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Results for "

H3K27

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apoptosis (6) Caspase (2) DNA/RNA Synthesis (1) Epigenetic Reader Domain (3) HDAC (2) Histone Acetyltransferase (8) Histone Demethylase (9) Histone Methyltransferase (15) PARP (1) PROTACs (2)
By Research Areas:	Cancer (36)

Inhibitors & Agonists

Peptides

Antibodies

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-148458

EZH2-IN-14	Histone Methyltransferase	Cancer
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 .

HY-143441

CBP/p300-IN-17	Histone Acetyltransferase	Cancer
CBP/p300-IN-17 (compound 7) is a potent EP300/CBP HAT inhibitor with IC₅₀s of 0.18, 0.69 µM for HAT EP300 and LK2 H3K27, respectively .

HY-143442

CBP/p300-IN-18	Histone Acetyltransferase	Cancer
CBP/p300-IN-18 (compound 8) is a potent EP300/CBP HAT inhibitor with IC₅₀s of 0.056, 0.46 µM for HAT EP300 and LK2 H3K27, respectively .

HY-143440

CBP/p300-IN-16	Histone Acetyltransferase	Cancer
CBP/p300-IN-16 (compound 1) is a potent EP300/CBP HAT inhibitor with IC₅₀s of 0.61, 2.24 µM for HAT EP300 and LK2 H3K27, respectively .

HY-143443

DS17701585	Histone Acetyltransferase Histone Demethylase	Cancer
DS17701585 (Compound 11) is a highly selective, orally active EP300 and CBP inhibitor with IC₅₀ values of 0.040, 0.15, 0.45 and 0.70 µM against CBP, EP300, *H3K27* and SOX2. DS17701585 can be used for cancer research .

HY-P2266

SAH-EZH2	Histone Methyltransferase	Cancer
SAH-EZH2, a stable EZH2 α-helical peptide, is an EZH2/EED interaction inhibitor. SAH-EZH2 targets native embryonic ectoderm development (EED), disturbs its interactions with EZH1 and EZH2, and selectively decreases trimethylation of H3K27 .

HY-136522

S2116	Histone Demethylase Apoptosis	Cancer
S2116, a N-alkylated tranylcypromine (TCP) derivative, is a potent lysine-specific demethylase 1 (LSD1) inhibitor. S2116 increases H3K9 methylation and reciprocal H3K27 deacetylation at super-enhancer regions. S2116 induces apoptosis in TCP-resistant T-cell acute lymphoblastic leukemia (T-ALL) cells by repressing transcription of the NOTCH3 and TAL1 genes. S2116 significantly retardes the growth of T-ALL cells in xenotransplanted mice .

HY-136523

S2157	Histone Demethylase Apoptosis	Cancer
S2157, a N-alkylated tranylcypromine (TCP) derivative, is a potent lysine-specific demethylase 1 (LSD1) inhibitor. S2157 increases H3K9 methylation and reciprocal H3K27 deacetylation at super-enhancer regions. S2157 induces apoptosis in TCP-resistant T-cell acute lymphoblastic leukemia (T-ALL) cells by repressing transcription of the NOTCH3 and TAL1 genes. S2157 efficiently pass through the blood-brain barrier and can almost completely eradicate CNS leukemia in mice transplanted with T-ALL cells .

HY-156094

JMJD3/HDAC-IN-1	HDAC Histone Demethylase Apoptosis	Cancer
JMJD3/HDAC-IN-1 (compound A5b) is a dual inhibitor targeting Jumonji domain-containing protein demethylase 3 (JMJD3) and histone deacetylase (HADC1, IC₅₀=16 nM). JMJD3/HDAC-IN-1 promotes hypermethylation of histone H3K27 and hyperacetylation of H3K9, and also cleaves caspase-7 and PARP to induce apoptosis. JMJD3/HDAC-IN-1 effectively inhibits cancer cell cloning, migration, and invasion .

HY-101508

GNA002	Histone Methyltransferase	Cancer
GNA002 is a highly potent, specific and covalent EZH2 (Enhancer of zeste homolog 2) inhibitor with an IC₅₀ of 1.1 μM. GNA002 can specifically and covalently bind to Cys668 within the EZH2-SET domain, triggering EZH2 degradation through COOH terminus of Hsp70-interacting protein (CHIP)-mediated ubiquitination. GNA002 efficiently reduces EZH2-mediated H3K27 trimethylation, reactivates polycomb repressor complex 2 (PRC2)-silenced tumor suppressor genes .

HY-156096

HDAC3-IN-2	HDAC Histone Methyltransferase Caspase Apoptosis DNA/RNA Synthesis	Cancer
HDAC3-IN-2 (compound 4i) is a pyrazinyl hydrazide-based HDAC3 inhibitor (IC₅₀: 14 nM) that efficiently targets triple-negative breast cancer cells. HDAC3-IN-2 is cytotoxic with an IC₅₀ of 0.55 μM against 4T1 and an IC₅₀ of 0.74 μM against MDA-MB-231. HDAC3-IN-2 has anti-tumor efficacy in vivo in tumor-bearing mouse models, selectively increasing the acetylation levels of H3K9, H3K27 and H4K12, increasing the contents of apoptosis-related caspase-3, caspase-7 and cytochrome c, and reducing Proliferation-related Bcl-2, CD44, EGFR, and Ki-67 levels .

HY-153191

EZH2-IN-15

Histone Methyltransferase Cancer

EZH2-IN-15 is a EZH2 inhibitor. EZH2-IN-15 has anti-tumor activity, and can be used for research of H3K27me3-dependent tumors .
HY-15648

GSK-J1

5+ Cited Publications

Histone Demethylase Cancer

GSK-J1 is a potent inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A, with IC₅₀ of 60 nM towards KDM6B.

EZH2-IN-15	Histone Methyltransferase	Cancer
EZH2-IN-15 is a EZH2 inhibitor. EZH2-IN-15 has anti-tumor activity, and can be used for research of H3K27me3-dependent tumors .

GSK-J1 5+ Cited Publications	Histone Demethylase	Cancer
GSK-J1 is a potent inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A, with IC₅₀ of 60 nM towards KDM6B.

HY-126327

UNC4976	Histone Methyltransferase	Cancer
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 .

HY-15648D

GSK-J1 lithium salt

Histone Demethylase Cancer

GSK-J1 lithium salt is a potent inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A, with IC₅₀ of 60 nM towards KDM6B.

GSK-J1 lithium salt	Histone Demethylase	Cancer
GSK-J1 lithium salt is a potent inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A, with IC₅₀ of 60 nM towards KDM6B.

HY-126327A

UNC4976 TFA	Histone Methyltransferase	Cancer
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 .

HY-15648G

GSK-J1 sodium

Histone Demethylase Cancer

GSK-J1 sodium is a potent inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A, with IC₅₀ value of 60 nM towards KDM6B .

GSK-J1 sodium	Histone Demethylase	Cancer
GSK-J1 sodium is a potent inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A, with IC₅₀ value of 60 nM towards KDM6B .

HY-15648A

GSK-J2 2 Publications Verification	Others	Cancer
GSK-J2 is an isomer of GSK-J1 that does not have any specific activity. GSK-J1 is a potent inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A.

HY-122595

EZH2-IN-1	Histone Methyltransferase	Cancer
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 .

HY-15648I

GSK-J2 sodium	Others	Cancer
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-demethylases JMJD3/KDM6B and UTX/KDM6A .

HY-15648F

GSK-J4 hydrochloride Maximum Cited Publications 34 Publications Verification	Histone Demethylase	Cancer
GSK-J4 hydrochloride is a potent dual inhibitor of H3K27me3/me2-demethylases JMJD3/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 .

HY-145765

JQAD1	PROTACs Histone Acetyltransferase Apoptosis Caspase PARP	Cancer
JQAD1 is a CRBN-dependent PROTAC that selectively targets EP300 for degradation. JQAD1 suppresses EP300 expression and the H3K27ac modification. JQAD1 induces apoptosis. JQAD1 can be used in research of cancer .

HY-15648B

GSK-J4 Maximum Cited Publications 34 Publications Verification	Histone Demethylase Apoptosis	Cancer
GSK-J4 is a potent dual inhibitor of H3K27me3/me2-demethylases JMJD3/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 . GSK-J4 induces endoplasmic reticulum stress-related apoptosis .

HY-119344

MS37452	Histone Methyltransferase	Cancer
MS37452 is a potent inhibitor of CBX7 chromodomain binding to *H3K27me3, with a K_d* 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 .

HY-132197

CBP/p300-IN-12	Epigenetic Reader Domain Histone Acetyltransferase	Cancer
CBP/p300-IN-12 is a potent and selective covalent histone acetyltransferases p300 (IC₅₀ of 166 nM) and CBP inhibitor. CBP/p300-IN-12 decreases the levels of H3K27Ac of PC-3 cells (EC₅₀ of 37 nM). CBP/p300-IN-12 forms a covalent adduct with C1450 .

HY-101117

EED226 5+ Cited Publications	Histone Methyltransferase	Cancer
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 .

HY-16705

BRD4770 2 Publications Verification	Histone Methyltransferase	Cancer
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 .

HY-144094

EZH2-IN-9	Histone Methyltransferase	Cancer
EZH2-IN-9 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-9 has the potential for the research of cancer diseases (extracted from patent WO2021180235A1, compound 17) .

HY-143616

EZH2-IN-7	Histone Methyltransferase	Cancer
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) .

HY-157164

PROTAC EZH2 Degrader-2	PROTACs Histone Methyltransferase	Cancer
PROTAC EZH2 Degrader-2 (compound E-3P-MDM2), an EZH2 inhibitor, is a PROTAC composed of Tazemetostat (EPZ6438) and an E3 ligase system ligand. PROTAC EZH2 Degrader-2 degrades EZH2 in SU-DHL-6 cells in a dose-dependent manner, inhibits the expression of H3K27me3, and simultaneously degrades EED and SUZ12 proteins without affecting their mRNA levels. PROTAC EZH2 Degrader-2 has anti-cancer and anti-proliferative activity .

HY-156292

IHMT-EZH2-426	Histone Methyltransferase	Cancer
IHMT-EZH2-426 (compound 38) is a potent and covalent EZH2 degrader with IC₅₀s of 1.3 nM, 1.2 nM, and 1.7-3.5 nM against EZH2 wild-type, EZH2-A687V, and EZH2-Y641F/Y641N/Y641S, respectively. IHMT-EZH2-426 exhibits potent antiproliferation effects against both B-cell lymphoma and triple negative breast cancer (TNBC) cell lines by reducing the levels of H3K27me3 and EZH2 .

HY-151812

CBP/p300-IN-20	Histone Acetyltransferase Epigenetic Reader Domain	Cancer
CBP/p300-IN-20 is a potent and selective p300/CBP inhibitor, with a pIC₅₀ of 10.1 for p300. CBP/p300-IN-20 can be used for the research of cancer .

HY-143339

CBP/p300-IN-15	Epigenetic Reader Domain Histone Acetyltransferase	Cancer
CBP/p300-IN-15 (compound 13a) is a potent p300/CBP inhibitor, with IC₅₀ values of 2.50 and 28.0 nM, respectively. CBP/p300-IN-15 shows good activity against OVCAR-3 and A2780 cell line, with EC₅₀ values of 0.865 and 2.71 μM, respectively. CBP/p300-IN-15 can be used for ovarian cancer research .

Cat. No.	Product Name	Target	Research Area

HY-P2254

H3K27(Me3) (15-34)	Peptides	Cancer
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) .

HY-P2252

H3K27(Me) (15-34)	Peptides	Cancer
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) .

HY-P2253

H3K27(Me2) (15-34)	Peptides	Cancer
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) .

HY-P2266

SAH-EZH2	Histone Methyltransferase	Cancer
SAH-EZH2, a stable EZH2 α-helical peptide, is an EZH2/EED interaction inhibitor. SAH-EZH2 targets native embryonic ectoderm development (EED), disturbs its interactions with EZH1 and EZH2, and selectively decreases trimethylation of H3K27 .

HY-126327

UNC4976	Histone Methyltransferase	Cancer
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 .

HY-126327A

UNC4976 TFA	Histone Methyltransferase	Cancer
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 .

TriMethyl-Histone H3 (Lys27) Antibody H3K27me3; H3 histone; HIST1H3A; Histone cluster 1; H3a	WB, IHC-F, IHC-P, ICC/IF, IP, ChIP	Human, Rat
TriMethyl-Histone H3 (Lys27) Antibody is a non-conjugated and Rabbit origined monoclonal antibody about 15 kDa, targeting to TriMethyl-Histone H3 (Lys27). It can be used for WB,IHC-F,IHC-P,ICC/IF,IP,ChIP assays with tag free, in the background of Human, Rat.

Acetyl-Histone H3 (Lys27) Antibody H3K27ac; H3/j; H3C1; H3C2; H3C3; H3C4; H3C6; H3C7; H3C8; H3FJ; H3C10; H3C11; HIST1H3J	WB, IHC-F, IHC-P, ICC/IF, IP, ChIP	Human
Acetyl-Histone H3 (Lys27) Antibody is a non-conjugated and Rabbit origined monoclonal antibody about 15 kDa, targeting to Acetyl-Histone H3 (Lys27). It can be used for WB,IHC-F,IHC-P,ICC/IF,IP,ChIP assays with tag free, in the background of Human.

DiMethyl-Histone H3 Antibody (YA783) H3K27me2; H3 histone; HIST1H3A; Histone cluster 1; H3a	WB, ICC/IF, IP	Human, Mouse, Rat
DiMethyl-Histone H3 Antibody (YA783) is a non-conjugated and Mouse origined monoclonal antibody about 15 kDa, targeting to DiMethyl-Histone H3 (Lys27) (5F6). It can be used for WB,ICC/IF,IP assays with tag free, in the background of Human, Mouse, Rat.

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