay | 96 hrs | Antiproliferative activity against human HCT116 cells after 96 hrs by celltiter 96 assay, IC50 = 0.048 μM. | 21634430 | |
| B16 | Growth inhibition assay | 48 hrs | Growth inhibition of mouse B16 cells incubated for 48 hrs by MTT assay, GI50 = 0.15 μM. | 23009203 | |
| HuH7 | Cytotoxicity assay | 3 days | Cytotoxicity against human HuH7 cells assessed as inhibition of cell viability after 3 days by CellTiter 96 assay, CC50 = 0.0035 μM. | 25490700 | |
| Sf9 | Function assay | 15 mins | Inhibition of full length C-terminal His/FLAG-tagged human recombinant HDAC1 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured a, IC50 = 0.00126 μM. | 27186676 | |
| Sf9 | Function assay | 15 mins | Inhibition of full length C-terminal His-tagged human recombinant HDAC3/NCOR2 (395 to 489 residues) expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substr, IC50 = 0.00227 μM. | 27186676 | |
| MV4-11 | Cytotoxicity assay | 24 hrs | Cytotoxicity against human MV4-11 cells assessed as growth inhibition after 24 hrs by MTT assay, IC50 = 0.00297 μM. | 27186676 | |
| Sf9 | Function assay | 15 mins | Inhibition of full length human recombinant HDAC2 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence a, IC50 = 0.00328 μM. | 27186676 | |
| HCT116 | Cytotoxicity assay | 24 hrs | Cytotoxicity against human HCT116 cells assessed as growth inhibition after 24 hrs by MTT assay, IC50 = 0.00336 μM. | 27186676 | |
| Sf9 | Function assay | 15 mins | Inhibition of full length human recombinant HDAC6 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence a, IC50 = 0.00416 μM. | 27186676 | |
| Sf9 | Inhibition of human | 15 mins | Inhibition of human recombinant HDAC10 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence assay, IC50 = 0.00445 μM. | 27186676 | |
| Sf9 | Function assay | 15 mins | Inhibition of full length C-terminal His-tagged human recombinant HDAC8 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after , IC50 = 0.00486 μM. | 27186676 | |
| A2780S | Cytotoxicity assay | 24 hrs | Cytotoxicity against human A2780S cells assessed as growth inhibition after 24 hrs by MTT assay, IC50 = 0.00832 μM. | 27186676 | |
| A2780S | Function assay | 6 hrs | Inhibition of HDAC6 in human A2780S cells assessed as tubulin acetylation incubated for 6 hrs by cytoblot assay, EC50 = 0.15071 μM. | 27186676 | |
| A2780S | Function assay | 6 hrs | Inhibition of HDAC1/2/3 in human A2780S cells assessed as histone H3 acetylation incubated for 6 hrs by cytoblot assay, EC50 = 0.1695 μM. | 27186676 | |
| Sf9 | Function assay | 15 mins | Inhibition of human recombinant HDAC5 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence assay, IC50 = 0.1903 μM. | 27186676 | |
| Sf9 | Function assay | 15 mins | Inhibition of N-terminal GST/C-terminal His-tagged human recombinant HDAC4 (627 to 1084 residues) expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrat, IC50 = 0.3378 μM. | 27186676 | |
| Sf9 | Function assay | 15 mins | Inhibition of C-terminal His-tagged human recombinant HDAC9 (604 to 1066 residues) expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition meas, IC50 = 0.8878 μM. | 27186676 | |
| Sf9 | Function assay | 15 mins | Inhibition of full length human recombinant HDAC11 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence , IC50 = 4.112 μM. | 27186676 | |
| Sf9 | Function assay | 15 mins | Inhibition of N-terminal GST-tagged human recombinant HDAC7 (518 to end residues) expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measu, IC50 = 4.354 μM. | 27186676 | |
| Sf9 | Function assay | 60 mins | Inhibition full length human recombinant HDAC2 expressed in baculovirus coexpressed in fall armyworm Sf9 cells using carboxyfluorescein (FAM)-labeled acetylated/ trifluoroacetylated peptide as substrate after 60 mins by fluorescence assay, IC50 = 0.002 μM. | 27377864 | |
| Sf9 | Function assay | 60 mins | Inhibition of human recombinant HDAC6 expressed in baculovirus coexpressed in fall armyworm Sf9 cells using carboxyfluorescein (FAM)-labeled acetylated/ trifluoroacetylated peptide as substrate after 60 mins by fluorescence assay, IC50 = 0.002 μM. | 27377864 | |
| Sf9 | Function assay | 60 mins | Inhibition of N-terminal GST-tagged full length human recombinant HDAC5 expressed in baculovirus coexpressed in fall armyworm Sf9 cells using carboxyfluorescein (FAM)-labeled acetylated/ trifluoroacetylated peptide as substrate after 60 mins by fluorescen, IC50 = 0.092 μM. | 27377864 | |
| Sf9 | Function assay | 60 mins | Inhibition of C-terminal His-tagged full length human recombinant HDAC8 expressed in baculovirus coexpressed in fall armyworm Sf9 cells using carboxyfluorescein (FAM)-labeled acetylated/ trifluoroacetylated peptide as substrate after 60 mins by fluorescen, IC50 = 0.231 μM. | 27377864 | |
| Sf9 | Function assay | 60 mins | Inhibition of C-terminal His-tagged human recombinant HDAC9 (604 to 1066 residues) expressed in baculovirus coexpressed in fall armyworm Sf9 cells using carboxyfluorescein (FAM)-labeled acetylated/ trifluoroacetylated peptide as substrate after 60 mins by, IC50 = 2.68 μM. | 27377864 | |
| Sf9 | Function assay | 60 mins | Inhibition of N-terminal GST-tagged human recombinant HDAC7 (518 to end residues) expressed in baculovirus coexpressed in fall armyworm Sf9 cells using carboxyfluorescein (FAM)-labeled acetylated/ trifluoroacetylated peptide as substrate after 60 mins by , IC50 = 2.83 μM. | 27377864 | |
| HEK293 | Cytotoxicity assay | 48 hrs | Cytotoxicity against HEK293 cells after 48 hrs by resazurin assay, IC50 = 0.07 μM. | 28241112 | |
| NFF | Cytotoxicity assay | 72 hrs | Cytotoxicity against human NFF cells after 72 hrs by SRB assay, IC50 = 0.07 μM. | 28241112 | |
| HUT78 | Apoptosis assay | 18 hrs | Pro-apoptotic activity in human HUT78 cells after 18 hrs by caspase-Glo 3/7 assay, EC50 = 0.0043 μM. | 30122227 | |
| NFF | Cytotoxicity assay | 72 hrs | Cytotoxicity against human NFF cells after 72 hrs by sulforhodamine B assay, IC50 = 0.07 μM. | 30245402 | |
| HEK293 | Cytotoxicity assay | 48 hrs | Cytotoxicity against HEK293 cells after 48 hrs by resazurin dye based assay, IC50 = 0.07 μM. | 30245402 | |
| M14 | Apoptosis assay | 24 to 48 hrs | Induction of apoptosis human M14 cells assessed as caspase activity after 24 to 48 hrs using DEVD peptide as substrate by ApoTox-Glo triplex assay | 24471466 | |
| Raji | Cytotoxicity assay | 24 hrs | Cytotoxicity against human Raji cells assessed as growth inhibition after 24 hrs by MTT assay | 27186676 | |
| Ramos | Cytotoxicity assay | 24 hrs | Cytotoxicity against human Ramos cells assessed as growth inhibition after 24 hrs by MTT assay | 27186676 | |
| U266 | Cytotoxicity assay | 24 hrs | Cytotoxicity against human U266 cells assessed as growth inhibition after 24 hrs by MTT assay | 27186676 | |
| RPMI8226 | Cytotoxicity assay | 24 hrs | Cytotoxicity against human RPMI8226 cells assessed as growth inhibition after 24 hrs by MTT assay | 27186676 | |
| HBL1 | Cytotoxicity assay | 24 hrs | Cytotoxicity against human HBL1 cells assessed as growth inhibition after 24 hrs by MTT assay | 27186676 | |
| MM1S | Cytotoxicity assay | 24 hrs | Cytotoxicity against human MM1S cells assessed as growth inhibition after 24 hrs by MTT assay | 27186676 | |
| OCI-LY1 | Cytotoxicity assay | 24 hrs | Cytotoxicity against human OCI-LY1 cells assessed as growth inhibition after 24 hrs by MTT assay | 27186676 | |
| SUDHL4 | Cytotoxicity assay | 24 hrs | Cytotoxicity against human SUDHL4 cells assessed as growth inhibition after 24 hrs by MTT assay | 27186676 | |
| THP89GFP | Growth Inhibition Assay | EC50=19.34 ± 6.43 nM | 26563568 | ||
| J89GFP | Growth Inhibition Assay | EC50=49.85 ± 12.65 nM | 26563568 | ||
| Cal62 | Growth Inhibition Assay | IC50=33 ± 4 nM | 23824064 | ||
| Hth7 | Growth Inhibition Assay | IC50=15 ± 2 nM | 23824064 | ||
| Hth83 | Growth Inhibition Assay | IC50=34 ± 5 nM | 23824064 | ||
| C643 | Growth Inhibition Assay | IC50=71 ± 10 nM | 23824064 | ||
| SW1736 | Growth Inhibition Assay | IC50=35 ± 8 nM | 23824064 | ||
| T241 | Growth Inhibition Assay | IC50=65 ± 7 nM | 23824064 | ||
| T351 | Growth Inhibition Assay | IC50=50 ± 10 nM | 23824064 | ||
| BHP2-7 | Growth Inhibition Assay | IC50=37 ± 6 nM | 23824064 | ||
| T238 | Growth Inhibition Assay | IC50=1,500 ± 200 nM | 23824064 | ||
| S2 | Function assay | Inhibition of Plasmodium falciparum HDAC1 expressed in Drosophila melanogaster S2 cells, IC50 = 0.0018 μM. | 19317450 | ||
| HEK293 | Function assay | Inhibition of HDAC3 (unknown origin) expressed in HEK293 cells using [3H]acetylated human histone H4 peptide as substrate by scintillation counting, IC50 = 0.0021 μM. | 22344701 | ||
| HEK293 | Function assay | Inhibition of HDAC1 (unknown origin) expressed in HEK293 cells using [3H]acetylated human histone H4 peptide as substrate by scintillation counting, IC50 = 0.0025 μM. | 22344701 | ||
| HEK293 | Function assay | Inhibition of HDAC6 (unknown origin) expressed in HEK293 cells using [3H]acetylated human histone H4 peptide as substrate by scintillation counting, IC50 = 0.011 μM. | 22344701 | ||
| SF21 | Function assay | Inhibition of flag-tagged HDAC2 (unknown origin) expressed in SF21 cells using [3H]acetylated human histone H4 peptide as substrate by scintillation counting, IC50 = 0.013 μM. | 22344701 | ||
| HEK293 | Function assay | Inhibition of HDAC4 (unknown origin) expressed in HEK293 cells using [3H]acetylated human histone H4 peptide as substrate by scintillation counting, IC50 = 0.2 μM. | 22344701 | ||
| SF9 | Function assay | Inhibition of his-strep-tagged HDAC8 (unknown origin) expressed in SF9 cells using [3H]acetylated human histone H4 peptide as substrate by scintillation counting, IC50 = 0.28 μM. | 22344701 | ||
| HeLa | Function assay | Inhibition of HDAC in human HeLa cells using Fluor de Lys as substrate by fluorescence assay, IC50 = 0.03 μM. | 23639537 | ||
| Sf9 | Function assay | Inhibition of C-terminal His-tagged and C-terminal FLAG-tagged full length human recombinant HDAC1 expressed in baculovirus coexpressed in fall armyworm Sf9 cells using carboxyfluorescein (FAM)-labeled acetylated/ trifluoroacetylated peptide as substrate , IC50 = 0.001 μM. | 27377864 | ||
| Sf9 | Function assay | Inhibition of N-terminal GST-tagged and C-terminal His-tagged human recombinant HDAC4 (627 to 1084 residues ) expressed in baculovirus coexpressed in fall armyworm Sf9 cells using carboxyfluorescein (FAM)-labeled acetylated/ trifluoroacetylated peptide as, IC50 = 0.373 μM. | 27377864 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Panobinostat (LBH589, NVP-LBH589)是一种新型的，广谱HDAC抑制剂，无细胞试验中IC50为5 nM。Panobinostat (LBH589) 可诱导自噬和凋亡。Panobinostat 可以有效地破坏体内 HIV 的潜伏期。Phase 3。 | ||||
|---|---|---|---|---|---|
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | LBH589诱导MOLT-4和Reh细胞凋亡，这种作用具有时间和剂量依赖性。而且，LBH589作用于MOLT-4细胞比作用于Reh细胞更有效。LBH589明显阻止MOLT-4 和Reh细胞的生长，处理48小时，具有剂量依赖性。与对照组细胞相比，用LBH589处理的细胞，在细胞周期的G2/M期的细胞数量增多2到3倍。LBH589与组蛋白H3K9和H4K8的乙酰化作用相关，LBH589也降低c-Myc的表达水平，具有剂量依赖性。LBH589也增强p21的表达水平。最低剂量的LBH589（10 nM）处理Reh细胞，最初增强c-Myc的表达水平，之后一直降低c-Myc的表达水平。此外，LBH589促进mRNA水平的促凋亡和DNA修复基因的大量增多。在GADD45G启动子作用下，LBH589诱导乙酰化的组蛋白H3 和H4水平的增多。[1]此外, LBH589抑制非小细胞肺癌细胞系生长，如人类H1299,L55和A549，IC50分别为5,11和30 nM；间皮瘤细胞生长，如人类OK-6和 Ok-5，IC50分别为5和7 nM；及小细胞肺癌细胞系生长，如人类RG-1和LD-T，IC50分别为4和5 nM。[2] | |||
|---|---|---|---|---|
| 细胞实验 | 细胞系 | MOLT-4细胞和Reh(前体B细胞) | ||
| 浓度 | 50 nM | |||
| 孵育时间 | 48小时 | |||
| 方法 | 没有处理的细胞和LBH589处理的细胞[人类急性成淋巴细胞性白血病MOLT-4(T 细胞)和Reh(前体-B细胞)]用膜联蛋白V和碘化丙啶染色，然后加入膜联蛋白V-FITC细胞凋亡检测试剂盒I。通过流式细胞仪测定细胞凋亡和不能存活细胞的百分比。用CyAn ADP Violet细胞计数器收集至少5×104个细胞。根据所有的膜联蛋白V-阳性和膜联蛋白V/PI-阳性细胞细胞计算凋亡百分比，根据所有的膜联蛋白V-阳性和PI-阳性及膜联蛋白V/PI-阳性细胞计算细胞活力丢失百分比。 | |||
| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | DNMT1 / EZH2 caspase-8 / cleaved caspase-8 / Sp1 c-Myc / IRF4 Ac-H3 / cleaved caspase-3 / CCND1 / ID1 / ID2 / ID3 / ID4 / Synaptophysin / NeuroD1 RAD51 / BRCA1 / CHK1 / RPL13a H3K9AC / H3K18AC / H3K56AC / H3 / H4K8AC / H4K16AC / H4 / p21 / p27 / cleaved PARP |
|
19279403 | |
| Immunofluorescence | Synaptophysin / NACM α-tubulin / Acetyl-α-tubulin BiP ATF4 IRE1α / S724-IRE1α |
|
28915627 | |
| Growth inhibition assay | Cell viability |
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27738323 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | LBH589作用于患肺癌和间皮瘤动物模型,明显降低肿瘤生长，与对照组相比平均降低62%。LBH589作用于免疫活性鼠和严重联合免疫缺陷鼠效果差不多，说明LBH589抑制肿瘤生长与免疫学无关。LBH589按20 mg/kg剂量腹腔注射，每周持续5天，导致在实验最后肿瘤生长平均下降70%。与相应的对照组肿瘤相比，LBH589作用于H526衍生的肿瘤下降53%，作用于BK-T衍生的肿瘤下降81%, 作用于RG-1衍生的肿瘤下降76%，作用于H69衍生的肿瘤下降 70%。在相同条件和剂量的情况下，LBH589 作用于NSCLC和Meso衍生的移植瘤，导致SCLC衍生的肿瘤中有两种衰退，伴随着BK-T衍生的平均肿瘤尺寸从实验开始时的296 mm3降低到实验结束时的116 mm3，RG-1衍生的平均肿瘤尺寸从实验开始时的185mm3降低到实验结束时的86 mm3。[2] | |
|---|---|---|
| 动物实验 | Animal Models | 携带10×106个M30细胞或5×106个A549细胞的SCID鼠 |
| Dosages | 10 mg/kg, 20 mg/kg | |
| Administration | 腹腔注射 | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT04341311 | Terminated | Diffuse Intrinsic Pontine Glioma|Pediatric Brainstem Glioma|Pediatric Brainstem Gliosarcoma Recurrent|Pediatric Cancer|Pediatric Brain Tumor|Diffuse Glioma |
Dana-Farber Cancer Institute|Celgene|Secura Bio Inc. |
August 10 2020 | Phase 1 |
| NCT03632317 | Withdrawn | Glioma|Diffuse Intrinsic Pontine Glioma |
University of Michigan Rogel Cancer Center |
October 2019 | Phase 2 |
| NCT03982134 | Withdrawn | Melanoma|Non Small Cell Lung Cancer |
Muhammad Furqan|Novartis Pharmaceuticals|University of Iowa |
September 2019 | Phase 1 |
| NCT04326764 | Terminated | Acute Myeloid Leukaemia (AML)|Myelodysplastic Syndromes (MDS) |
Goethe University|Stichting Hemato-Oncologie voor Volwassenen Nederland|Polish Adult Leukemia Group|Schweizerische Arbeitsgemeinschaft für klinische Krebsforschung |
July 24 2018 | Phase 3 |
| NCT03515915 | Unknown status | Patients With Recurrent or Refractory Multiple Myeloma |
University Hospital Montpellier|Poitiers University Hospital |
April 23 2018 | -- |
化学信息&溶解度
| 分子量 | 349.43 | 分子式 | C21H23N3O2 |
| CAS号 | 404950-80-7 | SDF | Download Panobinostat (LBH589) SDF |
| Smiles | CC1=C(C2=CC=CC=C2N1)CCNCC3=CC=C(C=C3)C=CC(=O)NO | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 69 mg/mL ( (197.46 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : Insoluble Ethanol : Insoluble |
摩尔浓度计算器 |
|
体内溶解配方 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | |||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
技术支持
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如果有其他问题，请给我们留言。
* 必填项
常见问题及建议解决方法
问题 1:
How to reconstitute the compound for in vivo mice study?
回答：
We recommend the vehicle is 2 % DMSO, 2 % Tween 80, 48%PEG300, 48% water. The compound is first dissolved in DMSO, then add Tween, PEG300, water in sequence.
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