For research use only. Not for therapeutic Use.
<p style=/line-height:25px/>PTC-209 is a specific inhibitor for BMI-1 with IC50 of 0.5 uM in in both GEMS reporter and ELISA assays.<br>IC50 value: 0.5 uM [1]<br>Target: BMI-1<br>PTC-209 inhibited not only the UTR-mediated reporter expression but also endogenous BMI-1 expression in human colorectal HCT116 and human fibrosarcoma HT1080 tumor cells. PTC-209 caused no inhibition of cell growth or viability in HEK293 human embryonic kidney cells after overnight treatment and had limited effects on cell proliferation in HT1080 cells after a 48-h treatment. PTC-209 selectively reduced global ubiquitinated histone H2A (uH2A) but not total H2A and RING1A levels indicating its ability to specifically reduce PRC1 activity. Compound PTC-209 preferentially inhibits the proliferation of human lymphoma U937 and HT1080 tumor cells, whereas it is lesseffective in primary human peripheral blood mononuclear cells and human hematopoietic stem cells.</p>
| Catalog Number | I003125 |
| CAS Number | 315704-66-6 |
| Synonyms | N-(2,6-dibromo-4-methoxyphenyl)-4-(2-methylimidazo[1,2-a]pyrimidin-3-yl)-2-thiazolamine |
| Molecular Formula | C₁₇H₁₃Br₂N₅OS |
| Purity | ≥95% |
| Target | Autophagy |
| Solubility | DMSO: ≥ 32 mg/mL |
| Storage | -20°C |
| IC50 | 0.5 uM [1] |
| 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) |
| InChIKey | XVOOCQSWCCRVDY-UHFFFAOYSA-N |
| SMILES | CC1=C(N2C=CC=NC2=N1)C3=CSC(=N3)NC4=C(C=C(C=C4Br)OC)Br |
| Reference | </br>1:Targeting of BMI-1 with PTC-209 shows potent anti-myeloma activity and impairs the tumour microenvironment. Bolomsky A, Schlangen K, Schreiner W, Zojer N, Ludwig H.J Hematol Oncol. 2016 Mar 2;9:17. doi: 10.1186/s13045-016-0247-4. PMID: 26935956 Free PMC Article</br>2:The BMI1 inhibitor PTC-209 is a potential compound to halt cellular growth in biliary tract cancer cells. Mayr C, Wagner A, Loeffelberger M, Bruckner D, Jakab M, Berr F, Di Fazio P, Ocker M, Neureiter D, Pichler M, Kiesslich T.Oncotarget. 2016 Jan 5;7(1):745-58. doi: 10.18632/oncotarget.6378. PMID: 26623561 Free PMC Article</br>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 Y, Maeda A, Chachad D, Ishizawa J, Qiu YH, Kornblau SM, Kimura S, Andreeff M, Kojima K.Cancer Sci. 2015 Dec;106(12):1705-13. doi: 10.1111/cas.12833. Epub 2015 Nov 20. PMID: 26450753 Free PMC Article |
