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BMI-1

BMI-1 inhibitors target a Polycomb group protein that silences genes and supports stem cell self-renewal. B cell-specific Moloney murine leukemia virus integration site 1 (BMI-1) is a core subunit of Polycomb repressive complex 1 (PRC1). In 2004, PRC1 was shown to monoubiquitinate histone H2A, a mark linked to Polycomb silencing. A 2003 mouse study found BMI-1 to be required for maintaining adult self-renewing hematopoietic stem cells. PTC-209 lowers BMI-1 protein levels and was used in 2014 to study self-renewal of colorectal cancer-initiating cells. PTC-028 and unesbulin are two further compounds listed here as BMI-1 inhibitors. PRT 4165 instead inhibits the ubiquitin ligase activity of the complex of BMI-1 with its partner ring finger protein 1A (RING1A).

Cat. No.

A13826

CAS No.

315704-66-6

PTC-209

PTC-209 is a novel potent and selective BMI-1 inhibitor, targeting the BMI-1 self-renewal machinery with an IC50 of ~0.5 μM.

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2 mg

$40.00

5 mg

$60.00

All 7 sizes
Cat. No.

A14280

CAS No.

1217022-63-3

PTC-209 HBr

Synonyms: PTX209

PTC-209 HBr is the hydrobromide salt of PTC-209. PTC-209 is a potent and selective BMI-1 inhibitor with IC50 of 0.5 μM in HEK293T cell line, and results in irreversible reduction of cancer-initiating cells (CICs).

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2 mg

$45.00

5 mg

$85.00

All 7 sizes
Cat. No.

A15453

CAS No.

31083-55-3

PRT 4165

PRT 4165 is an inhibitor of Bmi1/Ring1A, subunits of the polycomb repressive complex 1 (PRC1). It prevents Bmi1/Ring1A-mediated ubiquitination and drug-induced degradation of topoisomerase 2alpha.

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5 mg

$30.00

10 mg

$40.00

All 8 sizes
Cat. No.

A16812

CAS No.

1782970-28-8

PTC-028

PTC-028 is an orally bioavailable compound that decreases BMI-1 levels by posttranslational modification

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1 mg

$30.00

2 mg

$45.00

All 9 sizes
Cat. No.

A19320

CAS No.

1610964-64-1

Unesbulin (PTC596)

Synonyms: PTC 596

PTC596 is an orally active and selective B-cell-specific Moloney murine leukemia virus integration site 1 (BMI-1) inhibitor.

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1 mg

$80.00

5 mg

$190.00

All 6 sizes

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