An inhibitor of P. falciparum HMT
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TM2-115

Item No. 42901

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-(hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-6-methoxy-N-(1-methyl-4-piperidinyl)-7-(phenylmethoxy)-4-quinazolinamine
CAS Number
1197196-47-6
Molecular Formula
C28H38N6O2
Formula Weight
490.7
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble: ≥10 mg/mlEthanol: Soluble: ≥10 mg/ml
SMILES
CN1CCCN(C2=NC(NC3CCN(CC3)C)=C4C(C=C(C(OC)=C4)OCC5=CC=CC=C5)=N2)CC1
InChi Code
InChI=1S/C28H38N6O2/c1-32-12-7-13-34(17-16-32)28-30-24-19-26(36-20-21-8-5-4-6-9-21)25(35-3)18-23(24)27(31-28)29-22-10-14-33(2)15-11-22/h4-6,8-9,18-19,22H,7,10-17,20H2,1-3H3,(H,29,30,31)
InChi Key
BSZDSEMSNHXVRW-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

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    Cayman Chemical
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    Product Description

    TM2-115 is an inhibitor of P. falciparum histone methyltransferase (HMT; IC50 = 43 nM).1 It is selective for P. falciparum HMT over the human HMT G9a (IC50 = >1,000 nM). TM2-115 (1 µM) decreases trimethylation of lysine 4 on histone H3 (H3K4me3) in P. falciparum.2 It is active against chloroquine-resistant and -sensitive strains of P. falciparum (IC50s = 100 and 116 nM, respectively). TM2-115 (1 µM) decreases parasite levels in P. falciparum-infected isolated human erythrocytes. It reduces parasitemia in P. berghei-infected mice when administered at a dose of 40 mg/kg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Sundriyal, S., Chen, P.B., Lubin, A.S., et al. Histone lysine methyltransferase structure activity relationships that allow for segregation of G9a inhibition and anti-Plasmodium activity. Medchemcomm 8(5), 1069-1092 (2017).

    2. Malmquist, N.A., Moss, T.A., Mecheri, S., et al. Small-molecule histone methyltransferase inhibitors display rapid antimalarial activity against all blood stage forms in Plasmodium falciparum. Proc. Natl. Acad. Sci. USA 109(41), 16708-16713 (2012).