Pracinostat | SB939 | HDAC/MBLAC2 Inhibitor | AmBeed-信号通路专用抑制剂

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Inaccessible (Haz class 6.1), International	USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic	USD 100+
Accessible (Haz class 3, 4, 5 or 8), International	USD 200+

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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	HDAC8 HDAC8, IC50:140 nM HDAC10 HDAC10, IC50:40 nM HDAC3 HDAC3, IC50:43 nM HDAC4 HDAC4, IC50:56 nM
描述	HDACs are a group of enzymes that remove acetyl groups and regulate the histone tail, protein-DNA interaction, chromatin conformation, and even transcription. There are 18 mammalian HDACs divided into four classes: class I (HDACs 1, 2, 3, 8), class II (HDACs 4, 5, 6, 7, 9, 10), class III (sirtuin family: sirt1-sirt7) and class IV (HDAC 11)^[1]. Pracinostat (SB-939) is identified as a potent hydroxamate-based inhibitor of class I, II and IV HDACs, inhibiting the isolated enzymes with IC50 values of 43 to 140 nM, 40 to 137 nM (class II), and 93 nM (class IV) with the exception of HDAC6. Pracinostat is effective on cell proliferation of various kinds of human cancer cell lines, including T-cell lymphoma cells and leukemia cells with IC50 values ranging from 50 nM to 170 nM, colon and prostate cancer cell lines with IC50 values ranging from 340 to 540 nM. However, no inhibition of the proliferation of normal human dermal fibroblasts at concentrations up to 100 μM can be observed. Treatment of pracinostat >0.125 μM can induce ac-H3 and the acetylation of α-tubulin in HCT-116 cells after 24h. Meanwhile, pracinostat >0.25 μM leads to decreased retinoblastoma serine phosphorylation on S807/811 and an increase of the cyclin-dependant kinase inhibitor p21Cip/WAF. Echoed to that, the increase in cell cycle arrest goes hand in hand with a dose-dependent increase of PARP. In animal study, a single dose of either 50 or 125 mg/kg of pracinostat causes increased ac-H3 in the tumor tissue of HCT-116 xenografted nude mice. Oral treatment of pracinostat once a day for 21 days, on dose of 100 mg/kg, achieves 94% tumor growth inhibition. These results show the superior pharmacokinetic and pharmacodynamic properties of pracinostat in in vivo study^[2]. A phase 3 study of pracinostat in combination with azacitidine in adults with acute myeloid leukemia and a phase 2 study of pracinostat with azacitidine in patients with previously untreated myelodysplastic syndrome can be seen (https://www.cancer.gov/).
作用机制	Pracinostat is an hydroxamate-based HDAC inhibitor, structure of which can chelate Zn ion of HDACs.

Cell Line HT29 FaDu cells LU505 cells 32D murine myeloid cells HEL92.1.7 and SET-2 cells MV4-11 and MOLM-13 cells HCT116 HEK293 cells DLBCL cells FaDu cells A253 cells UMSCC11b cells NCI-H1299 BCR-DLBCL and OxPhos-DLBCL cells AML cells Human Neural Progenitor Cells (HNPCs)	Concentration	Treated Time	Description	References
HT29	0–2 µM	24 hours	Pracinostat increased the number of fragmented mitochondria.	J Pharm Anal. 2023 Oct;13(10):1168-1182.
FaDu cells	0.2 µM	15 days	Suppressed 3D spheroid growth of FaDu cells, significantly reducing spheroid volume when combined with X-ray irradiation	Cancers (Basel). 2024 Dec 7;16(23):4108.
LU505 cells	125 nM	21 days	Pracinostat treatment resulted in increased E-CADHERIN expression and global H3K27Ac levels.	Cancer Discov. 2018 Nov;8(11):1422-1437.
32D murine myeloid cells	125-500 nM	24 hours	Pracinostat treatment decreased both pJAK2 (Y1007/08) and pSTAT5 (Y694) levels, and also total JAK2 and STAT5 protein in JAK2V617F mutant cells.	Blood Cancer J. 2012 May;2(5):e69.
HEL92.1.7 and SET-2 cells	125-500 nM	24 hours	Pracinostat treatment decreased both pJAK2 (Y1007/08) and pSTAT5 (Y694) levels, and also total JAK2 and STAT5 protein in JAK2V617F mutant cells.	Blood Cancer J. 2012 May;2(5):e69.
MV4-11 and MOLM-13 cells	500 nM	24 hours	Pracinostat treatment nearly completely ablated pFLT3 (Y591), accompanied by a decrease in total FLT3 and pSTAT5.	Blood Cancer J. 2012 May;2(5):e69.
HCT116	1 µM	24 hours	Pracinostat significantly induced mitochondrial fragmentation in CRC cells, as evidenced by the elevated number of fragmented mitochondria, the decrease in tubular mitochondria and the ratio of rod/branch length.	J Pharm Anal. 2023 Oct;13(10):1168-1182.
HEK293 cells	1 µM	48 hours	Confirming the effect of Pracinostat on BDNF mRNA expression, it was shown to significantly increase BDNF mRNA levels	Int J Mol Sci. 2019 Mar 5;20(5):1109.
DLBCL cells	250 nM	6 hours or 72 hours	To evaluate the antiproliferative activity of Pracinostat on DLBCL cells, the results showed that Pracinostat exhibited robust activity across all lymphoma histotypes.	Blood Adv. 2021 May 25;5(10):2467-2480.
FaDu cells	1 µM	7-14 days	Enhanced radiosensitivity of FaDu cells, significantly inhibiting clonogenic survival	Cancers (Basel). 2024 Dec 7;16(23):4108.
A253 cells	1 µM	7-14 days	Enhanced radiosensitivity of A253 cells, significantly inhibiting clonogenic survival	Cancers (Basel). 2024 Dec 7;16(23):4108.
UMSCC11b cells	1 µM	7-14 days	Enhanced radiosensitivity of UMSCC11b cells, significantly inhibiting clonogenic survival	Cancers (Basel). 2024 Dec 7;16(23):4108.
NCI-H1299	500 nM	72 hours	To evaluate the effect of Pracinostat on NCI-H1299 cells, results showed that Pracinostat induced transcription of non-annotated transcription start sites (TINATs).	Nat Genet. 2017 Jul;49(7):1052-1060.
BCR-DLBCL and OxPhos-DLBCL cells	250 nM	72 hours	To evaluate the apoptosis induction effect of Pracinostat on BCR-DLBCL and OxPhos-DLBCL cells, the results showed marked apoptosis induction in BCR-DLBCLs, while the percentage of apoptotic cells in OxPhos-DLBCLs was lower.	Blood Adv. 2021 May 25;5(10):2467-2480.
AML cells	100 nM	96 hours	To evaluate the effect of Pracinostat on the growth of AML cells, results showed that Pracinostat inhibited the growth of AML cells	Blood Adv. 2022 Mar 22;6(6):1827-1843.
Human Neural Progenitor Cells (HNPCs)	1 µM		Screening for small compounds capable of modulating BDNF expression, Pracinostat was found to have a significant impact on BDNF expression	Int J Mol Sci. 2019 Mar 5;20(5):1109.

Species NOD-SCID mice Mice Mice BalB/c Nude mice Nude mice BALB/c nude mice Mice	Animal Model DLBCL xenograft model Rb1/Trp53/Crebbp-deficient SCLC model Neuroblastoma xenograft model A549 xenograft model CRC xenograft model MV4-11 xenograft model AML model	Administration	Dosage	Frequency	Description	References
NOD-SCID mice	DLBCL xenograft model	Oral gavage	100 mg/kg	Once daily, 5 days per week for 11 days	To evaluate the antilymphoma activity of Pracinostat in the DLBCL xenograft model, the results showed that Pracinostat significantly delayed tumor growth in the TMD8 model and remained effective throughout the experiment.	Blood Adv. 2021 May 25;5(10):2467-2480.
Mice	Rb1/Trp53/Crebbp-deficient SCLC model	Oral	100mg/kg	Daily, 5 days per week for 3 weeks	To evaluate the efficacy of Pracinostat in the Rb1/Trp53/Crebbp-deficient SCLC model, it was found that Pracinostat treatment significantly inhibited tumor growth, with some mice showing complete regression.	Cancer Discov. 2018 Nov;8(11):1422-1437.
Mice	Neuroblastoma xenograft model	Intraperitoneal injection	150 mg/kg	Once daily for 5 days	To evaluate the effect of Pracinostat on the neuroblastoma xenograft model, results showed that Pracinostat significantly increased transcription of LTR12C.	Nat Genet. 2017 Jul;49(7):1052-1060.
BalB/c Nude mice	A549 xenograft model	Intraperitoneal injection	20 mg/kg	Once daily for 21 days	To evaluate the antitumor efficacy of 3b in the A549 xenograft model, showing significant inhibition of tumor growth with negligible effect on mean body weight.	J Enzyme Inhib Med Chem. 2024 Dec;39(1):2318645
Nude mice	CRC xenograft model	Oral	25 mg/kg	Every two days	Pracinostat significantly suppressed the growth of CRC tumors with high CDK5 expression.	J Pharm Anal. 2023 Oct;13(10):1168-1182.
BALB/c nude mice	MV4-11 xenograft model	Oral	25 or 50 mg/kg	Daily for 21 days	Pracinostat significantly inhibited tumor growth (TGI), by 59% and 116%, respectively. Complete tumor regression was observed in 6 out of 10 animals at the end of the treatment after the 50-mg dose.	Blood Cancer J. 2012 May;2(5):e69.
Mice	AML model	Oral	50 nM		To evaluate the effect of Pracinostat on AML model mice, results showed that Pracinostat significantly suppressed the growth of AML cells	Blood Adv. 2022 Mar 22;6(6):1827-1843.

CAS号	929016-96-6
分子式	C₂₀H₃₀N₄O₂
分子量	358.48
SMILES Code	O=C(NO)/C=C/C1=CC=C2C(N=C(CCCC)N2CCN(CC)CC)=C1
MDL No.	MFCD17215206

别名	SB939
运输	蓝冰
InChI Key	JHDKZFFAIZKUCU-ZRDIBKRKSA-N
Pubchem ID	49855250

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HDAC8	HDAC8, IC50:140 nM
HDAC10	HDAC10, IC50:40 nM
HDAC3	HDAC3, IC50:43 nM
HDAC4	HDAC4, IC50:56 nM
HDAC6	HDAC6, IC50:1.008 μM
HDAC9	HDAC9, IC50:70 nM
HDAC11	HDAC11, IC50:93 nM
HDAC7	HDAC7, IC50:137 nM
HDAC5	HDAC5, IC50:47 nM
HDAC2	HDAC2, IC50:96 nM
HDAC1	HDAC1, IC50:49 nM

HCT116 cells	Proliferation assay	48 h	Antiproliferative activity against human HCT116 cells after 48 hrs by sulforhodamine B assay, GI50=0.24 μM	24119555
MCF7 cells	Proliferation assay	48 h	Antiproliferative activity against human MCF7 cells after 48 hrs by sulforhodamine B assay, GI50=0.17 μM	24119555
MDA-MB-435 cells	Proliferation assay	48 h	Antiproliferative activity against human MDA-MB-435 cells after 48 hrs by sulforhodamine B assay, GI50=0.48 μM	24119555
NCI-H460 cells	Proliferation assay	48 h	Antiproliferative activity against human NCI-H460 cells after 48 hrs by sulforhodamine B assay, GI50=0.22 μM	24119555
OVCAR5 cells	Proliferation assay	48 h	Antiproliferative activity against human OVCAR5 cells after 48 hrs by sulforhodamine B assay, GI50=0.61 μM	24119555

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