Drug intelligence / Profile preview

BK10007S

Development stage
Preclinical
Modality
Small Molecules
Administration
Unknown (studied In Vitro And Animal Models)
01

Overview

BK10007S is a **piperazine derivative** that acts as a **T-type calcium channel (CaV3.1, a1G isoform) blocker** and a small molecule anticancer candidate. It demonstrates significant **cytotoxicity and anti-proliferative effects** in hepatocellular carcinoma (HCC) cell lines (HepG2, SK-Hep1) and other tumor cell types. Its **mechanism of action** involves induction of apoptosis through **activation of caspase cascades (caspase 8, 9, and 3), cleavage of poly (ADP-ribose) polymerase (PARP),** and **downregulation of CUG-binding protein 1 (CUGBP1, also known as CELF1), cyclin D1, and survivin**. BK10007S promotes both mitochondrial (intrinsic) and death receptor (extrinsic) apoptotic pathways. It has shown antiproliferative and pro-apoptotic activity in in vitro and xenograft cancer models, including HCC and pancreatic carcinoma[1][3].

02

Targets

CELF1 (CUGBP Elav-like family member 1)CACNA1G (T-type Calcium Channel Protein Subunit Alpha-1G)CASP3 (Caspase-3)CASP8 (Caspase-8)CASP9 (Caspase-9)

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