An Hsf1 inhibitor
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KRIBB11

Item No. 9002528

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N2-1H-indazol-5-yl-N6-methyl-3-nitro-2,6-pyridinediamine
CAS Number
342639-96-7
Molecular Formula
C13H12N6O2
Formula Weight
284.3
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS(pH 7.2) (1:4): 0.2 mg/mlEthanol: 1 mg/mlPBS (pH 7.2): slightly soluble
λmax
242, 294, 418 nm
SMILES
CNC1=NC(NC2=CC=C(NN=C3)C3=C2)=C([N+]([O-])=O)C=C1
InChi Code
InChI=1S/C13H12N6O2/c1-14-12-5-4-11(19(20)21)13(17-12)16-9-2-3-10-8(6-9)7-15-18-10/h2-7H,1H3,(H,15,18)(H2,14,16,17)
InChi Key
NDJJEQIMIJJCLL-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $69

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    10 mg

    $127

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    Cayman Chemical
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    Product Description

    KRIBB11 is an inhibitor of heat shock factor 1 (Hsf1) with an IC50 value of 1.2 μM in a luciferase reporter assay.1 It blocks heat shock-induced Hsp70, Hsp40, and Hsp27 mRNA expression and down-regulates protein expression of the Hsf1 target proteins Hsp70 and Hsp27 in HCT116 cells in a dose-dependent manner. KRIBB11 specifically binds to Hsf1 over other Hsf1-associated proteins, lacking activity at heat shock protein 90 (Hsp90), Hsf2, and Cdk9 in an in vitro pull-down assay. It inhibits growth of HCT116, Mia-PaCa-2, SW620, HT-29, A549, and MDA-MB-231 cancer cell lines (IC50s = 3-8 μM) via induction of cell cycle arrest at the G2/M phase and apoptosis. In vivo, administration of KRIBB11 decreases tumor growth in a mouse HCT116 xenograft model. KRIB11 administration also attenuates dengue virus progression and reduces mortality without affecting bodyweight in infected mice.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Yoon, Y.J., Kim, J.A., Shin, K.D., et al. KRIBB11 inhibits HSP70 synthesis through inhibition of heat shock factor 1 function by impairing the recruitment of positive transcription elongation factor b to the hsp70 promoter. The Journal of Biological Chemisty 286(3), 1737-1747 (2011).

    2. Tsai, T.T., Chen, C.L., Tsai, C.C., et al. Targeting heat shock factor 1 as an antiviral strategy against dengue virus replication in vitro and in vivo. Antiviral Res. 145, 44-53 (2017).