2. Apoptosis PROTAC
  3. c-Myc Molecular Glues
  4. WBC100

WBC100  (Synonyms: 14-D-Valine-TPL)

Cat. No.: HY-145898
COA Handling Instructions

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.

For research use only. We do not sell to patients.

WBC100 Chemical Structure

WBC100 Chemical Structure

CAS No. : 2095780-08-6

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WBC100 Related Antibodies

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Description

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].

In Vitro

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].

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

WBC100 Related Antibodies

Cell Viability Assay[1]

Cell Line: c-Myc overexpressing cancer cells: Mia-paca2, H9, and MOLM-13 cell
c-Myc-low normal human cell lines: L02, MRC-5 and WI38
Concentration:
Incubation Time: 72 hours
Result: Preferentially killed c-Myc overexpressing cancer cells.

Western Blot Analysis[1]

Cell Line: Mia-paca2 cells, MOLM-13 cell
Concentration: 0 nM, 20 nM, 40 nM, 80 nM, 160 nM,320 nM
Incubation Time: 24 hours
Result: Selectively induced degradation of c-Myc protein through E3 ubiquitin ligase CHIP mediated 26S proteasome pathway.
In Vivo

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].

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

Animal Model: Orthotopic human AML model using NOD/SCID/IL2Rγ-/- (NSG) mice with refractory MOLM-13-luciferase cells with high c-Myc levels
Dosage: 0.1 mg/kg; 0.2 mg/kg; 0.4 mg/kg
Administration: p.o.; 0.1-0.4 mg/kg; Twice daily; 21 days
Result: Regresses c-Myc overexpressing refractory acute myeloid leukemia model.
Clinical Trial
Molecular Weight

459.53

Appearance

Solid

Formula

C25H33NO7
CAS No.
SMILES

C[C@@]([C@@]1([H])C2)(CCC3=C1COC3=O)[C@]4([C@@]([C@@](O5)([H])[C@@]65C(C)C)([H])O4)[C@@]7([C@@]2([H])O7)[C@@H]6OC([C@H](N)C(C)C)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Purity & Documentation
References
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WBC100 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Keywords:

WBC1002095780-08-614-D-Valine-TPLWBC 100WBC-100c-MycMolecular GluesMyccancerc-Myc oncoproteinproteolysis targeting moleculetargeted therapyacute myeloid leukemiapancreaticgastric cancermolecular glueInhibitorinhibitorinhibit

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