An inhibitor of Mediator/Pdr1 interactions
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iKIX1

Item No. 19839

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-cyano-acetic acid, 2-[[(3,4-dichlorophenyl)amino]thioxomethyl]hydrazide
CAS Number
656222-54-7
Molecular Formula
C10H8Cl2N4OS
Formula Weight
303.2
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: soluble
λmax
241, 279 nm
SMILES
ClC1=C(Cl)C=CC(NC(NNC(CC#N)=O)=S)=C1
InChi Code
InChI=1S/C10H8Cl2N4OS/c11-7-2-1-6(5-8(7)12)14-10(18)16-15-9(17)3-4-13/h1-2,5H,3H2,(H,15,17)(H2,14,16,18)
InChi Key
XKQJVBSDCOCZFV-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $55

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    10 mg

    $495

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    Cayman Chemical
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    Product Description

    iKIX1 is an inhibitor of interactions between the transcription co-activator Mediator complex and the pleitropic drug resistance (CgPdr1) transcription factor in the pathogen C. glabrata.1 It inhibits the interaction between the KIX domain of the Mediator subunit CgGal11A and the activation domain of CgPdr1 (IC50 = 190.2 μM). iKIX1 (10 and 30 μM) inhibits ketoconazole-induced expression of CgPdr1-target genes involved in multidrug resistance and drug efflux in C. glabrata. It increases the sensitivity of azole-resistant C. glabrata strains expressing CgPDR1 gain-of-function mutations to the antifungal compounds fluconazole (Item No. 11594) and ketoconazole (Item No. 15212) in a concentration-dependent manner. iKIX1 (100 mg/kg) decreases fungal burden in the kidney and spleen in a mouse model of infection with azole-sensitive or -resistant C. glabrata when administered in combination with low and high doses of fluconazole, respectively.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Nishikawa, J.L., Boeszoermenyi, A., Vale-Silva, L.A., et al. Inhibiting fungal multidrug resistance by disrupting an activator-Mediator interaction. Nature 530(7591), 485-489 (2016).