HDAC5
HDAC5 (histone deacetylase 5) is a member of the class IIa histone deacetylase family and functions as a signal-responsive transcriptional regulator through its conserved N-terminal transcription factor-binding domain and C-terminal catalytic domain[1][2]. HDAC5 interacts with transcription factors such as myocyte enhancer factor 2 (MEF2), and phosphorylation-dependent binding to 14-3-3 proteins promotes its nuclear export, thereby relieving transcriptional repression of target genes[1][2]. Mechanistically, HDAC5 participates in chromatin-dependent gene regulation and integrates extracellular signaling pathways that control cellular differentiation, survival, and tissue-specific transcriptional programs[2][3]. These properties place HDAC5 within a broader class IIa HDAC regulatory network that functions primarily through transcriptional repression complexes rather than strong intrinsic deacetylase activity[2]. In disease-related settings, aberrant HDAC5 expression has been reported across multiple cancer types, where it is associated with regulation of cell proliferation, invasion, stemness maintenance, immune-related processes, and cell-cycle progression[1]. Experimental studies summarized in cancer models further indicate that HDAC5 can influence oncogenic pathways including DLL4, Notch1, c-Met, and Six1 signaling, supporting its relevance as a molecular regulator of tumor biology[1]. Compared with related HDAC isoforms, HDAC5 shares the characteristic class IIa adaptor architecture and signal-dependent nucleocytoplasmic shuttling mechanism, yet retains distinct tissue distribution patterns and target-gene regulatory functions that contribute to biological specificity[1][2]. For experimental applications, HDAC5 is widely investigated as a candidate therapeutic target, and ongoing efforts to develop class IIa-selective HDAC modulators aim to improve isoform selectivity while minimizing off-target effects associated with pan-HDAC inhibition[2][3].
References:
- [1]. Yang J, et al. Insights Into the Function and Clinical Application of HDAC5 in Cancer Management. Front Oncol. 2021 Jun 10;11:661620. [Content Brief]
- [2]. Park SY, et al. A short guide to histone deacetylases including recent progress on class II enzymes. Exp Mol Med. 2020 Feb;52(2):204-212. [Content Brief]
- [3]. Ujlaky-Nagy L, et al. Disrupting EGFR-HER2 Transactivation by Pertuzumab in HER2-Positive Cancer: Quantitative Analysis Reveals EGFR Signal Input as Potential Predictor of Therapeutic Outcome. Int J Mol Sci. 2024 May 29;25(11):5978. [Content Brief]
All Product Categories
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HDAC5 Related Products (56)
Related Products (56)
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HDAC8-IN-3
0 ImagesCat. No.: HY-147934CAS No.: 2432825-93-7
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HDAC6-IN-10
0 ImagesCat. No.: HY-150595CAS No.: 2408286-73-5HDAC6-IN-10 is a highly selective HDAC6 inhibitor with the IC50 of 0.73 nM. HDAC6-IN-10 has 144~10941-fold selectivity over other HDAC isoforms. HDAC6-IN-10 shows anti-proliferative activities against multiple myeloma cells.
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HDAC-IN-38
0 ImagesCat. No.: HY-146351CAS No.: 2408123-36-2HDAC-IN-38 (compound 13) is a potent HDAC inhibitor. HDAC-IN-38 shows similar micro-molar inhibitory activity toward HDAC1, 2, 3, 5, 6, and 8. HDAC-IN-38 increases cerebral blood flow (CBF), attenuates cognitive impairment, and improves hippocampal atrophy. HDAC-IN-38 also increases the level of histone acetylation (H3K14 or H4K5).
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MC2590
0 ImagesMC2590 is a potent pyridine-containing histone deacetylase (HDAC) inhibitor. MC2590 is a inhibitor of HDAC1-3, -6, -8, and -10 (class I/IIb-selective inhibitor) with IC50s of 0.015 μM-0.156 μM. MC2590 also inhibits HDAC isoforms HDAC4, HDAC5, HDAC7, HDAC9, HDAC11 with IC50s of 1.35 μM-3.98 μM. MC2625 induces G2/M cell cycle arrest and modulates pro- and anti-apoptotic microRNAs towards apoptosis induction.
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HDAC-IN-94
0 ImagesCat. No.: HY-179019HDAC-IN-94 is a potent, selective HDAC6 inhibitor (IC50 = 4.5 nM). HDAC-IN-94 shows >1000-fold selectivity over HDAC8 and shows minimal activity against other isoforms (HDAC1-3/10). HDAC-IN-94 induces α-tubulin hyperacetylation, apoptosis, and G2/M cell cycle arrest, exhibiting potent anti-tumor efficacy with low cytotoxicity. HDAC-IN-94 can be used for neuroblastoma and glioblastoma research.
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C1A
0 ImagesCat. No.: HY-124946CAS No.: 1021463-02-4
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Nanatinostat TFA
0 ImagesCat. No.: HY-13432ACAS No.: 1256448-48-2Synonyms: CHR-3996 TFANanatinostat (CHR-3996) TFA is a potent, class I selective and orally active HDAC inhibitor with IC50s of 3 nM, 4 nM, and 7 nM for HDAC1, HDAC2, and HDAC3, respectively. Nanatinostat TFA has low activity against HDAC5 (IC50 of 200 nM) and HDAC6 (IC50 of 2100 nM). Nanatinostat TFA induces apoptosis in myeloma cells. Nanatinostat TFA has potent anticancer effects, such as myeloma, advanced solid tumours and colorectal cancer.
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MC2625
0 ImagesCat. No.: HY-152225CAS No.: 1776116-75-6MC2625 is a potent pyridine-containing histone deacetylase (HDAC) inhibitor. MC2625 show selective HDAC3 and HDAC6 inhibition with IC50s of 80 nM and 11 nM. MC2625 increases acetyl-H3 and acetyl-tubulin levels and inhibits cancer stem cells (CSCs) growth by apoptosis induction.
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Rodin-C
0 ImagesCat. No.: HY-176868CAS No.: 2065162-16-3Rodin-C is a selective HDAC inhibitor with IC50s of 0.059, 0.18 and 5.39 μM for HDAC1, HDAC2 and HDAC11, respectively, over HDAC3-10. Rodin-C significantly inhibits the HDAC-CoREST complex with low hematological toxicity. Rodin-C can be used for neurologic disorders such as Alzheimer’s disease research.
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HDAC6-IN-61
0 ImagesCat. No.: HY-176733HDAC6-IN-61 (Compound 4e) is a HDAC6 inhibitor (IC50: 73 nM) with selectivity over other HDAC isoforms. HDAC6-IN-61 is also a GPR40 activator. HDAC6-IN-61 increases acetylated tubulin and ERK phosphorylation levels. HDAC6-IN-61 can be used for research of neuroinflammation such as Alzheimer's disease.
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PIM-1/HDAC-IN-2
0 ImagesCat. No.: HY-174302CAS No.: 3103925-33-0PIM-1/HDAC-IN-2 is a robust PIM/HDAC inhibitor (IC50 = 0.11 μM in MV4-11cells), which exerts a synergistic antiproliferative effect through a dual mechanism of inhibiting PIM1 kinase and selectively inhibiting HDAC6. PIM-1/HDAC-IN-2 induces cell apoptosis. PIM-1/HDAC-IN-2 remarkably induces the cleavage of PARP, thereby initiating the arrest of the cell cycle in G1 phase and a reduction in S phase. PIM-1/HDAC-IN-2 demonstrates significant anticancer efficacyin the MV4-11 xenograft model without notable toxicity[1].
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JAK/HDAC-IN-2
0 ImagesCat. No.: HY-149283CAS No.: 3029138-43-7JAK/HDAC-IN-2 is a potent 2-amino-4-phenylaminopyrimidine JAK/HDAC dual-target inhibitor. JAK/HDAC-IN-2 potently inhibits HDAC3/6 and JAK1/2 at nanomolar levels. JAK/HDAC-IN-2 has proapoptotic activity and inhibits histone deacetylation and STAT3 phosphorylation. JAK/HDAC-IN-2 presents remarkable antiproliferative activity in both hematological malignancies and solid cancers.
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ZG-126
0 ImagesCat. No.: HY-161778CAS No.: 3049802-32-3ZG-126 is an agonist for vitamin D receptor (VDR) and an inhibitor for histone deacetylase (HDAC) (IC50=0.63-67.6 μM). ZG-126 exhibits cytotoxicity in cancer cells MDA-MB-231 and 4T1. ZG-126 exhibits antitumor and anti-metastatic efficacy against melanoma and triple-negative breast cancer (TNBC) in mouse models. ZG-126 also exhibits anti-inflammatory activity, through the reduction of macrophage infiltration and immunosuppressive M2-polarization.
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Quisinostat hydrochloride
0 ImagesCat. No.: HY-15433BCAS No.: 1083078-98-1Synonyms: JNJ26481585 hydrochlorideQuisinostat (JNJ-26481585) hydrochloride is a potent and orally active pan-HDAC inhibitor (HDACi), with IC50 values ranging from 0.11 nM to 0.64 nM for HDAC1, HDAC2, HDAC4, HDAC10 and HDAC11. Quisinostat hydrochloride has a broad spectrum antitumoral activity. Quisinostat hydrochloride can induce autophagy in neuroblastoma cells.
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CM-444
0 ImagesCat. No.: HY-163803CAS No.: 2256079-52-2CM-444 is inhibitor for HDAC (IC50 is 6 nM-0.6 μM) and DNA methyltransferases (DNMT, IC50 is 1.8-2.3 μM). CM-444 is an inducer for the differentiation of acute myeloid leukemia cells. CM-444 exhibits anti-leukemic activity and improves the survival rate in mouse models.
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HDAC6-IN-74
0 ImagesCat. No.: HY-181579HDAC6-IN-74 is an orally active, selective histone deacetylase 6 (HDAC6) inhibitor with an IC50 of 0.036 μM. HDAC6-IN-74 induces tumor cell apoptosis, arrests cells at the S phase of the cell cycle, and impairs cell migration, invasion and colony-forming abilities. HDAC6-IN-74 exerts anticancer effects with no obvious toxicity. HDAC6-IN-74 can be used in the research of cancers such as liver cancer.
