2366272-43-5

2366272-43-5 structure

Name: DNMT3A-IN-2
Chemical Name: DNMT3A-IN-2
CAS Number: 2366272-43-5
Molecular Formula: C₃₃H₄₀N₆O₄
Molecular Weight: 584.71
Catalog: Signaling Pathways Apoptosis Apoptosis
Create Date: 2022-08-31 10:54:09
Modify Date: 2024-04-09 22:01:47
DNMT3A-IN-2 (compound 2) is a potent and allosteric inhibitor of DNMT3A. DNMT3A-IN-2 inhibits DNMT3A activity by disrupting protein-protein interactions. DNMT3A-IN-2 induces apoptosis of acute myeloid leukemia (AML) cell lines. DNMT3A-IN-2 induces differentiation of distinct AML cell lines including cells with mutated DNMT3A R882[1].

Name	DNMT3A-IN-2

Description	DNMT3A-IN-2 (compound 2) is a potent and allosteric inhibitor of DNMT3A. DNMT3A-IN-2 inhibits DNMT3A activity by disrupting protein-protein interactions. DNMT3A-IN-2 induces apoptosis of acute myeloid leukemia (AML) cell lines. DNMT3A-IN-2 induces differentiation of distinct AML cell lines including cells with mutated DNMT3A R882[1].
Related Catalog	Signaling Pathways >> Apoptosis >> Apoptosis Research Areas >> Cancer Signaling Pathways >> Epigenetics >> DNA Methyltransferase
Target	DNMT3A
In Vitro	DNMT3A-IN-2 (compound 2) (60 μM) disrupts DNMT3A-DNMT3L interactions at the DNMT3A tetramer interface, inhibits the stimulation of DNMT3A_WT activity by DNMT3L, but does not inhibit the activation of DNMT3A_WT by H3 peptides[1]. DNMT3A-IN-2 (0-120 μM, 100 min) inhibits the activation of DNMT3A_R882H by DNMT3L[1]. DNMT3A-IN-2 (0-30 μM, 72 h) induces apoptosis and and differentiation in AML cell lines in a concentration-dependent manner[1]. DNMT3A-IN-2 (5 μM, 20 days) leads to a time-dependent decrease of global 5-methylcytosine[1]. Apoptosis Analysis[1] Cell Line: Human AML cell lines Concentration: 0, 1, 5, 10, 20, and 30 μM Incubation Time: 72 h Result: Showed a dose-response effect with a marked increase in apoptosis in the 7-12 μM range. Led to a concentration-dependent increase in the myeloid differentiation marker, CD11b, in multiple PI-negative AML cell lines: MV411 (biphenotypic B myelomonocytic leukemia), MOLM13 (acute monocytic leukemia), THP-1 (acute monocytic leukemia), OCI-AML3 (DNMT3A R882 mutant, AML), KASUMI (acute myeloblastic leukemia), HL60 (acute promyelocytic leukemia), and K562 (chronic myelogenous leukemia).
References	[1]. Sandoval JE, et al. First-in-Class Allosteric Inhibitors of DNMT3A Disrupt Protein-Protein Interactions and Induce Acute Myeloid Leukemia Cell Differentiation. J Med Chem. 2022 Jul 22.

Molecular Formula	C₃₃H₄₀N₆O₄
Molecular Weight	584.71

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