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GSK-J4 is a potent dual inhibitor of H3K27me3/me2-demethylasesJMJD3/KDM6B and UTX/KDM6A with IC50s of 8.6 and 6.6 μM, respectively. GSK-J4 inhibits LPS-induced TNF-α production in human primary macrophages with an IC50 of 9 μM. GSK J4 is a cell permeable proagent of GSK-J1 [3]. GSK-J4 induces endoplasmic reticulum stress-related apoptosis .
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 .
EED226 is a polycomb repressive complex 2 (PRC2) inhibitor, which binds to the K27me3-pocket on embryonic ectoderm development (EED) and shows strong antitumor activity in xenograft mice model . EED226 is a potent, selective, and orally bioavailable EED inhibitor . EED226 inhibits PRC2 with an IC50 of 23.4 nM when the H3K27me0 peptide is used as a substrate in the in vitro enzymatic assays [3].
GSK-J4 hydrochloride is a potent dual inhibitor of H3K27me3/me2-demethylasesJMJD3/KDM6B and UTX/KDM6A with IC50s of 8.6 and 6.6 μM, respectively. GSK-J4 hydrochloride inhibits LPS-induced TNF-α production in human primary macrophages with an IC50 of 9 μM. GSK-J4 hydrochloride is a cell permeable proagent of GSK-J1 [3].
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 .
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 [3] .
F5446 (Compound 1) is a selective small molecule inhibitor of SUV39H1 methyltransferase. F5446 decreases H3K9me3 deposition at the FAS promoter, increases Fas expression and increases colorectal carcinoma cell sensitivity to FasL-induced apoptosis in vitro. F5446 suppresses human colon tumor xenograft growth in vivo [3].
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 .
MS37452 is a potent inhibitor of CBX7 chromodomain binding to H3K27me3, with a Kd of 27.7 μM. MS37452 can derepress transcription of polycomb repressive complex target gene p16/CDKN2A by displacing CBX7 binding to the INK4A/ARF locus in prostate cancer cells .
GSK-J2 is an isomer of GSK-J1 that does not have any specific activity. GSK-J1 is a potent inhibitor of H3K27me3/me2-demethylasesJMJD3/KDM6B and UTX/KDM6A.
EZH2-IN-14 is a selective EZH2 (Histone Methyltransferase) inhibitor with an IC50 of 12 nM. EZH2-IN-14 inhibits the methyltransferase activity of EZH2/PRC2 (that is, reducing H3K27me3). EZH2-IN-14 shows >200-fold selective for EZH2 over the highly homologous H3K27 methyltransferase EZH1 .
KDM4-IN-3 (Compound 15) is a KDM4 inhibitor (IC50 = 871 nM) that exhibits improved potency in biochemical assays. KDM4-IN-3 is cell-permeable and kills prostate cancer cells at low micro molar concentrations. KDM4-IN-3 inhibits growth of prostate cancer cell lines and increases the H3K9me3 abundance. KDM4-IN-3 can be studied in research for prostate cancer .
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) .
H3K27(Me3) (15-34), a histone peptide, is a repressive chromatin mark derived from human histone. Polycomb Repressive Complex 2 (PRC2) is a multiprotein complex that catalyzes the methylation of H3K27(Me) .
NV03 is a potent and selective antagonist of Ubiquitin-like with PHD and RING finger domains 1(UHRF1)-H3K9me3 interaction by binding to UHRF1 tandem tudor domain, with a Kd of 2.4 μM. NV03 is also a ligand for E3 ligase. NV03 can be studied in anticancer research .
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 .
Progerinin (SLC-D011) is an orally active progerin-lamin A binding inhibitor. Progerinin selectively binds to the C-terminal region of progerin, disrupting its interaction with lamin A and promoting progerin degradation while sparing wild-type lamin A, B, and C. Progerinin ameliorates nuclear deformation, increases H3K9me3 levels, and reduces progerin expression in HGPS patient-derived fibroblasts. Progerinin extends lifespan in Lmna G609G/G609G mice and Lmna G609G/+ mice, improves body weight, hair morphology, cardiac function, and histological phenotypes. Progerinin can be used for the study of Hutchinson-Gilford progeria syndrome (HGPS) .
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 .
GSK3735967 is an selective, reversible, non-nucleoside inhibitor of DNMT1 with an IC50 value of 40 nM. GSK3735967 contains a planar dicyanopyridine core that can specifically embed DNMT1 bound hemimethylated CpG dinucleotides. GSK3735967 has three binding sites, one of which can bind to histone H4K20me3 .
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 [3].
UNC4976 TFA is a positive allosteric modulator (PAM) peptidomimetic of CBX7 chromodomain binding to nucleic acids. UNC4976 TFA simultaneously antagonizes H3K27me3-specific recruitment of CBX7 to target genes while increasing non-specific binding to DNA and RNA .
Nε,Nε,Nε-Trimethyllysine-d9 (chloride) is the deuterium labeled Nε,Nε,Nε-Trimethyllysine (chloride) . Nε,Nε,Nε-Trimethyllysine chloride serves as a precursor for gut flora-dependent formation of N,N,N-trimethyl-5-aminovaleric acid (TMAVA) .
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 .
ME3 Human Pre-designed siRNA Set A contains three designed siRNAs for ME3 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
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 .
1,4,7-Trimethyl-1,4,7-triazonane, also known as TMT or trimethylenetris(aziridine), is a cyclic organic compound. TMT is commonly used as a crosslinking agent and a precursor for polymer and resin synthesis. In addition, it is used as a stabilizer in the production of polyurethane foam and as a curing agent for epoxy resins. Due to its high reactivity and stability, TMT is considered to be a versatile and efficient reagent in various applications.
ssK36 is a supersubstrate peptide of the histone methyltransferase (SET) domain protein 2 (SETD2), and ssK36 is designed for the SETD2 protein, a specific PKMT. ssK36 is responsible in human cells for adding methyl groups to the 36th lysine residue of histone H3(H3K36) to form H3K36me3. ssK36 can be methylated by SETD2 at a rate more than 100 times faster than the natural substrate H3K36. ssK36 can be used to study the catalytic mechanism of PKMTs, especially substrate specificity and catalytic efficiency .
Me3 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Me3 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
Me3 Rat Pre-designed siRNA Set A contains three designed siRNAs for Me3 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
5-Me-3’-dU-2’-phosphoramidite is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc .
5Me3F4AP is a potent blocker of potassium channel, with the IC50 of 220 μM to 693 μM when the pH is increased from 6.4 to 9.1. 5Me3F4AP has the potential to cross the blood-brain barrier and potential application in positron emission tomography (PET) .
UNC4976 is a positive allosteric modulator (PAM) peptidomimetic of CBX7 chromodomain binding to nucleic acids. UNC4976 simultaneously antagonizes H3K27me3-specific recruitment of CBX7 to target genes while increasing non-specific binding to DNA and RNA .
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 .
NCDM-32B is a potent and selective KDM4 inhibitor, with IC50 values of 3.0 μM for KDM4A and 1.0 μM for KDM4C in in vitro enzyme assays. NCDM-32B specifically increases global H3K9me3/me2 levels in basal breast cancer cells. NCDM-32B impairs the viability of KDM4C-amplified basal breast cancer cell lines (HCC1954 and Colo824). NCDM-32B can be used for the study of breast cancer .
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 .
WQQ-345 is an orally active BCAT1 inhibitor with an IC50 values of 10.8 mM. WQQ-345 reduces cellular α-KG levels, upregulating H3K27me3 expression, decreasing glycolytic enzyme expression, and impairing glycolysis activity. WQQ-345 reduces colony formation, suppresses growth of BCAT1-high TKI-resistant lung cancer cells. WQQ-345 exerts in vitro and in vivo antitumor activity. WQQ-345 can be used for the research of TKI-resistant non-small cell lung cancer and TKI-resistant lung cancer .
ssK36 TFA is a supersubstrate peptide of the histone methyltransferase (SET) domain protein 2 (SETD2) , and ssK36 TFA is designed for the SETD2 protein, a specific PKMT. ssK36 TFA is responsible in human cells for adding methyl groups to the 36th lysine residue of histone H3(H3K36) to form H3K36me3. ssK36 TFA can be methylated by SETD2 at a rate more than 100 times faster than the natural substrate H3K36. ssK36 TFA can be used to study the catalytic mechanism of PKMTs, especially substrate specificity and catalytic efficiency .
PROTAC EZH2 Degrader-3 (compound ZJ-20) is a EZH2 PROTAC degrader. PROTAC EZH2 Degrader-3 (5 μM, 24 h) not only potently inhibits the expression of EZH2 protein, but also had a strong inhibits effect on the expression levels of other subunits of PRC2 as well as H3k27me3 protein. PROTAC EZH2 Degrader-3 shows anti-proliferative activity and blocks the cell cycle in the G0-G1 phase and induces cell apoptosis((Blue: cereblon ligand Pomalidomide (HY-10984), Black: linker HY-W361751；Pink: EZH2 inhibitor Tazemetostat (HY-13803)) .
Histone H3K9me3 (1-15) (H3(1-15)K9me3) TFA is used as substrate. Histone H3K9me3 is a histone posttranslational modification (PTM) that has emerged as hallmark of pericentromeric heterochromatin .
HP1-IN-2 (Compound (R)-18) is a HP1/H3K9me3 interaction inhibitor with an IC50 of 18.1 μM. HP1-IN-2 can be used for studying various cancers with overexpression of HP1 .
NPD13668 is an EZH2-mediated gene silencing modulator. NPD13668 inhibits EZH2/PRC2 (polycomb repressive complex 2) activity. NPD13668 reactivates the expression of silenced H3K27me3 target genes together with depletion of the H3K27me3 modification. NPD13668 can be used for the study of prostate cancer and ovarian cancer .
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 .
GSK-J4 (hydrochloride) (Standard) is the analytical standard of GSK-J4 (hydrochloride). This product is intended for research and analytical applications. GSK-J4 hydrochloride is a potent dual inhibitor of H3K27me3/me2-demethylasesJMJD3/KDM6B and UTX/KDM6A with IC50s of 8.6 and 6.6 μM, respectively. GSK-J4 hydrochloride inhibits LPS-induced TNF-α production in human primary macrophages with an IC50 of 9 μM. GSK-J4 hydrochloride is a cell permeable proagent of GSK-J1 [3].
GSK-J4 (Standard) is the analytical standard of GSK-J4. This product is intended for research and analytical applications. GSK-J4 is a potent dual inhibitor of H3K27me3/me2-demethylasesJMJD3/KDM6B and UTX/KDM6A with IC50s of 8.6 and 6.6 μM, respectively. GSK-J4 inhibits LPS-induced TNF-α production in human primary macrophages with an IC50 of 9 μM. GSK J4 is a cell permeable proagent of GSK-J1 [3]. GSK-J4 induces endoplasmic reticulum stress-related apoptosis .
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 .
IHMT-EZH2-426 (compound 38) is an effective covalent EZH2 degrader, with IC50 values of 1.3 nM, 1.2 nM, and 1.7-3.5 nM for EZH2 wild type, EZH2-A687V, and EZH2-Y641F/Y641N/Y641S, respectively. IHMT-EZH2-426 reduces H3K27me3 and EZH2 levels and shows effective anti-proliferative effects in B-cell lymphoma and TNBC cell lines.
DC-PRC2in-01 is a potent EZH2-EED interaction inhibitor with an IC50 of 4.21 μM and a Kd of 4.56 μM. DC-PRC2in-01 disrupts the EZH2-EED interaction, leading to degradation of PRC2 core proteins and decrease of H3K27me3 levels, inhibition of PRC2-driven lymphoma cell proliferation, and cell cycle arrest. DC-PRC2in-01 can be used for the research of PRC2-related cancers, such as Diffuse Large B-cell Lymphoma (DLBCL) and follicular lymphoma (FL) .
DC541 (Compound 20) is a selective NTMT1 inhibitor with an IC50 of 0.34 μM. DC541 reduces the level of me3-RCC1 in colorectal cancer cells. DC541 is applicable to research related to colorectal cancer .
OHM 11638 (Atilmotin), an analogue of the (1-14) fragment of porcine motilin, is a motilin receptor agonist with a pKd of 8.94 for the motilin receptor. OHM 11638 affects esophageal, lower esophageal sphincter (LES), and gastric motility. OHM 11638 increases LES and gastric pressures, OHM 11638 can be used as prokinetic agents .
H3K27(Me) (15-34), a histone peptide, is a repressive chromatin markderived from human histone. Polycomb Repressive Complex 2 (PRC2) is a multiprotein complex that catalyzes the methylation of H3K27(Me) .
GSK-J2 sodium is the sodium form of GSK-J2 (HY-15648A). GSK-J2 is an isomer of GSK-J1, and does not have any specific activity. GSK-J1 (HY-15648) is a potent inhibitor of H3K27me3/me2-demethylasesJMJD3/KDM6B and UTX/KDM6A .
H3K27(Me2) (15-34), a histone peptide, is a repressive chromatin mark derived from human histone. Polycomb Repressive Complex 2 (PRC2) is a multiprotein complex that catalyzes the methylation of H3K27(Me) .
EED-IN-3 is an orally active EED inhibitor. EED-IN-3 effectively inhibits PRC2 by binding to EED (IC50 = 0.62 μM for EED) and downregulates H3K27me3. EED-IN-3 can efficiently and selectively inhibit PC3 cells with the IC50 of 3.69 μΜ and could significantly suppress colony formation and migration. EED-IN-3 can be used for research on prostate cancer.
D-01 is a dual-targeting inhibitor of HIF-1α and EZH2 (IC50: 4.86 μM and 0.99 μM respectively). D-01 inhibits the expression of H3K27me3 protein. D-01 inhibits the migration, clone and the invasion of A549 cells, and also inhibits tube formation of HUVECs. D-01 can be used for research of lung cancer .
HDM-IN-1 (Compound A4) is an inhibitor for fungal histone demethylase (HDM), that inhibits the H3K27me3 in Cryptococcus neoformans and in Candida auris with IC50s of 134 and 12 nM. HDM-IN-1 exhibits inhibitory efficacy against C. neoformans and C. auris with MIC80 of 0.5-2 μg/mL, through inhibition of the biofilm and capsule formation. HDM-IN-1 exhibits antifungal activity in ICR mouse model .
EZH2-IN-1 (compound 3) is a selective and SAM-competitive EZH2 and EZH1 inhibitor with an IC50s of 32 nM, 197 nM and 213 nM for EZH2wt, EZH2 Y641N mutant and EZH1, respectively. EZH2-IN-1 reduces bulk H3K27me3 and H3K27me2 levels. EZH2-IN-1 has the potential for diffuse large B cell lymphoma research .
EZH2-IN-7 is a potent inhibitor of EZH2. EZH2 overexpression or mutations in the SET region (Y641F, Y641N, A687V, A677G point mutations) all lead to abnormal elevation of H3K27me3 and promote the growth and development of many types of tumors, such as breast cancer, prostate cancer, leukemia, etc. EZH2-IN-7 has the potential for the research of cancer diseases (extracted from patent WO2021129629A1, compound 259) .
7-Methylguanosine 5-disphosphoimidazolide disodium (7-Me-3'-OMe-GDP imidazole) is a guanosine diphosphate imidazolide and starting material for synthesis of alkyne-containing C-phosphonate and phosphoester clickable mononucleotide building blocks for triazole-modified mRNA cap analogues .
TDI-11904 is a peripherally active EZH2 inhibitor with an EZH2IC50 of 0.9 nM. TDI-11904 inhibits EZH2 methyltransferase activity, reduces the trimethylation level of H3K27me3, and decreases intracellular H3K27me3 content. TDI-11904 inhibits the proliferation of lymphoma cells. TDI-11904 can be used for the research of lymphoma .
EED-IN-4 is an orally active, EZH2-selective immunomodulator and EED-H3K27me3 inhibitor (EED, IC50=28.21 nM) with anti-inflammatory activity. In mouse models, EED-IN-4 preferentially and persistently accumulates in lymph nodes after oral administration. By reducing the H3K27me3 level of dendritic cells and inhibiting their migration, EED-IN-4 reduces the infiltration of immune cells into the central nervous system and effectively alleviates spinal cord inflammation. EED-IN-4 shows weak inhibitory activity against hERG channels and is non-mutagenic, with no obvious toxicity observed upon long-term oral administration. EED-IN-4 can be used for the research of multiple sclerosis .
EED-IN-5 is an orally active, EZH2-selective trisubstituted pyridine-based EED-H3K27me3 inhibitor and immunomodulator with anti-inflammatory activity. The IC50 value of EED-IN-5 against EED is 28.21 nM. In mouse models, EED-IN-5 preferentially and persistently accumulates in lymph nodes after oral administration. By reducing the H3K27me3 level of dendritic cells and inhibiting their migration, EED-IN-5 decreases the infiltration of specific dendritic cells, macrophages and T cells into the spinal cord and brain. EED-IN-5 exhibits hERG inhibitory activity, shows negative results in the Mini-Ames test, and causes no obvious toxicity upon long-term high-dose administration. EED-IN-5 can be used for the research of multiple sclerosis .
CBX2-IN-1 is a CBX2 inhibitor with an IC50 of 9.6 μM. CBX2-IN-1 binds the CBX2 chromodomain’s H3K27me3 binding channel, blocks interaction between CBX2 and H3K27me3, and exhibits selective affinity toward CBX2, CBX4, CBX6, CBX7, and CBX8 over CBX1, CBX3, and CBX5. CBX2-IN-1 can be used for the research of prostate cancers .
EED226 (Standard) is the analytical standard of EED226 (HY-101117). This product is intended for research and analytical applications. EED226 is a polycomb repressive complex 2 (PRC2) inhibitor, which binds to the K27me3-pocket on embryonic ectoderm development (EED) and shows strong antitumor activity in xenograft mice model . EED226 is a potent, selective, and orally bioavailable EED inhibitor . EED226 inhibits PRC2 with an IC50 of 23.4 nM when the H3K27me0 peptide is used as a substrate in the in vitro enzymatic assays [3].
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].
Gallocatechin-3-O-(3''-O-methyl)-gallate (GCG3''Me) is a catechin polyphenol. Gallocatechin-3-O-(3''-O-methyl)-gallate inhibits histamine release. Gallocatechin-3-O-(3''-O-methyl)-gallate can be used in allergy-related studies .
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 .
UNC7242 is an antagonist that binds to the Tudor domains of PHF1 and PHF19, with a Kd of 1.13 μM for PHF1 and 0.64 μM for PHF19. UNC7242 fails to displace full-length PHF1 or PHF19 from H3K36me3 nucleosomes or chromatin. UNC7242 can be used in studies related to multiple myeloma, endometrial stromal sarcoma, and ossifying fibromyxoid tumor .
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 .
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) .
PROTAC EZH2 Degrader-9 is orally active EZH2 PROTAC degrader degrading EZH2 via the ubiquitin-proteasome pathway. PROTAC EZH2 Degrader-9 downregulates PRC2 core subunits and potent inhibition of H3K27me3 without affecting common CRBN neosubstrates while it was selective over GSp'T1 and ikZF1/3. PROTAC EZH2 Degrader-9 exhibits potent antiproliferative activity against multiple cancer cell lines by inducing cell cycle and apoptosis. PROTAC EZH2 Degrader-9 reverses PRC2-mediated gene silencing and inhibiting EZH2 non-catalytic target gene activation. PROTAC EZH2 Degrader-9 can be used for leukemia, lymphoma, and non-small cell lung cancer research .
PROTAC EZH2 Degrader-44 (compound 60) is a highly efficient PROTAC degrader targeting the EZH2-PRC2 complex. By recruiting the CRBN E3 ligase and relying on the proteasome system, PROTAC EZH2 Degrader-44 simultaneously induces the degradation of core components EZH2, SUZ12 and EED, thereby significantly reducing the levels of H3K27me3 and CARM1. PROTAC EZH2 Degrader-44 exerts antiproliferative effects through a dual mechanism: on the one hand, it triggers mitochondrial dysfunction leading to decreased membrane potential; on the other hand, it strongly promotes apoptosis by regulating Bcl-2 family proteins (upregulating Bax, Caspase-3 and PARP, and downregulating Bcl-2). PROTAC EZH2 Degrader-44 exhibits only extremely low cytotoxicity in human normal mammary epithelial, liver and kidney cells, showing a favorable safety window. PROTAC EZH2 Degrader-44 is an ideal tool molecule for exploring the mechanisms of targeted therapy for triple-negative breast cancer .
1,4,7-Trimethyl-1,4,7-triazonane, also known as TMT or trimethylenetris(aziridine), is a cyclic organic compound. TMT is commonly used as a crosslinking agent and a precursor for polymer and resin synthesis. In addition, it is used as a stabilizer in the production of polyurethane foam and as a curing agent for epoxy resins. Due to its high reactivity and stability, TMT is considered to be a versatile and efficient reagent in various applications.
H3K27(Me3) (15-34), a histone peptide, is a repressive chromatin mark derived from human histone. Polycomb Repressive Complex 2 (PRC2) is a multiprotein complex that catalyzes the methylation of H3K27(Me) .
UNC4976 TFA is a positive allosteric modulator (PAM) peptidomimetic of CBX7 chromodomain binding to nucleic acids. UNC4976 TFA simultaneously antagonizes H3K27me3-specific recruitment of CBX7 to target genes while increasing non-specific binding to DNA and RNA .
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 .
ssK36 is a supersubstrate peptide of the histone methyltransferase (SET) domain protein 2 (SETD2), and ssK36 is designed for the SETD2 protein, a specific PKMT. ssK36 is responsible in human cells for adding methyl groups to the 36th lysine residue of histone H3(H3K36) to form H3K36me3. ssK36 can be methylated by SETD2 at a rate more than 100 times faster than the natural substrate H3K36. ssK36 can be used to study the catalytic mechanism of PKMTs, especially substrate specificity and catalytic efficiency .
UNC4976 is a positive allosteric modulator (PAM) peptidomimetic of CBX7 chromodomain binding to nucleic acids. UNC4976 simultaneously antagonizes H3K27me3-specific recruitment of CBX7 to target genes while increasing non-specific binding to DNA and RNA .
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 .
ssK36 TFA is a supersubstrate peptide of the histone methyltransferase (SET) domain protein 2 (SETD2) , and ssK36 TFA is designed for the SETD2 protein, a specific PKMT. ssK36 TFA is responsible in human cells for adding methyl groups to the 36th lysine residue of histone H3(H3K36) to form H3K36me3. ssK36 TFA can be methylated by SETD2 at a rate more than 100 times faster than the natural substrate H3K36. ssK36 TFA can be used to study the catalytic mechanism of PKMTs, especially substrate specificity and catalytic efficiency .
Histone H3K9me3 (1-15) (H3(1-15)K9me3) TFA is used as substrate. Histone H3K9me3 is a histone posttranslational modification (PTM) that has emerged as hallmark of pericentromeric heterochromatin .
Histone H3K9me3 (1-15) (H3(1-15)K9me3) is a histone posttranslational modification (PTM) that has emerged as hallmark of pericentromeric heterochromatin. Trimethylation of histone H3 at lysine 9 is associated with gene repression, prevents transcription factor binding .
OHM 11638 (Atilmotin), an analogue of the (1-14) fragment of porcine motilin, is a motilin receptor agonist with a pKd of 8.94 for the motilin receptor. OHM 11638 affects esophageal, lower esophageal sphincter (LES), and gastric motility. OHM 11638 increases LES and gastric pressures, OHM 11638 can be used as prokinetic agents .
H3K27(Me) (15-34), a histone peptide, is a repressive chromatin markderived from human histone. Polycomb Repressive Complex 2 (PRC2) is a multiprotein complex that catalyzes the methylation of H3K27(Me) .
H3K27(Me2) (15-34), a histone peptide, is a repressive chromatin mark derived from human histone. Polycomb Repressive Complex 2 (PRC2) is a multiprotein complex that catalyzes the methylation of H3K27(Me) .
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 [3].
Gallocatechin-3-O-(3''-O-methyl)-gallate (GCG3''Me) is a catechin polyphenol. Gallocatechin-3-O-(3''-O-methyl)-gallate inhibits histamine release. Gallocatechin-3-O-(3''-O-methyl)-gallate can be used in allergy-related studies .
Nε,Nε,Nε-Trimethyllysine-d9 (chloride) is the deuterium labeled Nε,Nε,Nε-Trimethyllysine (chloride) . Nε,Nε,Nε-Trimethyllysine chloride serves as a precursor for gut flora-dependent formation of N,N,N-trimethyl-5-aminovaleric acid (TMAVA) .
TriMethyl-Histone H3 (Lys27) Antibody (YA030) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to TriMethyl-Histone H3 (Lys27).
TriMethyl-Histone H3 (Lys27) Antibody (YA9825) is a Rabbit-derived and non-conjugated IgG Recombinant, Monoclonal antibody, targeting to TriMethyl-Histone H3 (Lys27).
MonoMethyl-Histone H3 (Lys9) Antibody (YA9826) is a Rabbit-derived and non-conjugated IgG Recombinant, Monoclonal antibody, targeting to MonoMethyl-Histone H3 (Lys9).
WB, ICC/IF, IHC-P, IF-Tissue, FC, ChIP, Dot Blot, IP
Human, Mouse, Rat
Acetyl-Histone H3 (Lys9) Antibody (YA9827) is a Rabbit-derived and non-conjugated IgG Recombinant, Monoclonal antibody, targeting to Acetyl-Histone H3 (Lys9).
Phospho-Histone H3 (Ser28) Antibody (YA9829) is a Rabbit-derived and non-conjugated IgG Recombinant, Monoclonal antibody, targeting to Phospho-Histone H3 (Ser28).
Acetyl-Histone H3 (Lys4) Antibody (YA9830) is a Rabbit-derived and non-conjugated IgG Recombinant, Monoclonal antibody, targeting to Acetyl-Histone H3 (Lys4).
DiMethyl-Histone H3 (Lys27) Antibody (YA9831) is a Rabbit-derived and non-conjugated IgG Recombinant, Monoclonal antibody, targeting to DiMethyl-Histone H3 (Lys27).
Acetyl-Histone H3 (Lys23) Antibody (YA9832) is a Rabbit-derived and non-conjugated IgG Recombinant, Monoclonal antibody, targeting to Histone H3 (acetyl Lys23).
MonoMethyl-Histone H3 (Lys4) Antibody (YA9833) is a Rabbit-derived and non-conjugated IgG Recombinant, Monoclonal antibody, targeting to MonoMethyl-Histone H3 (Lys4).
Acetyl-Histone H3 (Lys36) Antibody (YA9834) is a Rabbit-derived and non-conjugated IgG Recombinant, Monoclonal antibody, targeting to Acetyl-Histone H3 (Lys36).
Phospho-Histone H3 (Ser10) Antibody (YA9835) is a Rabbit-derived and non-conjugated IgG Recombinant, Monoclonal antibody, targeting to Phospho-Histone H3 (Ser10).
DiMethyl-Histone H3 (Lys4) Antibody (YA9836) is a Rabbit-derived and non-conjugated IgG Recombinant, Monoclonal antibody, targeting to DiMethyl-Histone H3 (Lys4).
MonoMethyl-Histone H3 (Lys14) Antibody (YA9837) is a Rabbit-derived and non-conjugated IgG Recombinant, Monoclonal antibody, targeting to MonoMethyl-Histone H3 (Lys14).
MonoMethyl-Histone H3 (Lys79) Antibody (YA9839) is a Rabbit-derived and non-conjugated IgG Recombinant, Monoclonal antibody, targeting to MonoMethyl-Histone H3 (Lys79).
TriMethyl-Histone H3 (Lys36) Antibody (YA9840) is a Rabbit-derived and non-conjugated IgG Recombinant, Monoclonal antibody, targeting to TriMethyl-Histone H3 (Lys36).
TriMethyl-Histone H3 (Lys27) Antibody (YA030) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to TriMethyl-Histone H3 (Lys27).
Mono+Di+TriMethyl-Histone H3 (Lys36) Antibody (YA9828) is a Rabbit-derived and non-conjugated IgG Recombinant, Monoclonal antibody, targeting to Mono+Di+TriMethyl-Histone H3 (Lys36).
Mono+Di+TriMethyl-Histone H3 (Lys4) Antibody (YA9838) is a Rabbit-derived and non-conjugated IgG Recombinant, Monoclonal antibody, targeting to Mono+Di+TriMethyl-Histone H3 (Lys4).
ME3 Human Pre-designed siRNA Set A contains three designed siRNAs for ME3 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
Me3 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Me3 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
Me3 Rat Pre-designed siRNA Set A contains three designed siRNAs for Me3 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
5-Me-3’-dU-2’-phosphoramidite is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc .
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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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