A PRMT9 inhibitor
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LD2

Item No. 42447

Technical Information
Formal Name
4-chloro-8-methoxy-5-methyl-5H-pyrimido[5,4-b]indole
CAS Number
1134334-55-6
Molecular Formula
C12H10ClN3O
Formula Weight
Purity
≥95%
Formulation
A solid
Acetonitrile: Soluble: ≥ 10 mg/mlDMSO: Sparingly soluble: 1/10 mg/mlEthanol: Slightly soluble: 0.1-1 mg/ml
SMILES
ClC1=NC=NC2=C1N(C)C3=C2C=C(C=C3)OC
InChi Code
InChI=1S/C12H10ClN3O/c1-16-9-4-3-7(17-2)5-8(9)10-11(16)12(13)15-6-14-10/h3-6H,1-2H3
InChi Key
VKWOHOPWHUHGQV-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    LD2 is an inhibitor of protein arginine methyltransferase 9 (PRMT9; IC50 = 0.9 µM).1 It reduces the proliferation of Rec-1 and Raji lymphoblasts, UPN1 mantle cell lymphoma, BL-41 Burkitt lymphoma, and OCI-Ly3 diffuse large B cell lymphoma (DLBCL) cells (IC50s = 2.5-5 µM). LD2 (2.5 µM) induces cell cycle arrest at the G2/M phase in THP-1 acute myeloid leukemia (AML) cells. It decreases phosphorylated levels of checkpoint kinase 1 (Chk1) and Chk2 in THP-1 cells. In vivo, LD2 (10 mg/kg twice per day), in combination with an anti-programmed cell death protein 1 (anti-PD-1) antibody, decreases tumor volume in an AML mouse xenograft model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Li, L., Dong, H., Zhang, L., et alProtein arginine methyltransferase 9 inhibitors and methods of use. AS 2024/0132887 Al, (2024).