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HDAC6 degrader-1 (Compound NP8) is the PROTAC degrader for HDAC6 with a DC50 of 3.8 nM in cell MM.1S .(Blue: ligand for E3 ligase Pomalidomide (HY-10984); Black: linker (HY-140213); Pink: ligand for target protein Nexturastat A (HY-16699))
HDAC6 degrader-3 is a potent and selective HDAC6 degrader via ternary complex formation and the ubiquitin-proteasome pathway with a DC50 value of 19.4 nM. HDAC6 degrader-3 has IC50s of 4.54 nM and 0.647 μM for HDAC6 and HDAC1, respectively. HDAC6 degrader-3 causes strong hyperacetylation of α-tubulin .
HDAC6 degrader-5 (Compound 6) exhibits inhibitory and degradation activity against HDAC6, with an IC50 of 4.95 nM and a DC50 of 0.96 nM. HDAC6 degrader-5 inhibits the release of TNF-α, IL-1β and IL-6, blocks the hepatocyte apoptosis. HDAC6 degrader-5 exhibits anti-inflammatory activity in mouse APAP (HY-66005)-induced liver injury models .
HDAC6-IN-3 (Compound 14), an antiprostate cancer agent, is a potent, orally active HDAC6 inhibitor with IC50s ranging from 0.02-1.54 μM for HDAC1/2/3/6/8/10. HDAC6-IN-3 is also an effective MAO-A (IC50=0.79 μM) and LSD1 inhibitor . HDAC6-IN-3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
HDAC6-IN-33 (compound 6) is a selective and irreversible HDAC6 inhibitor with an IC50 of 193 nM. HDAC6-IN-33 shows no activity against HDAC1-4. HDAC6-IN-33 is a tight-binding HDAC6 inhibitor capable of inhibiting HDAC6 via a two-step slow-binding mechanism .
HDAC6-IN-46 (compound 12) is a selective histone deacetylase 6(HDAC6) inhibitor with an IC50 value of 6.2 nM. HDAC6-IN-46 can be used in Alzheimer's disease research .
HDAC6/8/BRPF1-IN-1 is a dual inhibitor of both HDAC6/8 and the bromodomain and PHD finger containing protein 1 (BRPF1). HDAC6/8/BRPF1-IN-1 has inhibitory activity for HDAC1, HDAC6 and HDAC8 with IC50 values of 797 nM, 344 nM and 908 nM, respectively. HDAC6/8/BRPF1-IN-1 has inhibitory activity for BRPF1 with an Kd value of 175.2 nM. HDAC6/8/BRPF1-IN-1 can be used for the research of cancer .
HDAC6 degrader-4 is a PROTAC and a selective HDAC6 degrader consists of a non-selective HDAC inhibitor and thalidomide-type E3 ligase ligand. HDAC6 degrader-4 can be used for cancer research .
PROTAC HDAC6 degrader 9 is a selective HDAC6PROTAC degrader. PROTAC HDAC6 degrader 9 can be used for the research cancers related to HDAC6 abnormalities, such as multiple myeloma .
HDAC6 ligand-7 (Compound 16a) is a positron emission tomography (PET) tracer for the deacetylase 6(HDAC6) enzyme with a Kd value of 1.66 nM. HDAC6 ligand-7 exhibits excellent HDAC6 inhibitory activity, with IC50 values of 2.7 and 3.7 nM for hHDAC6 and mHDAC6, respectively, and has high selectivity for HDAC1/4/7/8. HDAC6 ligand-7 after being radioactively labeled with fluorine-18, [¹⁸F]HDAC6 ligand-7 shows varying degrees of radioactive uptake in PET, which can reflect the specific binding to HDAC6. HDAC6 ligand-7 can be used for the study of HDAC6 imaging .
PROTAC HDAC6 degrader 6 (Compound 12) is a selective HDAC6-targeting photochemically targeting chimeras (PHOTACs) (subset of PROTAC) degrader with a ∼50% Dmax only upon activation to its cis-state with 390 nm light irradiation . Pink: HDAC6 ligand; Blue: CRBN ligase ligand (HY-A0003); Black: linker
PROTAC HDAC6 degrader 7 is an orally active, highly efficient, and selective PROTAC degrader targeting histone deacetylase 6(HDAC6) (IC50 = 118 nM). PROTAC HDAC6 degrader 7 can eliminate both the catalytic and zinc-finger ubiquitin-binding domain. PROTAC HDAC6 degrader 7 inhibits NLRP3 inflammasome assembly and activation, as well as blocks NF-κB signaling, thereby reducing the transcription and release of key inflammatory factors. PROTAC HDAC6 degrader 7 can reduce the mRNA levels of NLRP3, pro-IL-1β, TNF-α, and IL-6. PROTAC HDAC6 degrader 7 can be used for the study of inflammatory bowel disease (IBD) .
HDAC6 ligand-linker conjugate 1 is a conjugate of HDAC6 ligand and linker, which can be used to synthesize PROTACs such as PROTAC HDAC6 degrader 5 (HY-174401) .
HDAC6-IN-27 (compound 8C) is a HDAC inhibitor with IC50 vales of 15.9 nM 136.5 nM and 6180.2 nM for HDAC6, HDAC8 and HDAC1, respectively. HDAC6-IN-27 shows potent antiparasitic effects .
HDAC6-IN-64 (Compound 8) is a HDAC6 inhibitor with an IC50 of 11.9 nM. HDAC6-IN-64 has poor cell permeability. HDAC6-IN-64 can be used for chemotherapy of cancers like NSCLC research .
HDAC6-IN-67 is a selective HDAC6 inhibitor (IC50 = 17.15 nM) that exhibits 19-fold selectivity over HDAC1. HDAC6-IN-67 selectively inhibits HDAC6 by interacting with Ser531 and His614. HDAC6-IN-67 induces apoptosis by inducing the cleavage of caspases 9, 8, 3, and PARP, upregulating Bax expression, and downregulating Bcl-2 expression. HDAC6-IN-67 effectively induces the acetylation of α-tubulin, without affecting histone H3 acetylation in MCF-7/ADR cells. HDAC6-IN-67 can be used for the study of breast cancer .
HDAC6-IN-65 is a selective HDAC6 inhibitor (IC50 = 0.9 nM) and also exhibits a certain suppressive effect on HDAC3 (IC50 = 39.4 nM). HDAC6-IN-65 can induce the accumulation of α-tubulin (ac-tubulin) and acetylated histone H3 (ac-histone H3, a class I HDAC inhibition marker) in Neuro-2a cells. HDAC6-IN-65 can be used for the study of melanoma .
HDAC6-IN-63 (Compound 7) is an orally active HDAC6 inhibitor with an IC50 of 145 nM. HDAC6-IN-63 inhibits the expression of Sp1 and RAD51, thereby inducing Caspase-dependent apoptosis. HDAC6-IN-63 has antitumor activity and sensitizes Etoposide (HY-13629) and Gemcitabine (HY-17026), promoting synergistic death of NSCLC cells through the inhibition of homologous recombination and non-homologous end joining (NHEJ) pathways involved in DNA DSB repair. HDAC6-IN-63 can be used for chemotherapy of cancers like NSCLC research .
HDAC6-IN-17 (compound 5b) is a potent HDAC6 inhibitor with IC50 values of 150 nM, 1400 nM, and 2300 nM for HDAC6, HDAC8, and HDAC4, respectively. HDAC6-IN-17 has cytotoxic activity on human cancer cell lines. HDAC6-IN-17 can be used in research of cancer .
HDAC6-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 .
HDAC6-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 .
Hdac6 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Hdac6 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
HDAC6 Human Pre-designed siRNA Set A contains three designed siRNAs for HDAC6 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
HDAC6 Rat Pre-designed siRNA Set A contains three designed siRNAs for HDAC6 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
HDAC6-IN-66 is a potent and selective histone deacetylase(HDAC) 6 inhibitor with an IC50 of 1.8 nM. HDAC6-IN-66 induces α-tubulin acetylation over histone H3. HDAC6-IN-66 can be used for the research of cancer .
HDAC6-IN-13 (Compound 35m) is a potent, highly selective, orally active HDAC6 inhibitor with an IC50 of 0.019 μM. HDAC6-IN-13 also inhibits HDAC1, HDAC2 and HDAC3 with IC50s of 1.53, 2.06 and 1.03 μM, respectively. HDAC6-IN-13 shows significant BBB permeability and anti-inflammatory activity .
HDAC6-IN-5 (compound 11b) is a potent and BBB-penetrated HDAC6 inhibitor, with an IC50 of 0.025 μM. HDAC6-IN-5 exhibits strong inhibitory activity against Aβ1-42 self-aggregation and AChE, with IC50 values of 3.0 and 0.72 μM. HDAC6-IN-5 can enhance neurite outgrowth without significant neurotoxicity .
HDAC6-IN-6 (compound 6a) is a potent and BBB-penetrated HDAC6 inhibitor, with an IC50 of 0.025 μM. HDAC6-IN-6 exhibits strong inhibitory activity against Aβ1-42 self-aggregation and AChE, with IC50 values of 3.0 and 0.72 μM. HDAC6-IN-6 can enhance neurite outgrowth without significant neurotoxicity .
HDAC6-IN-45 (Compound 15) is a selective inhibitor for HDAC6 with IC50 of 15.2 nM. HDAC6-IN-45 exhibits neurotrophic through the upregulation of GAP43 and Beta-3 tubulin markers. HDAC6-IN-45 activates the Nrf2 signaling pathway, reduces H2O2-induced ROS production, inhibits apoptosis in PC12, and exhibits neuroprotective efficacy in SCOP-induced zebrafish Alzheimer's Disease models. HDAC6-IN-45 exhibits antioxidant activity and good blood-brain barrier (BBB) permeability .
HDAC6/HSP90-IN-1 (compound 17) is a potent and selective dual inhibitor of HDAC6 and HSP90, with IC50 values of 4.3 and 46.8 nM, respectively. HDAC6/HSP90-IN-1 down-regulates PD-L1 expression in INF-γ treated H1975 lung cancer cells. HDAC6/HSP90-IN-1 inhibits tumor growth in human H1975 xenograft mice .
HDAC6-IN-60 (Compound 12) is an orally active and selective HDAC6 inhibitor. HDAC6-IN-60 exerts effects on tumor cell proliferation by inhibiting the enzymatic activity of HDAC6 and regulating pathways related to protein homeostasis. HDAC6-IN-60 is promising for research of HDAC6- related cancers .
HDAC6-IN-36 (compound 11d) is an inhibitor of HDAC6 with IC50 value of 8.64 nM. HDAC6-IN-36 induces neurite outgrowth of PC12 cells without producing toxic effects.
HDAC6-IN-59 (Compound 38k) is a highly selective histone deacetylase 6(HDAC6) inhibitor (IC50=3.12 nM, with 352-fold selectivity over HDAC1). HDAC6-IN-59 is promising for research of esophageal cancer .
HDAC6-IN-12 (compound GZ) is a potent HDAC6 inhibitor. HDAC6-IN-12 has anticancer activity through merges into DNA strands causing DNA damage. HDAC6-IN-12 can be used for cancer research .
HDAC6-IN-50 (Compound 4) is a potent HDAC6 inhibitor with an IC50 of 35 nM. HDAC6-IN-50 can be used for the study of Parkinson's disease (PD) and Alzheimer's disease (AD) research .
HDAC6-IN-31 (compound 8m) is a selective HDAC6 inhibitor, with the IC50 value of 0.026 μM, that significantly inhibits the production and release of pro-inflammatory cytokines. While HDAC6 is critically involved in the activation of inflammasomes, HDAC6-IN-31 has the potential to inhibit NLRP3 inflammasome-driven inflammatory diseases. HDAC6-IN-31 also inhibits glioblastoma cell migration .
HDAC6-IN-54 (Compound 9m) is a highly selective HDAC6 (histone deacetylase 6) inhibitor with an IC50 value of 0.021 μM. HDAC6-IN-54 blocks the activation of the NLRP3 inflammasome, which alleviates symptoms of NLRP3 inflammasome-related diseases such as acute peritonitis, inflammatory bowel disease, and psoriasis .
HDAC6-IN-28 (compound 10C) is a potent inhibitor of HDAC6 with an IC50 of 261 nM. HDAC6-IN-28 significantly induces apoptosis and S-phase arrest in B16-F10 cells. HDAC6-IN-28 efficiently increases the expression of acetylated-α-tubulin in vitro and in vivo .
HDAC6 ligand-Linker Conjugate 3 is a Target Protein Ligand-Linker Conjugate that incorporates a ligand for HDAC (HY-179422) and a PROTAC linker, which recruits E3 ligases. HDAC6 ligand-Linker Conjugate 3 can be used in the synthesis of PROTAC HDAC6 degrader 7 (HY-179421) .
HDAC6-IN-18 (Compound 4) is a first irreversible HDAC6 isoform selective inhibitor with potent anti-multiple myeloma activity. HDAC6-IN-18 has HDAC6 inhibitory activity in RPMI8266, U266 and MM.1S cells with IC50 values of 0.17, 0.7 and 0.42 μM, respectively .
HDAC6-IN-14 is a highly selective HDAC6 (HDAC) inhibitor with an IC50 of 42 nM. HDAC6-IN-14 displays >100-fold selectivity over HDAC1/HDAC2/HDAC3/HDAC4 .
HDAC6-IN-37 (compound W5) is an inhibitor of HDAC6 and has neuroprotective effects. HDAC6-IN-37 can restore the morphology of hippocampal neurons, reduce the expression of Aβ, Tau, and p-Tau proteins in the hippocampus of AD rats, and inhibit the formation of senile plaques and neurofibrillary tangles. Thus, HDAC6-IN-37 improves the Aβ/Cu 2+-induced AD model in rats, regulates oxidative stress status, and balances neurotransmitter disorders in brain tissue .
HDAC6/HSP90-IN-3 (Compound 17) is an orally active dual histone deacetylase 6(HDAC6) and heat shock protein 90 (HSP90) inhibitor with IC50 values of 28 nM and 0.88 μM, respectively. HDAC6/HSP90-IN-3 is promising for research of malignant tumors such as prostate cancer .
HDAC6-IN-15 is a selective histone deacetylase 6(HDAC6) inhibitor. HDAC6-IN-15 has potent inhibitory activity for HDAC6 with IC50 value of 38.2 nM. HDAC6-IN-15 can be used for the research of cancer and neurodegenerative diseases .
HDAC6-IN-32 (compound 25202) is a selective and potent inhibitor of HDAC6. HDAC6-IN-32 blocks HDAC6 activity and interferes with microtubule dynamics, leading to SAC activation and prolonged mitotic arrest, ultimately leading to apoptosis in CRPC cells .
HDAC6-IN-58 (compound 24c) is a selective HDAC6 inhibitor with IC50 values of 9.5 nM and 7374.5 nM for HDAC6 and HDAC1, respectively. HDAC6-IN-58 increases tubulin acetylation, exerts antiproliferative effects, and induces autophagy .
HDAC6-IN-43 (compound 26) is a potent HDAC inhibitor. HDAC6-IN-43 effectively inhibits several HDACs, notably HDAC1, HDAC2, and HDAC6 (IC50 < 150 nM), displaying a particularly high sensitivity towards HDAC6 (IC50 = 11 nM). HDAC6-IN-43 can be used for the research of autosomal dominant polycystic kidney disease (ADPKD) .
HDAC6-IN-41 (Compound E24) is a selective inhibitor for histone deacetylase 6(HDAC6), with IC50 of 14 and 422 nM, for HDAC6 and HDAC8, respectively. HDAC6-IN-41 upregulates the acetylation of α-tubulin and histone site SMC3 .
HDAC6-IN-22 (compound 30) is a inhibitor of HDAC6, with the IC50 of 4.63 nM. HDAC6-IN-22 has antiproliferative effects in vitro and in vivo towards multiple myeloma. HDAC6-IN-22
induces cell cycle arrest in the G2 phase and promotes apoptosis through the mitochondrial pathway .
HDAC6-IN-11 (Compound 9) is a selective HDAC6 inhibitor with the IC50 value of 20.7 nM. HDAC6-IN-11 has more than 300-fold selectivity over HDAC other isoforms. HDAC6-IN-11 shows anti-proliferative activities against cancer cells .
HDAC6-IN-42 (compound 2b) is an HDAC6 inhibitor (IC50=0.009 μM). HDAC6-IN-42 shows significant anti-leukemia activity and synergistic effect with Decitabine (HY-A0004). HDAC6-IN-42 can be used for the AML research .
HDAC6-IN-48 (compound 5i) is a potent and selective HDAC6 inhibitor with IC50 values of 5.16, 396.72, 638.08 nM for HDAC6, HDAC3, HDAC1, respectively. HDAC6-IN-48 induces apoptosis and cell cycle arrest at G0/G1 phase. HDAC6-IN-48 increases the protein expression of acetylated α-tubulin .
HDAC6-IN-44 (compound H10) is a selective HDAC6 inhibitor with an IC50 value of 8.97 nM. HDAC6-IN-44 can inhibit the idiopathic pulmonary fibrosis (IPF) phenotype and exhibits antifibrotic activity. Additionally, HDAC6-IN-44 reduces fibrogenesis in a bleomycin-induced pulmonary fibrosis mouse model and demonstrates good metabolic stability. HDAC6-IN-44 holds promise for research in the field of idiopathic pulmonary fibrosis .
HDAC6-IN-38 (Compound Z-7) is an inhibitor for histone deacetylase 6(HDAC6), with an IC50 of 3.25 nM. HDAC6-IN-38 inhibits proliferation of cells MGC 803 .
HDAC6-IN-62 (Compound 2.12) is a selective HDAC6 inhibitor, with an IC50 value of 0.25 nM. HDAC6-IN-62 can be used in the research of Charcot-Marie-Tooth disease .
HDAC6-IN-16 (compound 5c) is a histone deacetylase 6 (HDAC6) inhibitor, based on Quinazolin-4(3H)-One. HDAC6-IN-16 exhibits anticancer effect, inhibits colony-forming. And HDAC6-IN-16 arrests cell cycle at G2 phase and induces apoptosis .
HDAC6-IN-56 (compound 18d) is an inhibitor of HDAC6 with an IC50 of 1.3 nM. HDAC6-IN-56 suppresses S phase and induces apoptosis in HCT-116 colon cancer cells .
HDAC6-IN-29 (compound 11g), hydroxamic analogue, is a HDAC6 inhibitor. HDAC6-IN-29 has potent antiproliferative activity against CAL-51 cells (IC50 = 1.17 μM) and is able to induce apoptosis and cause accumulation of cells in the S phase of the cell cycle. HDAC6-IN-29 can be used for the research of cancer .
HDAC6-IN-4 (C10) is a potent, orally active and highly selective HDAC6 inhibitor with an IC50 value of 23 nM. HDAC6-IN-4 induces cancer cells apoptosis and shows significant antitumor efficacy, without obvious toxicity .
HDAC6-IN-19 (Compound 14g) is a HDAC6 inhibitor (IC50: 2.68 nM). HDAC6-IN-19 also inhibits HDAC1, HDAC2 and HDAC3 with IC50s of 61.6 nM, 98.7 nM and 103 nM. HDAC6-IN-19 potently inhibits multiple cancer cell proliferation, including leukemia, colon cancer, melanoma, and breast cancer cell lines .
HDAC6-IN-34 (compound 21) is an oral active and selective HDAC6 inhibitor with the IC50 of 18 nM. HDAC6-IN-34 increases the acetylation level of tubulin without affecting histone acetylation in cutaneous T-cell lymphoma cells and inhibits TNF-α secretion in LPS (HY-D1056)-stimulated macrophage cells. HDAC6-IN-34 shows excellent anti-arthritic efficacy in rat .
HDAC6-IN-35 (compound C4 (ZINC000077541942)) is a potent and BBB-penetrated HDAC6 inhibitor with the IC50 of 4.7 μM. HDAC6-IN-35 shows cell toxicity against MDA-MB-231 with EC50 of 40.6 μM .
HDAC6-IN-52 (EX.1) is a potent inhibitor of HDAC6, with the inhibitory rate of 100% at 10 μM. HDAC6-IN-52 plays an important role in central nervous system diseases including neurodegenerative diseases such as Alzheimer’s disease andprogressive supranuclear palsy .
HDAC6-IN-55 (Compound 15B) is a potent HDAC6 inhibitor and an effective anti-inflammatory agent. HDAC6-IN-55 alleviates atopic dermatitis through anti-inflammatory effects facilitated via TLR4/MAPK, STAT3 and NF-κB pathways. HDAC6-IN-55 alleviates symptoms such as skin edema, dryness, crusting, and peeling in 2,4-dinitrochlorobenzene (DNCB)-induced atopic dermatitis mice .
HDAC6-IN-49 (Compound 3) is an inhibitor for HDAC with IC50 of 0.012 and 0.735 μM for HDAC6 and HDAC1. HDAC6-IN-49 also exhibits inhibitory activities against MAO-B, cholinesterase (ChE), histamine receptor (H3R) and serotonin 6 receptor (5-HT6R). HDAC6-IN-49 exhibits neuroprotective efficacy on SH-SY5Y cell. HDAC6-IN-49 improves cognitive function and locomotor ability in Drosophila Parkinson's disease models and in C. elegans Alzheimer's disease models .
HDAC6-IN-53 (Compound W28) is an inhibitor targeting histone deacetylase 6 (HDAC6) with an IC50 of 19.65 nM. HDAC6-IN-53 exerts the activity of inhibiting the phenotype of idiopathic pulmonary fibrosis (IPF) by suppressing the collagen expression induced by TGF-β1, and it has demonstrated a good therapeutic effect in a mouse model of pulmonary fibrosis induced by Bleomycin (HY-17565A). HDAC6-IN-53 can be used in the research of idiopathic pulmonary fibrosis and other related pulmonary fibrosis diseases.
HDAC6-IN-47 (Compound S-29b) is inhibitor for HDAC, which exhibits high affinities to HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, HDAC10 with Ki of 60, 56, 162, 0.44, 362 and 849 nM, respectively. HDAC6-IN-47 causes tubulin hyperacetylation in MV4-11, inhibits the proliferation of MV4-11 with an EC50 of 0.50 µM. HDAC6-IN-47 can be used in research of leukemia .
HDAC6/HSP90-IN-2 (compound 6e) is a dual inhibitor of HDAC6 and Hsp90, with IC50s of 105.7 and 61 nM, respectively. HDAC6/HSP90-IN-2 can be used for the research of cancer .
A variety of compounds were designed and synthesized by modifying cap groups. The enzyme inhibition test showed that compound 12C had broad-spectrum enzyme inhibitory activity, and compounds 9m and 9q were more inclined to inhibit HDAC6, showing a certain selective inhibitory activity among the representative subtypes.
HDAC6-IN-69 is a brain-penetrant and highly selective HDAC6 inhibitor with an IC50 of 4.0 nM. HDAC6-IN-69 shows >176-fold against other HDAC isoforms. HDAC6-IN-69 engages the target in neuronal cells by dose-dependently upregulating acetylated α-tubulin in virto. HDAC6-IN-69 has neuroprotective effect and can be used for ischemic stroke research .
HDAC6-IN-72 is a HDAC6 zinc finger ubiquitin-binding domain (ZnF-UBD) inhibitor that inhibits the interaction between HDAC6 ZnF-UBD and ubiquitin with an IC50 of 2.7 μM. HDAC6-IN-72 can be used for the research of breast cancer, colorectal cancer, multiple myeloma .
HDAC6-IN-77 is a highly selective HDAC6 inhibitor with an IC50 of 7.0 nM.HDAC6-IN-77 induces neurite outgrowth.HDAC6-IN-77 exerts neuroprotective activity.HDAC6-IN-77 shows no significant toxicity on dopaminergic cells.HDAC6-IN-77 can be used for the research of Alzheimer's disease .
HDAC6-IN-82 is a selective HDAC6 inhibitor with an IC50 of 4.9 nM against HDAC6. HDAC6-IN-82 inhibits HDAC1 (112 nM), HDAC2 (737 nM), HDAC3 (623 nM), HDAC8 (1140 nM), HDAC10 (91.4 nM) and HDAC11 (219 nM). HDAC6-IN-82 reduces cancer cell viability, induces cell cycle arrest, triggers apoptosis, and increases the acetylation levels of H3K9 and α-tubulin. HDAC6-IN-82 can be used in cancer-related research such as leukemia .
HDAC6-IN-75 is a selective HDAC6 inhibitor with an IC50 of 0.17 nM against HDAC6. HDAC6-IN-75 induces the accumulation of acetylated α-tubulin in glioma cells. HDAC6-IN-75 triggers cell cycle changes, increases the SubG1 cell population, and promotes apoptosis in glioma cells and glioblastoma stem cells. HDAC6-IN-75 is applicable for glioma-related research .
HDAC6-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 .
HDAC6-IN-76 (Compound G25) is a selective HDAC6 inhibitor with an IC50 of 12 nM. HDAC6-IN-76 induces Autophagy in a p53-dependent manner. HDAC6-IN-76 induces Apoptosis in a p53-dependent manner. HDAC6-IN-76 exhibits anticancer activity against hematologic malignancies, including acute myeloid leukemia .
HDAC6-IN-81 is a potent selective HDAC6 inhibitor with an IC50 of 1 nM. HDAC6-IN-81 exhibits selectivity over class I HDAC isoforms (HDAC1/2/3/8).HDAC6-IN-81 can be used for the research of cancer .
HDAC6-IN-80 is an orally active, selective HDAC6 inhibitor with an IC50 of 8.5 nM. HDAC6-IN-80 inhibits lipopolysaccharide-induced microglial activation, reduces the levels of iNOS, COX-2, TNF-α and IL-6, and alleviates sensory hypersensitivity behaviors. HDAC6-IN-80 can be used for the research of inflammatory pain and chemotherapy-induced peripheral neuropathy .
HDAC6-IN-73 is a highly potent and selective HDAC6 inhibitor with an IC50 of 0.007 μM ± 0.001, ~1771-fold selectivity over HDAC1, ~131-fold selectivity over HDAC8, and antiproliferative activity in hematological cancer cell lines.HDAC6-IN-73 can be used for the research of hematological malignancies .
HDAC6-IN-79 is a HDAC6 inhibitor with an IC50 of 98.40 nM, and it also exhibits inhibitory activity against other HDAC subtypes (HDAC1: 639.0 nM, HDAC2: 798.9 nM, HDAC8: 865.7 nM, HDAC4: 1187 nM). HDAC6-IN-79 induces acetylation of α-tubulin and histone H3, reduces the viability of cancer cells, activates the autophagy pathway and induces apoptosis. HDAC6-IN-79 can be used for research related to urothelial carcinoma (bladder cancer) .
HDAC6-IN-70 (Compound 9q) is a selective HDAC6 inhibitor with an IC50 of 29 nM. HDAC6-IN-70 effectively inhibits tubulin polymerization and HDAC6. HDAC6-IN-70 causes Apoptosis. HDAC6-IN-70 shows anticancer effects on hematological malignancies and colorectal cancers .
HDAC6-IN-71 (Compound 24) is a HDAC6 inhibitor with IC50 values for HDAC6 and HDAC1 of 13.68 and 443.12 nM respectively. HDAC6-IN-71 effectively inhibits the production of NO by mouse macrophages, with its IC50 being 2.31 μM. HDAC6-IN-71 inhibits the HDAC6-NF-κB signaling pathway, reduces the levels of phosphorylated IκB-α and IKK-α/β, and suppresses the expression of downstream inflammatory proteins COX-2 and iNOS. HDAC6-IN-71 significantly alleviates ulcerative colitis in mice .
HDAC6-IN-57 (compound 9c) is an HDAC6 inhibitor with an IC50 value of 7 nM. HDAC6-IN-57 inhibits 60 cancer cell lines with a mean GI50 of 2.64 μM while exhibiting significantly lower cytotoxicity towards non-tumor cell lines .
HDAC6degrader-6 (Compound 11b) is a potent and selective HDAC6 PROTAC degrader with a DC50 of 1.9 nM. HDAC6degrader-6 has no effect on the protein levels of other HDAC family members and does not degrade IKZF1, IKZF3, and GSPT1. HDAC6degrader-6 can be used to study multiple myeloma (Pink: HDAC6 ligand (HY-177776); Blue: CRBN ligand (HY-W998281); Black: Linker) .
PROTAC HDAC6 degrader 2 (Compound 1) is a HDAC6 PROTAC degrader, with IC50 of 0.643 μM. PROTAC HDAC6 degrader 2 promotes ubiquitination and degradation of HDAC6. PROTAC HDAC6 degrader 2 can be used for the research of haematological and solid cancers (Pink: HDAC6 ligand (HY-171141); Blue: E3 ligase CRBN ligand (HY-10984)) .
PROTAC HDAC6 degrader (Compound A6) is a potent and selective PROTAC HDAC6 degrader with a DC50 of 3.5 nM. PROTAC HDAC6 degrader shows promising antiproliferative activity via inducing apoptosis in myeloid leukemia cell lines .
PROTAC HDAC6 degrader 4 (Compound 17c) is the PROTAC degrader for HDAC6 with a DC50 of 14 nM. PROTAC HDAC6 degrader 4 exhibits inhibitory activit against HDAC1, HDAC2, HDAC3 and HDAC6 with IC50s of 2.2, 2.37, 0.61 and 0.295 μM, respectively . (Pink: ligand for target protein HDAC6 ligand-3 (HY-172360); Black: linker (HY-138387); Blue: ligand for cereblon E3 ligase (HY-W093272))
PROTAC HDAC6 degrader 3 (Compound 4) is a selective inhibitor and degrader for HDAC6 with an IC50 of 686 nM and a DC50 of 171 nM. PROTAC HDAC6 degrader 3 promotes the acetylation of α-tubulin . (Pink: ligand for target protein (HY-171141); Blue: ligand for E3 ligase VHL (HY-150803))
mTOR/HDAC6-IN-1 is a potent mTOR and HDAC6 dual inhibitor (IC50s of 133.7 nM and 56 nM for mTOR and HDAC6, respectively). mTOR/HDAC6-IN-1 can induce significant autophagy, apoptosis and suppress migration. mTOR/HDAC6-IN-1 has potential to research Triple-negative breast cancer (TNBC) .
PD-L1/HDAC6-IN-1 TFA is an orally active dual inhibitor of PD-L1 and HDAC6, with IC50 values of 26.8 nM and 78 nM, respectively. PD-L1/HDAC6-IN-1 TFA binds to human and murine PD-L1 proteins with high affinity, while it reduces STAT3 phosphorylation and downregulates PD-L1 expression by inhibiting HDAC6, thus blocking the PD-1/PD-L1 interaction. PD-L1/HDAC6-IN-1 TFA exhibits potent anti-tumor activity in a mouse melanoma model. PD-L1/HDAC6-IN-1 is suitable for research on tumor immune regulation related to melanoma .
LSD1/HDAC6-IN-2 (JBI-802) is an orally active LSD1/HDAC6/MAO-A inhibitor, with IC50 values of 5 nM, 11 nM, and 5 nM, respectively. LSD1/HDAC6-IN-2 can inhibit the growth of multiple myeloma cells MM.1S, MM.1R, and RPMI-8226. LSD1/HDAC6-IN-2 can be used for research on diseases such as acute myeloid leukemia and lymphoma .
LSD1/HDAC6-IN-1 is an orally active dual inhibitor of lysine specific demethylase 1(LSD1)/Histone deacetylase 6(HDAC6), with anti-tumor activity. LSD1/HDAC6-IN-1 can be used for the research of multiple myeloma (MM) .
COX-2/HDAC6-IN-1 (Compound 11e) is a dual COX-2 and HDAC6 inhibitor, with an IC50 of 0.12 μM against HDAC6 and an IC50 of 0.66 μM against COX-2. COX-2/HDAC6-IN-1 enhances the acetylation level of α-tubulin, regulates epigenetic gene expression, and inhibits the expression of pro-inflammatory mediators (COX-2, IL-1β, IL-6 and TNF-α). COX-2/HDAC6-IN-1 promotes Amyloid-β clearance and reduces excessive phosphorylation of Tau protein. COX-2/HDAC6-IN-1 maintains neuronal morphology by stabilizing MAP2, protects synaptic integrity by regulating synapsin, and restores the expression of memory-related genes. COX-2/HDAC6-IN-1 possesses neuroprotective activity and improves learning and memory abilities in Scopolamine (HY-N0296)-induced Alzheimer's disease mouse models. COX-2/HDAC6-IN-1 is applicable to research related to Alzheimer's disease .
DNA-PK/HDAC6-IN-1 is a selcetive and orally active dual DNA-PK and HDAC6 inhibitor with IC50 values of 84.2 and 64.8 nM. DNA-PK/HDAC6-IN-1 suppresses cancer cells proliferation, induces cancer cell cycle G2/M arrest, apoptosis, and decreases the mitochondrial membrane potential. DNA-PK/HDAC6-IN-1 induces DNA damage and elevates γ-H2AX levels. DNA-PK/HDAC6-IN-1 exhibits antitumor efficacy in AML animal mouse model. DNA-PK/HDAC6-IN-1 can be used for the research of acute myeloid leukemia .
PI3Kα/HDAC6-IN-1 (compound 21j) is a dual PI3Kα/HDAC6 inhibitor with IC50 of 2.9 and 26 nM, respectively. PI3Kα/HDAC6-IN-1 also inhibits AKT(Ser473) phosphorylation and induces the accumulation of acetylated α-tubulin without affecting acetylated histones H3 and H4. PI3Kα/HDAC6-IN-1 efficiently inhibits L-363 cell line (IC50=0.17 μM) and has good anti-cancer activity .
sEH/HDAC6-IN-1 (compound M9) is a selective, orally active dual inhibitor for sEH and HDAC6, with IC50s of 2 nM, 0.72 nM and 5 nM, for human sEH, murine sEH and HDAC6, respectively. sEH/HDAC6-IN-1 reveals analgesic and anti-inflammatory effects .
sEH/HDAC6-IN-2 is a potent dual soluble epoxide hydrolase (sEH) and HDAC6 inhibitor with IC50s of 0.9 nM, 46.8 nM, and 8 nM for human sEH, mouse sEH, and HDAC6, respectively. sEH/HDAC6-IN-2 can be used for the study of inflammatory pain .
BChE/HDAC6-IN-2 (compound 29a) is a dual inhibitor of BChE and HDAC6 with IC50s of 1.8 nM and 71.0 nM, respectively. BChE/HDAC6-IN-2 has prominently neuroprotective effects and reactive oxygen species (ROS) scavenging activity. BChE/HDAC6-IN-2 is also an effective chelator of metal ion (Fe 2+ and Cu 2+). BChE/HDAC6-IN-2 inhibits phosphorylation of tau, and exhibits moderate immunomodulatory effect.
PD-L1/HDAC6-IN-1 is an orally active dual inhibitor of PD-L1 and HDAC6, with IC50 values of 26.8 nM and 78 nM, respectively. PD-L1/HDAC6-IN-1 binds to human and murine PD-L1 proteins with high affinity, while it reduces STAT3 phosphorylation and downregulates PD-L1 expression by inhibiting HDAC6, thus blocking the PD-1/PD-L1 interaction. PD-L1/HDAC6-IN-1 exhibits potent anti-tumor activity in a mouse melanoma model. PD-L1/HDAC6-IN-1 is suitable for research on tumor immune regulation related to melanoma .
CYP17A1/HDAC6-IN-1 (compound 12) is a potent inhibitor of CYP17A1/HDAC6, with IC50 of 0.284μM and 0.6015 μM,respectively. CYP17A1/HDAC6-IN-1 has anti-tumor activity .
BChE/HDAC6-IN-1 is a potent and selective dual BChE/HDAC6 inhibitor with IC50 values of 4 and 8.9 nM, respectively. BChE/HDAC6-IN-1 ameliorates the cognitive impairment in an Aβ1–42-induced mouse model and has the potental for AD research .
PI3Kδ/HDAC6-IN-1 (Compound 22E) is an orally active and dual inhibitor of PI3Kδ and HDAC6 with IC50 values of 2.4 nM and 6.2 nM, respectively. PI3Kδ/HDAC6-IN-1 exhibits potent antiproliferative effects on non-Hodgkin lymphoma (NHL) cells and possesses in vivo antitumor activity without significant toxicity. PI3Kδ/HDAC6-IN-1 arrests the cell cycle at the G0/G1 phase and induces apoptosis. PI3Kδ/HDAC6-IN-1 blocks the PI3K/AKT/mTOR signaling pathway and increases the acetylation levels of α-tubulin and histone H3 .
Nexturastat A is a potent, selective HDAC6 inhibitor. Nexturastat A has inhibitory for HDAC6 with an IC50 of 5 nM. Nexturastat A can be used for the research of multiple myeloma (MM) .
Bufexamac is a selective Ⅱb HDAC (HDAC6, HDAC10) and LTA4H dual inhibitor, with Kds of 0.53 µM and 0.22 µM for HDAC6 and HDAC10. Bufexamac is a nonsteroida anti-inflammatory drug .
BRD9757 is a potent, capless and selective HDAC6 inhibitor with an IC50 of 30 nM. BRD9757 shows excellent selectivity toward HDAC6 versus the class I (>20-fold) and class II (>400-fold) HDACs .
TO-1187 is a selective HDAC6PROTAC degrader (DC50: 5.81 nM). TO-1187 promotes the ubiquitination and degradation of HDAC6 and can be used in the study of hematological malignancies and solid tumors (Pink: HDAC6 ligand (HY-173386); Blue: CRBN ligase ligand (HY-41547); Black: linker (HY-140212)) .
Bavarostat (EKZ-001) is a blood-brain barrier-permeable, potent HDAC6 inhibitor and PET radiotracer, with an IC50 as low as 17 nM against human HDAC6. Bavarostat can be labeled with 18F and used as a probe to map HDAC6 distribution and measure target occupancy in the brains of non-human primates. Bavarostat also selectively modulates tubulin acetylation, but not histone acetylation. Bavarostat is applicable for research on Alzheimer's disease, other neurodegenerative disorders, and cancers .
TO-1187 TFA is a selective HDAC6PROTAC degrader (DC50: 5.81 nM). TO-1187 TFA promotes the ubiquitination and degradation of HDAC6 and can be used in the study of hematological malignancies and solid tumors (Pink: HDAC6 ligand (HY-173386); Blue: CRBN ligase ligand (HY-41547); Black: linker (HY-140212)) .
Bufexamac (Standard) is the analytical standard of Bufexamac. This product is intended for research and analytical applications. Bufexamac is a selective Ⅱb HDAC (HDAC6, HDAC10) and LTA4H dual inhibitor, with Kds of 0.53 μM and 0.22 μM for HDAC6 and HDAC10. Bufexamac is a nonsteroida anti-inflammatory drug .
C1A is a class I/II HDACs and sirtuin inhibitor with an IC50 of 479 nM for HDAC6. C1A induces sustained acetylation of HDAC6 substrates, α-tubulin and HSP90. C1A shows srtong anticancer effcts, and induces apoptosis in cancer cells .
ITF5924 (compound 1) is a potent and highly selective HDAC6 inhibitor with an IC50 of 7.7 nM. ITF5924 shows greater than 104-fold selectivity for HDAC6 over all other HDAC subtypes. ITF5924 containing a difluoromethyl-1,3,4-oxadiazole (DFMO) moiety is slow-binding substrate analog of HDAC6 that undergo an enzyme-catalyzed ring opening reaction, forming a tight and long-lived enzyme-inhibitor complex .
HDAC-IN-97 is a PROTAC HDAC6degrader-6that can be used for synthesis of PROTACs, such as HDAC6degrader-6 (HY-177758). HDAC6degrader-6 is a potent HDAC6 PROTAC degrader with anticancer activity .
(S)-Trichostatin A ((S)-TSA) is a HDAC6-selective inhibitor with IC50s of 9.88 nM and 11.1 nM for Zebrafish HDAC6 and Human HDAC6, respectively. (S)-Trichostatin A weakly inhibits other human HDACs .
(R)-Dihydrolipoic acid is a compound that inhibits histone deacetylase 6 (HDAC6) activity. The structure of its complex with HDAC6 has been resolved. (R)-Dihydrolipoic acid can inhibit HDAC6 through specific interactions, providing a basis for understanding the relationship between HDAC function and oxidative stress.
QTX125 TFA is a potent and highly selective HDAC6 inhibitor. QTX125 TFA exhibits excellent selectivity over other HDACs. QTX125 has antitumor effects .
HDAC-IN-40 is a potent alkoxyamide-based HDAC inhibitor with Ki values of 60 nM and 30 nM for HDAC2 and HDAC6, respectively. HDAC-IN-40 had antitumor effects .
PB200 is an HDAC6 inhibitor with an IC50 value of 1.97 nM. PB200 demonstrates significant antidepressant effects by restoring abnormal HDAC6 expression levels and alleviating neuroinflammation .
CG347B is a selective HDAC6 inhibitor, also involves in synthesis of other metalloenzyme inhibitors. HDAC6 inhibitors can be used for oncology, immunology, and neurology research .
BRD73954 is a potent HDAC inhibitor and selectively inhibiting both HDAC6 and HDAC8 with IC50 values of 0.0036, 0.12, 9, 12, 23 µM for HDAC6, HDAC8, HDAC2, HDAC1 and HDAC3, respectively. BRD73954 decreases the levels of HDAC6, associated with upregulation of Ac-Tubulin .
Nicoxamat (N-Hydroxynicotinamide) is a HCV inhibitor as well as a selective HDAC6 inhibitor. Nicoxamat is applicable to research related to hepatitis C virus (HCV) infection .
PARP-1/HDAC-IN-1 is a PARP-1/HDAC6 dual targeting inhibitor with IC50s of 68.90 nM and 510 nM, respectively. PARP-1/HDAC-IN-1 displays remarkable anticancer, anti-migration and anti-angiogenesis activities .
HDAC6degrader-6 (compound 10c) is a ByeTAC protein degrader targeting HDAC6, with IC50 values of 0.034 μM, 0.166 μM, 0.703 μM, and 0.293 μM for HDAC6, HDAC1, HDAC2, and HDAC3, respectively. HDAC6degrader-6 induces cell apoptosis and can be used for the study of multiple myeloma(Blue: USP14 ligand HY-159808; Pink: HDAC ligand HY-176209; Black: linker HY-W016871)
GV-001 is a selective and orally active HDAC6 inhibitor with an IC50 of 1.18 nM against HDAC6. GV-001 selectively enhances α-tubulin acetylation, reduces sIL-6 and Collagen I levels, suppresses renal cyst growth, and upregulates PC1 expression. GV-001 can be used for the study of autosomal dominant polycystic kidney disease (ADPKD) .
HDAC-MB a probe that is activated by HDAC6 and can detect and eliminate glioma cells through activation by HDAC6. HDAC-MB reveals antimetastatic and antiproliferative properties, inhibits glioma invasion and induces cellular apoptosis .
AES-135, a hydroxamic acid-based pan-HDAC inhibitor, prolongs survival in an orthotopic mouse model of pancreatic cancer. AES-135 inhibits HDAC3, HDAC6, HDAC8, and HDAC11 with IC50s ranging from 190-1100 nM .
UBD1031 (SGC-UBD1031) is a selective USP16/HDAC6-UBD antagonist with a human USP16-UBD IC50 of 10.6 μM, KD value of 48 nM, and a human HDAC6-UBDKD of 16 nM. UBD1031 disrupts ISG15 C-terminus interactions with USP16-UBD and HDAC6-UBD, and exhibits cooperative inhibition of full-length USP16 deubiquitinase activity via USP16-UBD binding. UBD1031 can be used in research on cancer, autoimmune diseases, and Down syndrome .
ACY-1083 is a selective and brain-penetrating HDAC6 inhibitor with an IC50 of 3 nM and is 260-fold more selective for HDAC6 than all other classes of HDAC isoforms. ACY-1083 effectively reverses chemotherapy-induced peripheral neuropathy .
SAHA-OH is a selective HDAC6 inhibitor (IC50=23 nM), shows a 10- to 47-fold selectivity for HDAC6 compared to HDAC 1, 2, 3, and 8. SAHA-OH shows anti-inflammatory activity, and attenuates macrophage apoptosis .
KH-259 (compound 1) is a potent, selective and CNS-penetrant HDAC6 inhibitor, with an IC50 of 0.26 μM. KH-259 has antidepressant effects in mice through the inhibition of HDAC6 in the brain. KH-259 can be used for neurodegenerative diseases research .
Citarinostat (ACY241) is a second generation potent, orally active and high-selective HDAC6 inhibitor with an IC50 of 2.6 nM (IC50s of 35 nM, 45 nM, 46 nM and 137 nM for HDAC1, HDAC2, HDAC3 and HDAC8, respectively). Citarinostat has anticancer effects .
HDAC-IN-67 (compound 27f) is an HDAC inhibitor against HDAC1 and HDAC6, with IC50 values of 22 nM and 8 nM, respectively. HDAC-IN-67 inhibits cell proliferation and induces cell apoptosis. HDAC-IN-67 exhibits antitumor activity .
SW-100, a selective histone deacetylase 6(HDAC6) inhibitor with an IC50 of 2.3 nM, shows at least 1000-fold selectivity for HDAC6 relative to all other HDAC isozymes. SW-100 displays a significantly improved ability to cross the blood-brain-barrier .
HPOB is a highly potent and selective inhibitor of HDAC6 with an IC50 of 56 nM. HPOB displays >30 fold less potent against other HDACs. HPOB enhances the effectiveness of DNA-damaging anticancer agents in transformed cells but not normal cells. HPOB does not block the ubiquitin-binding activity of HDAC6 .
KT-531 is a potent and selective inhibitor of HDAC6 with an IC50 of 8.5 nM. KT-531 exhibits strong inhibition against SUP-T11 cells with an IC50 of 0.42 μM. KT-531 can be used in study hematological cancers .
T-518 is an orally active, BBB-penetrant and potent DFMO-based HDAC6 inhibitor with high selectivity (IC50 = 36 nM). T-518 improves axonal transport. T-518 ameliorates object recognition deficit. T-518 can be studied in research for Alzheimer’s disease and tauopathy .
CM-545, the cis-isomer of CM-414 (HY-119316), is a dual inhibitor of PDE5, HDAC1, HDAC2, HDAC3, and HDAC6 with pIC50 values of 7.47, 6.65, 6.14, 6.55, and 6.84, repectively .
VEGFR2/HDAC-IN-1 is a dual selective enzymatic inhibitor of VEGFR2 kinase and HDAC6 with oral activity. VEGFR2/HDAC-IN-1 has an IC50 of 19.19 nM for VEGFR2 and 0.165 μM for HDAC6. VEGFR2/HDAC-IN-1 increases α-tubulin acetylation, exerts antiproliferative effects, inhibits tumor growth, and exhibits antiangiogenic activity. VEGFR2/HDAC-IN-1 can be used for the research of colorectal carcinoma and hepatocellular carcinoma .
ZMF-23 is a PAK1/HDAC6 dual inhibitor. ZMF-23 inhibits PAK1 and HDAC6 regulated aerobic glycolysis and migration. ZMF-23 induces TNF-α-regulated necroptosis, and further enhances apoptosis. ZMF-23 inhibits the Warburg effect and cell migration. ZMF-23 can be used for research of triple-negative breast cancer (TNBC) .
Droxinostat (NS 41080) is a histone deacetylase (HDAC) inhibitor. Droxinostat selectively inhibits HDAC3, HDAC6, and HDAC8 with IC50 values of 16.9 μM, 2.47 μM, and 1.46 μM, respectively. Droxinostat can be used for the research of hepatocellular carcinoma (HCC) .
HDAC-IN-73 (compound P-503) is a histone deacetylase (HDAC) inhibitor. HDAC-IN-73 shows IC50s values of 0.17, 0.49 µM for HDAC1 and HDAC6, respectively. Notably, HDAC-IN-73's inhibitory potency against HDAC6 is heightened, exhibiting a 9-fold greater efficacy than PsA (HY-N2150) (IC50=3.9 μM). HDAC-IN-73 shows potent antiproliferative activity, induces apoptosis, and causes cell cycle arrest at G2 / M phase. HDAC-IN-73 has the potential to be used for the research of cancer such as colon cancer .
GSK-3β/HDAC-IN-2 is a potent inhibitor of GSK-3β (IC50 = 0.04 μM), HDAC2 (IC50 = 1.05 μM, Ki = 0.070 μM) and HDAC6 (IC50 = 1.52 μM, Ki = 0.017 μM). GSK-3β/HDAC-IN-2 inhibits HDAC2 and HDAC6 activities and blocks tau hyperphosphorylation. GSK-3β/HDAC-IN-2 exerts neuroprotective effects and shows no significant toxicity. GSK-3β/HDAC-IN-2 can be used in the research of Alzheimer's disease.
anti-TNBC agent-12 (Compound 23a) is a multi-target antitumor agent targeting HDAC6 (IC50=30.3 nM), DNA, and inducing nitric oxide (NO) release. anti-TNBC agent-12 induces tumor cell apoptosis and G2/M phase cell cycle arrest. anti-TNBC agent-12 is promising for research of triple-negative breast cancer (TNBC) .
J22352 is a PROTAC (proteolysis-targeting chimeras)-like and highly selective HDAC6 inhibitor with an IC50 value of 4.7 nM. J22352 promotes HDAC6 degradation and induces anticancer effects by inhibiting autophagy and eliciting the antitumor immune response in glioblastoma cancers, and leading to the restoration of host antitumor activity by reducing the immunosuppressive activity of PD-L1 .
(2R,4R,6S)-Tubacin is the 2R,4R,6S enantiomer of Tubacin (HY-13428). Tubacin is a potent and selective inhibitor of HDAC6, with an IC50 value of 4 nM and approximately 350-fold selectivity over HDAC1. Tubacin also inhibits metallo-β-lactamase domain-containing protein 2 (MBLAC2) .
Antitumor agent-123 (Copmound 4d) effectively inhibits multiple kinase targets with anti-cancer effects, including JAK2, JAK3, HDAC1 and HDAC6, with IC50 values of 34.6 and 2.6 μM for JAK2 and JAK3, respectively. Antitumor agent-123 exhibits moderate activity in solid tumor models .
NCT-10b (compound 17b) is a selective HDAC6 inhibitor.NCT-10b mediates preferential α-tubulin acetylation without major histone H4 acetylation.NCT-10b can be used for the research of multiple myeloma .
NN-429 is a selective HDAC6 inhibitor. NN-429 induces apoptosis, increases the acetylation level of α-tubulin, and exhibits cytotoxicity against cancer cells. NN-429 is applicable to research related to acute myeloid leukemia, multiple myeloma and lymphoma .
HDAC3/6-IN-2 (compound 15) is a potent HDAC6 and HDAC3 inhibitor, with IC50 values of 0.368 and 0.635 μM, respectively. HDAC3/6-IN-2 shows antitumor activity, and induces cancer cell apoptosis. HDAC3/6-IN-2 decreases the levels of HDAC6 and HDAC3, associated with upregulation of acetylated H3 and α-tubulin .
HDAC-IN-58 is a HDAC inhibitor. HDAC-IN-58 has HDAC6-specific inhibition activity with an IC50 value of 2.06 nM. HDAC-IN-58 can be used for the research of chronic diseases, including neurodegenerative and psychiatric conditions .
HDAC-IN-84 (compound 4d) is a potent HDAC inhibitor, with IC50 values of 0.0045, 0.015, 0.013, 0.038, 5.8 and 26 μM for HDAC1, HDAC2, HDAC3, HDAC6, HDAC8 and HDAC11, respectively. HDAC-IN-84 effectively inhibits the proliferation of leukemia cells without causing toxicity .
Fibrostat (Compound 5n) is a selective HDAC6 inhibitor that exerts antifibrotic effects by inhibiting HDAC6 activity, with an IC50 value of 63 nM. It also exhibits good selectivity over HDAC1, HDAC3, HDAC5, HDAC8, HDAC10, and HDAC11. Fibrostat significantly downregulates fibrotic markers (fibronectin and collagen 1) in fibroblasts. Additionally, Fibrostat demonstrated no toxicity in rat-perfused heart and zebrafish larvae models. Fibrostat shows potential for research into fibrosis-related diseases .
KA2507 is a potent, orally active and selective HDAC6 inhibitor, with an IC50 of 2.5 nM. KA2507 shows antitumor activities and immune modulatory effects in preclinical models .
MC2625 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 .
KA2507 hydrochloride is a potent and highly selective inhibitor of HDAC6 (IC50=2.5 nM) with no significant toxicities. KA2507 hydrochloride shows antitumor efficacy and immune modulatory effects .
CM-414 is a brain-penetrant phosphodiesterase 5 (PDE5) and HDAC inhibitor with IC50s of 60 nM, 91 nM, 310 nM, 322 nM and 490 nM for PDE5, HDAC6, HDAC1, HDAC3 and HDAC2, respectively. CM-414 diminishes brain Aβ and tau phosphorylation (pTau) level in Tg2576 mice. CM-414 can be used for the study of Alzheimer's disease (AD) .
HDAC9-IN-1 is a selective class IIa HDAC inhibitor that binds to HDAC9 with an IC50 of 40 nM. HDAC9-IN-1 potently inhibits HDACs 4 and 7 while showing weak activity against HDAC6 (IC50 values: 180 nM (HDAC4), 190 nM (HDAC7), 970 nM (HDAC6)). HDAC9-IN-1 significantly inhibits several human cancer cells, induces apoptosis and DNA damage in human cancer cells, and modulates caspase-related proteins and p38 in human cancer cells. HDAC9-IN-1 can be used for the research of oral cancer, breast cancer, gastric cancer .
MPT0G211 mesylate is a potent, orally active and selective HDAC6 inhibitor (IC50=0.291 nM). MPT0G211 mesylate displays >1000-fold selective for HDAC6 over other HDAC isoforms. MPT0G211 mesylate can penetrate the blood-brain barrier. MPT0G211 mesylate ameliorates tau phosphorylation and cognitive deficits in an Alzheimer’s disease model. MPT0G211 mesylate has anti-metastatic and neuroprotective effects. Anticancer activities .
MPT0G211 is a potent, orally active and selective HDAC6 inhibitor (IC50=0.291 nM). MPT0G211 displays >1000-fold selective for HDAC6 over other HDAC isoforms. MPT0G211 can penetrate the blood-brain barrier. MPT0G211 ameliorates tau phosphorylation and cognitive deficits in an Alzheimer’s disease model. MPT0G211 has anti-metastatic and neuroprotective effects. Anticancer activities .
Tinostamustine (EDO-S101) is a pan HDAC inhibitor; inhibits HDAC6, HDAC1, HDAC2 and HDAC3 with IC50 values of 6 nM, 9 nM, 9 nM and 25 nM, respectively .
ITF 3756 is a selective, orally active HDAC6 inhibitor. ITF 3756 antagonizes TNF-α-induced activation of the NF-κB pathway. ITF 3756 reduces PD-L1 expression on human monocytes and CD8 + T cells, and exhibits antitumor activity. ITF 3756 can be used in colon cancer-related research .
HDAC-IN-35 (Compound 14) is a potent, selective HDAC and VEGFR-2 inhibitor, with IC50 values of 0.166 and 13.2 µM for HDAC6 and VEGFR-2, respectively .
Thalidomide-F-NH-C6-adize is the conjugate of an E3 ligase (Cereblon) ligand and a linker, and can be used for synthesis of PROTAC HDAC6 degrader 4 (HY-172359) .
WT-161 is a potent and selective HDAC6 inhibitor with an IC50 of 0.40 nM . WT-161 also inhibits metallo-β-lactamase domain-containing protein 2 (MBLAC2) .
Resminostat hydrochloride is a potent inhibitor of HDAC1, HDAC3 and HDAC6, with mean IC50 values of 42.5, 50.1, 71.8 nM, respectively, and shows less potent activities against HDAC8, with an IC50 of 877 nM.
Ricolinostat (ACY-1215) is a potent and selective HDAC6 inhibitor, with an IC50 of 5 nM. ACY-1215 also inhibits HDAC1, HDAC2, and HDAC3 with IC50s of 58, 48, and 51 nM, respectively.
Tubacin is a potent and selective inhibitor of HDAC6, with an IC50 value of 4 nM and approximately 350-fold selectivity over HDAC1. Tubacin also inhibits metallo-β-lactamase domain-containing protein 2 (MBLAC2).
Daphnegiravone D (compound 70) is an HDAC6 inhibitor with anti-hepatocellular carcinoma activity. Daphnegiravone D can induce apoptosis and selectively inhibit the proliferation of liver cancer cells through the p38 and JNK MAPK pathways .
HDAC-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 .
CRA-026440 hydrochloride is a potent, broad-spectrum HDAC(HDAC) inhibitor. The Ki values against recombinant HDAC isoenzymes HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, and HDAC10 are 4 nM, 14 nM, 11 nM, 15 nM, 7 nM, and 20 nM respectively. CRA-026440 hydrochloride shows antitumor and antiangiogenic activities . CRA-026440 (hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
ACY-775 is a potent and selective inhibitor of the of histone deacetylase 6(HDAC6) with an IC50 of 7.5 nM . ACY775 also inhibits metallo-β-lactamase domain-containing protein 2 (MBLAC2) .
PB131 is a selective and brain-permeable HDAC6 inhibitor with high binding affinity (IC50: 1.8 nM). PB131 has potent anti-inflammatory activity. PB131 can be used for research of inflammation, especially neuroinflammation .
ACY-738 is a potent, selective and orally-bioavailable HDAC6 inhibitor, with an IC50 of 1.7 nM; ACY-738 also inhibits HDAC1, HDAC2, and HDAC3, with IC50s of 94, 128, and 218 nM.
PTG-0861 is a selective histone deacetylase 6(HDAC6) inhibitor with the IC50 value of 5.92 nM. PTG-0861 induces apoptosis and can be used in the study of acute myeloid leukemia, multiple myeloma and other hematological cancers .
DNMT/HDAC-IN-1 (Compund 15a) is a dual DNMT and HDAC inhibitor with IC50 values for HDAC1 and HDAC6 are 56.84 nM and 17.39 nM respectively. DNMT/HDAC-IN-1 can induce apoptosis and be used in tumor research.
NN-390 is a potent and selective HDAC6 inhibitor, with an IC50 of 9.8 nM. NN-390 penetrates the blood-brain barrier (BBB). NN-390 shows study potential in metastatic Group 3 MB (medulloblastoma) .
SKLB-23bb is a potent and selective inhibitor for HDAC6 with an IC50 of 17 nM and shows 25-fold and 200-fold selectivity relative to HDAC1 (IC50=422 nM) and HDAC8 (IC50=3398 nM), respectively.
MPI_5a is a potent and selective HDAC6 inhibitor (IC50=36 nM). MPI_5a weakly inhibits other HDAC isoforms. MPI_5a inhibits acyl-tubulin accumulation in cells with an IC50 value of 210 nM .
Resminostat (RAS2410; 4SC-201) is a potent inhibitor of HDAC1, HDAC3 and HDAC6, with mean IC50 values of 42.5, 50.1, 71.8 nM, respectively, and shows less potent activities against HDAC8, with an IC50 of 877 nM.
FT108 is a selective HDAC6 inhibitor with an IC50 of 0.026 μM. FT108 exhibits only modest in vitro activity against HDAC3 and HDAC8 with IC50 values of 6.68 and 4.07 μM. FT108 increases acetylation of tubulin and has little to no effect on acetylated histone H3 levels. FT108 lacks activity against myeloproliferative neoplasm cell lines, and does not suppress JAK2 phosphorylation or its downstream targets pSTAT3 and pSTAT5 .
HDAC-IN-75 (5d) is a HDAC inhibitor, with IC50 values of 6.32 nM and 1352 nM for HDAC6 and HDAC1, respectively. HDAC-IN-75 (5d) promotes vision rescue in the atp6v0e1–/– zebrafish model of photoreceptor dysfunction .
SP-2-225 is a selective HDAC6 inhibitor. SP-2-225 enhance the production of cancer-associated antigens and macrophage antigen cross-presentation to T cells. SP-2-225 reduces the tumor volume in a syngeneic SM1 melanoma model .
TYA-018 is an orally active, potent and highly selective HDAC6 inhibitor. TYA-018 can protect heart function in mice. TYA-018 also enhances energetics in mice by increasing expression of targets associated with fatty acid metabolism, protein metabolism, and oxidative phosphorylation .
BG45 is a potent HDAC3 inhibitor with IC50 values of 0.289, 2, 2.2 and ﹥20 μM for HDAC3, HDAC1, HDAC2 and HDAC6, respectively. BG45 selectively targets multiple myeloma (MM) cells and induces caspase-dependent apoptosis .
HIT211504993 is a selective histone deacetylase 6(HDAC6) inhibitor with an IC50 of 0.070 μM. HIT211504993 suppresses cancer cell proliferation, cause G1 phase cell cycle arrest and induces apoptosis. HIT211504993 inhibits Myc-driven tumorigenesis via nucleocytoplasmic acetylation, p53 modulation, and Wnt/β-catenin signaling modulation. HIT211504993 inhibits tumor growth in a colon cancer xenograft mouse model. HIT211504993 can be used for the research of colon cancer .
PTACH (NCH-51) is a potent HDAC inhibitor with IC50s of 48 nM, 32 nM, and 41 nM for HDAC1, HDAC4, and HDAC6, respectively. PTACH exerts potent growth inhibition against various cancer cells (EC50s of 1.1-9.1 μM) .
HDAC-IN-71 (Compound 17q) is a potent HDAC inhibitor with IC50 values of 12.6, 14.1, 20, 3, and 72 nM for HDAC1, HDAC2, HDAC3, HDAC6, and HDAC10, respectively. HDAC-IN-71 induces apoptosis and can be used in cancer research .
Ricolinostat (Standard) is the analytical standard of Ricolinostat. This product is intended for research and analytical applications. Ricolinostat (ACY-1215) is a potent and selective HDAC6 inhibitor, with an IC50 of 5 nM. ACY-1215 also inhibits HDAC1, HDAC2, and HDAC3 with IC50s of 58, 48, and 51 nM, respectively.
Tubacin (Standard) is the analytical standard of Tubacin. This product is intended for research and analytical applications. Tubacin is a potent and selective inhibitor of HDAC6, with an IC50 value of 4 nM and approximately 350-fold selectivity over HDAC1. Tubacin also inhibits metallo-β-lactamase domain-containing protein 2 (MBLAC2).
HDAC-IN-83 (compound 9D) is an inhibitor of deacetylases (HDACs) (IC50=0.01 μM/0.44 μM HDAC1/HDAC6) with anticancer, antiproliferative and caspase 3/7 activation activities. HDAC-IN-83 inhibits Cal27, HepG2 and MRC-5 with IC50s of 0.693 μM, 0.427 μM and 3.19 μM, respectively .
HDAC-IN-36 (compound 23 g) is an orally active and potent HDAC (histone deacetylase) inhibitor, with an IC50 of 11.68 nM (HDAC6).HDAC-IN-36 promotes apoptosis, autophagy and suppresses migration. HDAC-IN-36 shows anti-tumor and anti-metastatic activity, and can be used for breast cancer research .
NR160 is a selective HDAC6 inhibitor with an IC50 value of 30 nM. NR160 shows low cytotoxicity against leukemia cell line. NR160 augments the apoptosis induction of Bortezomib (HY-10227) (proteasome inhibitor), Epirubicin (HY-13624) and Daunorubicin (HY-13062A) significantly .
Tubastatin A is a potent and selective HDAC6 inhibitor with an IC50 of 15 nM in a cell-free assay, and is selective (1000-fold more) against all other isozymes except HDAC8 (57-fold more). Tubastatin A also inhibits HDAC10 and metallo-β-lactamase domain-containing protein 2 (MBLAC2).
NL-103 is an inhibitor of histone deacetylases (HDACs) and Hedgehog, with the IC50 values of 21.3 nM, 57 nM, 74 nM, and 680 nM for HDAC1, HDAC2, HDAC3, and HDAC6, respectively. NL-103 can downregulate the expression of Gli2. NL-103 can be used in anti-cancer research .
CAY10603 (BML-281) is a potent and selective HDAC6 inhibitor, with an IC50 of 2 pM; CAY10603 (BML-281) also inhibits HDAC1, HDAC2, HDAC3, HDAC8, HDAC10, with IC50s of 271, 252, 0.42, 6851, 90.7 nM.
HDAC-IN-33 is a potent HDAC inhibitor with IC50s of 24, 46, and 47 nM for HDAC1, HDAC2 and HDAC6, respectively. HDAC-IN-33 possesses potent antiproliferation activities against tumor cells. HDAC-IN-33 shows potent antitumor efficacy in vivo That trigger antitumor immunity .
AC-340 is a potent hybrid VDRagonist/HDAC inhibitor. AC-340 superinduces VDR target genes (e.g., CYP24A1) and inhibits HDAC6 (IC50 = 0.37 μM) with ~10-fold selectivity over HDAC2. AC-340 induces VDR hyperagonism by causing widespread protein hyperacetylation (e.g., tubulin and H3K9/K27), which leads to elevated H3K27 acetylation on VDR target genes. AC-340 can be used for melanoma cancer research .
HDAC-IN-54 is a HDAC inhibitor with an IC50 of 25 nM against human HDAC1, 66 nM against HDAC2, 6.5 nM against HDAC3, and 281 nM against HDAC6. HDAC-IN-54 induces acetylation of α-tubulin and histone H3. HDAC-IN-54 acts synergistically with cisplatin to induce cancer cell apoptosis. HDAC-IN-54 can be used in research related to head and neck cancer, ovarian cancer, and tongue squamous cell carcinoma .
HDAC-IN-32 is a potent HDAC inhibitor with IC50s of 5.2, 11, and 28 nM for HDAC1, HDAC2 and HDAC6, respectively. HDAC-IN-32 possesses potent antiproliferation activities against tumor cells. HDAC-IN-32 shows potent antitumor efficacy in vivo That trigger antitumor immunity .
Tubastatin A Hydrochloride (Tubastatin A HCl) is a potent and selective HDAC6 inhibitor with IC50 of 15 nM in a cell-free assay, and is selective (1000-fold more) against all other isozymes except HDAC8 (57-fold more). Tubastatin A Hydrochloride also inhibits HDAC10 and metallo-β-lactamase domain-containing protein 2 (MBLAC2).
LMK-235 is a potent and selective HDAC4/5 inhibitor, inhibits HDAC5, HDAC4, HDAC6, HDAC1, HDAC2, HDAC11 and HDAC8, with IC50s of 4.22 nM, 11.9 nM, 55.7 nM, 320 nM, 881 nM, 852 nM and 1278 nM, respectively, and is used in cancer research.
Vorinostat (GMP) is a GMP grade Vorinosta (HY-10221). GMP-grade small molecules can be used as auxiliary agents in cell therapy. Vorinostat is a potent, orally available HDAC1, HDAC2, HDAC3 (Class I), HDAC6 and Inhibitors of HDAC7 (Class II) and Class IV (HDAC11) .
WT-161 (Standard) is the analytical standard of WT-161 (HY-100871). This product is intended for research and analytical applications. WT-161 is a potent and selective HDAC6 inhibitor with an IC50 of 0.40 nM . WT-161 also inhibits metallo-β-lactamase domain-containing protein 2 (MBLAC2) .
HDAC-IN-42 (compound 14f) is a potent and selective HDAC inhibitor with IC50 values of 0.19 and 4.98 µM for HDAC1 and HDAC6, respectively. HDAC-IN-42 shows anticancer and anti-proliferative activity. HDAC-IN-42 induces apoptosis and cell cycle arrest at G2/M phase .
GRK2 modulator 1 is an orally active, brain-penetrant and selective GRK2 modulator. GRK2 modulator 1 enhances the active, non-phosphorylated GRK2 and prevents mitochondrial GRK2 and TOMM6 aggregation. GRK2 modulator 1 enhances the non-amyloidogenic processing of APP and prevent PHF-tau, neurodegeneration, and neuronal loss. GRK2 modulator 1 decreases the senescence marker, UPAR, reduces the Alzheimer disease (AD)-related mortality, and prolongs survival. GRK2 modulator 1 exerts neuroprotection by inhibiting HDAC6, and counteracts age-related cardiac dysfunction. GRK2 modulator 1 can be used for research on AD .
Mocetinostat (MGCD0103) is a potent, orally active and isotype-selective HDAC (Class I/IV) inhibitor with IC50s of 0.15, 0.29, 1.66 and 0.59 μM for HDAC1, HDAC2, HDAC3 and HDAC11, respectively. Mocetinostat shows no inhibition on HDAC4, HDAC5, HDAC6, HDAC7, or HDAC8.
HDAC-IN-87 (Compound XII6) is a nonselective HDAC inhibitor, with pIC50 of 6.9 (HDAC4) and 5.8 (HDAC6) respectively. HDAC-IN-87 has fungicidal activity against P. sorghi and P. pachyrhizi. HDAC-IN-87 shows an acute oral LD50 of greater than 500 mg/kg in male and female rats .
PIM-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].
Tubastatin A (TSA) TFA is a potent and selective?HDAC6?inhibitor with?IC50?of 15 nM in a cell-free assay, and is selective (1000-fold more) against all other isozymes except HDAC8 (57-fold more). Tubastatin A TFA also inhibits HDAC10 and metallo-β-lactamase domain-containing protein?2 (MBLAC2).
NMDAR/HDAC-IN-1 (Compound 9d) is a dual NMDAR and HDAC inhibitor with a Ki of 0.59 μM for NMDAR and IC50 values of 2.67, 8.00, 2.21, 0.18 and 0.62 μM for HDAC1, HDAC2, HDAC3, HDAC6 and HDAC8, respectively. NMDAR/HDAC-IN-1 efficiently penetrates the blood brain barrier .
HDAC-IN-57 is an orally active inhibitor of histone deacetylases (HDAC), with IC50s of 2.07 nM, 4.71 nM, 2.4 nM and 107 nM for HDAC1, HDAC2, HDAC6, HDAC8, respectively. HDAC-IN-57 can inhibits LSD1, with IC50 of 1.34 μΜ. HDAC-IN-57 induces apoptosis, and has anti-tumor activity .
ZYJ-25e is a potent histone deacetylase inhibitor (HDACi) with IC50s of 0.047 μM and 0.139 μM for HDAC6 and HDAC8, respectively. ZYJ-25e is a tetrahydroisoquinoline-bearing hydroxamic acid analogue. ZYJ-25e shows marked antitumor potency in the MDA-MB231 xenograft model .
SelSA is a selective, orally active inhibitor for histone deacetylase 6(HDAC6) with IC50 of 56.9 nM. SelSA inhibits the phosphorylation of ERK1/2. SelSA inhibits the proliferation of breast cancer cells and hepatocellular carcinoma cells with IC50 of 0.58-2.6 μM, inhibits cell migration and invasion of Huh7, and induces apoptosis. SelSA exhibits antitumor activity in mouse model .
Romidepsin (FK 228) is a Histone deacetylase (HDAC) inhibitor with anti-tumor activities. Romidepsin (FK 228) inhibits HDAC1, HDAC2, HDAC4, and HDAC6 with IC50s of 36 nM, 47 nM, 510 nM and 1.4 μM, respectively . Romidepsin (FK 228) is produced by Chromobacterium violaceum, induces cell G2/M phase arrest and apoptosis .
Tubastatin A (Standard) is the analytical standard of Tubastatin A. This product is intended for research and analytical applications. Tubastatin A is a potent and selective HDAC6 inhibitor with an IC50 of 15 nM in a cell-free assay, and is selective (1000-fold more) against all other isozymes except HDAC8 (57-fold more). Tubastatin A also inhibits HDAC10 and metallo-β-lactamase domain-containing protein 2 (MBLAC2).
AMC-3-030 is a selective and potent dual inhibitor targeting HDAC6 and chymotrypsin-like proteasome with IC50 values of 884 and 4.17 nM. AMC-3-030 has a proliferation inhibitory effect. AMC-3-030 can reduce α-tubulin and β-actin levels. AMC-3-030 can be used for research of multiple myeloma .
JAK/HDAC-IN-4 (compound 11 i) is a JAK/HDAC inhibitor with the IC50 values of 0.49 nM and 12 nM for JAK2 and HDAC6, respectively. JAK/HDAC-IN-4 inhibits the cell proliferation and the production of nitric oxide. JAK/HDAC-IN-4 ameliorates psoriasis-like skin lesions in an Imiquimod (HY-B0180)-induced murine model with low toxicity .
MPT0G413 (Compound 6) is a potent, selective, orally active and brain-penetrant HDAC6 inhibitor with an IC50 of 3.92 nM. MPT0G413 decreases not only the level of phosphorylation of tau proteins but also the aggregation of tau proteins. MPT0G413 can ameliorate the impaired learning and memory. MPT0G413 can be used for the research of neurological disease, such as Alzheimer's disease .
CAY10603 (Standard) is the analytical standard of CAY10603. This product is intended for research and analytical applications. CAY10603 (BML-281) is a potent and selective HDAC6 inhibitor, with an IC50 of 2 pM; CAY10603 (BML-281) also inhibits HDAC1, HDAC2, HDAC3, HDAC8, HDAC10, with IC50s of 271, 252, 0.42, 6851, 90.7 nM.
Tubastatin A (Hydrochloride) (Standard) is the analytical standard of Tubastatin A (Hydrochloride). This product is intended for research and analytical applications. Tubastatin A Hydrochloride (Tubastatin A HCl) is a potent and selective HDAC6 inhibitor with IC50 of 15 nM in a cell-free assay, and is selective (1000-fold more) against all other isozymes except HDAC8 (57-fold more). Tubastatin A Hydrochloride also inhibits HDAC10 and metallo-β-lactamase domain-containing protein 2 (MBLAC2).
XP5 is a potent, orally active HDAC6 inhibitor with an IC50 of 31 nM. XP5 displays high antiproliferative activity against various cancer cell lines including the HDACi-resistant YCC3/7 gastric cancer cells (IC50=0.16-2.31 μM). XP5 enhances antitumor immunity when combined with a PD-L1 inhibitor in melanoma .
Vorinostat (SAHA) is a potent and orally active pan-inhibitor of HDAC1, HDAC2 and HDAC3 (Class I), HDAC6 and HDAC7 (Class II) and HDAC11 (Class IV), with ID50 values of 10 nM and 20 nM for HDAC1 and HDAC3, respectively. Vorinostat induces cell apoptosis . Vorinostat is also an effective inhibitor of human papillomaviruse (HPV)-18 DNA amplification .
LSD1/HDAC-IN-1 (compound 2) is a potent inhibitor of HDAC and LSD1, with IC50s of 0.125 nM, 0.373 nM, 0.0118 nM, 0.103 nM, and 0.571 μM for HDAC1, HDAC2, HDAC6, HDAC8 and LSD1, respectively. LSD1/HDAC-IN-1 plays an important role in cancer research .
FF2039 (compound 1j) is a specific HDAC1, HDAC6, and HDAC isoforms of class I, IIa and IIb PROTAC degrader. FF2039 demonstrates s significant antiproliferative activity against both hematological and solid cancer cell lines, driven by cell cycle arrest and Apoptosis induction. FF2039 inhibits HDAC isoform of HDAC1, HDAC2, HDAC4 and HDAC6 with IC50s of 1.03, 2.15, 12.4 and 0.053 μM, respectively. FF2039 shows antiproliferative activity against different tumor entities of MM.1S, MDA-MB-231 and U-87MG with EC50s of 2.8, 28 and 30 μM, respectively. (Pink: PRMT5 ligand (HY-168864); Blue: E3 ligase ligand HY-W957284); Black: linker (HY-W881439); E3+linker (HY-172185 )) .
HDAC-IN-62 (Compound 5) a HDAC inhibitor, with IC50s of 0.78, 1.0, 1.2? μM for HDAC6/8/11 respectively. HDAC-IN-62 inhibits-induced microglial activation by the initiation of autophagy, and inhibits nitric oxide production. HDAC-IN-62 has anti-inflammatory and anti-depressant effects. HDAC-IN-62 inhibits microglial activation in mouse brain .
HDAC3-IN-4 is a selective and orally active HDAC3 inhibitor with an IC50 of 89 nM. HDAC3-IN-4 induces the degradation of PD-L1 by regulating cathepsin B (CTSB) in the lysosomes, with a DC50 of 5.7 μM. HDAC3-IN-4 shows better selectivity for HDAC3 over HDAC1, HDAC6, HDAC7, and HDAC8 .
PHD2/HDACs-IN-1 is a potent PHD2/HDACs hybrid inhibitor (IC50s of 1.15 μM, 19.75 μM, 26.60 μM and 15.98 μM for PHD2, HDAC1, HDAC2 and HDAC6, respectively). PHD2/HDACs-IN-1 is a low-toxicity renoprotective agent for research of cisplatin-induced acute kidney injury (AKI) .
HDSI-18 is an orally active HDAC6 selective inhibitor (IC50: 1.6 nM). HDSI-18 is cytotoxic to K562, MV4-11, MOLM-13, THP-1, and Jurkat cells (IC50: 0.48, 0.58, 0.91, 1.79, and 4.31 μM, respectively). HDSI-18 activates Caspase-3, induces mitochondrial depolarization and apoptosis, and has antitumor activity .
DNMT/HDAC-IN-2 (Compound Y7) is a DNMT and HDAC inhibitor with IC50 values for DNMT1, HDAC1, and HDAC6 of 365, 0.2, and 8.91 nM respectively. DNMT/HDAC-IN-2 inhibits the proliferation of breast cancer cells. DNMT/HDAC-IN-2 significantly reduces tumor growth in xenografts and transgenic breast cancer mouse models. DNMT/HDAC-IN-2 can be used for the study of breast cancer .
CHDI-390576, a potent, cell permeable and CNS penetrant class IIa histone deacetylase (HDAC) inhibitor with IC50s of 54 nM, 60 nM, 31 nM, 50 nM for class IIa HDAC4, HDAC5, HDAC7, HDAC9, respectively, shows >500-fold selectivity over class I HDACs (1, 2, 3) and ~150-fold selectivity over HDAC8 and the class IIb HDAC6 isoform .
1-Naphthohydroxamic acid (Compound 2) is a potent and selective HDAC8 inhibitor with an IC50 of 14 μM. 1-Naphthohydroxamic acid is more selectively for HDAC8 than class I HDAC1 and class II HDAC6 (IC50 >100 μM). 1-Naphthohydroxamic acid does not increase global histone H4 acetylation and also does not reduce total intracellular HDAC activity .1-Naphthohydroxamic acid can induce tubulin acetylation .
HDAC-IN-37 is a potent HDAC inhibitor with IC50s of 0.0551 μM, 1.24 μM, 0.948 μM and 34.2 μM for HDAC1, HDAC3, HDAC8 and HDAC6, respectively. HDAC-IN-37 induces histone acetylation in a slow-off manner. HDAC-IN-37 prevents cell transition from G1 phase to S phase and induces early cell apoptosis .
AES-350 is a potent and orally active HDAC6 inhibitor with an IC50 and a Ki of 0.0244 μM and 0.035 μM, respectively. AES-350 is also against HDAC3, HDAC8 in an enzymatic activity assay with IC50 values of 0.187 μM and 0.245 μM, respectively. AES-350 triggers apoptosis in AML cells through HDAC inhibition and can be used for acute myeloid leukemia (AML) research .
Nanatinostat (CHR-3996) 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 has low activity against HDAC5 (IC50 of 200 nM) and HDAC6 (IC50 of 2100 nM). Nanatinostat induces apoptosis in myeloma cells. Nanatinostat has potent anticancer effects, such as myeloma, advanced solid tumours and colorectal cancer .
HDAC-IN-34 (compound 27) is a potent HDAC inhibitor, with IC50 values of 0.022 and 0.45 μM for HDAC1 and HDAC6, respectively. HDAC-IN-34 can bind to DNA and cause DNA damage. HDAC-IN-34 causes cells apoptosis through p53 signaling pathway. HDAC-IN-34 exhibits significant anti-proliferation effect against HCT-116 cells, with an IC50 of 1.41 μM .
HDACs/mTOR Inhibitor 1 is a dual HDACs and mTOR inhibitor, with IC50s of 0.19 nM, 1.8 nM, 1.2 nM for HDAC1, HDAC6, mTOR, respectively. HDACs/mTOR Inhibitor 1 stimulates cell cycle arrest in G0/G1 phase and induces tumor cell apoptosis with low toxicity in vivo. HDACs/mTOR Inhibitor 1 can be used in the research of hematologic malignancies .
Mocetinostat (Standard) is the analytical standard of Mocetinostat. This product is intended for research and analytical applications. Mocetinostat (MGCD0103) is a potent, orally active and isotype-selective HDAC (Class I/IV) inhibitor with IC50s of 0.15, 0.29, 1.66 and 0.59 μM for HDAC1, HDAC2, HDAC3 and HDAC11, respectively. Mocetinostat shows no inhibition on HDAC4, HDAC5, HDAC6, HDAC7, or HDAC8.
PI3K/HDAC-IN-2 is a potent dual PI3K/HDAC inhibitor with IC50s of 226 nM, 279 nM, 467 nM, 29 nM for PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ, respectively, and IC50s of 1.3 nM, 3.4 nM, 972 nM, 17 nM, 12 nM for HDAC1, HDAC2, HDC4, HDAC6, HDAC8, respectively. PI3K/HDAC-IN-2 exhibits PI3Kδ and class I and IIb HDAC selectivity. PI3K/HDAC-IN-2 has remarkable anticancer effects .
Imofinostat (ABT-301; MPT0E028) is an orally active and selective HDAC inhibitor with IC50s of 53.0 nM, 106.2 nM, 29.5 nM for HDAC1, HDAC2 and HDAC6, respectively. Imofinostat has a weak inhibitory effect on HDAC8 (IC50 of 2.5 μM), but no inhibitory effect on HDAC4 (IC50>10 μM). Imofinostat reduces the viability of B-cell lymphomas by inducing apoptosis and possesses potent direct Akt targeting ability and reduces Akt phosphorylation in B-cell lymphoma. Imofinostat has a broad-spectrum antitumor activity, including colorectal cancer, B-cell lymphoma, non-small cell lung carcinoma (NSCLC), and pancreatic cancer, while also showing therapeutic potential in non-tumor diseases like emphysema and pulmonary fibrosis [6].
HDAC10-IN-3 (Compound 2a) is a potent HDAC10 inhibitor with an IC50s of 0.41, 37, 350 and 4500 nM against HDAC10, HDAC6, HDAC8 and HDAC1. HDAC10-IN-3 exhibits moderate cytotoxicity in KB and SK-OV-3 cells, but does not show significant cytotoxicity against most cancer cell lines. HDAC10-IN-3 can be used for the study of cancers .
Vorinostat (Standard) is the analytical standard of Vorinostat. This product is intended for research and analytical applications. Vorinostat (SAHA) is a potent and orally active pan-inhibitor of HDAC1, HDAC2 and HDAC3 (Class I), HDAC6 and HDAC7 (Class II) and HDAC11 (Class IV), with ID50 values of 10 nM and 20 nM for HDAC1 and HDAC3, respectively. Vorinostat induces cell apoptosis . Vorinostat is also an effective inhibitor of human papillomaviruse (HPV)-18 DNA amplification .
HDAC/Top-IN-1 is an orally active and pan HDAC/Top dual inhibitor with IC50s of 0.036 μM, 0.14 μM, 0.059 μM, 0.089 μM and 9.8 μM for HDAC1, HDAC2, HDAC3, HDAC6 and HDAC8. HDAC/Top-IN-1 efficiently induces apoptosis with S cell-cycle arrest in HEL cells. HDAC/Top-IN-1 has exhibits excellent in vivo antitumor efficacy .
Nanatinostat (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 .
HDAC-IN-46 (compound 12c) is a potent HDAC inhibitor with an IC50 value of 0.21 μM and 0.021 μM for HDAC1 and HDAC6, respectively. HDAC-IN-46 upregulates p-p38, and downregulates Bcl-xL and cyclin D1 in MDA-MB-231 cells. HDAC-IN-46 induces significant G2 phase arrest and apoptosis. HDAC-IN-46 can be used for researching triple-negative breast cancer (TNBC) .
Romidepsin-d7 (FK 228-d7) is deuterium labeled Romidepsin. Romidepsin (FK 228) is a Histone deacetylase (HDAC) inhibitor with anti-tumor activities. Romidepsin (FK 228) inhibits HDAC1, HDAC2, HDAC4, and HDAC6 with IC50s of 36 nM, 47 nM, 510 nM and 1.4 μM, respectively . Romidepsin (FK 228) is produced by Chromobacterium violaceum, induces cell G2/M phase arrest and apoptosis .
Tubastatin A (GMP) is the Tubastatin A (HY-13271A) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Tubastatin A is a potent and selective HDAC6 inhibitor with an IC50 of 15 nM in a cell-free assay, and is selective (1000-fold more) against all other isozymes except HDAC8 (57-fold more). Tubastatin A also inhibits HDAC10 and metallo-β-lactamase domain-containing protein 2 (MBLAC2).
Top/HDAC-IN-1 (Compound 29b) is a topoisomerase/HDAC dual inhibitor with IC50s of 18, 230, 790, 87, and 5250 nM for HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8, respectively. Top/HDAC-IN-1 exhibits potent antitumor activities against the HCT116 cell line with the IC50 of 180 nM. Top/HDAC-IN-1 efficiently induces apoptosis with G2 cell cycle arrest in HCT116 cells .
SE-7552, a 2-(difluoromethyl)-1,3,4-oxadiazole (DFMO) derivative, is an orally active, highly selective, non-hydroxamate HDAC6 inhibitor with an IC50 of 33 nM. SE-7552 is greater than 850-fold selectivity versus all other known HDAC isozymes. SE-7552 is capable of blocking multiple myeloma growth in vivo. SE-7552 acts as an anti-obesity agent in diet-induced obese mice .
CS4 is a selective HDAC inhibitor with the IC50 values of 38 nM, 12 nM, 5.8 μM, 19 μM and 61 μM against of HDAC1, HDAC6, HDAC8, HDAC4 and HDAC11, respectively. CS4 promotes α-tubulin and histone 3 acetylation. CS4 activates PPARγ and blocks glycolysis. CS4 induces cell cycle arrest at G2 phase and apoptosis, and shows anticancer effect both in vivo and in vitro .
CRA-026440 is a potent, broad-spectrum HDAC inhibitor. The Ki values against recombinant HDAC isoenzymes HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, and HDAC10 are 4, 14, 11, 15, 7, and 20 nM respectively. CRA-026440 shows antitumor and antiangiogenic activities . CRA-026440 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
ROCK/HDAC-IN-2 (Compound C-9) is a ROCK/HDAC inhibitor, with IC50 values of 0.185 µM, 0.8 µM, and 0.7 µM for HDAC6, ROCK1, and ROCK2, respectively. ROCK/HDAC-IN-2 can induce apoptosis and changes in mitochondrial membrane potential in cancer cells, demonstrating significant antitumor activity. ROCK/HDAC-IN-2 can be used in the research of pancreatic ductal adenocarcinoma (PDAC) and triple-negative breast cancer (TNBC) .
BRD2492 (compound 6d) is a potent, selective HDAC1 and HDAC2 inhibitor with IC50s of 13.2 nM and 77.2 nM, respecrtively. BRD2492 exhibits >100-fold selectivity for HDAC1/2 over selectivity over HDAC3 and HDAC6. BRD2492 inhibits breast cancer cell lines growth with IC50s of 1.01 μM and 11.13 μM for T-47D and MCF-7 cells, respectively .
HDAC1-IN-5 is a potent HDAC1 inhibitor with IC50 values of 15 nM and 20 nM for HDAC1 and HDAC6, respectively. HDAC1-IN-5 can enhance the acetylation of histone H3 and α-tubulin, as well as promote the activation of caspase 3 in cancer cells, thereby inducing apoptosis. HDAC1-IN-5 induces chromatin damage by binding with DNA. HDAC1-IN-5 has strong inhibitory activity against tumor growth in xenograft mice .
HDAC1/6-IN-1 (compound D7) is a potent multitarget inhibitor of GLP, HDAC6 and HDAC1, with IC50 values of 1.3, 13, and 89 nM, respectively. HDAC1/6-IN-1 can inhibit the methylation and deacetylation of H3K9 on protein level. HDAC1/6-IN-1 induces cancer cell apoptosis, G0/G1 cell cycle arrest, and blocks migration and invasion .
FLT3/HDAC-IN-3 is a dual inhibitor of FLT3 and HDAC. FLT3/HDAC-IN-3 potently inhibits FLT3 (IC50 = 14 nM), HDAC1 (IC50 = 27 nM), HDAC6 (IC50 = 20 nM), and FLT3 D853Y (IC50 = 55 nM), exhibits weak activity against HDAC8, and shows no activity against HDAC4. FLT3/HDAC-IN-3 possesses kinase selectivity, plasma stability, and stability in human liver microsomes. FLT3/HDAC-IN-3 demonstrates anti-proliferative effects in a variety of hematological malignancy cell lines. FLT3/HDAC-IN-3 shows efficacy in the Jeko-1 xenograft model without observed significant toxicity. FLT3/HDAC-IN-3 can be used in the study of hematological malignancies .
MC1742 is a potent HDAC inhibitor, with IC50s of 0.1 μM, 0.11 μM, 0.02 μM, 0.007 μM, 0.61 μM, 0.04 μM and 0.1 μM for HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, HDAC10 and HDAC11, respectively. MC1742 can increase acetyl-H3 and acetyl-tubulin levels and inhibits cancer stem cells growth. MC1742 can induce growth arrest, apoptosis, and differentiation in sarcoma CSC .
TNI-97 is a selective and orally active HDAC6 inhibitor, with an IC50 of 0.2 nM. TNI-97 potently inhibited TNBC cell MDA-MB-453 growth and clonogenicity. TNI-97 induces PANoptosis including apoptosis, necroptosis and pyroptosis in MDA-MB-453 cells. TNI-97 shows antitumor activity in the mice carrying the MDA-MB-453 xenograft or carrying murine-derived TNBC cell allografts. TNI-97 can be used for the study of triple-negative breast cancer .
GSK-3β/HDAC-IN-1 (Compd 4) is a brain-penetrant and first in class dual non-ATP-competitive Glycogen Synthase Kinase 3β/Histone Deacetylases (GSK-3β/HDACs) Inhibitor with IC50s of 0.142, 0.03 and 0.045 μM against GSK-3β, HDAC2 and HDAC6, respectively. GSK-3β/HDAC-IN-1 can be used for Alzheimer’s disease research .
AAK1/HDACs-IN-1 (Compound 12) is the dual inhibitor for AAK1 and HDAC, that inhibits AAK1, HDAC1, and HDAC6 with IC50s of 15.9, 148.6, and 5.2 nM, respectively. AAK1/HDACs-IN-1 inhibits SARS-CoV-2 infection, suppresses the endocytosis of ACE2-SARS-CoV-2 complex, as well as AP2M1-ACE2 interaction .
WJ35435 is a dual-targeted anticancer hybrid that induces anti-HDAC (in particular HDAC1 and HDAC6) and anti-topoisomerase I activities that causes DNA damage associated with a low DNA repair capability and induces cell cycle arrest at G1- and G2-phase to apoptosis. WJ35435 induces histone H3 acetylation and phosphorylation, α-tubulin acetylation and γ-H2AX formation to achieve anti-HDAC effect. WJ35435 is promising for research of cancer .
PROTAC HDAC degrader-2 is a selective IIb HDACs PROTAC degrader, with DC50s of 13 nM for HDAC6, 29 nM for HDAC10, respectively. PROTAC HDAC degrader-2 exhibits low cytotoxicity against hematological and solid cancer cell lines. PROTAC HDAC degrader-2 can be used for the chemical knockdown of class IIb HDACs. ( Pink: HDAC ligand : (HY-174471), Blue: E3 ligase CRBN Ligand (HY-131717), E3 ligase ligand-linker conjugate (HY-174473)) .
HDAC-IN-76 (compound 6i) is a histone deacetylase (HDAC) inhibitor. HDAC-IN-76 IC50 values of 30 nM and 98 nM for Pf3D7 (chloroquine (HY-17589A) drug-susceptible strain) and PfDd2 (chloroquine (HY-17589A) drug-resistant strain), has a highly potent antimalarial activity against asexual blood-stage Plasmodium, respectively, and exhibits selective inhibition against parasites, with IC50 values of 7 nM and 9 nM for human HDAC1 and HDAC6, respectively, while inhibiting PfHDAC1 .
Crebinostat is a potent histone deacetylase (HDAC) inhibitor with IC50 values of 0.7 nM, 1.0 nM, 2.0 nM and 9.3 nM for HDAC1, HDAC2, HDAC3 and HDAC6, respectively. Crebinostat potently induces acetylation of both histone H3 and histone H4 as well as enhances the expression of the cAMP response element-binding protein (CREB) target gene Egr1. Crebinostat increases the density of synapsin-1 punctae along dendrites in cultured neurons. Crebinostat can modulate chromatin-mediated neuroplasticity and exhibits enhanced memory in mice .
HDAC1-IN-13 is an orally active HDAC1 inhibitor with IC50 values of 91, 185, 170, and 280 nM against HDAC1, HDAC2, HDAC3, and HDAC10, respectively, and shows no activity against HDAC4, HDAC5, HDAC6, HDAC7, and HDAC9. HDAC1-IN-13 induces extrinsic apoptosis by activating the caspase-8 pathway and triggers G0/G1 cell cycle arrest. HDAC1-IN-13 can be used for the research of leukemia .
ZYJ-34c is an orally active and potent histone deacetylase inhibitor (HDACi) with IC50s of 0.056 μM and 0.146 μM for HDAC6 and HDAC8, respectively. ZYJ-34c causes G1 phase arrest in low concentration. ZYJ-34c has antiproliferative activities. ZYJ-34c exhibits antitumor potency in MDA-MB-231 and HCT116 xenograft models and possesses antimetastatic potential in a mouse hepatoma-22 (H22) pulmonary metastasis model .
HDAC1-IN-8 (compound 5c) is a potent and selective HDAC1 inhibitor with IC50 values of 11.94, 22.95, >500 µM for HDAC1, HDAC6, HDAC8, respectively. HDAC1-IN-8 shows antiproliferative activity. HDAC1-IN-8 induces cell cycle arrest at G1 and G2/M. HDAC1-IN-8 induces autophagy. HDAC1-IN-8 shows anticancer activity and has the potential for the research of lung cancer .
HDACs/EZH2-IN-1 (Compound 22a) is a HDACs/EZH2 inhibitor (EZH2 Y641N inhibition rate at 50 nM: 98%), with selective inhibition against HDAC1 and HDAC6 (IC50: 0.23 μM and 0.07 μM, respectively). HDACs/EZH2-IN-1 exerts a antiproliferative effect on diffuse large B-cell lymphoma cells harboring an EZH2 mutation and on various acute myeloid leukemia cells. HDACs/EZH2-IN-1 has the ability to induce cell differentiation and Apoptosis .
HDAC3 degrader-1 (Compound Z8) is a selective HDAC3 degrader with a DC50 of 2.42 μM. HDAC3 degrader-1 has almost no effect on HDAC1, HDAC2, and HDAC6. HDAC3 degrader-1 inhibits the activation of the NLRP3 inflammasome and reduces the secretion of IL-1β and caspase-1. HDAC3 degrader-1 shows significant efficacy in septic shock and colitis models. HDAC3 degrader-1 can be used in anti-inflammatory research .
Romidepsin (GMP) (FK 228 (GMP)) is Romidepsin (HY-15149) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Romidepsin (FK 228) is a Histone deacetylase (HDAC) inhibitor with anti-tumor activities. Romidepsin (FK 228) inhibits HDAC1, HDAC2, HDAC4, and HDAC6 with IC50s of 36 nM, 47 nM, 510 nM and 1.4 μM, respectively . Romidepsin (FK 228) is produced by Chromobacterium violaceum, induces cell G2/M phase arrest and apoptosis .
Tubulin/HDAC-IN-4 (compound 9n) is a dual Tubulin and HDAC inhibitor with IC50 values of 0.73, 0.43, 0.62, 2.34 µM for HDAC1, HDAC2, HDAC6, HDAC7, respectively. Tubulin/HDAC-IN-4 inhibits the tubulin polymerization by targeting the colchicine binding site. Tubulin/HDAC-IN-4 induces apoptosis and cell cycle arrest at G2/M phase. Tubulin/HDAC-IN-4 induces a significant elevation of intracellular ROS levels. Tubulin/HDAC-IN-4 shows anti-angiogenesis activity and anticancer activity .
ST13, an ortho-hydroxyanilide, is a selective, slow- and tight-binding HDAC1 and HDAC2 inhibitor with IC50s of 23 nM and 49 nM, respectively. ST13 shows a weak inhibition of HDAC3 (IC50 = 4.30 μM) and HDAC6 (IC50 > 10 μM). The induced fit mechanism of ST13 proceeds through a two-step process: first, the enzyme and inhibitor rapidly form a collision complex (EI), which then slowly transforms into the stable complex E*I. ST13 induces apoptosis in cancer cells. ST13 can be used for the study of melanoma and triple-negative breast .
FNDR-20123 is a safe, first-in-class, and orally active anti-malarial HDAC inhibitor with IC50s of 31 nM and 3 nM for Plasmodium and human HDAC, respectively. FNDR-20123 exerts anti-malarial activity against Plasmodium falciparum asexual stage (IC50=41 nM) and sexual blood stage (IC50=190 nM for male gametocytes). FNDR-20123 inhibits HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8 (IC50=25/29/2/11/282 nM, respectively.) and inhibits Class III HDAC isoforms at nanomolar concentrations .
HDAC-IN-50 is a potent and orally active FGFR and HDAC dual inhibitor with IC50 values of 0.18, 1.2, 0.46, 1.4, 1.3, 1.6, 2.6, 13 nM for FGFR1, FGFR2, FGFR3, FGFR4, HDAC1, HDAC2, HDAC6, HDAC8, respectively. HDAC-IN-50 induces Apoptosis and cell cycle arrest at G0/G1 phase. HDAC-IN-50 decreases the expression of pFGFR1, pERK, pSTAT3. HDAC-IN-50 shows anti-tumor activity .
HDAC-IN-79 (compound 4) is an orally active dual xanthine oxidase-HDAC inhibitor (Xanthine oxidase: IC50=6.6 nM; HDAC1: IC50=134 nM; HDAC2: IC50=284 nM; HDAC3: IC50=173 nM; HDAC6: IC50=1.32 nM;), with significant in vivo anti-hyperuricemia and anti-tumor activities. HDAC-IN-79 is the most potent cell growth inhibitor (IC50=0.706 μM) of leukemia HL60 cells, induces apoptosis and autophagy, and can regulate the expression levels of signature biomarkers associated with intracellular HDAC inhibition .
PROTAC HDAC degrader-2 TFA is the trifluoroacetate salt of PROTAC HDAC degrader-2. PROTAC HDAC degrader-2 is a selective IIb HDACs PROTAC degrader, with DC50s of 13 nM for HDAC6, 29 nM for HDAC10, respectively. PROTAC HDAC degrader-2 exhibits low cytotoxicity against hematological and solid cancer cell lines. PROTAC HDAC degrader-2 can be used for the chemical knockdown of class IIb HDACs. ( Pink: HDAC ligand : (HY-174471), Blue: E3 ligase CRBN Ligand (HY-131717), E3 ligase ligand-linker conjugate (HY-174473)) .
FNDR-20123 free base is a safe, first-in-class, and orally active anti-malarial HDAC inhibitor with IC50s of 31 nM and 3 nM for Plasmodium and human HDAC, respectively. FNDR-20123 free base exerts anti-malarial activity against Plasmodium falciparum asexual stage (IC50=41 nM) and sexual blood stage (IC50=190 nM for male gametocytes). FNDR-20123 free base inhibits HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8 (IC50=25, 29, 2, 11, and 282 nM, respectively) and inhibits Class III HDAC isoforms at nanomolar concentrations .
HDAC1/6-IN-3 is a potent HDAC inhibitor. HDAC1/6-IN-3 shows excellent inhibitory activities against HDAC1 (IC50 = 1.1 nM) and HDAC6 (IC50 = 2.7 nM). HDAC1/6-IN-3 significantly arrests HepG2 cells at the G0/G1 phase and induces apoptosis and pyroptosis. HDAC1/6-IN-3 exhibits significant antitumor activity in the HepG2 xenograft mode. HDAC1/6-IN-3 can be used for the study of cancers such as liver cancer, lung cancer, colon cancer and breast cancer .
DS-103 is an inhibitor for HDAC that inhibits HDAC1, HDAC2, HDAC3, HDAC6 and HDAC8 with IC50s of 0.029, 0.123, 0.022, 0.367 and 9.26 μM, respectively. DS-103 inhibits Plasmodium falciparum 3D7 with IC50 of 5.08 μM. DS-103 exhibits cytotoxicity in cells A2780 and Cal27 with IC50 of 1.48 μM and 1.47 μM, reverses Cisplatin (HY-17394) resistance in A2780 and Cal27 with IC50 of 4.62 μM and 2.23 μM. DS-103 exhibits synergistic effect with Cisplatin (HY-17394), enhances Cisplatin-induced apoptosis .
HDAC-IN-99 is a histone deacetylase (HDAC) inhibitor with an IC50 of 37.73 nM, and it exhibits potent inhibitory activity against HDAC1 (IC50 = 48.09 nM), HDAC2 (IC50 = 300.28 nM) and HDAC6 (IC50 = 9.16 nM). HDAC-IN-99 exerts broad-spectrum antiproliferative activity in various cancer cell lines. HDAC-IN-99 induces S-phase cell cycle arrest and apoptosis in colon cancer cells, increases the acetylation levels of histone H3, histone H4 and α-tubulin, and upregulates the expression of p21 as well as the cleavage of caspase-3. HDAC-IN-99 displays antitumor activity in colon cancer xenograft models. HDAC-IN-99 can be used for the research of colon cancer .
WMJ-J-09 is an HDAC inhibitor with IC50 values of 7.5 nM (HDAC1), 21.3 nM (HDAC2), 18.4 nM (HDAC3), 90.9 nM (HDAC8), 3.9 nM (HDAC6) and 8715.7 nM (HDAC4). WMJ-J-09 blocks the cell cycle and induces apoptosis in cancer cells. WMJ-J-09 induces cancer cell death through the LKB1-AMPK-p38MAPK-p63-survivin signaling cascade.WMJ-J-09 inhibits HDAC enzyme activity, leading to acetylation of key proteins and thereby regulating cancer cell death. WMJ-J-09 can be used in HCT116 cells and FaDu cells research[1][2].
PROTAC HDAC8 Degrader-2 (compound 32a) is a degrader of HDAC8 with a DC50 of 8.9 nM and HDAC6 with a DC50 of 14.3 nM. PROTAC HDAC8 Degrader-2 is composed of PROTAC target protein ligand HDAC8 ligand 1 (HY-168176) (red part), E3 ligase ligand Thalidomide-4-OH (HY-103596) (blue part) and PROTAC Linker 1,5-Diaminopentane (HY-W540541) (black part), among which the conjugate of E3 ubiquitin ligase ligand + Linker is Thalidomide-NH-C5-NH2 (HY-134986) .
LSD1/HDAC-IN-2 (Compound 20c) is the inhibitor for LSD and HDAC, that inhibits LSD1, HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8, with IC50s of 39.0, 1.4, 1.0, 1.3, 2.9 and 16.0 nM, respectively. LSD1/HDAC-IN-2 inhibits the proliferation of cancer cells, especially the colorectal cancer cells. LSD1/HDAC-IN-2 arrests the cell cycle at G2/M phase, inhibits cell migration, and induces apoptosis in HCT-116 and HT-29 cells. LSD1/HDAC-IN-2 exhibits antitumor efficacy in mouse model without significant toxicity .
Wee1/HDAC-IN-1 is a dual Wee1/HDAC inhibitor with an IC50 of 1.2 nM for Wee1 and IC50 values of 196 nM for HDAC1, 156 nM for HDAC3, and 55 nM for HDAC6. Wee1/HDAC-IN-1 exhibits strong antiproliferative activity against MV4-11 cells with an IC50 of 0.076 μM. Wee1/HDAC-IN-1 selectively binds to Wee1 and HDACs. Wee1/HDAC-IN-1 interferes with DNA damage repair pathways and induces apoptosis in MV4-11 cells. Wee1/HDAC-IN-1 Wee1/HDAC-IN-1 can be used for the research of acute myeloid leukemia (AML) .
ALK/HDAC-IN-2 (Compound 19b) is an ALK/HDAC inhibitor with IC₅₀ values for ALK WT and total HDACs of 8 nM and 1.18 μM, respectively. ALK/HDAC-IN-2 exhibits inhibitory activity against ALK mutants G1202R, F1174L, and L1196M, with IC₅₀ values of 2.74, 9.23, and 34.28 nM, respectively. ALK/HDAC-IN-2 shows potent and selective inhibition against HDAC1 (IC₅₀ = 0.24 μM), while its inhibitory activity against HDAC7, HDAC6, and HDAC11 is weak (IC₅₀ > 10 μM). ALK/HDAC-IN-2 has broad-spectrum anti-proliferative activity against various cancer cells, inducing cell cycle arrest and apoptosis. ALK/HDAC-IN-2 can be used for the study of neuroblastoma .
HDAC-IN-88 (Compound HJ-9) is the inhibitor for HDAC that inhibits HDAC6, HDAC1, HDAC2, HDAC8 and HDAC3 with IC50s of 0.226, 1.103, 2.308, 3.255 and 3.864 μM, respectively. HDAC-IN-88 inhibits the proliferation of cancer cell HepG2, HCT116 and MV4-11 with IC50 of 5.47, 9.78 and 0.38 μM, inhibits the migration of HCT116, arrests the cell cycle at G0/G1 phase, and induces apoptosis and autophagy in MV4-11. HDAC-IN-88 reduces ROS level and mitochondrial membrane potential. HDAC-IN-88 exhibits antimalarial activity that inhibits P. falciparum 3D7 with EC50 of 165 nM. HDAC-IN-88 also exhibits anti-angiogenic activity .
HDAC-IN-93 is a HDAC inhibitor with promising total pan-HDAC inhibitory activity. HDAC-IN-93 demonstrates significant broad-spectrum antiproliferative activity across various cancer cell lines. HDAC-IN-93 induces cell apoptosis along with necrosis. HDAC-IN-93 can be used for the studies of prostate cancer and breast cancer .
PIM-1/HDAC-IN-1 (compound 4d) is a PIM-1 inhibitor, with an IC50 of 343.87 nM. PIM-1/HDAC-IN-1 has strong inhibitory activity and selectivity against HDAC 1 and HDAC 6, with IC50 values of 63.65 and 62.39 nM, respectively. PIM-1/HDAC-IN-1 exhibits apoptosis inducing potential in MCF-7 cell lines. PIM-1/HDAC-IN-1 shows pre-G1 apoptosis and cell cycle arrest at G2/M phase .
4-Ethylphenyl sulfate is an orally active and brain-penetrant gut microbial metabolite. 4-Ethylphenyl sulfate downregulates Bcl2 expression, upregulates Bax expression, and induces cancer cell apoptosis via the endogenous apoptotic pathway. 4-Ethylphenyl sulfate induces G2/M cell cycle arrest and reactive oxygen species (ROS) production. 4-Ethylphenyl sulfate impairs oligodendrocyte maturation, reduces oligodendrocyte-neuron interactions, decreases axonal myelination levels, and shifts the oligodendrocyte population toward immature precursor cells. 4-Ethylphenyl sulfate alters brain region-specific neural activity and functional connectivity in mice, and correlates with anxiety-like behaviors in mice .
NHNB is a selective HDAC8 inhibitor (IC50 = 66.0 μM) and Peptidoglycan N-acetylglucosamine (GlcNAc) deacetylases (PGNGdacs) inhibitor. NHNB shows antibacterial and bactericidal activity against B. anthracis and B. cereus. NHNB can be used for the research of acute myeloid leukemia, Bacillus anthracis infection, and Bacillus cereus infection .
HDAC1-IN-14 is an indole-based benzamide selective HDAC1 inhibitor with an IC50 of 77 nM. HDAC1-IN-14 acts as an antiproliferative agent, with GI50 values ranging from nanomolar to low micromolar levels in various cancer cells. HDAC1-IN-14 induces G0-G1 cell cycle arrest in colon cancer cells. HDAC1-IN-14 upregulates the expression of Caspase-3, Cyto-C and Bax, and downregulates the expression of AKT-1. HDAC1-IN-14 can be used in research related to leukemia, non-small cell lung cancer, colon cancer, central nervous system cancer, melanoma, ovarian cancer, renal cancer, prostate cancer and breast cancer .
JAK/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 .
Kevetrin (3-Cyanopropyl carbamimidothioate; 4-Isothioureidobutyronitrile) is an apoptosis inducer that exhibits p53-dependent and p53-independent antitumor activity. In TP53 wild-type models, Kevetrin activates and stabilizes the p53 protein by altering the processing of MDM2, thereby inducing cell cycle arrest and apoptosis. Kevetrin shows higher sensitivity in mutant models. Kevetrin is applicable for the research of various cancers including acute myeloid leukemia and breast cancer .
MC2590 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 .
Romidepsin (GMP) (FK 228 (GMP)) is Romidepsin (HY-15149) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Romidepsin (FK 228) is a Histone deacetylase (HDAC) inhibitor with anti-tumor activities. Romidepsin (FK 228) inhibits HDAC1, HDAC2, HDAC4, and HDAC6 with IC50s of 36 nM, 47 nM, 510 nM and 1.4 μM, respectively . Romidepsin (FK 228) is produced by Chromobacterium violaceum, induces cell G2/M phase arrest and apoptosis .
Vorinostat (GMP) is a GMP grade Vorinosta (HY-10221). GMP-grade small molecules can be used as auxiliary agents in cell therapy. Vorinostat is a potent, orally available HDAC1, HDAC2, HDAC3 (Class I), HDAC6 and Inhibitors of HDAC7 (Class II) and Class IV (HDAC11) .
Tubastatin A (GMP) is the Tubastatin A (HY-13271A) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Tubastatin A is a potent and selective HDAC6 inhibitor with an IC50 of 15 nM in a cell-free assay, and is selective (1000-fold more) against all other isozymes except HDAC8 (57-fold more). Tubastatin A also inhibits HDAC10 and metallo-β-lactamase domain-containing protein 2 (MBLAC2).
Romidepsin (GMP) (FK 228 (GMP)) is Romidepsin (HY-15149) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Romidepsin (FK 228) is a Histone deacetylase (HDAC) inhibitor with anti-tumor activities. Romidepsin (FK 228) inhibits HDAC1, HDAC2, HDAC4, and HDAC6 with IC50s of 36 nM, 47 nM, 510 nM and 1.4 μM, respectively . Romidepsin (FK 228) is produced by Chromobacterium violaceum, induces cell G2/M phase arrest and apoptosis .
Vorinostat (GMP) is a GMP grade Vorinosta (HY-10221). GMP-grade small molecules can be used as auxiliary agents in cell therapy. Vorinostat is a potent, orally available HDAC1, HDAC2, HDAC3 (Class I), HDAC6 and Inhibitors of HDAC7 (Class II) and Class IV (HDAC11) .
Tubastatin A (GMP) is the Tubastatin A (HY-13271A) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Tubastatin A is a potent and selective HDAC6 inhibitor with an IC50 of 15 nM in a cell-free assay, and is selective (1000-fold more) against all other isozymes except HDAC8 (57-fold more). Tubastatin A also inhibits HDAC10 and metallo-β-lactamase domain-containing protein 2 (MBLAC2).
Daphnegiravone D (compound 70) is an HDAC6 inhibitor with anti-hepatocellular carcinoma activity. Daphnegiravone D can induce apoptosis and selectively inhibit the proliferation of liver cancer cells through the p38 and JNK MAPK pathways .
The HDAC6 protein coordinates multiple functions, deacetylating histones and proteins such as tubulin and CTTN. Its role in epigenetic repression affects transcription, cell cycle, and development. HDAC6 Protein, Human (sf9, His) is the recombinant human-derived HDAC6 protein, expressed by Sf9 insect cells, with C-8*His labeled tag.
The HDAC6 protein coordinates multiple functions, deacetylating histones and proteins such as tubulin and CTTN. Its role in epigenetic repression affects transcription, cell cycle, and development. HDAC6 Protein, Human (His) is the recombinant human-derived HDAC6 protein, expressed by E. coli , with N-6*His labeled tag.
Romidepsin-d7 (FK 228-d7) is deuterium labeled Romidepsin. Romidepsin (FK 228) is a Histone deacetylase (HDAC) inhibitor with anti-tumor activities. Romidepsin (FK 228) inhibits HDAC1, HDAC2, HDAC4, and HDAC6 with IC50s of 36 nM, 47 nM, 510 nM and 1.4 μM, respectively . Romidepsin (FK 228) is produced by Chromobacterium violaceum, induces cell G2/M phase arrest and apoptosis .
HDAC6-IN-3 (Compound 14), an antiprostate cancer agent, is a potent, orally active HDAC6 inhibitor with IC50s ranging from 0.02-1.54 μM for HDAC1/2/3/6/8/10. HDAC6-IN-3 is also an effective MAO-A (IC50=0.79 μM) and LSD1 inhibitor . HDAC6-IN-3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
HDAC6-IN-50 (Compound 4) is a potent HDAC6 inhibitor with an IC50 of 35 nM. HDAC6-IN-50 can be used for the study of Parkinson's disease (PD) and Alzheimer's disease (AD) research .
Thalidomide-F-NH-C6-adize is the conjugate of an E3 ligase (Cereblon) ligand and a linker, and can be used for synthesis of PROTAC HDAC6 degrader 4 (HY-172359) .
Hdac6 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Hdac6 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
HDAC6 Human Pre-designed siRNA Set A contains three designed siRNAs for HDAC6 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
HDAC6 Rat Pre-designed siRNA Set A contains three designed siRNAs for HDAC6 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
Tubastatin A (GMP) is the Tubastatin A (HY-13271A) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Tubastatin A is a potent and selective HDAC6 inhibitor with an IC50 of 15 nM in a cell-free assay, and is selective (1000-fold more) against all other isozymes except HDAC8 (57-fold more). Tubastatin A also inhibits HDAC10 and metallo-β-lactamase domain-containing protein 2 (MBLAC2).
Romidepsin (GMP) (FK 228 (GMP)) is Romidepsin (HY-15149) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Romidepsin (FK 228) is a Histone deacetylase (HDAC) inhibitor with anti-tumor activities. Romidepsin (FK 228) inhibits HDAC1, HDAC2, HDAC4, and HDAC6 with IC50s of 36 nM, 47 nM, 510 nM and 1.4 μM, respectively . Romidepsin (FK 228) is produced by Chromobacterium violaceum, induces cell G2/M phase arrest and apoptosis .
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Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
MedchemExpress Validation 03
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
MedchemExpress Validation 04
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
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