WBC100

• CAT Number: I041194
• CAS Number: 2095780-08-6
• Molecular Formula: C25H33NO7
• Molecular Weight: 459.53
• Purity: ≥95%
• Synonyms: [(1S,2S,4S,5S,7S,8R,9R,11S,13S)-1-methyl-17-oxo-7-propan-2-yl-3,6,10,16-tetraoxaheptacyclo[11.7.0.02,4.02,9.05,7.09,11.014,18]icos-14(18)-en-8-yl] (2R)-2-amino-3-methylbutanoate
• InChI: InChI=1S/C25H33NO7/c1-10(2)16(26)20(28)30-21-23(11(3)4)17(32-23)18-25(33-18)22(5)7-6-12-13(9-29-19(12)27)14(22)8-15-24(21,25)31-15/h10-11,14-18,21H,6-9,26H2,1-5H3/t14-,15-,16+,17-,18-,21+,22-,23-,24+,25+/m0/s1
• InChIKey: OWLJDBBFRJXPGM-VBIGTWTASA-N
• SMILES: CC(C)C(C(=O)OC1C23C(O2)CC4C5=C(CCC4(C36C(O6)C7C1(O7)C(C)C)C)C(=O)OC5)N

WBC100 (14-D-Valine-TPL) is a potent, selective, and orally active c-Myc molecule glue degrader. 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].
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 for c-Myc overexpressing cancer cells, respectively. Whereas the IC50 values for normal cell lines are 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].
WBC100 (p.o.; 0.1-0.4 mg/kg; twice daily; 21 days) exerts dose-dependent antitumor activity in vivo. Higher or medium (0.4/0.2 mg/kg) doses of WBC100 eradicates MOLM-13-luciferase cells in vivo and all the mice were disease-free survival on day 35. Additionally, at a low dose (0.1 mg/kg), WBC100 also significantly inhibits tumor growth and prolongs survival of leukemia mice[1].
WBC100 (p.o.; 0.4-0.8 mg/kg; once daily; 14 days) eliminates refractory MOLM-13-luciferase cells in vivo, but both (+)-JQ1 (50 mg/kg, intraperitoneal (i.p.), once a day for 14 d) is ineffective in suppressing tumor growth. WBC100 exhibits stronger antitumor activity than c-Myc transcription inhibitor (+)-JQ1[1].

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.
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