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Sinefungin is a potent inhibitor of virion mRNA(guanine-7-)-methyltransferase, mRNA(nucleoside-2'-)-methyltransferase, and viral multiplication . Sinefungin, a SET7/9 inhibitor, ameliorates renal fibrosis by inhibiting H3K4 methylation .
OICR-9429, a chemical probe, is high affinity WD repeat domain 5 (WDR5) inhibitor, competitively blocks WDR5 interaction with MLL protein via binding the central peptide-binding pocket of WDR5. OICR-9429 can suppress histone H3K4 trimethylation and can be used for the research of various cancers including non-MLL-rearranged leukaemia, colon, pancreatic, prostate cancer and bladder cancer (BCa) .
CPI-455 is a specific, pan-KDM5 inhibitor with an IC50 of 10 nM for KDM5A. CPI-455 mediates KDM5 inhibition, elevates global levels of H3K4me3, and decreases the number of drug-tolerant persister cancer cells in multiple cancer cell line models treated with standard chemotherapy or targeted agents .
KDM5-C70 is an ethyl ester derivative of KDM5-C49 and a potent, cell-permeable and pan-KDM5 histone demethylase inhibitor. KDM5-C70 has an antiproliferative effect in myeloma cells, leading to genome-wide elevation of H3K4me3 levels .
Bomedemstat (IMG-7289) is an orally active and irreversible lysine-specific demethylase 1 (LSD1) inhibitor. Bomedemstat can increase H3K4 and H3K9 methylation, and then alter gene expression. Bomedemstat shows anti-cancer activities, inhibits cancer cell proliferation and induces apoptosis .
A-366, a chemical probe, is a potent, highly selective, peptide-competitive histone methyltransferase G9a inhibitor with IC50s of 3.3 and 38 nM for G9a and GLP (EHMT1), respectively. A-366 shows >1000-fold selectivity over 21 other methyltransferases. A-366 is also a potent, nanomolar inhibitor of the Spindlin1-H3K4me3-interaction (IC50=182.6 nM). A-366 displays high affinity at human histamine H3 receptor (Ki=17 nM) and shows subtype selectivity among subsets of the histaminergic and dopaminergic receptor families .
MM-102 (HMTase Inhibitor IX) is a cell-permeable and tightly binding inhibitor of MLL1-WDR5 interaction (IC50=2.4 nM). MM-102 can specifically inhibit the growth and induce apoptosis of leukemia cells containing MLL1 fusion protein, and reduce renal fibrosis and inflammation in mice with ischemia-reperfusion injury. In addition, MM-102 also acts as an H3K4 histone methyltransferase inhibitor to improve the development of porcine somatic cell nuclear transfer (SCNT) embryos .
KDOAM-25 citrate is a potent and highly selective histone lysine demethylases 5 (KDM5) inhibitor with IC50s of 71 nM, 19 nM, 69 nM, 69 nM for KDM5A, KDM5B, KDM5C, KDM5D, respectively. KDOAM-25 citrate increases global H3K4 methylation at transcriptional start sites and impairs proliferation in multiple myeloma MM1S cells .
BRD4770 is a histone methyltransferase G9a inhibitor. BRD4770 reduces di- and trimethylation of lysine 9 on histone H3 (H3K9) with an EC50 of 5 μM, and has less or little effect toward H3K27me3, H3K36me3, H3K4me3, and H3K79me3. BRD4770 can activate the ataxia telangiectasia mutated (ATM) pathway and induce cell senescence .
CPI-455 hydrochloride is a specific, pan-KDM5 inhibitor with an IC50 of 10 nM for KDM5A. CPI-455 hydrochloride mediates KDM5 inhibition, elevates global levels of H3K4me3, and decreases the number of drug-tolerant persister cancer cells in multiple cancer cell line models treated with standard chemotherapy or targeted agents .
T-448 is a specific, orally active, CNS-penetrant and irreversible inhibitor of lysine-specific demethylase 1 (LSD1, an H3K4 demethylase), with an IC50 of 22 nM. T-448 enhances H3K4 methylation in primary cultured rat neurons .
iZMYND8-34 is a ZMYND8 inhibitor with an IC50 of 0.66 μM. iZMYND8-34 inhibits the binding of H3K4me1–H3K14ac peptide to the ZMYND8 protein. iZMYND8-34 inhibits ZMYND8’s histone recognition. iZMYND8-34 blocks neuroendocrine prostate cancer development .
Bomedemstat (IMG-7289) ditosylate is an orally active and irreversible lysine-specific demethylase 1 (LSD1) inhibitor. Bomedemstat ditosylate can increase H3K4 and H3K9 methylation, and then alter gene expression. Bomedemstat ditosylate shows anti-cancer activities, inhibits cancer cell proliferation and induces apoptosis .
KDM5A-IN-1 is a potent, orally bioavailable pan-histone lysine demethylases 5 (KDM5) inhibitor with IC50s of 45 nM, 56 nM and 55 nM for KDM5A, KDM5B and KDM5C, respectively, and with an EC50 value of 960 nM for PC9 H3K4Me3. KDM5A-IN-1 is significantly less potent against other KDM5B enzymes (1A, 2B, 3B, 4C, 6A, 7B) .
MRK-740, a chemical probe, is a potent, selective and substrate-competitive PRDM9 histone methyltransferase inhibitor with an IC50 of 80?nM. MRK-740 is more selective for PRDM9 than other histone methyltransferases and other non-epigenetic targets. MRK-740 reduces PRDM9-dependent trimethylation of H3K4 (IC50?=?0.8?μM) .
MM-401 (TFA) is a MLL1 H3K4 methyltransferase inhibitor. MM-401 inhibits MLL1 activity (IC50 = 0.32 μM) by blocking MLL1-WDR5 interaction. MM-401 can induce cell cycle arrest, apoptosis and differentiation. MM-401 can be used for the research of MLL leukemia .
Bomedemstat (IMG-7289) hydrochloride is an orally active and irreversible lysine-specific demethylase 1 (LSD1) inhibitor. Bomedemstat hydrochloride can increase H3K4 and H3K9 methylation, and then alter gene expression. Bomedemstat hydrochloride shows anti-cancer activities, inhibits cancer cell proliferation and induces apoptosis .
YUKA1 is a potent and cell permeable Lysine demethylase 5A (KDM5A) inhibitor, with an IC50 of 2.66 μM. YUKA1 has less inhibitory active on KDM5C (IC50 = 7.12 μM) and is inactive on KDM5B, KDM6A or KDM6B. YUKA1 can increase H3K4me3 levels and inhibit cell proliferation. YUKA1 can be used for the research of cancer, such as lung and breast cancers .
HBI-2375 (HYBI-084) is a brain-penetrant WDR5 inhibitor with an IC50 of 4.48 nM. HBI-2375 binds to the WINR5 and disrupts MLL1-WDR5 protein-protein interactions. HBI-2375 inhibits cancer cells proliferation and shows anti-tumor activity in AML mouse models, and increases tumor CD8 + cytotoxic T lymphocyte infiltration. HBI-2375 inhibits hERG with an IC50 of 17 µM .
MM-401 is a MLL1 H3K4 methyltransferase inhibitor. MM-401 inhibits MLL1 activity (IC50 = 0.32 μM) by blocking MLL1-WDR5 interaction. MM-401 can induce cell cycle arrest, apoptosis and differentiation. MM-401 can be used for the research of MLL leukemia .
KDOAM-25 is a potent and highly selective histone lysine demethylases 5 (KDM5) inhibitor with IC50s of 71 nM, 19 nM, 69 nM, 69 nM for KDM5A, KDM5B, KDM5C, KDM5D, respectively. KDOAM-25 increases global H3K4 methylation at transcriptional start sites and impairs proliferation in multiple myeloma MM1S cells .
JQKD82 (JADA82) trihydrochloride is a cell-permeable and selective KDM5 inhibitor. JQKD82 trihydrochloride increases H3K4me3 and can be used for the research of multiple myeloma .
KDM5B-IN-4 (compound 11ad) is a lysine demethylase 5B (KDM5B) inhibitor with an IC50 of 0.025 μM KDM5B-IN-4 increases substrate H3K4me1/2/3 level by inhibiting KDM5B in PC-3 cells. KDM5B-IN-4 downregulates PI3K/AKT. KDM5B-IN-4 reduces tumor volume in mice and shows less toxic to organs .
LD-110 is a highly efficient and effective LSD1 PROTAC degrader (DC50 = 0.44 μM). LD-110 promotes LSD1 degradation and increases the level of H3K4 dimethylation in a ubiquitin-proteasome-dependent manner. LD-110 inhibits the growth and survival of multiple esophagus squamous cancer cell (ESCC) lines by inducing apoptosis. LD-110 can be used for the study of esophagus squamous cancer .
GT-653 is a PROTAC degrader for lysine-specific demethylase 5B (KDM5B). GT-653 degrades 68.35% KDM5B at 10 μM in a ubiquitin proteasome-dependent manner, upregulates H3K4me3 levels, and activates the type-I interferon signaling pathway in prostate cancer cells 22RV1. (Pink: KDM5B ligand (HY-158433); Black: Linker (HY-W004896); Blue: E3 ligase ligand (HY-103596))
Deoxyandrographolide is an orally active lactone found in the Andrographis paniculata Nees. Deoxyandrographolide shows a KD of 38.4 μM of HDAC1. Deoxyandrographolide enhances GLUT4 plasma membrane translocation, activates PI3K and AMPK-dependent signaling pathways, suppresses fasting blood glucose, serum insulin, triglycerides, and LDL-cholesterol levels. Deoxyandrographolide enhances HDAC1 expression via inhibited ubiquitination degradation, represses H3K4me3, improves chromosome stability, and restrains aging biomarkers p16, p21, γH2A.X, p53 and ROS production. Deoxyandrographolide interacts with Foot-and-Mouth Disease Virus 3Cpro active site, inhibits protease and IFN-antagonist activity, derepresses ISG expression, and inhibits viral replication. Deoxyandrographolide can be used for the researches of type 2 diabetes mellitus, vascular senescenceand virus infection .
H3K4(Me) (1-20), a histone peptide. H3K4me is an intricately regulated posttranslational modification, which is broadly associated with enhancers and promoters of actively transcribed genomic loci .
MM-589 is a potent inhibitor of WD repeat domain 5 (WDR5) and mixed lineage leukemia (MLL) protein-protein interaction. MM-589 binds to WDR5 with an IC50 of 0.90 nM and inhibits the MLL H3K4 methyltransferase activity with an IC50 of 12.7 nM .
Arborinine is a potent and orally activeLSD1 inhibitor. Arborinine increases the expression of H3K4me1/2, H3K9me1/2, E-cad protein and decreases the expression of UBE2O protein level. Arborinine induces cell cycle arrest at S phase. Arborinine shows antitumor activity .
Bomedemstat (IMG-7289) dihydrochloride is an orally active and irreversible lysine-specific demethylase 1 (LSD1) inhibitor. Bomedemstat dihydrochloride can increase H3K4 and H3K9 methylation, and then alter gene expression. Bomedemstat dihydrochloride shows anti-cancer activities, inhibits cancer cell proliferation and induces apoptosis .
MS31 trihydrochloride is a potent, highly affinity and selective fragment-like methyllysine reader protein spindlin 1 (SPIN1) inhibitor. MS31 trihydrochloride potently inhibits the interactions between SPIN1 and H3K4me3 (IC50=77 nM, AlphaLISA; 243 nM, FP). MS31 trihydrochloride selectively binds Tudor domain II of SPIN1 (Kd=91 nM). MS31 trihydrochloride potently inhibits binding of trimethyllysine-containing peptides to SPIN1, and is not toxic to nontumorigenic cells .
H3K4(Me3) (1-20) is a histone peptide. Trimethylation of histone H3 on lysine 4 (H3K4 me3) is found in active euchromatin but not in silent heterochromatin .
CBB1007 trihydrochloride is a reversible and selective LSD1 inhibitor with an IC50 of 5.27 µM for human LSD1. CBB1007 trihydrochloride significantly blocks the demethylase activity of LSD1 on H3K4Me2 and H3K4Me. CBB1007 trihydrochloride shows selectivity for LSD1 over LSD2 or JARID1A, and induces differentiation-related genes in pluripotent cells. CBB1007 trihydrochloride is studied in non-pluripotent cancer research, targeting teratocarcinoma, embryonic carcinoma, and seminoma .
KDOAM-25 trihydrochloride is a potent and highly selective histone lysine demethylases 5 (KDM5) inhibitor with IC50s of 71 nM, 19 nM, 69 nM, 69 nM for KDM5A, KDM5B, KDM5C, KDM5D, respectively. KDOAM-25 trihydrochloride increases global H3K4 methylation at transcriptional start sites and impairs proliferation in multiple myeloma MM1S cells .
MM-589 TFA is a potent inhibitor of WD repeat domain 5 (WDR5) and mixed lineage leukemia (MLL) protein-protein interaction. MM-589 binds to WDR5 with an IC50 of 0.90 nM and inhibits the MLL H3K4 methyltransferase activity with an IC50 of 12.7 nM .
KDM4-IN-4 (compound 47) is a potent histone lysine demethylase 4 (KDM4) inhibitor with a modest affinity binding to ~80 μM for KDM4A-Tudor domain. KDM4-IN-4 can inhibit H3K4Me3 binding to the Tudor domain in cells with an EC50 value of 105 μM. KDM4-IN-4 can be used for researching anticancer .
T-448 free base is a specific, orally active, CNS-penetrant and irreversible inhibitor of lysine-specific demethylase 1 (LSD1, an H3K4 demethylase), with an IC50 of 22 nM. T-448 free base enhances H3K4 methylation in primary cultured rat neurons .
MM-589 (racemic mixture) TFA, is a racemic mixture of MM-589 TFA (HY-100869A). MM-589 TFA is a potent inhibitor of WD repeat domain 5 (WDR5) and mixed lineage leukemia (MLL) protein-protein interaction. MM-589 binds to WDR5 with an IC50 of 0.90 nM and inhibits the MLL H3K4 methyltransferase activity with an IC50 of 12.7 nM .
cis-4-Br-2,5-F2-PCPA (S1024) is a selective inhibitor of lysine-specific demethylase 1 (LSD1), with a Ki value of 94 nM instead of 8.4 μM for LSD2. There is aberrant expression of LSD1 in cancer stem cells, cis-4-Br-2,5-F2-PCPA inhibits LSD1 cell proliferation and by increasing the level of dimethylated histone H3 at K4 (H3K4) in CCRF-CEM cells .
JQKD82 (JADA82) dihydrochloride is a cell-permeable and selective KDM5 inhibitor. JQKD82 dihydrochloride increases H3K4me3 and can be used for the research of multiple myeloma .
E67-2, as the E67 derivative, is a low-toxicity, selective KIAA1718 Jumonji domain inhibitor with an IC50 value of 3.4 µM. E67-2 selectively inhibits histone H3 lysine 9 (H3K9) Jumonji demethylase as well as histone H3 lysine 4 (H3K4) demethylase .
LSD1-IN-47 is a highly efficient PROTAC degrader targeting LSD1 (IC50 = 43 nM). LSD1-IN-47 does not alter LSD1 protein levels and does not increase the histone marker H3K4me2. LSD1-IN-47 can be used for the study of colon carcinoma .
Tubulin/LSD1-IN-1 is an effective dual inhibitor of Tubulin polymerization and LSD1 (IC50 = 1.72 μM). Tubulin/LSD1-IN-1 has broad-spectrum antiproliferative activity against cancer cell lines. Tubulin/LSD1-IN-1 inhibits tubulin polymerization by targeting colchicine binding sites, thereby disrupting the microtubule network in gastric cancer cells. Tubulin/LSD1-IN-1 increases the methylation levels of H3K4me1/2 and H3K9me2/3, thereby achieving epigenetic regulation. Tubulin/LSD1-IN-1 induces G2/M arrest, promotes apoptosis, and effectively inhibits colony formation of gastric cancer cells .
MS31 is a potent, highly affinity and selective fragment-like methyllysine reader protein spindlin 1 (SPIN1) inhibitor. MS31 potently inhibits the interactions between SPIN1 and H3K4me3 (IC50=77 nM, AlphaLISA; 243 nM, FP). MS31 selectively binds Tudor domain II of SPIN1 (Kd=91 nM). MS31 potently inhibits binding of trimethyllysine-containing peptides to SPIN1. MS31 is not toxic to nontumorigenic cells .
LSD1/TLK1-IN-1 is an orally active LSD1, TLK1, TLK2, TTK inhibitor with an LSD1IC50 of 0.247 μM. LSD1/TLK1-IN-1 suppresses phosphorylation of Nek1 at T141 and Rad9 at S328, abrogates the TLK1>Nek1>ATR>Chk1 axis, protects H3K4me1/2 from demethylation, and does not affect LSD2, MAO-A, or MAO-B. LSD1/TLK1-IN-1 induces apoptosis, bypasses cell-cycle arrest, suppresses tumor growth, acts as a weak D4R antagonist, downregulates PD-L1 expression, enhances T-cell killing response, inhibits gastric cancer cell proliferation, shows minimal toxicity, and has no significant effect on normal prostate cells. LSD1/TLK1-IN-1 can be used for the research of prostate cancer and gastric cancer .
Sinefungin (Standard) is the analytical standard of Sinefungin (HY-101938). This product is intended for research and analytical applications. Sinefungin is a potent inhibitor of virion mRNA(guanine-7-)-methyltransferase, mRNA(nucleoside-2'-)-methyltransferase, and viral multiplication . Sinefungin, a SET7/9 inhibitor, ameliorates renal fibrosis by inhibiting H3K4 methylation .
CBB1007 hydrochloride is a reversible and selective LSD1 inhibitor with an IC50 of 5.27 µM for human LSD1. CBB1007 hydrochloride significantly blocks the demethylase activity of LSD1 on H3K4Me2 and H3K4Me. CBB1007 hydrochloride shows selectivity for LSD1 over LSD2 or JARID1A, and induces differentiation-related genes in pluripotent cells. CBB1007 hydrochloride is studied in non-pluripotent cancer research, targeting teratocarcinoma, embryonic carcinoma, and seminoma .
CBB1007 is a reversible and selective LSD1 inhibitor with an IC50 of 5.27 µM for human LSD1. CBB1007 significantly blocks the demethylase activity of LSD1 on H3K4Me2 and H3K4Me. CBB1007 shows selectivity for LSD1 over LSD2 or JARID1A, and induces differentiation-related genes in pluripotent cells. CBB1007 is studied in non-pluripotent cancer research, targeting teratocarcinoma, embryonic carcinoma, and seminoma .
LSD1-IN-35 (Compound Z-1) is a selective LSD1 Inhibitor (IC50: 108 nM). LSD1-IN-35 inhibits the demethylation on H3K4me1/2. LSD1-IN-35 is an immunomodulator. LSD1-IN-35 promotes response of gastric cancer cells to T-cell killing effect by decreasing PD-L1 expression and further attenuates the PD-1/PD-L1 interaction .
S9-CMC1 TFA is a covalent peptide lysine-specific demethylase 1 (LSD1) inhibitor with an IC50 value of 2.53 μM. S9-CMC1 TFA specifically recognizes Cys360 in the enzyme-active region. S9-CMC1 TFA inhibits LSD1 activity, increasing H3K4me1 and H3K4me2 levels, leading to G1 cell cycle arrest and apoptosis and inhibiting cell proliferation. S9-CMC1 TFA significantly inhibits tumor growth in A549 xenograft animal models .
LD-110 trihydrochloride is a highly efficient and effective LSD1 PROTAC degrader (DC50 = 0.44 μM). LD-110 trihydrochloride promotes LSD1 degradation and increases the level of H3K4 dimethylation in a ubiquitin-proteasome-dependent manner. LD-110 trihydrochloride inhibits the growth and survival of multiple esophagus squamous cancer cell (ESCC) lines by inducing apoptosis. LD-110 trihydrochloride can be used for the study of esophagus squamous cancer .
ZJY-54 is an orally active dual-target inhibitor of EGFR/LSD1, with IC50 values of 3.8 nM and 0.6 μM, respectively. ZJY-54 can inhibit the proliferation of non-small cell lung cancer cells, induce the accumulation ofH3K4me2 and H3K9me2, and inhibit the phosphorylation of the EGFR signaling pathway. ZJY-54 has anti-tumor activity .
PRMT/HKMT-IN-1 is an epigenetic multi-target protein arginine methyltransferases (PRMTs) and histone lysine methyltransferases (HKMTs) inhibitor. PRMT/HKMT-IN-1 inhibits Aspergillus nidulans RmtA with an IC50 of 29 μM. PRMT/HKMT-IN-1 inhibits human PRMT1, p300/CBP HAT, CARM1, SET7, SIRT1 and SIRT2. PRMT/HKMT-IN-1 inhibits methylation of histone H3K4, H4R3, and H3R17 residues. CBP/p300-IN-23 induces apoptosis, arrests cell cycle in S phase, and triggers granulocytic differentiation in leukemia cells. PRMT/HKMT-IN-1 can be used for the research of leukemia .
LD-110 triTFA is a highly efficient and effective LSD1 PROTAC degrader (DC50 = 0.44 μM). LD-110 triTFA promotes LSD1 degradation and increases the level of H3K4 dimethylation in a ubiquitin-proteasome-dependent manner. LD-110 triTFA inhibits the growth and survival of multiple esophagus squamous cancer cell (ESCC) lines by inducing apoptosis. LD-110 triTFA can be used for the study of esophagus squamous cancer .
LSD1/2-IN-3 is a selective inhibitor of lysine-specific demethylase 1 (LSD1), with a Ki value of 11 nM instead of 7 μM for LSD2. There is aberrant expression of LSD1 in cancer stem cells, LSD1/2-IN-1 inhibits LSD1 cell proliferation .
LSD1-IN-48 is a tranylcypromine-pyrimidine derivative and selective LSD1 inhibitor with a human IC50 of 7.87 nM. LSD1-IN-48 increases H3K4me1/2 histone methylation levels. LSD1-IN-48 induces apoptosis, upregulates CD86, downregulates SOX2 and CD44, inhibits proliferation in cancer cells. LSD1-IN-48 can be used for the research of acute myeloid leukemia .
FRC-222 is a CHD1 tandem chromodomain inhibitor with a Kd of 0.15 μM and an IC50 of 0.18 μM. FRC-222 binds to the H3K4me3 binding site of CHD1 tandem chromodomain via aromatic cage interactions and extended ligand contacts. FRC-222 can be used for the research of prostate cancer[1].
MS40 is a WDR5 PROTAC degrader (Kd = 125 nM). MS40 promotes the ubiquitination and degradation of WDR5. MS40-induced WDR5 degradation leads to the dissociation of the MLL/KMT2A complex from chromatin, resulting in decreased H3K4me2 levels. MS40 can be used in the study of primary leukemia .
EML631 is a SPIN1 inhibitor with a Kd of 3-7 μM. EML631 interacts with the second Tudor domain of SPIN1 and blocks its ability to read the H3K4me3 histone mark. EML631 inhibits the coactivator activity of SPIN1 in the Wnt signaling pathway and reduces the activity of Wnt response reporter genes. EML631 can be used in cancer-related research .
FRC-303 is a CHD1 inhibitor with a Kd of 0.14 μM and an IC50 of 0.18 μM. FRC-303 binds to the H3K4me3 binding site of CHD1 tandem chromodomain, forms aromatic cage interactions and extended ligand contacts, acts as a methyl-lysine mimic, and occupies natural peptide ligand-binding regions. FRC-303 can be used for the research of prostate cancer .
CPI-455 (Standard) is the analytical standard of CPI-455 (HY-100421). This product is intended for research and analytical applications. CPI-455 is a specific, pan-KDM5 inhibitor with an IC50 of 10 nM for KDM5A. CPI-455 mediates KDM5 inhibition, elevates global levels of H3K4me3, and decreases the number of drug-tolerant persister cancer cells in multiple cancer cell line models treated with standard chemotherapy or targeted agents .
YUKA1 (Standard) is the analytical standard of YUKA1 (HY-100764). This product is intended for research and analytical applications. YUKA1 is a potent and cell permeable Lysine demethylase 5A (KDM5A) inhibitor, with an IC50 of 2.66 μM. YUKA1 has less inhibitory active on KDM5C (IC50 = 7.12 μM) and is inactive on KDM5B, KDM6A or KDM6B. YUKA1 can increase H3K4me3 levels and inhibit cell proliferation. YUKA1 can be used for the research of cancer, such as lung and breast cancers .
DC551040 is an orally active and selective lysine demethylase 1 (LSD1) inhibitor with a human IC50 of 2.14 nM. DC551040 binds to LSD1 via π-π stacking with Trp552, polar interactions with Phe538, and covalent adduct formation with FAD, and disrupts the LSD1-GFI1B-CoREST complex. DC551040 induces H3K4me2 accumulation, apoptosis, and cell differentiation, activates STAT5, NF-κB, AKT, and IL6-STAT3 pathways, and upregulates IL6 expression. DC551040 can be used for the research of acute myeloid leukemia .
KDM5A-IN-1 (Standard) is the analytical standard of KDM5A-IN-1 (HY-100014). This product is intended for research and analytical applications. KDM5A-IN-1 is a potent, orally bioavailable pan-histone lysine demethylases 5 (KDM5) inhibitor with IC50s of 45 nM, 56 nM and 55 nM for KDM5A, KDM5B and KDM5C, respectively, and with an EC50 value of 960 nM for PC9 H3K4Me3. KDM5A-IN-1 is significantly less potent against other KDM5B enzymes (1A, 2B, 3B, 4C, 6A, 7B) .
MM-401 is a MLL1 H3K4 methyltransferase inhibitor. MM-401 inhibits MLL1 activity (IC50 = 0.32 μM) by blocking MLL1-WDR5 interaction. MM-401 can induce cell cycle arrest, apoptosis and differentiation. MM-401 can be used for the research of MLL leukemia .
H3K4(Me) (1-20), a histone peptide. H3K4me is an intricately regulated posttranslational modification, which is broadly associated with enhancers and promoters of actively transcribed genomic loci .
H3K4(Me3) (1-20) is a histone peptide. Trimethylation of histone H3 on lysine 4 (H3K4 me3) is found in active euchromatin but not in silent heterochromatin .
S9-CMC1 TFA is a covalent peptide lysine-specific demethylase 1 (LSD1) inhibitor with an IC50 value of 2.53 μM. S9-CMC1 TFA specifically recognizes Cys360 in the enzyme-active region. S9-CMC1 TFA inhibits LSD1 activity, increasing H3K4me1 and H3K4me2 levels, leading to G1 cell cycle arrest and apoptosis and inhibiting cell proliferation. S9-CMC1 TFA significantly inhibits tumor growth in A549 xenograft animal models .
Deoxyandrographolide is an orally active lactone found in the Andrographis paniculata Nees. Deoxyandrographolide shows a KD of 38.4 μM of HDAC1. Deoxyandrographolide enhances GLUT4 plasma membrane translocation, activates PI3K and AMPK-dependent signaling pathways, suppresses fasting blood glucose, serum insulin, triglycerides, and LDL-cholesterol levels. Deoxyandrographolide enhances HDAC1 expression via inhibited ubiquitination degradation, represses H3K4me3, improves chromosome stability, and restrains aging biomarkers p16, p21, γH2A.X, p53 and ROS production. Deoxyandrographolide interacts with Foot-and-Mouth Disease Virus 3Cpro active site, inhibits protease and IFN-antagonist activity, derepresses ISG expression, and inhibits viral replication. Deoxyandrographolide can be used for the researches of type 2 diabetes mellitus, vascular senescenceand virus infection .
Arborinine is a potent and orally activeLSD1 inhibitor. Arborinine increases the expression of H3K4me1/2, H3K9me1/2, E-cad protein and decreases the expression of UBE2O protein level. Arborinine induces cell cycle arrest at S phase. Arborinine shows antitumor activity .
The SETD7 protein is a histone methyltransferase that specifically monomethylates H3K4, a mark associated with transcriptional activation. Its role in gene activation extends to the collagenase and insulin genes, specifically at the insulin promoter when IPF1/PDX-1 is recruited. SETD7 Protein, Human (His) is the recombinant human-derived SETD7 protein, expressed by E. coli , with N-His labeled tag.
The SETD7 protein is a histone methyltransferase that specifically monomethylates H3K4, a mark associated with transcriptional activation. Its role in gene activation extends to the collagenase and insulin genes, specifically at the insulin promoter when IPF1/PDX-1 is recruited. SETD7 Protein, Human (sf9, GST) is the recombinant human-derived SETD7 protein, expressed by Sf9 insect cells , with N-GST labeled tag.
ZJY-54 is an orally active dual-target inhibitor of EGFR/LSD1, with IC50 values of 3.8 nM and 0.6 μM, respectively. ZJY-54 can inhibit the proliferation of non-small cell lung cancer cells, induce the accumulation ofH3K4me2 and H3K9me2, and inhibit the phosphorylation of the EGFR signaling pathway. ZJY-54 has anti-tumor activity .
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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