Abexinostat | 阿贝司他 | Pci-24781 | HDAC/MBLAC2 Inhibitor

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产品名称	HD1 ↓ ↑	HD2 ↓ ↑	HDAC ↓ ↑	HDAC1 ↓ ↑	HDAC10 ↓ ↑	HDAC11 ↓ ↑	HDAC2 ↓ ↑	HDAC3 ↓ ↑	HDAC4 ↓ ↑	HDAC5 ↓ ↑	HDAC6 ↓ ↑	HDAC7 ↓ ↑	HDAC8 ↓ ↑	HDAC9 ↓ ↑	其他靶点	纯度
Givinostat HCl monohydrate	++++ HD1-A, IC50: 16 nM HD1-B, IC50: 7.5 nM	+++ HD2, IC50: 10 nM														99%+
MC1568	++ HD1-A (Maize), IC50: 100 nM HD1-B (Maize), IC50: 3.4 μM															96%
Trichostatin A			++++ HDAC, IC50: ~1.8 nM													99%+
Scriptaid			✔													99%+
Valproic acid sodium			✔												Autophagy	97%
AR-42			+++ HDAC, IC50: 30 nM													99%+
Dacinostat			+++ HDAC, IC50: 32 nM													98+%
CUDC-101			++++ HDAC, IC50: 4.4 nM	++++ HDAC1, IC50: 4.5 nM	+++ HDAC10, IC50: 26.1 nM		+++ HDAC2, IC50: 12.6 nM	++++ HDAC3, IC50: 9.1 nM	+++ HDAC4, IC50: 13.2 nM	+++ HDAC5, IC50: 11.4 nM	++++ HDAC6, IC50: 5.1 nM	+ HDAC7, IC50: 373 nM	++ HDAC8, IC50: 79.8 nM	++ HDAC9, IC50: 67.2 nM	HER2,EGFR	99%+
M344			++ HDAC, IC50: 100 nM													99%+
Splitomicin			+ Sir2p, IC50: 60 μM													99%
Panobinostat			++++ HDAC (Reh cells), IC50: 20 nM HDAC (MOLT-4 cells), IC50: 5 nM													98%
Sodium 4-Phenylbutyrate			✔													98%
Vorinostat			+++ HDAC, IC50: ~10 nM													98%
Curcumin			✔												Nrf2,NF-κB	98%
Belinostat			+++ HDAC, IC50: 27 nM													98%
RG-2833				++ HDAC1, Ki: 32 nM				++ HDAC3, Ki: 5 nM								98%
Valproic acid				+ HDAC1, IC50: 0.4 mM												98%
BG45				+ HDAC1, IC50: 2 μM			+ HDAC2, IC50: 2.2 μM	+ HDAC3, IC50: 289 nM								99%+
Entinostat				+ HDAC1, IC50: 0.51 μM				+ HDAC3, IC50: 1.7 μM								98%
Resminostat				+++ HDAC1, IC50: 42.5 nM				++ HDAC3, IC50: 50.1 nM			++ HDAC6, IC50: 71.8 nM					98+%
Romidepsin				+++ HDAC1, IC50: 36 nM			+++ HDAC2, IC50: 47 nM									99%+
Parthenolide				✔											p53,NF-κB	97% HPLC
Tacedinaline				+ HDAC1, IC50: 0.9 μM			+ HDAC2, IC50: 0.9 μM	+ HDAC3, IC50: 1.2 μM								98%
Mocetinostat				++ HDAC1, IC50: 0.15 μM		+ HDAC11, IC50: 0.59 μM	+ HDAC2, IC50: 0.29 μM	+ HDAC3, IC50: 1.66 μM								98%
WT-161				++++ HDAC1, IC50: 8.35 nM			+++ HDAC2, IC50: 15.4 nM				++++ HDAC6, IC50: 0.4 nM					99%+
Fimepinostat				++++ HDAC1, IC50: 1.7 nM	++++ HDAC10, IC50: 2.8 nM	++++ HDAC11, IC50: 5.4 nM	++++ HDAC2, IC50: 5.0 nM	++++ HDAC3, IC50: 1.8 nM			+++ HDAC6, IC50: 27 nM					99%+
Tucidinostat				++ HDAC1, IC50: 95 nM	++ HDAC10, IC50: 78 nM		++ HDAC2, IC50: 160 nM	++ HDAC3, IC50: 67 nM								99%+
Santacruzamate A							++++ HDAC2, IC50: 119 pM									99%+
(E,E)-RGFP966								++ HDAC3, IC50: 80 nM								99%+
LMK-235									+++ HDAC4, IC50: 11.9 nM	++++ HDAC5, IC50: 4.2 nM						99%+
Tasquinimod									✔							99%+
CAY10603											++++ HDAC6, IC50: 2 pM					98%
Tubastatin A											+++ HDAC6, IC50: 15 nM					98%
Tubacin											++++ HDAC6, IC50: 4 nM					99%+
ACY-738											++++ HDAC6, IC50: 1.7 nM					99%+
Nexturastat A											++++ HDAC6, IC50: 5 nM					99%+
BRD73954											+++ HDAC6, IC50: 36 nM		++ HDAC8, IC50: 120 nM			99%
Tubastatin A HCl											+++ HDAC6, IC50: 15 nM		+ HDAC8, IC50: 854 nM			98%
PCI-34051													+++ HDAC8, IC50: 10 nM			99%+
Ricolinostat				++ HDAC1, IC50: 58 nM			++ HDAC2, IC50: 48 nM	++ HDAC3, IC50: 51 nM			++++ HDAC6, IC50: 4.7 nM		++ HDAC8, IC50: 100 nM			99%+
Droxinostat								+ HDAC3, IC50: 16.9 μM			+ HDAC6, IC50: 2.47 μM		+ HDAC8, IC50: 1.46 μM			99%+
Abexinostat				++++ HDAC1, Ki: 7 nM	+++ HDAC10, IC50: 24 nM		+++ HDAC2, Ki: 19 nM	++++ HDAC3/SMRT, Ki: 8.2 nM			+++ HDAC6, Ki: 17 nM		+ HDAC8, IC50: 280 nM			98%+
Citarinostat				+++ HDAC1, IC50: 35 nM			+++ HDAC2, IC50: 45 nM	+++ HDAC3, IC50: 46 nM			++++ HDAC6, IC50: 2.6 nM		++ HDAC8, IC50: 137 nM			99%+
HPOB				+ HDAC1, IC50: 2.9 μM	+ HDAC10, IC50: 3.0 μM		+ HDAC2, IC50: 4.4 μM	+ HDAC3, IC50: 1.7 μM			++ HDAC6, IC50: 56 nM		+ HDAC8, IC50: 2.8 μM			97%
Quisinostat 2HCl				++++ HDAC1, IC50: 0.11 nM	++++ HDAC10, IC50: 0.46 nM	++++ HDAC11, IC50: 0.37 nM	++++ HDAC2, IC50: 0.33 nM	++++ HDAC3, IC50: 4.86 nM	++++ HDAC4, IC50: 0.64 nM	++++ HDAC5, IC50: 3.69 nM			++++ HDAC8, IC50: 4.26 nM			97%
Domatinostat				+ HDAC1, IC50: 1.20 μM	+ HDAC10, IC50: 21 μM	+ HDAC11, IC50: 9.7 μM	+ HDAC2, IC50: 1.12 μM	+ HDAC3, IC50: 0.57 μM		+ HDAC5, IC50: 11.3 μM				+ HDAC9, IC50: 50 μM		99%+
TMP269									++ HDAC4, IC50: 157 nM	++ HDAC5, IC50: 97 nM		+++ HDAC7, IC50: 43 nM		+++ HDAC9, IC50: 23 nM		99%+
Pracinostat				++ HDAC1, IC50: 49 nM	+++ HDAC10, IC50: 40 nM	++ HDAC11, IC50: 93 nM	++ HDAC2, IC50: 96 nM	+++ HDAC3, IC50: 43 nM	++ HDAC4, IC50: 56 nM	+++ HDAC5, IC50: 47 nM	+ HDAC6, IC50: 1.008 μM	++ HDAC7, IC50: 137 nM	++ HDAC8, IC50: 140 nM	++ HDAC9, IC50: 70 nM		99%+
TMP195									++ HDAC4, Ki: 59 nM	++ HDAC5, Ki: 60 nM		+++ HDAC7, Ki: 26 nM		+++ HDAC9, Ki: 15 nM		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

靶点	HDAC8 HDAC8, IC50:280 nM HDAC10 HDAC10, IC50:24 nM HDAC3 HDAC3/SMRT, Ki:8.2 nM HDAC6 HDAC6, Ki:17 nM
描述	PCI-24781 is a novel hydroxamic acid–based pan-HDAC inhibitor with Ki values of 7nM, 19nM, 8.2nM, 17nM, 280nM and 24nM for HDAC1 HDAC2, HDAC3/SMRT, HDAC6, HDAC8 and HDAC10. Treatment with PCI-24781 at concentration ranging in 0.5-10μM resulted in the accumulation of acetylated histone and acetylated tubulin in a dose-dependent manner, accompanied with increase of p21, and resulted in an inhibition of tumor cell growth and the induction of apoptosis shown by increased γH2AX and cleaved PARP in HCT116, DLD-1 and HUVEC cells. Administration of PCI-24781 (i.v., formulated in 30% HP-cyclodextrin) to mice harboring HCT116 or DLD-1 colon tumor xenografts resulted in a statistically significant reduction in tumor growth. Inhibition of HDAC enzymes by PCI-24781 led to a significant reduction in the transcription of genes specifically associated with HR, including RAD51. RAD51 protein levels were significantly decreased after 24 h of drug exposure both in vitro and in vivo.
作用机制	PCI-24781 is a hydroxamic acid–based inhibitor which can chelate the Zn²⁺ of HDAC.^[1]

Cell Line Human CD34+ cells Human skeletal (mesenchymal) stem cells (hMSCs) HCT116 colon cancer cells MDA-MB-231 Ramos cells SUDHL4 cells HF1 cells L428 cells U87 U251 U-118MG DRAA8/CHO cells MDA-MB-231 MDA-MB-231	Concentration	Treated Time	Description	References
Human CD34+ cells	10 to 100 nM	24 hours	Abexinostat inhibited CFU-MK growth, megakaryocyte (MK) proliferation and differentiation. These effects required only a short incubation period.	Cell Death Dis. 2013 Jul 25;4(7):e738.
Human skeletal (mesenchymal) stem cells (hMSCs)	500 nM	24 hours	Abexinostat promoted adipocytic differentiation of hMSCs by inducing the expression of several proadipocytic genes and significantly increasing the enrichment of the H3K9Ac epigenetic mark on the promoter regions of AdipoQ, FABP4, PPARγ, KLF15, CEBPA, SP7, and ALPL.	Stem Cells Transl Med. 2016 Aug;5(8):1036-47.
HCT116 colon cancer cells	0.2 µM, 0.5 µM, 1.0 µM	24 hours	To measure the effect of PCI-24781 on RAD51 protein levels, results showed a significant decrease in RAD51 protein levels by 24 hours.	Proc Natl Acad Sci U S A. 2007 Dec 4;104(49):19482-7.
MDA-MB-231	30 µM	48 hours	To screen for epigenetic small molecule inhibitors with anti-tumor activity	Theranostics. 2021 Jan 1;11(5):2058-2076.
Ramos cells	0.5 µM to 2.0 µM	48 hours	PCI-24781 induced concentration-dependent apoptosis in Ramos cells with an IC50 of 0.5 μM	Clin Cancer Res. 2009 May 15;15(10):3354-65.
SUDHL4 cells	0.5 µM to 2.0 µM	48 hours	PCI-24781 induced concentration-dependent apoptosis in SUDHL4 cells with an IC50 of 0.8 μM	Clin Cancer Res. 2009 May 15;15(10):3354-65.
HF1 cells	0.5 µM to 2.0 µM	48 hours	PCI-24781 induced concentration-dependent apoptosis in HF1 cells with an IC50 of 0.9 μM	Clin Cancer Res. 2009 May 15;15(10):3354-65.
L428 cells	0.5 µM to 2.0 µM	48 hours	PCI-24781 induced concentration-dependent apoptosis in L428 cells with an IC50 of 1.4 μM	Clin Cancer Res. 2009 May 15;15(10):3354-65.
U87	0.5–1.25 µM	48 hours	To evaluate the inhibitory effect of PCI-24781 on GBM cell proliferation, results showed that PCI-24781 significantly inhibited the proliferation of U87 cells.	J Exp Clin Cancer Res. 2021 Oct 25;40(1):335.
U251	0.5–1.25 µM	48 hours	To evaluate the inhibitory effect of PCI-24781 on GBM cell proliferation, results showed that PCI-24781 significantly inhibited the proliferation of U251 cells.	J Exp Clin Cancer Res. 2021 Oct 25;40(1):335.
U-118MG	0.5–1.25 µM	48 hours	To evaluate the inhibitory effect of PCI-24781 on GBM cell proliferation, results showed that PCI-24781 significantly inhibited the proliferation of U-118MG cells.	J Exp Clin Cancer Res. 2021 Oct 25;40(1):335.
DRAA8/CHO cells	2.0 µM, 3.0 µM	6 hours	To determine the effect of PCI-24781 on homologous recombinational repair, results showed that 2.0 µM and 3.0 µM PCI-24781 reduced the recombination frequency to 0.27% and 0.16%, respectively.	Proc Natl Acad Sci U S A. 2007 Dec 4;104(49):19482-7.
MDA-MB-231	3 µM	72 hours	To screen for inhibitors that can kill cancer cells with high efficiency	Theranostics. 2021 Jan 1;11(5):2058-2076.
MDA-MB-231	0.3 µM and 0.15 µM	72 hours	To explore the most effective inhibitor at a low dose	Theranostics. 2021 Jan 1;11(5):2058-2076.

Species Mice BALB/c Nude mice Nude mice Rats	Animal Model GBM mouse model HCT116 colon cancer xenograft model MDA-MB-231 xenograft model Sprague-Dawley rats	Administration	Dosage	Frequency	Description	References
Mice	GBM mouse model	Oral	12.5 mg/kg	BID, 5 days a week for 4 weeks	To evaluate the inhibitory effect of PCI-24781 on GBM tumor growth in vivo, results showed that PCI-24781 significantly reduced tumor burden and increased survival.	J Exp Clin Cancer Res. 2021 Oct 25;40(1):335.
BALB/c Nude mice	HCT116 colon cancer xenograft model	Oral	200 mg/kg	1×, 2×, or 3× over 4, 22, and 28 hours, respectively	To examine the effect of PCI-24781 on RAD51 protein levels in tumors, results showed a 69% decrease in RAD51 protein levels after 3 doses over 28 hours.	Proc Natl Acad Sci U S A. 2007 Dec 4;104(49):19482-7.
Nude mice	MDA-MB-231 xenograft model	Intravenous injection	50 mg/kg	Every other day for four weeks	To evaluate the anti-tumor effect of PCI-24781 in vivo	Theranostics. 2021 Jan 1;11(5):2058-2076.
Rats	Sprague-Dawley rats	Oral	8.00 mg/kg	Single dose	To study the pharmacokinetic properties of Abexinostat in rats, the results showed that after oral administration, the absorption was rapid, the maximum plasma concentration (Cmax) was 28.20 ± 7.67 ng/mL, the time to peak (Tmax) was about 1.39 ± 1.29 h, and the half-life (t1/2) was 13.80 ± 2.50 h.	BMC Chem. 2024 Feb 20;18(1):37

CAS号	783355-60-2
分子式	C₂₁H₂₃N₃O₅
分子量	397.42
SMILES Code	O=C(C1=C(CN(C)C)C2=CC=CC=C2O1)NCCOC3=CC=C(C(NO)=O)C=C3
MDL No.	MFCD10565969

别名	阿贝司他 ;Pci-24781; CRA 024781; CRA-24781
运输	蓝冰
InChI Key	MAUCONCHVWBMHK-UHFFFAOYSA-N
Pubchem ID	11749858

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HDAC8	HDAC8, IC50:280 nM
HDAC10	HDAC10, IC50:24 nM
HDAC3	HDAC3/SMRT, Ki:8.2 nM
HDAC6	HDAC6, Ki:17 nM
HDAC2	HDAC2, Ki:19 nM
HDAC1	HDAC1, Ki:7 nM

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