An inhibitor of T. brucei N-myristoyltransferase
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DDD85646

Item No. 13839

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2,6-dichloro-4-[2-(1-piperazinyl)-4-pyridinyl]-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)-benzenesulfonamide
CAS Number
1215010-55-1
Synonyms
  • IMP-366
Molecular Formula
C21H24Cl2N6O2S
Formula Weight
495.4
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 25 mg/mlDMSO: 25 mg/mlDMSO:PBS (pH 7.2) (1:1): 0.5 mg/mlEthanol: slightly solublePBS (pH 7.2): slightly soluble
λmax
226, 258 nm
SMILES
ClC1=CC(C2=CC=NC(N3CCNCC3)=C2)=CC(Cl)=C1S(NC4=C(C)N(C)N=C4C)(=O)=O
InChi Code
InChI=1S/C21H24Cl2N6O2S/c1-13-20(14(2)28(3)26-13)27-32(30,31)21-17(22)10-16(11-18(21)23)15-4-5-25-19(12-15)29-8-6-24-7-9-29/h4-5,10-12,24,27H,6-9H2,1-3H3
InChi Key
XMBSZPZJLPTFMV-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Cayman Chemical
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    Product Description

    DDD85646 is a moderately bioavailable pyrazole sulphonamide inhibitor of T. brucei N-myristoyltransferase (TbNMT) with an apparent Ki value of 1.44 nM.1 T. brucei is the parasite responsible for human African trypanosomiasis (HAT), also known as African sleeping sickness, and is transmitted through the tsetse fly. DDD85646 administration in mice (12.5 mg/kg for four days) ameliorated T. brucei in an acute mouse model of HAT.1 It less potently inhibits growth of T. cruzi (EC50 = 6.9 µM).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Frearson, J.A., Brand, S., McElroy, S.P., et al. N-myristoyltransferase inhibitors as new leads to treat sleeping sickness. Nature 464(7829), 728-732 (2010).