| Bioactivity | WBC100 is a potent, selective, and orally active c‐Myc molecule glue. WBC100 is a c‐Myc degrader and targets ubiquitin E3 ligase CHIP mediated 26S proteasome pathway. WBC100 is used for c‐Myc overexpressing tumors research[1]. |
| Invitro | WBC100 selectively kills c‐Myc overexpressing cancer cells Mia‐paca2, H9, and MOLM‐13 cell as well as c‐Myc‐low normal human cell lines L02, MRC‐5 and WI38, the IC50 values are 61 × 10−9, 17 × 10−9, and 16 × 10−9 m, respectively. Whereas the IC50 values for normal cell lines L02, MRC‐5 and WI38 were 2205 × 10−9, 151 × 10−9, and 570 × 10−9 m, respectively[1].WBC100 (0-320 nM; 24 hour) decreases c‐Myc protein levels in MOLM‐13 cells and Mia‐paca2 cells in a dose‐dependent manner, but has no obvious impact on XPB, Rpb1, and STAT3. Additionally, MG132 can rescue the WBC100‐induced decline in c‐Myc protein[1]. Cell Viability Assay[1] Cell Line: |
| In Vivo | WBC100 (p.o.; 0.1-0.4 mg/kg; Twice daily; 21 days) 在体内表现出剂量依赖性的抗肿瘤活性。高剂量或中剂量 (0.4/0.2 mg/kg) 的 WBC100 可在体内根除 MOLM‐13‐荧光素酶细胞，所有小鼠在第 35 天均无病存活。此外，在低剂量 (0.1 mg/kg) 下，WBC100还能显著抑制白血病小鼠肿瘤生长，延长生存期[1]。WBC100 (p.o.; 0.4-0.8 mg/kg; once daily; 14 days) 在体内消除难治性MOLM‐13‐荧光素酶细胞，但 (+)‐JQ1 (50 mg/kg，腹腔注射(i.p)，每天一次，持续14天)对抑制肿瘤生长无效。WBC100表现出比c‐Myc转录抑制剂 (+)‐JQ1更强的抗肿瘤活性[1]。 Animal Model: |
| Name | WBC100 |
| CAS | 2095780-08-6 |
| Formula | C25H33NO7 |
| Molar Mass | 459.53 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Ying Xu, et al. A Selective Small-Molecule c-Myc Degrader Potently Regresses Lethal c-Myc Overexpressing Tumors. Adv Sci (Weinh). 2022 Mar;9(8):e2104344. |