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Catalog No.
Product Name
Application
Product Information
Product Citation
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HDAC inhibitor
Belinostat (PXD101) is a HDAC inhibitor that inhibits HDAC activity in HeLa cell extracts with an IC50 of 27 nM.- Shariful Islam, .et al. , Blood Adv, 2020, 4(20): 5297-5310 PMID: 33108458
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HDAC inhibitor
Droxinostat is a selective inhibitor of HDAC3, HDAC6, and HDAC8 that shows comparable inhibition of HDAC6 and HDAC8 with IC50 = 2.47 and 1.46 μmol/L, respectively. -
HDAC inhibitor
ITF2357 (Givinostat) is a HDACs inhibitor with potential anti-inflammatory, anti-angiogenic, and antineoplastic activities.- Flavien Bizot, .et al. , Mol Ther Nucleic Acids, 2022, Nov 21;30:606-620 PMID: 36514350
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HDAC Inhibitor
LBH589 is a hydroxamic acid and acts as a non-selective HDAC inhibitor with IC5o of HDAC1 to be 0.23 nM.- Jalila Chagraoui, .et al. , Cell Stem Cell, 2021, Jan 7;28(1):48-62.e6 PMID: 33417871
- Gils Jose, .et al. , Cancers (Basel), 2020, Oct 31;12(11):E3211 PMID: 33142721
- Shariful Islam, .et al. , Blood Adv, 2020, 4(20): 5297-5310 PMID: 33108458
- Giovanni Bocci, .et al. , ACS Pharmacol Transl Sci, 2020, Oct 14
- Justin Kale, .et al. , EMBO Rep, 2018, Sep; 19(9): e45235 PMID: 29987135
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HDAC Inhibitor
MC1568 is a member of HDAC inhibitors that inhibits the histone deacetylase class II by modifying the genetic expression of various important genes of cell cycle mostly at G1 phase, resulting in the death of breast cancer cells by apoptosis.- Vivek Bora, .et al. , Can J Physiol Pharmacol, 2021, 6 October
- Minoru Ueda, .et al. , Plant Physiol, 2017, Dec; 175(4): 1760-1773 PMID: 29018096
- S Ishikawa, .et al. , Int J Cancer., 2014, 135(11): 2528-2536 PMID: 24346863
- Usui T, .et al. , Hypertension., 2014, Feb;63(2):397-403 PMID: 24166750
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HDAC Inhibitor
MGCD0103 (Mocetinostat) is a benzamide histone deacetylase inhibitor by inhibiting mainly histone deacetylase 1 (HDAC1), but also HDAC2, HDAC3, and HDAC11.- Mari Ishigami-Yuasa, .et al. , Biol Pharm Bull, 2019, 42, 448-452 PMID: 30828077
- Guang Bai, .et al. , Epigenetics of Chronic Pain, 2019, Pages 1-48
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HDAC inhibitor
MS-275 (Entinostat) is a potent HDAC inhibitor with IC50 of 0.3 and 8uM for HDAC1 and HDAC3, respectively.- Vivek Bora, .et al. , Can J Physiol Pharmacol, 2021, 6 October
- Taito Kashio, .et al. , Tissue Barriers, 2021, May 6;1911195 PMID: 33955828
- Ting-Yu Chang, .et al. , Biomed Pharmacother, 2021, Jun;138:111485 PMID: 33740521
- Arshdeep Singh, .et al. , Eur J Med Chem, 2021, Apr 5;215:113169 PMID: 33588178
- Minoru Ueda, .et al. , Plant Physiol, 2017, Dec; 175(4): 1760-1773 PMID: 29018096
- Parthenolide ((-)-Parthenolide) is a sesquiterpene lactone which occurs naturally in the plant feverfew (Tanacetum parthenium).
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HDAC Inhibitor
PCI-24781 is a broad-spectrum phenyl hydroxamic acid HDAC inhibitor.- Kazuya Tsumagari, .et al. , Biochem Biophys Res Commun, 2021, Jul 23;563:60-65 PMID: 34062387
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HDAC Inhibitor
Pyroxamide (NSC 696085) is a potent inhibitor of affinity-purified HDAC1 and causes the accumulation of acetylated core histones in MEL cells cultured with the agent. -
HDAC inhibitor
SB939 is an oral inhibitor of HDAC, selective for class I, II and IV HDACs and displays an IC50 value of 77 nM in an in vitro HDAC1 activity assay.- Giovanni Bocci, .et al. , ACS Pharmacol Transl Sci, 2020, Oct 14
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HDAC inhibitor
Sodium butyrate (NaB, Butanoic acid sodium salt), sodium salt of butyric acid, is a histone deacetylase inhibitor and competitively binds to the zinc sites of class I and II histone deacetylases (HDACs). -
HDAC inhibitor
Valproic acid sodium salt (Sodium Valproate) is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. -
HDAC inhibitor
Vorinostat is an inhibitor of HDACs, inhibiting deacetylation and leading to an accumulation of both hyperacetylated histones and transcription factors.- Amy E Neely, .et al. , Commun Biol, 2023, Jun 23;6(1):664 PMID: 37353594
- Ting-Yu Chang, .et al. , Biomed Pharmacother, 2021, Jun;138:111485 PMID: 33740521
- David Diaz-Carballo, .et al. , Commun Biol, 2021, Mar 3;4(1):276 PMID: 33658617
- Arshdeep Singh, .et al. , Eur J Med Chem, 2021, Apr 5;215:113169 PMID: 33588178
- Shariful Islam, .et al. , Blood Adv, 2020, 4(20): 5297-5310 PMID: 33108458
- Giovanni Bocci, .et al. , ACS Pharmacol Transl Sci, 2020, Oct 14
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HDAC inhibitor
AR-42 is a novel HDAC inhibitor, exhibits biologic activity against malignant mast cell lines via down-regulation of constitutively activated Kit.- Yong-Hui Liao, .et al. , Mol Med Rep, 2018, Feb; 17(2): 2803-2810 PMID: 29257262
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HDAC6 inhibitor
Tubastatin A is a potent and selective HDAC6 inhibitor with IC50 of 15 nM in a cell-free assay. It is selective against all the other isozymes (1000-fold) except HDAC8 (57-fold).- Isin Cakir, .et al. , Nat Metab, 2022, Jan;4(1):44-59 PMID: 35039672
- Isin Cakir, .et al. , Elife, 2022, Mar 24 PMID: 35323110
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PI3K/HDAC inhibitor
CUDC-907 (Fimepinostat) is a single small molecule inhibitor that targets both PI3K and HDAC. CUDC-907 is more efficacious than either a single PI3K or HDAC inhibitor reference compound or a combination of the two single agents at maximally tolerated doses.- Caner Gunaydın, .et al. , Immunopharmacol Immunotoxicol, 2022, Jun;44(3):447-455 PMID: 35291899
- Chie Ishikawa, .et al. , Eur J Haematol, 2020, Eur J Haematol PMID: 32780889
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IKK inhibitor
BMS 345541 is a cell-permeable and highly selective IKB kinase (IKK) inhibitor that binds at allosteric site of the enzyme and blocks NF-kB-dependent transcription in mice. -
IκB/IKK inhibitor
Bardoxolone methyl is an orally-available first-in-class synthetic triterpenoid. It is an inducer of the Nrf2 pathway, which can suppress oxidative stress and inflammation.- Nakamura S, .et al. , Invest Ophthalmol Vis Sci, 2019, 60: 1943-1952 PMID: 31050722
- Hisamichi M, .et al. , Hypertens Res, 2018, Jan;41(1):8-17 PMID: 28978980
- Takahiko Imai, .et al. , Neurobiol Dis, 2016, May;89:136-46 PMID: 26850917
- Takagi T, .et al. , Free Radic Biol Med, 2014, 72:124-33 PMID: 24746614
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IKK-2 inhibitor
TPCA-1 is a potent and selective inhibitor of human IκB kinase-2 (IKK-2) with IC50 = 17.9 nM for IKK-2 compared to 400nm for IKK-1. -
HDAC inhibitor
Romidepsin strongly inhibits HDAC1 and HDAC2 with IC5N/A of 1.6 nM and 3.9 nM, respectively, but is relatively weak in inhibiting HDAC4 and HDAC6 with IC5N/A 25 nM and 79N/A nM, respectively.- Yu-Fang Liu, .et al. , J Biochem Mol Toxicol, 2022, Jun;36(6):e23044 PMID: 35499365
- David Diaz-Carballo, .et al. , Commun Biol, 2021, Mar 3;4(1):276 PMID: 33658617
- Eva Hesping, .et al. , Int J Parasitol Drugs Drug Resist, 2020, 14: 249-256
- Shariful Islam, .et al. , Blood Adv, 2020, 4(20): 5297-5310 PMID: 33108458
- Elena Netchiporouk, .et al. , Oncotarget, 2017, Nov 10; 8(56): 95981-95998 PMID: 29221181
- Ivan V. Litvinov, .et al. , Clin Cancer Res, 2014, 20(14): 3799-3808 PMID: 24850846
- Ivan V Litvinov, .et al. , Cell Cycle., 2014, 15; 13(18): 2975-2982 PMID: 25486484
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HDAC6 inhibitor
ACY-1215 selectively targets and binds to HDAC6, thereby disrupting the Hsp90 protein chaperone system through hyperacetylation of Hsp90 and preventing the subsequent aggresomal protein degradation. -
E2 ubiquitin conjugating enzyme inhibitor
Bay 11-7821 is an irreversible inhibitor of TNF-α-stimulated IκBα phosphorylation.- Ali Nasrollahzadeh, .et al. , Rep Biochem Mol Biol, 2022, Jan;10(4):602-613 PMID: 35291620
- Ali Nasrollahzadeh, .et al. , Life Sci, 2020, Jul 6;257:118060 PMID: 32645343
- Momeny M, .et al. , Int J Biochem Cell Biol, 2018, Jun;99:1-9 PMID: 29567488
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HDAC Inhibitor
CI-994 is a histone deacetylase (HDAC) inhibitor and induces histone hyperacetylation in living cells. -
IκB/IKK inhibitor
BAY 11-7085 is an irreversible inhibitor of TNFα-induced IκBα phosphorylation with IC50 of 10 μM- Byungki Jang, .et al. , Int J Mol Sci, 2017, Nov; 18(11): 2258 PMID: 29077055
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IKK2/IKK1 inhibitor
BMS-345541 is a highly selective inhibitor of the catalytic subunits of IKK-2 and IKK-1 with IC50 of 0.3 μM and 4 μM -
HDAC4 inhibitor
Tasquinimod is an orally active antiangiogenic agent by allosterically inhibiting HDAC4 signalling. -
NF-κB inhibitor
QNZ inhibits the activation of the transcription factor NF-κB and has been used to investigate NF-κB signaling. -
IKK Inhibitor
IKK 16 is a selective IκB kinase (IKK) inhibitor for IKK-2, IKK complex and IKK-1 with IC50 of 40 nM, 70 nM and 200 nM, respectively.- Rulina AV, .et al. , Cell Death Dis, 2016, Dec 1;7(12):e2505 PMID: 27906189
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IKK Inhibitor
IMD 0354 is an inhibitor of IκB kinase-β (IKKβ) that blocks NF-κB nuclear translocation.- Anton Lennikov, .et al. , Angiogenesis, 2018, 21(2): 267-285 PMID: 29332242
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HDAC inhibitor
RG2833 ( is a brain-penetrant HDAC inhibitor with IC50 of 60 nM and 50 nM for HDAC1 and HDAC3. -
HDAC3 inhibitor
RGFP966 is an HDAC3 inhibitor with IC50 of 0.08 μM, exhibits > 200-fold selectivity over other HDAC.- Vijaya Bharti, .et al. , Cell Rep, 2022, Dec 20;41(12):111826 PMID: 36543138
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NF-κB activation inhibitor
Caffeic acid phenethyl ester is a potent and specific inhibitor of NF-κB activation -
HDAC6 inhibitor
Nexturastat A is an aryl urea derivative that acts as a potent and highly selective inhibitor of histone deacetylase 6 (HDAC6) (IC50= 5.02 +/- 0.60 nM). -
NF-κB inhibitor
JSH 23 is an inhibitor of NF-kB, blocking its translocation into the nucleus (IC50 = 7.1 uM)- Yu N, .et al. , Radiat Res, 2018, Apr;189(4):409-417 PMID: 29420126
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NAD(+)-dependent histone deacetylase Sir2p inhibitor
Splitomicin is a selective NAD(+)-dependent histone deacetylase Sir2p inhibitor with IC50 of 60 uM, showing a higher activity in a cell-based assay. -
HDAC inhibitor
Santacruzamate A (CAY10683) is a potent and selective HDAC inhibitor with IC50 of 119 pM for HDAC2, >3600-fold selectivity over other HDACs.