PTC-209 - CAS 315704-66-6
Catalog number: B0084-462442
Category: Inhibitor
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Molecular Formula:
C17H13Br2N5OS
Molecular Weight:
495.19
COA:
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Targets:
Others
Description:
PTC-209 is a potent BMI-1 inhibitor with potential anticancer activity. PTC-209 inhibits endogenous BMI-1 expression in human colorectal HCT116 and human fibrosarcoma HT1080 tumor cells.
Ordering Information
Catalog Number Size Price Stock Quantity
B0084-462442 25 mg $188 In stock
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Synonyms:
PTC-209; PTC 209; PTC209
MSDS:
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InChIKey:
XVOOCQSWCCRVDY-UHFFFAOYSA-N
InChI:
InChI=1S/C17H13Br2N5OS/c1-9-15(24-5-3-4-20-16(24)21-9)13-8-26-17(22-13)23-14-11(18)6-10(25-2)7-12(14)19/h3-8H,1-2H3,(H,22,23)
Canonical SMILES:
CC1=C(N2C=CC=NC2=N1)C3=CSC(=N3)NC4=C(C=C(C=C4Br)OC)Br
1.Targeting of BMI-1 with PTC-209 shows potent anti-myeloma activity and impairs the tumour microenvironment.
Bolomsky A1, Schlangen K2, Schreiner W3, Zojer N4, Ludwig H5. J Hematol Oncol. 2016 Mar 2;9:17. doi: 10.1186/s13045-016-0247-4.
BACKGROUND: The polycomb complex protein BMI-1 (BMI-1) is a putative oncogene reported to be overexpressed in multiple myeloma (MM). Silencing of BMI-1 was shown to impair the growth and survival of MM cells. However, therapeutic agents specifically targeting BMI-1 were not available so far. Here, we investigated PTC-209, a novel small molecule inhibitor of BMI-1, for its activity in MM.
2.The BMI1 inhibitor PTC-209 is a potential compound to halt cellular growth in biliary tract cancer cells.
Mayr C1,2, Wagner A1, Loeffelberger M2, Bruckner D3, Jakab M4, Berr F2, Di Fazio P5, Ocker M6,7,8, Neureiter D8, Pichler M9, Kiesslich T1,2. Oncotarget. 2016 Jan 5;7(1):745-58. doi: 10.18632/oncotarget.6378.
BMI1 is a core component of the polycomb repressive complex 1 (PRC1) and is up-regulated in biliary tract cancer (BTC), contributing to aggressive clinical features. In this study we investigated the cytotoxic effects of PTC-209, a recently developed inhibitor of BMI1, in BTC cells. PTC-209 reduced overall viability in BTC cell lines in a dose-dependent fashion (0.04 - 20 µM). Treatment with PTC-209 led to slightly enhanced caspase activity and stop of cell proliferation. Cell cycle analysis revealed that PTC-209 caused cell cycle arrest at the G1/S checkpoint. A comprehensive investigation of expression changes of cell cycle-related genes showed that PTC-209 caused significant down-regulation of cell cycle-promoting genes as well as of genes that contribute to DNA synthesis initiation and DNA repair, respectively. This was accompanied by significantly elevated mRNA levels of cell cycle inhibitors. In addition, PTC-209 reduced sphere formation and, in a cell line-dependent manner, aldehyde dehydrogease-1 positive cells.
3.Preclinical activity of the novel B-cell-specific Moloney murine leukemia virus integration site 1 inhibitor PTC-209 in acute myeloid leukemia: Implications for leukemia therapy.
Nishida Y1, Maeda A1, Chachad D2, Ishizawa J2, Qiu YH2, Kornblau SM2, Kimura S1, Andreeff M2, Kojima K1,2. Cancer Sci. 2015 Dec;106(12):1705-13. doi: 10.1111/cas.12833. Epub 2015 Nov 20.
Curing patients with acute myeloid leukemia (AML) remains a therapeutic challenge. The polycomb complex protein B-cell-specific Moloney murine leukemia virus integration site 1 (BMI-1) is required for the self-renewal and maintenance of leukemia stem cells. We investigated the prognostic significance of BMI-1 in AML and the effects of a novel small molecule selective inhibitor of BMI-1, PTC-209. BMI-1 protein expression was determined in 511 newly diagnosed AML patients together with 207 other proteins using reverse-phase protein array technology. Patients with unfavorable cytogenetics according to Southwest Oncology Group criteria had higher levels of BMI-1 compared to those with favorable (P = 0.0006) or intermediate cytogenetics (P = 0.0061), and patients with higher levels of BMI-1 had worse overall survival (55.3 weeks vs. 42.8 weeks, P = 0.046). Treatment with PTC-209 reduced protein level of BMI-1 and its downstream target mono-ubiquitinated histone H2A and triggered several molecular events consistent with the induction of apoptosis, this is, loss of mitochondrial membrane potential, caspase-3 cleavage, BAX activation, and phosphatidylserine externalization.
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CAS 315704-66-6 PTC-209

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