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Merck

SML1143

PTC-209

≥98% (HPLC)

Sinónimos:

N-(2,6-Dibromo-4-methoxyphenyl)-4-(2-methylimidazo[1,2-a]pyrimidin-3-yl)-2-thiazolamine

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Fórmula empírica (notación de Hill):
C17H13Br2N5OS
Número CAS:
Peso molecular:
495.19
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
Assay:
≥98% (HPLC)
Form:
powder
Quality level:
Servicio técnico
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Quality Level

assay

≥98% (HPLC)

form

powder

color

white to brown

solubility

DMSO: 20 mg/mL, clear

storage temp.

2-8°C

SMILES string

BrC1=CC(OC)=CC(Br)=C1NC2=NC(C3=C(C)N=C4N3C=CC=N4)=CS2

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)

InChI key

XVOOCQSWCCRVDY-UHFFFAOYSA-N

Application

PTC-209 has been used as a B lymphoma Mo-MLV insertion region 1 homolog (BMI1) inhibitor to study its effects on:
  • the cell viability of canine osteosarcoma (OSA) cell lines
  • lipidated microtubule-associated protein 1 light chain 3 (LC3B-II) and Sequestosome 1 (SQSTM1) protein levels in ovarian cancer (OvCa) cells
  • cardiac reprogramming efficiency in mouse embryonic fibroblasts (MEF)

Biochem/physiol Actions

PTC-209 inhibits the expression of the oncogene BMI-1 (B lymphoma Mo-MLV insertion region 1 homolog), which encodes a polycomb group RING finger protein involved in cell cycle. PTC-209 lowers the self-renewal properties of colorectal cancer-initiating cells (CICs) The compound inhibits tumor growth, and reduces the levels of CICs present in colon cancer tumor xenografts in mice.
PTC-209 inhibits the expression of the oncogene BMI-1 (B lymphoma Mo-MLV insertion region 1 homolog).

Features and Benefits

This compound is a featured product for Gene Regulation research. Click here to discover more featured Gene Regulation products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.


Clase de almacenamiento

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable



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Inhibition of BMI1 induces autophagy-mediated necroptosis
Dey A, et al.
Autophagy, 12(4), 659-670 (2016)
BMI1 is expressed in canine osteosarcoma and contributes to cell growth and chemotherapy resistance
Shahi M H, et al.
PLoS ONE, 10(6), e0131006-e0131006 (2015)
Sami Al-Nadaf et al.
Veterinary and comparative oncology, 20(4), 871-880 (2022-07-15)
The BMI1 proto-oncogene, polycomb ring finger protein (BMI1) is a key component of the epigenetic polycomb repressor complex 1, and has been associated with aggressive behaviour and chemotherapeutic resistance in various malignances including human gliomas. Similar to humans, spontaneous canine