BI 2536 

BI 2536 (GMP) is BI 2536 (HY-50698) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. BI 2536 is a dual PLK1 and BRD4 inhibitor with IC₅₀s of 0.83 and 25 nM, respectively^[1]. BI-2536 suppresses IFNB (encoding IFN-β) gene transcription^[4].

Exceeding a 100-fold concentration range starting at 10 nM, BI 2536 (GMP) causes HeLa cells to accumulate with a 4N DNA content, indicative of a cell-cycle block in either G2 phase or mitosis. In addition to HeLa cells, BI 2536 (GMP) potently inhibits the proliferation of a panel of 32 human cancer cell lines, representing diverse organ derivations (including carcinomas of the breast, colon, lung, pancreas, and prostate, melanomas, and hematopoietic cancers) and varied patterns of tumor suppressor or oncogene mutations (including RB1, TP53, PTEN, andKRAS status). The half-maximal effective concentration (EC₅₀) values in this cell panel ranged 2-25 nM, whereas a concentration of 100 nM of BI 2536 (GMP) is typically sufficient for inducing a complete mitotic arrest. The proliferation of exponentially growing hTERT-RPE1, human umbilical vein endothelial cells (HUVECs), and normal rat kidney (NRK) cells is blocked at EC₅₀values ranging 12-31 nM, indicating a comparable sensitivity of cycling nontransformed cells to BI 2536 (GMP)^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

BI 2536 (GMP) (40-50 mg/kg, i.v.) blocks the growth of human cancer xenografts in immunodeficient, nu/nu mice. Consecutive cycles of 40-50 mg/kg BI 2536 (GMP) given i.v. once or twice per week are found to be highly efficacious in diverse xenograft models, such as the HCT 116 colon cancer with complete tumor suppression with the twice per week schedule (treated versus the control (T/C) value 0.3%) and a T/C value of 16% with once per week treatment; both schedules are well-tolerated, as judged by clinical signs and absence of major body-weight changes^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

521.65

C₂₈H₃₉N₇O₃

755038-02-9

O=C1[C@H](N(C2=C(N1C)C=NC(NC3=CC=C(C(NC4CCN(C)CC4)=O)C=C3OC)=N2)C5CCCC5)CC

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Malik N, et al. Suppression of IFN β gene transcription by inhibitors of bromodomain and extra-terminal (BET) family members. Biochem J. 2015 Jun 15;468(3):363-72.  [Content Brief]

  [2]. Chen L, et al. BRD4 Structure-Activity Relationships of Dual PLK1 Kinase/BRD4 Bromodomain Inhibitor BI-2536. ACS Med Chem Lett. 2015 May 18;6(7):764-9.  [Content Brief]

  [3]. Steegmaier M, et al. BI 2536, a Potent and Selective Inhibitor of Polo-like Kinase 1, Inhibits Tumor Growth In Vivo. Current Biology (2007), 17(4), 316-322.  [Content Brief]

  [4]. Lénárt P, et al. The Small-Molecule Inhibitor BI 2536 Reveals Novel Insights into Mitotic Roles of Polo-like Kinase 1. Curr Biol. 2007 Feb 20;17(4):304-15.  [Content Brief]