Histone Methyltransferase Inhibitor

Histone Methyltransferase Inhibitors (197):

Cat. No.	Product Name	Effect	Purity

HY-158102

ORIC-944	Inhibitor	99.90%
ORIC-944 is a selective, orally active, allosteric inhibitor targeting the EED subunit of polycomb repressive complex 2 (PRC2). ORIC-944 is synergistic with androgen receptor pathway inhibitors (ARPIs) for the study of metastatic prostate cancer.

HY-139400

Pociredir	Inhibitor	99.97%
Pociredir (FTX-6058) is a potent and orally active inhibitor of Embryonic Ectoderm Development (EED). Pociredir can induce HbF protein expression in cell and murine models. Pociredir can be used for the research of select hemoglobinopathies, including sickle cell disease and β-thalassemia.

HY-100832

UNC3866	Inhibitor	99.50%
UNC3866 is a potent antagonist of the CBX7-H3 interaction as determined by AlphaScreen (IC₅₀=66±1.2 nM) and is more than 100-fold selective for CBX7 over the other nine members of this methyl-lysine (Kme) reader panel.

HY-148669A

Bleximenib oxalate	Inhibitor	≥98.0%
Bleximenib (JNJ-75276617) oxalate is an orally active and selective menin-KMT2A inhibitor, with IC₅₀ values of 0.1 nM, 0.045 nM, and ≤0.066 nM for humans, mice, and dogs, respectively. Bleximenib oxalate can inhibit the proliferation and induce apoptosis and differentiation of tumor cells. Bleximenib oxalate can be used in the research of tumors such as leukemia.

HY-119344

MS37452	Inhibitor	99.81%
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-129441

Metoprine	Inhibitor	99.90%
Metoprine (BW 197U) is a potent histamine N-methyltransferase (HMT) inhibitor. Metoprine, a diaminopyrimidine derivative, can cross the blood-brain barrier and increase brain histamine levels by inhibiting HMT. Metoprine is an antifolate and antitumor agent.

HY-122181

OTS186935	Inhibitor	98.55%
OTS186935 is a potent protein methyltransferase SUV39H2 inhibitor with an IC₅₀ of 6.49 nM. OTS186935 shows significant inhibition of tumor growth in mouse xenograft models without any detectable toxicity. OTS193320 regulates the production of γ-H2AX in cancer cells.

HY-N2420

Flavokawain A	Inhibitor	99.93%
Flavokawain A is a chalcone compound and an orally active inhibitor of PRMT5 and cytochrome P450. Flavokawain A has anti-inflammatory, anti-tumor, and immunomodulatory effects. Flavokawain A can inhibit the proliferation of tumor cells and induce apoptosis. Flavokawain A can be used in the research of diseases such as bladder cancer.

HY-116804

ZLD1039	Inhibitor	99.19%
ZLD1039 is a potent, highly selective, and orally bioavailable EZH2 inhibitor. ZLD1039 shows potent and concentration-dependent inhibition of PRC2 enzymatic activity against EZH2 wild-type as well as Y641F, and A677G mutant enzymes with IC₅₀ values of 5.6, 15, and 4.0 nM, respectively. ZLD1039 inhibits breast tumor growth and metastasis.

HY-148669

Bleximenib	Inhibitor	99.36%
Bleximenib (JNJ-75276617) is an orally active and selective menin-KMT2A inhibitor, with IC₅₀ values of 0.1 nM, 0.045 nM, and ≤0.066 nM for humans, mice, and dogs, respectively. Bleximenib can inhibit the proliferation and induce apoptosis and differentiation of tumor cells. Bleximenib can be used in the research of tumors such as leukemia.

HY-138283

MR837	Inhibitor	99.82%
MR837 is an inhibitor of NSD2-PWWP1. MR837 can bind with human nuclear receptor binding SET domain protein 2 (PWWP domain).

HY-147058

SW2_152F	Inhibitor	99.77%
SW2_152F is a potent, selective chromobox 2 chromodomain (CBX2 ChD) inhibitor with a K_d of 80 nM. SW2_152F displays 24-1000-fold selectivity for CBX2 ChD over other CBX paralogs in vitro. SW2_152F is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-12845

UNC2400	Inhibitor	99.92%
UNC2400 is a close analog of UNC1999 with >1,000-fold lower potency than UNC1999 as a negative control for cell-based studies.

HY-130815A

MAK683-CH2CH2COOH hydrochloride	Inhibitor	98.03%
MAK683-CH2CH2COOH binds to EED (embryonic ectoderm development protein). MAK683-CH2CH2COOH and a VHL ligand for the E3 ubiquitin ligase have been used to design PROTAC EED degrader-1 (HY-130614) and PROTAC EED degrader-2 (HY-130615).

HY-132922

EEDi-5273	Inhibitor	99.09%
EEDi-5273 is an exceptionally potent and orally efficacious EED inhibitor (IC₅₀ = 0.2 nM) capable of achieving complete and persistent tumor regression.

HY-139400A

Pociredir hydrochloride	Inhibitor	99.89%
Pociredir (FTX-6058) hydrochloride is a potent and orally active inhibitor of Embryonic Ectoderm Development (EED). Pociredir hydrochloride can induce HbF protein expression in cell and murine models. Pociredir hydrochloride can be used for the research of select hemoglobinopathies, including sickle cell disease and β-thalassemia.

HY-15227A

EPZ004777 hydrochloride	Inhibitor	99.46%
EPZ004777 hydrochloride is a potent, selective DOT1L inhibitor with an IC₅₀ of 0.4 nM.

HY-136977

EEDi-5285	Inhibitor	99.98%
EEDi-5285 is an exceptionally potent and orally active embryonic ectoderm development (EED) inhibitor with an IC₅₀ value of 0.2 nM for binds to the EED protein. EEDi-5285 has anti-cancer activity.

HY-155814

EML734	Inhibitor	99.48%
EML734 is a potent and selective PRMT7/9 inhibitor with IC₅₀ values of 315 nM and 0.89 μM, respectively.

HY-134086

NSD-IN-2	Inhibitor
NSD-IN-2 (compound 151) is a potent and irreversible NSD1 inhibitor. NSD-IN-2 can be used in research of cancer.

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