(R)-DNMDP

• CAT Number: I045963
• CAS Number: 1630760-60-9
• Molecular Formula: C15H20N4O3
• Molecular Weight: 304.34
• Purity: ≥95%
• Synonyms: (4R)-3-[4-(diethylamino)-3-nitrophenyl]-4-methyl-4,5-dihydro-1H-pyridazin-6-one
• InChI: InChI=1S/C15H20N4O3/c1-4-18(5-2)12-7-6-11(9-13(12)19(21)22)15-10(3)8-14(20)16-17-15/h6-7,9-10H,4-5,8H2,1-3H3,(H,16,20)/t10-/m1/s1
• InChIKey: YOSSKNZHADPXJX-SNVBAGLBSA-N
• SMILES: CCN(CC)C1=C(C=C(C=C1)C2=NNC(=O)CC2C)[N+](=O)[O-]

(R)-DNMDP is a potent and selective cancer cell cytotoxic agent. (R)-DNMDP, the R-form of DNMDP, binds PDE3A directly. (R)-DNMDP has a 500-fold lower EC50 compared to the (S)-enantiomer in HeLa cell line[1][2].
(R)-DNMDP (0.1 pM-1 mM; for 48 hours) has a 500-fold lower EC50 compared to the (S)-enantiomer in HeLa cell line[1].
(S)-DNMDP has non-cytotoxic. Binding of PDE3A to the linker analogue is blocked by both trequinsin and (R)-DNMDP, but not by the (S)-DNMDP[1].

Reference

[1]. de Waal L, et al. Identification of cancer-cytotoxic modulators of PDE3A by predictive chemogenomics. Nat Chem Biol. 2016 Feb;12(2):102-8. Nat Chem Biol. 2016 Feb;12(2):102-8.
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[2]. Luc DE WAAL, et al. Compositions and methods for cancer expressing pde3a or slfn12. WO2017027854A1.