AR-42 | HDAC-42 | Pan HDAC Inhibitor | AmBeed-信号通路专用抑制剂

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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-B, IC50: 7.5 nM HD1-A, IC50: 16 nM	+++ HD2, IC50: 10 nM														99%+
MC1568	++ HD1-B (Maize), IC50: 3.4 μM HD1-A (Maize), IC50: 100 nM															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			✔												NF-κB,Nrf2	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				✔											NF-κB,p53	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	HDAC HDAC, IC50:30 nM
描述	AR-42 (HDAC-42; OSU-HDAC42) is a potent, orally bioavailable pan-HDAC inhibitor (IC50=16 nM). It causes growth inhibition, cell-cycle arrest, apoptosis, and activates caspases-3/7. AR-42 also leads to hyperacetylation of H3, H4, and alpha-tubulin, and up-regulation of p21. It exhibits cytotoxic effects against a variety of human cancer cell lines^[1]^[2].
体内研究	AR-42 (10 mg/kg; administered via tail vein injection; twice weekly for three weeks) markedly suppresses tumor progression^[4].
体外研究	AR-42 (0.125-1 μM; 24 hours) inhibits cell proliferation in a dose-dependent manner. The median IC50 values for P815, C2, and BR cells are 0.65, 0.30, and 0.23 μM, respectively^[3]. AR-42 (0.5 μM; 24 hours) triggers cell-cycle arrest at the G1 phase in P815 cells and at the G1/G2 phases in C2 cells^[3]. AR-42 (0.13-1 μM; 24 hours) induces apoptosis in P815, C2, and BR cells in a dose-dependent manner^[3]. AR-42 (0.5-3 μM; 24 hours) triggers increased acetylation levels of histones H3 and H4 as well as α-tubulin^[3].
作用机制	AR-42 is a phenylbutyrate-derived inhibitor which can chelate the Zn²⁺ ion.^[1]

Cell Line Ben-Men-1 cells Normal meningeal cells SW780 cells HT1376 cells THP-1 cells Mouse embryonic fibroblasts MOLM13 cells Kasumi-1 cells Kasumi-1, NB4, and FDC-P1-KITmut cells	Concentration	Treated Time	Description	References
Ben-Men-1 cells	1 µM	2 days	AR-42 inhibited the proliferation of Ben-Men-1 cells by increasing the expression of p16INK4A, p21CIP1/WAF1, and p27KIP1, and induced G2/M cell cycle arrest.	Cancer Res. 2013 Jan 15;73(2):792-803.
Normal meningeal cells	1 µM	2 days	AR-42 inhibited the proliferation of normal meningeal cells by increasing the expression of p16INK4A, p21CIP1/WAF1, and p27KIP1, and induced G1 cell cycle arrest.	Cancer Res. 2013 Jan 15;73(2):792-803.
SW780 cells	5 µM	24 hours	The combination of AR-42 and cisplatin synergistically destroyed bladder cancer cells via apoptosis.	J Urol. 2015 Aug;194(2):547-55.
HT1376 cells	5 µM	24 hours	The combination of AR-42 and cisplatin synergistically destroyed bladder cancer cells via apoptosis.	J Urol. 2015 Aug;194(2):547-55.
THP-1 cells	2 µM	24 hours	To evaluate the effect of AR-42 on miR-199b expression in THP-1 cells, results showed that AR-42 significantly elevated miR-199b expression.	Exp Hematol Oncol. 2016 Feb 3;5:4.
Mouse embryonic fibroblasts	5 µM	24 hours	H3K4me3 reporter activity was reduced in Kmt2d+/βGeo cells but normalized after AR-42 treatment	Sci Transl Med. 2014 Oct 1;6(256):256ra135.
MOLM13 cells	0.1 µM	48 hours	AR-42 and KPT-9274 co-treatment significantly reduced the survival of MOLM13 cells, showing synergistic effects.	Clin Cancer Res. 2021 Apr 15;27(8):2352-2366.
Kasumi-1 cells	0.1 µM	48 hours	AR-42 and KPT-9274 co-treatment significantly reduced the survival of Kasumi-1 cells, showing synergistic effects.	Clin Cancer Res. 2021 Apr 15;27(8):2352-2366.
Kasumi-1, NB4, and FDC-P1-KITmut cells	0.3 µM to 1 µM	72 hours or 48 hours	To assess the effects of AR-42 on cell proliferation and miR-29b expression.	Leukemia. 2013 Apr;27(4):871-8.

Species CD2F1 mice Kmt2d+/βGeo mice NCG mice SCID C.B17 mice NSG mice Mice Mice	Animal Model C-26 tumor model Mouse model of Kabuki syndrome MOLM13 xenograft model Intracranial xenograft model Subcutaneous xenograft model C-26 colon adenocarcinoma and LLC models Mll4 mutant mouse models	Administration	Dosage	Frequency	Description	References
CD2F1 mice	C-26 tumor model	Oral gavage	10 mg/kg	Once daily for 13 days	To evaluate the anti-cachectic effects of AR-42, results showed that AR-42 significantly improved body weight, hindlimb muscle mass, and grip strength in the C-26 model.	EMBO Mol Med. 2020 Feb 7;12(2):e9910
Kmt2d+/βGeo mice	Mouse model of Kabuki syndrome	Oral	10 mg/kg/day	Daily for 14 days	AR-42 treatment improved H3K4me3 deficiency and hippocampal memory defects in Kmt2d+/βGeo mice	Sci Transl Med. 2014 Oct 1;6(256):256ra135.
NCG mice	MOLM13 xenograft model	Oral gavage	20 mg/kg	Every other day, continued treatment	AR-42 and KPT-9274 combination therapy significantly prolonged the survival of MOLM13 xenograft mice and reduced leukemic cell infiltration.	Clin Cancer Res. 2021 Apr 15;27(8):2352-2366.
SCID C.B17 mice	Intracranial xenograft model	Oral	25mg/kg/day	Daily for 6 months	AR-42 significantly inhibited the growth of Ben-Men-1-LucB tumors, leading to tumor regression, and showed minimal regrowth after treatment cessation.	Cancer Res. 2013 Jan 15;73(2):792-803.
NSG mice	Subcutaneous xenograft model	Intraperitoneal injection	50 mg/kg	3 times per week for AR-42, once weekly for cisplatin, continued treatment	The combination of AR-42 and cisplatin significantly reduced tumor growth and size.	J Urol. 2015 Aug;194(2):547-55.
Mice	C-26 colon adenocarcinoma and LLC models	Oral	50 mg/kg	Every other day, 11 days	AR-42 significantly mitigated body weight loss and muscle atrophy, improved survival rates, and maintained muscle mass in tumor-bearing mice.	J Natl Cancer Inst. 2015 Oct 12;107(12):djv274
Mice	Mll4 mutant mouse models	Intraperitoneal injection	50 mg/kg	Daily, from 9 days post-conception until embryo harvest	AR-42 restored the expression of GHRH neurons in Mll4-deficient mice, partially repairing the developmental program of GHRH neurons	Nat Commun. 2021 Jan 11;12(1):256

Dose	Mice: 10 mg/kg^[2] (i.p.); 25 mg/kg^[3] (p.o., q.d.), 75 mg/kg^[4] (p.o.)
Administration	i.p., p.o.

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT01798901	Adult Acute Myeloid Leukemia W... 展开 >>ith 11q23 (MLL) Abnormalities Adult Acute Myeloid Leukemia With Del(5q) Adult Acute Myeloid Leukemia With Inv(16)(p13;q22) Adult Acute Myeloid Leukemia With t(15;17)(q22;q12) Adult Acute Myeloid Leukemia With t(16;16)(p13;q22) Adult Acute Myeloid Leukemia With t(8;21)(q22;q22) Recurrent Adult Acute Myeloid Leukemia Recurrent Childhood Acute Myeloid Leukemia Secondary Acute Myeloid Leukemia Untreated Adult Acute Myeloid Leukemia 收起 <<	Phase 1	Completed	-	United States, Ohio ... 展开 >> Cincinnati Children's Hospital Cincinnati, Ohio, United States, 45229 Nationwide Children's Hospital Columbus, Ohio, United States, 43205 Arthur G. James Cancer Hospital and Solove Research Institute at Ohio State University Medical Center Columbus, Ohio, United States, 43210 收起 <<
NCT01129193	Adult Nasal Type Extranodal NK... 展开 >>/T-cell Lymphoma Anaplastic Large Cell Lymphoma Angioimmunoblastic T-cell Lymphoma Cutaneous B-cell Non-Hodgkin Lymphoma Extranodal Marginal Zone B-cell Lymphoma of Mucosa-associated Lymphoid Tissue Hepatosplenic T-cell Lymphoma Intraocular Lymphoma Nodal Marginal Zone B-cell Lymphoma Peripheral T-cell Lymphoma Post-transplant Lymphoproliferative Disorder Prolymphocytic Leukemia Recurrent Adult Burkitt Lymphoma Recurrent Adult Diffuse Large Cell Lymphoma Recurrent Adult Diffuse Mixed Cell Lymphoma Recurrent Adult Diffuse Small Cleaved Cell Lymphoma Recurrent Adult Grade III Lymphomatoid Granulomatosis Recurrent Adult Hodgkin Lymphoma Recurrent Adult Immunoblastic Large Cell Lymphoma Recurrent Adult Lymphoblastic Lymphoma Recurrent Adult T-cell Leukemia/Lymphoma Recurrent Cutaneous T-cell Non-Hodgkin Lymphoma Recurrent Grade 1 Follicular Lymphoma Recurrent Grade 2 Follicular Lymphoma Recurrent Grade 3 Follicular Lymphoma Recurrent Mantle Cell Lymphoma Recurrent Marginal Zone Lymphoma Recurrent Mycosis Fungoides/Sezary Syndrome Recurrent Small Lymphocytic Lymphoma Refractory Chronic Lymphocytic Leukemia Refractory Multiple Myeloma Stage III Adult Burkitt Lymphoma Stage III Adult Diffuse Large Cell Lymphoma Stage III Adult Diffuse Mixed Cell Lymphoma Stage III Adult Diffuse Small Cleaved Cell Lymphoma Stage III Adult Hodgkin Lymphoma Stage III Adult Immunoblastic Large Cell Lymphoma Stage III Adult Lymphoblastic Lymphoma Stage III Adult T-cell Leukemia/Lymphoma Stage III Chronic Lymphocytic Leukemia Stage III Cutaneous T-cell Non-Hodgkin Lymphoma Stage III Grade 1 Follicular Lymphoma Stage III Grade 2 Follicular Lymphoma Stage III Grade 3 Follicular Lymphoma Stage III Mantle Cell Lymphoma Stage III Marginal Zone Lymphoma Stage III Multiple Myeloma Stage III Mycosis Fungoides/Sezary Syndrome Stage III Small Lymphocytic Lymphoma Stage IV Adult Burkitt Lymphoma Stage IV Adult Diffuse Large Cell Lymphoma Stage IV Adult Diffuse Mixed Cell Lymphoma Stage IV Adult Diffuse Small Cleaved Cell Lymphoma Stage IV Adult Hodgkin Lymphoma Stage IV Adult Immunoblastic Large Cell Lymphoma Stage IV Adult Lymphoblastic Lymphoma Stage IV Adult T-cell Leukemia/Lymphoma Stage IV Chronic Lymphocytic Leukemia Stage IV Cutaneous T-cell Non-Hodgkin Lymphoma Stage IV Grade 1 Follicular Lymphoma Stage IV Grade 2 Follicular Lymphoma Stage IV Grade 3 Follicular Lymphoma Stage IV Mantle Cell Lymphoma Stage IV Marginal Zone Lymphoma Stage IV Mycosis Fungoides/Sezary Syndrome Stage IV Small Lymphocytic Lymphoma Testicular Lymphoma Waldenstrom Macroglobulinemia 收起 <<	Phase 1	Completed	-	United States, Ohio ... 展开 >> The Ohio State University James Cancer Hospital Columbus, Ohio, United States, 43210 收起 <<
NCT02569320	Recurrent Plasma Cell Myeloma	Phase 1	Suspended(Internal data analys... 展开 >>is) 收起 <<	March 31, 2019	United States, Ohio ... 展开 >> Ohio State University Comprehensive Cancer Center Columbus, Ohio, United States, 43210 收起 <<

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CAS号	935881-37-1
分子式	C₁₈H₂₀N₂O₃
分子量	312.36
SMILES Code	O=C(NO)C1=CC=C(NC([C@H](C2=CC=CC=C2)C(C)C)=O)C=C1
MDL No.	MFCD17676151

别名	HDAC-42; OSU-HDAC42; OSU-42; NSC-736012; (S)-HDAC-42
运输	蓝冰
InChI Key	LAMIXXKAWNLXOC-INIZCTEOSA-N
Pubchem ID	6918848

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