PBITE-1 | ERG PNT domain binder | Probechem Biochemicals

Chemical Structure : PBITE-1

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PBITE-1 (Y0636)

货号: PC-27273Not For Human Use, Lab Use Only.

PBITE-1 is a small molecule that selectively binds ERG N-terminal Pointed (PNT) domain with Kd of 264 uM in BLI assays, directly engages ERG, selectively inhibits proliferation and invasion, and induces apoptosis in ERG-driven prostate and hematologic malignancies.

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生物&药学活性

PBITE-1 is a small molecule that selectively binds ERG N-terminal Pointed (PNT) domain with Kd of 264 uM in BLI assays, directly engages ERG, selectively inhibits proliferation and invasion, and induces apoptosis in ERG-driven prostate and hematologic malignancies.
PBITE-1 selectively inhibits proliferation in all ERG+ prostate cancer and leukemia cell lines, whereas ERG- cell lines remains largely unaffected.
PBITE-1 inhibits ERG-mediated oncogenic activities.
PBITE-1 potently suppresses VCaP viability with an IC50 of 80.1 µM, whereas enzalutamide and bicalutamide shows minimal effects.
PBITE-1 suppresses growth of ERG-positive organoids, selectively suppresses the growth and survival of ERG-driven prostate cancer organoids across both mouse and human systems.
PBITE-1 treatment induces cellular apoptosis in VCaP xenograft models, through suppression of ERG-dependent transcriptional programs and induction of tumor-selective apoptosis.

物理化学性质&存储条件

分子量	340.45
分子式	C18H20N4OS
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	N-(4-(2-methyl-1H-indol-3-yl)thiazol-2-yl)piperidine-4-carboxamide

参考文献

1. Wang X, et al. Proc Natl Acad Sci U S A. 2026 Jul 14;123(28):e2537437123.

PBITE-1 (Y0636)

生物&药学活性

物理化学性质&存储条件

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PBITE-1 (Y0636)

生物&药学活性

物理化学性质&存储条件

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