2. Epigenetics Apoptosis
  3. DNA Methyltransferase Apoptosis
  4. (4aS,8aR)-NPD-001

(4aS,8aR)-NPD-001 is a potent and allosteric inhibitor of DNMT3A. (4aS,8aR)-NPD-001 inhibits DNMT3A activity by disrupting protein-protein interactions. (4aS,8aR)-NPD-001 induces apoptosis of acute myeloid leukemia (AML) cell lines. (4aS,8aR)-NPD-001 induces differentiation of distinct AML cell lines including cells with mutated DNMT3A R882.

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(4aS,8aR)-NPD-001 Chemical Structure

(4aS,8aR)-NPD-001 Chemical Structure

CAS No. : 2366272-43-5

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(4aS,8aR)-NPD-001 Related Antibodies

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Description

(4aS,8aR)-NPD-001 is a potent and allosteric inhibitor of DNMT3A. (4aS,8aR)-NPD-001 inhibits DNMT3A activity by disrupting protein-protein interactions. (4aS,8aR)-NPD-001 induces apoptosis of acute myeloid leukemia (AML) cell lines. (4aS,8aR)-NPD-001 induces differentiation of distinct AML cell lines including cells with mutated DNMT3A R882[1].

IC50 & Target

DNMT3A

 

In Vitro

(4aS,8aR)-NPD-001 (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].
(4aS,8aR)-NPD-001 (0-120 μM, 100 min) inhibits the activation of DNMT3A_R882H by DNMT3L[1].
(4aS,8aR)-NPD-001 (0-30 μM, 72 h) induces apoptosis and and differentiation in AML cell lines in a concentration-dependent manner[1].
(4aS,8aR)-NPD-001 (5 μM, 20 days) leads to a time-dependent decrease of global 5-methylcytosine[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

(4aS,8aR)-NPD-001 Related Antibodies

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).
Molecular Weight

584.71

Formula

C33H40N6O4
CAS No.
SMILES

O=C1N(C2CCCCCC2)N=C(C3=CC=C(OC)C(OCCCCOC4=CC=C(C5=NN=NN5)C=C4)=C3)[C@@]6([H])CC=CC[C@@]16[H]
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Room temperature in continental US; may vary elsewhere.
Storage

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Purity & Documentation
References
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(4aS,8aR)-NPD-001 Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

(4aS,8aR)-NPD-0012366272-43-5DNA MethyltransferaseApoptosisDNMTsDNA MTasesHL60OCI-AML3K562MV411MOLM13THP1acute myeloid leukemiaAMLprotein–protein interactionsInhibitorinhibitorinhibit

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