BMI-1026
BMI-1026 is a potent cdk inhibitor with potential anticancer activity. BMI-1026 induced a strong cell cycle alteration with potent inhibitory activities against cyclin-dependent kinases, collectively known as Cdks. BMI-1026 imposes a potent G(2)-M arrest and mild G(1)-S and S arrests. In vitro BMI-1026 induces a mitotic catastrophe and precocious mitotic exit even in the presence of nocodazole. These defects appeared to lead to apoptotic cell death in tumorigenic cell lines. Consistent with the induction of mitotic defects and apoptosis, BMI-1026 imposed a selective sensitivity to proliferating versus differentiating or growth-arrested mouse keratinocytes. These data suggest that BMI-1026 could be developed as a potential anti-Cdk1 chemotherapeutic agent.
1: Seo HJ, Park HJ, Choi HS, Hwang SY, Park JS, Seong YS. BMI-1026 treatment can induce SAHF formation by activation of Erk1/2. BMB Rep. 2008 Jul 31;41(7):523-8. PubMed PMID: 18682036.
2: Genazzani AD, Lanzoni C, Ricchieri F, Baraldi E, Casarosa E, Jasonni VM. Metformin administration is more effective when non-obese patients with polycystic ovary syndrome show both hyperandrogenism and hyperinsulinemia. Gynecol Endocrinol. 2007 Mar;23(3):146-52. PubMed PMID: 17454168.
3: Niiya F, Xie X, Lee KS, Inoue H, Miki T. Inhibition of cyclin-dependent kinase 1 induces cytokinesis without chromosome segregation in an ECT2 and MgcRacGAP-dependent manner. J Biol Chem. 2005 Oct 28;280(43):36502-9. Epub 2005 Aug 23. PubMed PMID: 16118207.
4: Collins I, Garrett MD. Targeting the cell division cycle in cancer: CDK and cell cycle checkpoint kinase inhibitors. Curr Opin Pharmacol. 2005 Aug;5(4):366-73. Review. PubMed PMID: 15964238.
5: Seong YS, Min C, Li L, Yang JY, Kim SY, Cao X, Kim K, Yuspa SH, Chung HH, Lee KS. Characterization of a novel cyclin-dependent kinase 1 inhibitor, BMI-1026. Cancer Res. 2003 Nov 1;63(21):7384-91. Erratum in: Cancer Res. 2004 May 15;64(10):3725. PubMed PMID: 14612537.
2: Genazzani AD, Lanzoni C, Ricchieri F, Baraldi E, Casarosa E, Jasonni VM. Metformin administration is more effective when non-obese patients with polycystic ovary syndrome show both hyperandrogenism and hyperinsulinemia. Gynecol Endocrinol. 2007 Mar;23(3):146-52. PubMed PMID: 17454168.
3: Niiya F, Xie X, Lee KS, Inoue H, Miki T. Inhibition of cyclin-dependent kinase 1 induces cytokinesis without chromosome segregation in an ECT2 and MgcRacGAP-dependent manner. J Biol Chem. 2005 Oct 28;280(43):36502-9. Epub 2005 Aug 23. PubMed PMID: 16118207.
4: Collins I, Garrett MD. Targeting the cell division cycle in cancer: CDK and cell cycle checkpoint kinase inhibitors. Curr Opin Pharmacol. 2005 Aug;5(4):366-73. Review. PubMed PMID: 15964238.
5: Seong YS, Min C, Li L, Yang JY, Kim SY, Cao X, Kim K, Yuspa SH, Chung HH, Lee KS. Characterization of a novel cyclin-dependent kinase 1 inhibitor, BMI-1026. Cancer Res. 2003 Nov 1;63(21):7384-91. Erratum in: Cancer Res. 2004 May 15;64(10):3725. PubMed PMID: 14612537.
| Chemical | |
|---|---|
| CAS Num | 477726-77-5 |
| Chemical Formula | C14H12N6O |
| Molecular Weight | 280.28 |
| IUPAC Chemical Name | 2,4-bis(2-aminopyrimidin-4-yl)phenol |
| Exact Mass | 280.10726 |
| Elemental Analysis | C, 59.99; H, 4.32; N, 29.98; O, 5.71 |
| Synonym | BMI1026; BMI 1026; BMI-1026 |
| Solubility | Soluble in DMSO, not in water |
| SMILES Code | OC1=CC=C(C2=NC(N)=NC=C2)C=C1C3=NC(N)=NC=C3 |
| Biological | |
| Targets and Effects | cyclin-dependent kinase (CDK) inhibitor |
| Pathways | Apoptosis |
| Physical | |
| Appearance | Solid powder |
| Purity | >98% (or refer to the Certificate of Analysis) |
| Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
| Storage Condition | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
| Shelf Life | >2 years if stored properly |
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