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MedKoo Cat#: 200845 | Name: Dacinostat free base
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Dacinostat, also known as LAQ824, is a hydroxamate histone deacetylase inhibitor with potential anticancer activity. LAQ824 sensitized nonsmall cell lung cancer to the cytotoxic effects of ionizing radiation. LAQ824 reduced clonogenic survival of the H23 and H460 cell lines five-fold compared with controls and four-fold compared with either agent alone (P<0.001). In phase I trials, LAQ824 was well tolerated at doses that induced accumulation of histone acetylation, with higher doses inducing changes consistent with HSP90 inhibition.

Chemical Structure

Dacinostat free base
Dacinostat free base
CAS#404951-53-7 (free base)

Theoretical Analysis

MedKoo Cat#: 200845

Name: Dacinostat free base

CAS#: 404951-53-7 (free base)

Chemical Formula: C22H25N3O3

Exact Mass: 379.1896

Molecular Weight: 379.45

Elemental Analysis: C, 69.64; H, 6.64; N, 11.07; O, 12.65

Price and Availability

Size Price Availability Quantity
10mg USD 150.00 Ready to ship
25mg USD 250.00 Ready to ship
50mg USD 450.00 Ready to ship
100mg USD 750.00 Ready to ship
200mg USD 1,250.00 Ready to ship
500mg USD 2,650.00 Ready to ship
1g USD 3,650.00 Ready to ship
2g USD 6,450.00 Ready to ship
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Related CAS #
404951-53-7 (free base) 591207-53-3 (free base) Dacinostat HCl 927176-79-2 (TFA) 1347751-13-6 (lactate)
Synonym
NVP-LAQ824; NVP-LAQ 824; NVP-LAQ-824; LAQ-824; LAQ824; LAQ 824; Dacinostat.
IUPAC/Chemical Name
(2E)-N-hydroxy-3-[4-[[(2-hydroxyethyl)[2-(1H-indol-3-yl)ethyl]amino]methyl]phenyl]-2-propenamide
InChi Key
BWDQBBCUWLSASG-MDZDMXLPSA-N
InChi Code
InChI=1S/C22H25N3O3/c26-14-13-25(12-11-19-15-23-21-4-2-1-3-20(19)21)16-18-7-5-17(6-8-18)9-10-22(27)24-28/h1-10,15,23,26,28H,11-14,16H2,(H,24,27)/b10-9+
SMILES Code
O=C(NO)/C=C/C1=CC=C(CN(CCO)CCC2=CNC3=C2C=CC=C3)C=C1
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Custom
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
soluble in DMSO, not soluble in water.
Shelf Life
>5 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
NVP-LAQ824 inhibits histone deacetylase enzymatic activities in vitro and transcriptionally activated the p21 promoter in reporter gene assays. When tested on a variety of solid tumour cell lines, NVP-LAQ824 exhibited selective anti-proliferative effects, inducing cell growth inhibition in some, while inducing cell death in others. To induce cell death, a minimum of 16 h exposure to NVP-LAQ824 is required. Flow cytometry studies revealed that both tumour cell lines and normal diploid fibroblasts arrested in the G2/M phase of the cell cycle after compound treatment. However, an increased sub-G1 population at 48 h (reminiscent of apoptotic cells) was only observed in the cancer cell lines. Annexin V staining data confirmed that NVP-LAQ824 induced apoptosis in tumour cells, but not in normal cells. To relate HDAC inhibition to the anti-proliferative effects of NVP-LAQ824, expression of HDAC 1 was inhibited using antisense and this was sufficient to activate p21 expression, hypophosphorylate Rb and inhibit cell growth. Furthermore, tumour cells treated with NVP-LAQ824 caused acetylation of HSP90 and degradation of its cargo oncoproteins. Finally, NVP-LAQ824 exhibited antitumour effects in a xenograft animal model. To determine if NVP-LAQ824 inhibited histone deacetylases in vivo, tumours treated with the drug were immunoblotted with an antibody specific for acetylated histones H3 and H4 and the results indicated increased histone H3 and 114 acetylation levels in NVP-LAQ824 treated cancer cells. Together, our data indicated that the activity of NVP-LAQ824 was consistent with its intended mechanism of action. This novel HDAC inhibitor is currently in clinical trials as an anticancer agent. see: http://www.ncbi.nlm.nih.gov/pubmed/15171259.       
Biological target:
Dacinostat is a potent HDAC inhibitor, with an IC50 of 32 nM that also inhibits HDAC1 with an IC50 of 9 nM, and is used in cancer research.
In vitro activity:
It was determined whether the acquisition of inflammatory properties by LAQ824-treated macrophages renders these cells better activators of antigen-specific CD4+ T-cells. PEMs were therefore treated with LAQ824, LPS or a combination of LPS plus LAQ824 for 24 hours. Following this treatment, naïve CD4+ T-cells specific for a MHC Class II restricted epitope of influenza hemagglutinin (HA) were added to the PEM monolayer and stimulated, or not, with cognate HA-peptide. LAQ824-treated PEMs triggered an enhanced effector function of clonotypic CD4+ T cells, as determined by their capacity to produce higher levels of IFN-γ in response to cognate peptide (Figure 5A-bottom). LAQ824-treated PEMs effectively prime naïve antigen-specific CD4+ T-cells and restore the responsiveness of anergic CD4+ T-cells. As shown in Figure 5D, IL-10 blockade was insufficient to enhance the APC function of LPS-treated macrophages to augment IFN-γ production by CD4+ T-cells (Fig. 5D, LPS alone, black bar versus gray bar), nor was it able to significantly enhance the effect of LAQ824 treatment (Fig. 5D, LAQ+LPS, black bar versus gray bar). Taken together, these data point to a contributory role of IL-10 inhibition in the enhanced APC function displayed by LAQ824-treated macrophages since this effect was reversed when recombinant IL-10 was added-back to the cultures. Reference: J Immunol. 2011 Apr 1;186(7):3986-96. https://pubmed.ncbi.nlm.nih.gov/21368229/
In vivo activity:
It was determined whether the in vitro effects correlate with the in vivo activity of NVP-LAQ824 using an immunodeficient mouse model. Immunodeficient BNX mice were inoculated subcutaneously in the flank with 3 × 107 RPMI 8226 MM cells in 100 μL RPMI 1640 medium, together with 100 μL Matrigel. Subcutaneous tumors became palpable in 90% of mice within 3 days and in all mice within 8 days, allowing randomization of mice to either treatment with NVP-LAQ824 or normal saline control cohorts. The data were log-transformed and modeled as a simple linear growth curve. There was no significant difference in the baseline intercept between control and treated groups (P = .83). Daily intraperitoneal administration of NVP-LAQ824 (25 mg/kg) significantly reduced MM tumor growth (Figure 8A-B) and increased survival (Figure 8C), compared with the control group treated with normal saline vehicle only. No significant toxicity, as evidenced by lack of weight changes, was observed in any treatment groups. Taken together, these findings provide the framework for NVP-LAQ824 as a novel therapeutic in MM. Reference: Blood. 2003 Oct 1;102(7):2615-22. https://pubmed.ncbi.nlm.nih.gov/12816865/
Solvent mg/mL mM
Solubility
DMSO 56.0 147.58
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 379.45 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Fuino L, Bali P, Wittmann S, Donapaty S, Guo F, Yamaguchi H, Wang HG, Atadja P, Bhalla K. Histone deacetylase inhibitor LAQ824 down-regulates Her-2 and sensitizes human breast cancer cells to trastuzumab, taxotere, gemcitabine, and epothilone B. Mol Cancer Ther. 2003 Oct;2(10):971-84. PMID: 14578462. 2. Wang H, Cheng F, Woan K, Sahakian E, Merino O, Rock-Klotz J, Vicente-Suarez I, Pinilla-Ibarz J, Wright KL, Seto E, Bhalla K, Villagra A, Sotomayor EM. Histone deacetylase inhibitor LAQ824 augments inflammatory responses in macrophages through transcriptional regulation of IL-10. J Immunol. 2011 Apr 1;186(7):3986-96. doi: 10.4049/jimmunol.1001101. Epub 2011 Mar 2. PMID: 21368229; PMCID: PMC3998678. 3. . Catley L, Weisberg E, Tai YT, Atadja P, Remiszewski S, Hideshima T, Mitsiades N, Shringarpure R, LeBlanc R, Chauhan D, Munshi NC, Schlossman R, Richardson P, Griffin J, Anderson KC. NVP-LAQ824 is a potent novel histone deacetylase inhibitor with significant activity against multiple myeloma. Blood. 2003 Oct 1;102(7):2615-22. doi: 10.1182/blood-2003-01-0233. Epub 2003 Jun 19. PMID: 12816865 4. Leyton J, Alao JP, Da Costa M, Stavropoulou AV, Latigo JR, Perumal M, Pillai R, He Q, Atadja P, Lam EW, Workman P, Vigushin DM, Aboagye EO. In vivo biological activity of the histone deacetylase inhibitor LAQ824 is detectable with 3'-deoxy-3'[18F]fluorothymidine positron emission tomography. Cancer Res. 2006 Aug 1;66(15):7621-9. doi: 10.1158/0008-5472.CAN-05-3962. PMID: 16885362.
In vitro protocol:
1. Fuino L, Bali P, Wittmann S, Donapaty S, Guo F, Yamaguchi H, Wang HG, Atadja P, Bhalla K. Histone deacetylase inhibitor LAQ824 down-regulates Her-2 and sensitizes human breast cancer cells to trastuzumab, taxotere, gemcitabine, and epothilone B. Mol Cancer Ther. 2003 Oct;2(10):971-84. PMID: 14578462. 2. Wang H, Cheng F, Woan K, Sahakian E, Merino O, Rock-Klotz J, Vicente-Suarez I, Pinilla-Ibarz J, Wright KL, Seto E, Bhalla K, Villagra A, Sotomayor EM. Histone deacetylase inhibitor LAQ824 augments inflammatory responses in macrophages through transcriptional regulation of IL-10. J Immunol. 2011 Apr 1;186(7):3986-96. doi: 10.4049/jimmunol.1001101. Epub 2011 Mar 2. PMID: 21368229; PMCID: PMC3998678.
In vivo protocol:
1.. Catley L, Weisberg E, Tai YT, Atadja P, Remiszewski S, Hideshima T, Mitsiades N, Shringarpure R, LeBlanc R, Chauhan D, Munshi NC, Schlossman R, Richardson P, Griffin J, Anderson KC. NVP-LAQ824 is a potent novel histone deacetylase inhibitor with significant activity against multiple myeloma. Blood. 2003 Oct 1;102(7):2615-22. doi: 10.1182/blood-2003-01-0233. Epub 2003 Jun 19. PMID: 12816865 2. Leyton J, Alao JP, Da Costa M, Stavropoulou AV, Latigo JR, Perumal M, Pillai R, He Q, Atadja P, Lam EW, Workman P, Vigushin DM, Aboagye EO. In vivo biological activity of the histone deacetylase inhibitor LAQ824 is detectable with 3'-deoxy-3'[18F]fluorothymidine positron emission tomography. Cancer Res. 2006 Aug 1;66(15):7621-9. doi: 10.1158/0008-5472.CAN-05-3962. PMID: 16885362.
1: Lian B, Chen X, Shen K. Inhibition of histone deacetylases attenuates tumor progression and improves immunotherapy in breast cancer. Front Immunol. 2023 Mar 9;14:1164514. doi: 10.3389/fimmu.2023.1164514. PMID: 36969235; PMCID: PMC10034161. 2: Zheng J, Lu Y, Xiao J, Duan Y, Zong S, Chen X, Hu T, Li L, Zhang Y. Pan-HDAC inhibitors augment IL2-induced proliferation of NK cells via the JAK2-STAT5B signaling pathway. Int Immunopharmacol. 2023 Mar;116:109753. doi: 10.1016/j.intimp.2023.109753. Epub 2023 Feb 2. PMID: 36738675. 3: Spriano F, Sartori G, Tarantelli C, Barreca M, Golino G, Rinaldi A, Napoli S, Mascia M, Scalise L, Arribas AJ, Cascione L, Zucca E, Stathis A, Gaudio E, Bertoni F. Pharmacologic screen identifies active combinations with BET inhibitors and LRRK2 as a novel putative target in lymphoma. EJHaem. 2022 Jul 27;3(3):764-774. doi: 10.1002/jha2.535. PMID: 36051080; PMCID: PMC9422027. 4: Looi CK, Gan LL, Sim W, Hii LW, Chung FF, Leong CO, Lim WM, Mai CW. Histone Deacetylase Inhibitors Restore Cancer Cell Sensitivity towards T Lymphocytes Mediated Cytotoxicity in Pancreatic Cancer. Cancers (Basel). 2022 Jul 29;14(15):3709. doi: 10.3390/cancers14153709. PMID: 35954379; PMCID: PMC9367398. 5: Sun Y, Yan K, Wang Y, Xu C, Wang D, Zhou W, Guo S, Han Y, Tang L, Shao Y, Shan S, Zhang QC, Tang Y, Zhang L, Xi Q. Context-dependent tumor-suppressive BMP signaling in diffuse intrinsic pontine glioma regulates stemness through epigenetic regulation of CXXC5. Nat Cancer. 2022 Sep;3(9):1105-1122. doi: 10.1038/s43018-022-00408-8. Epub 2022 Aug 1. PMID: 35915262. 6: Liu F, Yu J, Zhang YX, Li F, Liu Q, Zhou Y, Huang S, Fang H, Xiao Z, Liao L, Xu J, Wu XY, Wu F. High-throughput tandem-microwell assay for ammonia repositions FDA-Approved drugs to inhibit Helicobacter pylori urease. FASEB J. 2021 Nov;35(11):e21967. doi: 10.1096/fj.202100465RR. PMID: 34613630. 7: Chu XY, Zhang CC, Zhang RX, Zhang JF, Xia B, Wu JW. Identification of Dacinostat as a potential anti-obesity compound through transcriptional activation of adipose thermogenesis in mice. Biochim Biophys Acta Mol Basis Dis. 2021 Sep 1;1867(9):166169. doi: 10.1016/j.bbadis.2021.166169. Epub 2021 May 15. PMID: 34000373. 8: Chaudhuri S, Fowler MJ, Baker C, Stopka SA, Regan MS, Sablatura L, Broughton CW, Knight BE, Stabenfeldt SE, Agar NYR, Sirianni RW. β-Cyclodextrin-poly (β-Amino Ester) Nanoparticles Are a Generalizable Strategy for High Loading and Sustained Release of HDAC Inhibitors. ACS Appl Mater Interfaces. 2021 May 12;13(18):20960-20973. doi: 10.1021/acsami.0c22587. Epub 2021 Apr 27. PMID: 33905245; PMCID: PMC8153536. 9: Cianferotti C, Faltoni V, Cini E, Ermini E, Migliorini F, Petricci E, Taddei M, Salvini L, Battistuzzi G, Milazzo FM, Anastasi AM, Chiapparino C, De Santis R, Giannini G. Antibody drug conjugates with hydroxamic acid cargos for histone deacetylase (HDAC) inhibition. Chem Commun (Camb). 2021 Jan 28;57(7):867-870. doi: 10.1039/d0cc06131j. PMID: 33433550. 10: Dushanan R, Weerasinghe S, Dissanayake DP, Senthilinithy R. Cracking a cancer code histone deacetylation in epigenetic: the implication from molecular dynamics simulations on efficacy assessment of histone deacetylase inhibitors. J Biomol Struct Dyn. 2022 Mar;40(5):2352-2368. doi: 10.1080/07391102.2020.1838328. Epub 2020 Nov 2. PMID: 33131428. 11: Rice CA, Colon BL, Chen E, Hull MV, Kyle DE. Discovery of repurposing drug candidates for the treatment of diseases caused by pathogenic free-living amoebae. PLoS Negl Trop Dis. 2020 Sep 24;14(9):e0008353. doi: 10.1371/journal.pntd.0008353. PMID: 32970675; PMCID: PMC7546510. 12: Zhang S, Gong Z, Oladimeji PO, Currier DG, Deng Q, Liu M, Chen T, Li Y. A high-throughput screening identifies histone deacetylase inhibitors as therapeutic agents against medulloblastoma. Exp Hematol Oncol. 2019 Nov 15;8:30. doi: 10.1186/s40164-019-0153-x. PMID: 31788346; PMCID: PMC6858705. 13: Mao Y, Zhou J, Liu X, Gu E, Zhang Z, Tao W. Comparison of Different Histone Deacetylase Inhibitors in Attenuating Inflammatory Pain in Rats. Pain Res Manag. 2019 Jan 27;2019:1648919. doi: 10.1155/2019/1648919. Erratum in: Pain Res Manag. 2021 May 24;2021:9760961. PMID: 30809320; PMCID: PMC6369477. 14: Samiec M, Skrzyszowska M. Intrinsic and extrinsic molecular determinants or modulators for epigenetic remodeling and reprogramming of somatic cell-derived genome in mammalian nuclear-transferred oocytes and resultant embryos. Pol J Vet Sci. 2018 Mar;21(1):217-227. doi: 10.24425/119040. PMID: 29624006. 15: Sixto-López Y, Bello M, Correa-Basurto J. Insights into structural features of HDAC1 and its selectivity inhibition elucidated by Molecular dynamic simulation and Molecular Docking. J Biomol Struct Dyn. 2019 Feb;37(3):584-610. doi: 10.1080/07391102.2018.1441072. Epub 2018 Mar 6. PMID: 29447615. 16: Garmpis N, Damaskos C, Garmpi A, Dimitroulis D, Spartalis E, Margonis GA, Schizas D, Deskou I, Doula C, Magkouti E, Andreatos N, Antoniou EA, Nonni A, Kontzoglou K, Mantas D. Targeting Histone Deacetylases in Malignant Melanoma: A Future Therapeutic Agent or Just Great Expectations? Anticancer Res. 2017 Oct;37(10):5355-5362. doi: 10.21873/anticanres.11961. PMID: 28982843. 17: Xu H, Roberts LR, Chou S, Pierce B, Narayanan A, Jones LH. Quantitative measurement of intracellular HDAC1/2 drug occupancy using a trans-cyclooctene largazole thiol probe. Medchemcomm. 2017 Jan 9;8(4):767-770. doi: 10.1039/c6md00633g. PMID: 30108795; PMCID: PMC6072125. 18: Mohseni J, Al-Najjar BO, Wahab HA, Zabidi-Hussin ZA, Sasongko TH. Transcript, methylation and molecular docking analyses of the effects of HDAC inhibitors, SAHA and Dacinostat, on SMN2 expression in fibroblasts of SMA patients. J Hum Genet. 2016 Sep;61(9):823-30. doi: 10.1038/jhg.2016.61. Epub 2016 Jun 2. PMID: 27251006. 19: Kopljar I, Gallacher DJ, De Bondt A, Cougnaud L, Vlaminckx E, Van den Wyngaert I, Lu HR. Functional and Transcriptional Characterization of Histone Deacetylase Inhibitor-Mediated Cardiac Adverse Effects in Human Induced Pluripotent Stem Cell-Derived Cardiomyocytes. Stem Cells Transl Med. 2016 May;5(5):602-12. doi: 10.5966/sctm.2015-0279. Epub 2016 Mar 31. PMID: 27034410; PMCID: PMC4835253. 20: Durlak M, Fugazza C, Elangovan S, Marini MG, Marongiu MF, Moi P, Fraietta I, Cappella P, Barbarani G, Font-Monclus I, Mauri M, Ottolenghi S, Gasparri F, Ronchi A. A Novel High-Content Immunofluorescence Assay as a Tool to Identify at the Single Cell Level γ-Globin Inducing Compounds. PLoS One. 2015 Oct 28;10(10):e0141083. doi: 10.1371/journal.pone.0141083. PMID: 26509275; PMCID: PMC4624791. 5: Ganai SA. Strategy for enhancing the therapeutic efficacy of histone deacetylase inhibitor dacinostat: the novel paradigm to tackle monotonous cancer chemoresistance. Arch Pharm Res. 2015 Oct 19. doi: 10.1007/s12272-015-0673-9. Epub ahead of print. PMID: 26481010. 6: Garmpis N, Damaskos C, Garmpi A, Dimitroulis D, Spartalis E, Margonis GA, Schizas D, Deskou I, Doula C, Magkouti E, Andreatos N, Antoniou EA, Nonni A, Kontzoglou K, Mantas D. Targeting Histone Deacetylases in Malignant Melanoma: A Future Therapeutic Agent or Just Great Expectations? Anticancer Res. 2017 Oct;37(10):5355-5362. doi: 10.21873/anticanres.11961. PMID: 28982843. 7: Samiec M, Skrzyszowska M. Intrinsic and extrinsic molecular determinants or modulators for epigenetic remodeling and reprogramming of somatic cell-derived genome in mammalian nuclear-transferred oocytes and resultant embryos. Pol J Vet Sci. 2018 Mar;21(1):217-227. doi: 10.24425/119040. PMID: 29624006. 8: Liu F, Yu J, Zhang YX, Li F, Liu Q, Zhou Y, Huang S, Fang H, Xiao Z, Liao L, Xu J, Wu XY, Wu F. High-throughput tandem-microwell assay for ammonia repositions FDA-Approved drugs to inhibit Helicobacter pylori urease. FASEB J. 2021 Nov;35(11):e21967. doi: 10.1096/fj.202100465RR. PMID: 34613630. 9: Lian B, Chen X, Shen K. Inhibition of histone deacetylases attenuates tumor progression and improves immunotherapy in breast cancer. Front Immunol. 2023 Mar 9;14:1164514. doi: 10.3389/fimmu.2023.1164514. PMID: 36969235; PMCID: PMC10034161. 10: Zhang S, Gong Z, Oladimeji PO, Currier DG, Deng Q, Liu M, Chen T, Li Y. A high-throughput screening identifies histone deacetylase inhibitors as therapeutic agents against medulloblastoma. Exp Hematol Oncol. 2019 Nov 15;8:30. doi: 10.1186/s40164-019-0153-x. PMID: 31788346; PMCID: PMC6858705. 11: Romanski A, Schwarz K, Keller M, Wietbrauk S, Vogel A, Roos J, Oancea C, Brill B, Krämer OH, Serve H, Ruthardt M, Bug G. Deacetylase inhibitors modulate proliferation and self-renewal properties of leukemic stem and progenitor cells. Cell Cycle. 2012 Sep 1;11(17):3219-26. doi: 10.4161/cc.21565. Epub 2012 Aug 16. PMID: 22895185; PMCID: PMC3466521. 12: Durlak M, Fugazza C, Elangovan S, Marini MG, Marongiu MF, Moi P, Fraietta I, Cappella P, Barbarani G, Font-Monclus I, Mauri M, Ottolenghi S, Gasparri F, Ronchi A. A Novel High-Content Immunofluorescence Assay as a Tool to Identify at the Single Cell Level γ-Globin Inducing Compounds. PLoS One. 2015 Oct 28;10(10):e0141083. doi: 10.1371/journal.pone.0141083. PMID: 26509275; PMCID: PMC4624791. 13: Cianferotti C, Faltoni V, Cini E, Ermini E, Migliorini F, Petricci E, Taddei M, Salvini L, Battistuzzi G, Milazzo FM, Anastasi AM, Chiapparino C, De Santis R, Giannini G. Antibody drug conjugates with hydroxamic acid cargos for histone deacetylase (HDAC) inhibition. Chem Commun (Camb). 2021 Jan 28;57(7):867-870. doi: 10.1039/d0cc06131j. PMID: 33433550. 14: Looi CK, Gan LL, Sim W, Hii LW, Chung FF, Leong CO, Lim WM, Mai CW. Histone Deacetylase Inhibitors Restore Cancer Cell Sensitivity towards T Lymphocytes Mediated Cytotoxicity in Pancreatic Cancer. Cancers (Basel). 2022 Jul 29;14(15):3709. doi: 10.3390/cancers14153709. PMID: 35954379; PMCID: PMC9367398. 15: Rice CA, Colon BL, Chen E, Hull MV, Kyle DE. Discovery of repurposing drug candidates for the treatment of diseases caused by pathogenic free-living amoebae. PLoS Negl Trop Dis. 2020 Sep 24;14(9):e0008353. doi: 10.1371/journal.pntd.0008353. PMID: 32970675; PMCID: PMC7546510. 16: Xu H, Roberts LR, Chou S, Pierce B, Narayanan A, Jones LH. Quantitative measurement of intracellular HDAC1/2 drug occupancy using a trans-cyclooctene largazole thiol probe. Medchemcomm. 2017 Jan 9;8(4):767-770. doi: 10.1039/c6md00633g. PMID: 30108795; PMCID: PMC6072125. 17: Shultz MD, Cao X, Chen CH, Cho YS, Davis NR, Eckman J, Fan J, Fekete A, Firestone B, Flynn J, Green J, Growney JD, Holmqvist M, Hsu M, Jansson D, Jiang L, Kwon P, Liu G, Lombardo F, Lu Q, Majumdar D, Meta C, Perez L, Pu M, Ramsey T, Remiszewski S, Skolnik S, Traebert M, Urban L, Uttamsingh V, Wang P, Whitebread S, Whitehead L, Yan-Neale Y, Yao YM, Zhou L, Atadja P. Optimization of the in vitro cardiac safety of hydroxamate-based histone deacetylase inhibitors. J Med Chem. 2011 Jul 14;54(13):4752-72. doi: 10.1021/jm200388e. Epub 2011 Jun 17. PMID: 21650221. 18: Mao Y, Zhou J, Liu X, Gu E, Zhang Z, Tao W. Comparison of Different Histone Deacetylase Inhibitors in Attenuating Inflammatory Pain in Rats. Pain Res Manag. 2019 Jan 27;2019:1648919. doi: 10.1155/2019/1648919. Erratum in: Pain Res Manag. 2021 May 24;2021:9760961. PMID: 30809320; PMCID: PMC6369477. 19: Kopljar I, Gallacher DJ, De Bondt A, Cougnaud L, Vlaminckx E, Van den Wyngaert I, Lu HR. Functional and Transcriptional Characterization of Histone Deacetylase Inhibitor-Mediated Cardiac Adverse Effects in Human Induced Pluripotent Stem Cell-Derived Cardiomyocytes. Stem Cells Transl Med. 2016 May;5(5):602-12. doi: 10.5966/sctm.2015-0279. Epub 2016 Mar 31. PMID: 27034410; PMCID: PMC4835253. 20: Zheng J, Lu Y, Xiao J, Duan Y, Zong S, Chen X, Hu T, Li L, Zhang Y. Pan-HDAC inhibitors augment IL2-induced proliferation of NK cells via the JAK2-STAT5B signaling pathway. Int Immunopharmacol. 2023 Mar;116:109753. doi: 10.1016/j.intimp.2023.109753. Epub 2023 Feb 2. PMID: 36738675.