| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
Ubiquitin E3 ligase CHIP and the 26S proteasome pathway. WBC100 is a c-Myc degrader that induces the degradation of c-Myc protein through the ubiquitin-proteasome system.
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| ln Vitro |
WBC100 specifically destroys c-Myc overexpressing cancer cells Mia-paca2, H9, and MOLM-13, as well as low-expressing c-Myc normal human cell lines L02, MRC-5, and WI38. The values of IC50 against cancer cells that overexpress are 61×10-9, 17×10-9, and 16×10-9 M, in that order. For normal cell lines, the IC50 values are, in order, 2205 × 10-9, 151 × 10-9, and 570 × 10-9 M [1]. WBC100 (0-320 nM; 24 hours) dose-dependently decreased the amounts of c-Myc protein in MOLM-13 and Mia-paca2 cells, but had no discernible effect on XPB, Rpb1, or STAT3. Furthermore, WBC100-induced c-Myc protein can be saved by MG132 [1].
WBC100 specifically destroys c-Myc overexpressing cancer cells Mia-paca2, H9, and MOLM-13, with IC₅0 values of 61 nM, 17 nM, and 16 nM, respectively. For normal cell lines L02, MRC-5, and WI38, IC₅0 values are 2205 nM, 151 nM, and 570 nM, respectively. It dose-dependently decreases c-Myc protein levels. |
| ln Vivo |
WBC100 (po; 0.1–0.4 mg/kg; twice daily; 21 days) demonstrates anticancer efficacy that is dose-dependent. In vivo WBC100 treatment of high or medium doses (0.4/0.2 mg/kg) completely eliminated MOLM-13-luciferase cells, and by day 35, all animals were disease-free. Furthermore, WBC100 has been shown to considerably reduce tumor growth and increase survival in leukemia mice at modest dosages (0.1 mg/kg) [1]. Refractory MOLM-13-luciferase cells are eliminated in vivo by WBC100 (po; 0.4-0.8 mg/kg; once daily for 14 days); nevertheless, +)-JQ1 (50 mg/kg, i.p., daily Once, for 14 days) is ineffective in preventing tumor growth. Compared to the c-Myc transcription inhibitor (+)-JQ1, WBC100 has greater anti-tumor efficacy [1].
WBC100 (oral; 0.1-0.4 mg/kg; twice daily; 21 days) demonstrates dose-dependent anticancer efficacy. High or medium doses (0.4/0.2 mg/kg) completely eliminated MOLM-13-luciferase cells, with all animals disease-free by day 35. Low doses (0.1 mg/kg) significantly reduce tumor growth and increase survival. |
| Enzyme Assay |
As a molecular glue degrader, WBC100 induces ternary complex formation between c-Myc and the E3 ubiquitin ligase CHIP. Binding affinity and degradation efficacy are assessed using biochemical assays such as surface plasmon resonance (SPR) or isothermal titration calorimetry (ITC) to measure protein-protein interactions.
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: c-Myc overexpressing cancer cells: Mia-paca2, H9, and MOLM-13 cell c- Myc-low normal human Cell Types: L02, MRC-5 and WI38 Tested Concentrations: Incubation Duration: 72 hrs (hours) Experimental Results: Preferentially killed c-Myc overexpressing cancer cells. Western Blot Analysis[1] Cell Types: Mia-paca2 cells, MOLM-13 cell Tested Concentrations: 0 nM, 20 nM, 40 nM, 80 nM, 160 nM, 320 nM Incubation Duration: 24 hrs (hours) Experimental Results: Selectively induced degradation of c-Myc protein through E3 ubiquitin ligase CHIP mediated 26S proteasome pathway. Cell viability is assessed in c-Myc overexpressing cancer cells (Mia-paca2, H9, MOLM-13) and normal cell lines using CellTiter-Glo or MTT assays after 72 hours of treatment. c-Myc protein levels are measured by Western blot analysis after 24 hours of treatment. |
| Animal Protocol |
Animal/Disease Models: Orthotopic human AML model using NOD/SCID/IL2Rγ-/- (NSG) mice with refractory MOLM-13-luciferase cells with high c-Myc levels
Doses: 0.1 mg/kg; 0.2 mg/kg; 0.4 mg/kg Route of Administration: po; 0.1-0.4 mg/kg; twice (two times) daily; 21 days Experimental Results: Regresses c-Myc overexpressing refractory acute myeloid leukemia model. Mice bearing MOLM-13-luciferase xenografts are administered WBC100 orally at doses of 0.1-0.4 mg/kg twice daily for 21 days. Tumor growth is monitored by bioluminescence imaging, and survival is recorded. |
| ADME/Pharmacokinetics |
WBC100 is orally bioactive. It has a molecular weight of approximately 427.5 (free base) and is typically supplied as the TFA salt. Detailed pharmacokinetic parameters (half-life, Cmax, AUC, bioavailability) have not been fully reported in available literature.
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| Toxicity/Toxicokinetics |
No detailed toxicity data has been published for WBC100 in standard toxicology studies. As a research compound, it is not intended for human therapeutic use. In vivo studies in mouse xenograft models indicate that the compound is tolerated at doses up to 0.4 mg/kg.
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| References | |
| Additional Infomation |
WBC100 is a c-Myc molecular glue degrader that targets the ubiquitin E3 ligase CHIP-mediated 26S proteasome pathway. It shows superior anti-tumor efficacy compared to the c-Myc transcription inhibitor (+)-JQ1. The compound is for research use only and has not entered clinical trials.
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| Molecular Formula |
C25H33NO7
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|---|---|
| Molecular Weight |
459.532027959824
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| Exact Mass |
459.225
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| CAS # |
2095780-08-6
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| PubChem CID |
134236278
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| Appearance |
White to off-white solid powder
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| LogP |
1.3
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
33
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| Complexity |
1020
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| Defined Atom Stereocenter Count |
10
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| SMILES |
CC(C)[C@H](C(=O)O[C@H]1[C@@]23[C@@H](O2)C[C@H]4C5=C(CC[C@@]4([C@]36[C@@H](O6)[C@H]7[C@@]1(O7)C(C)C)C)C(=O)OC5)N
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| InChi Key |
OWLJDBBFRJXPGM-VBIGTWTASA-N
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| InChi Code |
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
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| Chemical Name |
[(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
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1761 mL | 10.8807 mL | 21.7614 mL | |
| 5 mM | 0.4352 mL | 2.1761 mL | 4.3523 mL | |
| 10 mM | 0.2176 mL | 1.0881 mL | 2.1761 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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