Drug intelligence / Profile preview

SP2509

Development stage
Preclinical
Lead developer
Salarius Pharmaceuticals
Modality
Small Molecules
Administration
Oral, Intraperitoneal
01

Overview

SP2509 is a small molecule inhibitor targeting **lysine-specific demethylase 1 (LSD1/KDM1A)**, functioning as a selective and potent antagonist of LSD1's enzymatic activity and protein interactions. It exhibits significant **antitumor activity** in multiple cancer types, including retinoblastoma, renal carcinoma, and prostate cancer, by inducing **cell cycle arrest at the G0/G1 phase**, promoting **apoptosis**, and downregulating antiapoptotic factors like Bcl-2 and Mcl-1[1][2][3][7]. SP2509 has also demonstrated inhibitory activity against the **JAK/STAT3 signaling pathway**, attributed to LSD1 inhibition, and can disrupt protein-protein interactions with epigenetic complexes such as **CoREST** and specific transcription factors (e.g., TBX2), affecting downstream oncogenic and resistance mechanisms[5][7]. Preclinical studies suggest that SP2509 may also reduce viral replication in HSV-1 infection and modulate epigenetic regulation impacting organelle homeostasis[4][5]. SP2509 is developed primarily as an **anticancer agent** and may hold potential for combination therapy with chemotherapeutic drugs.

Other names
CAS 1423715-09-6CAS1423715-09-6CAS-1423715-09-6
02

Targets

KDM1A (LSD1)

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