A prodrug form of KDM5-C49
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JQKD82 (hydrochloride)

Item No. 41542

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-[[[2-[[2-(dimethylamino)ethyl]ethylamino]-2-oxoethyl]amino]methyl]-4-pyridinecarboxylic acid, 2,4-bis(1-methylethoxy)phenyl ester, trihydrochloride
CAS Number
2863676-87-1
Synonyms
  • JADA82
  • PCK82
Molecular Formula
C27H40N4O5 • 3HCl
Formula Weight
610.0
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingy soluble: 1-10 mg/mlPBS (pH 7.2): Soluble: ≥10 mg/ml
SMILES
O=C(C1=CC(CNCC(N(CCN(C)C)CC)=O)=NC=C1)OC2=CC=C(OC(C)C)C=C2OC(C)C.Cl.Cl.Cl
InChi Code
InChI=1S/C27H40N4O5.3ClH/c1-8-31(14-13-30(6)7)26(32)18-28-17-22-15-21(11-12-29-22)27(33)36-24-10-9-23(34-19(2)3)16-25(24)35-20(4)5;;;/h9-12,15-16,19-20,28H,8,13-14,17-18H2,1-7H3;3*1H
InChi Key
VSTHCFWHQMJPDZ-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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    1 mg

    $72

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    5 mg

    $304

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    10 mg

    $537

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    25 mg

    $1,073

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    Cayman Chemical
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    Product Description

    JQKD82 is a prodrug form of KDM5-C49, an inhibitor of Jumonji AT-rich interactive domain 1A (JARID1A), also known as lysine-specific demethylase 5A (KDM5A).1 It increases the levels of trimethylated lysine 4 on histone 3 (H3K4me3) in MOLP-8 and MM.1S multiple myeloma cells when used at concentrations of 0.3 and 1 µM. JQKD82 reduces the proliferation of MOLP-8 and MM.1S cells in a concentration-dependent manner and decreases the viability of primary CD138+ cells from patients with multiple myeloma when used at a concentration of 3 µM. It induces cell cycle arrest at the G0/G1 phase, as well as induces apoptosis, in MOLP-8 and MM.1S cells when used at a concentration of 1 µM. JQKD82 (50 mg/kg twice per day) decreases tumor growth and increases survival in a MOLP-8 mouse xenograft model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Ohguchi, H., Park, P.M.C., Wang, T., et al. Lysine demethylase 5A is required for MYC-driven transcription in multiple myeloma. Blood Cancer Discov. 2(4), 370-387 (2021).