Research Area
Product Type
United States ( Change Country )
PCI-24781 Chemical Structure
Recommended Products
LBH589 (Panobinostat)
LBH589 (Panobinostat) is a HDAC inhibitor, IC50 for inhibition of proliferation in MOLT-4 cells is approximately 5 μM and for Reh cells is approximately 20 μM.
Trichostatin A (TSA)
Inhibitor of HDAC, HDAC inhibitory activity of TSA was similar in all cell lines with mean ± SD IC50 of 2.4 ± 0.5 nm (range, 1.5–2.9 nm)
Vorinostat (SAHA)
Vorinostat also known as SAHA, Zolinza, MK-0683 is an HDAC inhibitor. Vorinostat CAS No 149647-78-9 with purity >99% & solubility DMSO is available.
MS-275 (Entinostat)
MS-275 (Entinostat) is a potent HDAC inhibitor with IC50 of 0.3 and 8µM for HDAC1 and HDAC3, respectively.
Belinostat (PXD101)
Belinostat also known as PXD101 is an HDAC inhibitor with IC50 of 27 nM.
LAQ824 (NVP-LAQ824)
LAQ824 (NVP-LAQ824) is an HDAC inhibitor with an IC50 of 0.032 μM.
JNJ-26481585
JNJ-26481585 is an orally bioavailable, second-generation, hydroxamic acid-based HDAC inhibitor with an IC50 of 2.43 nM for 5T33MMvt cells.
MGCD0103 (Mocetinostat)
MGCD0103 (Mocetinostat) is a potent HDAC inhibitor with IC50 of 0.15, 0.29 and 1.66 μM for HDAC 1, HDAC 2 and HDAC 3, respectively.
CUDC-101
CUDC-101 is a potent multitargeted HDAC, EGFR and HER2 inhibitor with IC50 of 4.4, 2.4, and 15.7 nM, respectively.
Droxinostat
Droxinostat is a selective inhibitor of HDAC3, HDAC6, and HDAC8 (IC50 at 16.9 ,2.47 and 1.46 μM, respectively).
Biological Activity
PCI-24781 (CRA-024781) is a novel broad spectrum hydroxamic acid-based inhibitor of histone deacetylase (HDAC) that shows antitumor activity in vitro and in vivo preclinically and is under evaluation in phase I clinical trials for cancer. [1,2,3,4]
PCI-24781 inhibited pure recombinant HDAC1 with a Ki of 0.007 Mmol/L, and also inhibited the other HDAC isozymes HDAC2, HDAC3/SMRT, HDAC6, HDAC8, and HDAC10 in the nanomolar range. [1]
Antitumor activity of PCI-24781 was observed in all 10 tumor cell lines tested, with GI50% values ranging from 0.15 to 3.09 μmol/L[1] .
CRA-024781 parenterally administered to mice harboring HCT116 or DLD-1 colon tumor xenografts resulted in a statistically significant reduction in tumor growth at doses that were well tolerated as measured by body weight[1] .
References on PCI-24781
- [1] Mol Cancer Ther 2006;5:1309-1317
- [2] Clin Cancer Res 2009 May 15;15(10): 3354–3365
- [3] Clin Cancer Res 2009;15:3472-3483
- [4] Clin Cancer Res 2007;13:6816-6826
Chemical Information
| Molecular Weight (WM): | 397.42 |
|---|---|
| Formula: | C21H23N3O5 |
| CAS No.: | 783355-60-2 |
| Synonyms: |
N/A
|
| Dissolve in (25°C): | DMSO ≥80mg/mL |
| Water <1mg/mL | |
| Ethanol <1mg/mL | |
| Storage: | 2 years-20°CPowder |
| 1 week-4°Cin DMSO | |
| 1 month-80°in DMSO |
Quality Control & MSDS
Research Area
Related Inhibitors
Recommended Screening Libraries
Chemical Library
A collection of 864 bioactive compounds
Inhibitor Library
A collection of 481 inhibitors
Kinase Inhibitor Library
A collection of 194 kinase inhibitors
Tyrosine Kinase Inhibitor Library
A collection of 85 tyrosine kinase inhibitors.
FDA Approved Drug Library
A collection of 426 FDA approved drugs
Natural Product Library
A collection of 139 natural products
Chemotherapeutic Agent Library
A collection of 40 chemotherapeutic agents
Epigenetics Compound library
A unique collection of 17 small molecule modulators
Stem Cell Compound library
A unique collection of 47 small molecule inhibitors
GPCR Compound library
A unique collection of 63 GPCR small molecules
Selleck's high quality products have been used in several published research findings, including the following:
Chemoproteomics profiling of HDAC inhibitors reveals selective targeting of HDAC complexes
We have 1 customer reviews of PCI-24781.
- (0)
- (1)
- (0)
- (0)
- (0)
- (0)
- (0)
- (0)
- (0)
Average Customer Review
(1 customer reviews)
-
Click to enlarge
Differential effects of HDAC inhibitors on histone and tubulin acetylation. Immunofluorescence analysis of histone H3 (K9ac/K14ac) and tubulin acetylation in HeLa cells treated for 4 h with vehicle, SAHA (10 μM), tacedinaline (50 μM), PCI-24781 (20 μM. (a) Mapping of histone acetylation in K562 cells treated with HDAC inhibitors by LC-MS/MS. Cells were treated with TSA (10 μM), SAHA (5 μM), PCI-24781 (2 μM), tacedinaline (50 μM) for 6 h. Histones were extracted from cells and acetylated peptides were quantified after isobaric tagging.
Differential effects of HDAC inhibitors on histone and tubulin acetylation. Immunofluorescence analysis of histone H3 (K9ac/K14ac) and tubulin acetylation in HeLa cells treated for 4 h with vehicle, SAHA (10 μM), tacedinaline (50 μM), PCI-24781 (20 μM. (a) Mapping of histone acetylation in K562 cells treated with HDAC inhibitors by LC-MS/MS. Cells were treated with TSA (10 μM), SAHA (5 μM), PCI-24781 (2 μM), tacedinaline (50 μM) for 6 h. Histones were extracted from cells and acetylated peptides were quantified after isobaric tagging.
Data from [Nature Biotechnology 2011.March;29:255-65] PCI-24781 purchased from Selleck
This product has been referenced in
Check our customer reviews
Differential effects of HDAC inhibitors on histone and tubulin acetylation. Immunofluorescence analysis of histone H3 (K9ac/K14ac) and tubulin acetylation in HeLa cells treated for 4 h with vehicle, SAHA (10 μM), tacedinaline (50 μM), PCI-24781 (20 μM. (a) Mapping of histone acetylation in K562 cells treated with HDAC inhibitors by LC-MS/MS. Cells were treated with TSA (10 μM), SAHA (5 μM), PCI-24781 (2 μM), tacedinaline (50 μM) for 6 h. Histones were extracted from cells and acetylated peptides were quantified after isobaric tagging. |
Data from [Nature Biotechnology 2011.March;29:255-65]
We give free samples and rewards to people who would like to provide us useful scientific data(western blot, etc.) > See Details
Recently Viewed Items
Keywords:buy PCI-24781 | PCI-24781 supplier | purchase PCI-24781 | PCI-24781 cost | PCI-24781 manufacturer | order PCI-24781 | PCI-24781 distributor