An HDAC6 inhibitor
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KA2507

Item No. 46343

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[(di-2-pyrazinylamino)methyl]-N-hydroxy-benzamide
CAS Number
1636894-46-6
Molecular Formula
C16H14N6O2
Formula Weight
322.3
Purity
≥98%
Formulation (Request formulation change)
A solid
SMILES
ONC(C(C=C1)=CC=C1CN(C2=NC=CN=C2)C3=NC=CN=C3)=O
InChi Code
InChI=1S/C16H14N6O2/c23-16(21-24)13-3-1-12(2-4-13)11-22(14-9-17-5-7-19-14)15-10-18-6-8-20-15/h1-10,24H,11H2,(H,21,23)
InChi Key
LXHMTDHBMRZSHJ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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Certificates of Analysis & Batch Specific Data

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    5 mg

    $97

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    10 mg

    $155

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    25 mg

    $291

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    Cayman Chemical
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    Product Description

    KA2507 is a histone deacetylase 6 (HDAC6; IC50 = 2.5 nM) inhibitor.1 It is selective for HDAC6 over HDAC8 (IC50 = 621 nM) and HDAC1-5, -7, and -9-11 (IC50s = >1,000 nM for all) and sirtuin 1 (SIRT1), -2, -3, and -5 (IC50s = >10,000 nM for all). KA2507 inhibits the deacetylation of acetylated α-tubulin (EC50 = 150 nM) but not acetylated histone H3 (EC50 = >10,000 nM) in A549 lung adenocarcinoma cells. It increases intratumoral MHC class I expression and reduces intratumoral programmed cell death 1 ligand 1 (PD-L1) levels and tumor volume in B16/F10 murine melanoma, CT26 murine colon carcinoma, and MC-38 murine colon carcinoma models.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Tsimberidou, A.M., Beer, P.A., Cartwright, C.A., et al. Preclinical development and first-in-human study of KA2507, a selective and potent inhibitor of histone deacetylase 6, for patients with refractory solid tumors. Clin. Cancer Res. 27(13), 3584-3594 (2021).