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

WBC100  (Synonyms: 14-D-Valine-TPL)

Cat. No.: HY-145898 Purity: ≥95.0%
COA Handling Instructions

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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

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 1618 In-stock
Solution
10 mM * 1 mL in DMSO USD 1618 In-stock
Solid
1 mg USD 550 In-stock
5 mg USD 1600 In-stock
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Based on 1 publication(s) in Google Scholar

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

Formula

C25H33NO7
CAS No.
Appearance

Solid

Color

White to off-white

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
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (217.61 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: 2.5 mg/mL (5.44 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (5.44 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: ≥95.0%

COA (261 KB) HNMR (141 KB) LCMS (235 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1761 mL 10.8807 mL 21.7614 mL 54.4034 mL
5 mM 0.4352 mL 2.1761 mL 4.3523 mL 10.8807 mL
10 mM 0.2176 mL 1.0881 mL 2.1761 mL 5.4403 mL
15 mM 0.1451 mL 0.7254 mL 1.4508 mL 3.6269 mL
20 mM 0.1088 mL 0.5440 mL 1.0881 mL 2.7202 mL
25 mM 0.0870 mL 0.4352 mL 0.8705 mL 2.1761 mL
30 mM 0.0725 mL 0.3627 mL 0.7254 mL 1.8134 mL
40 mM 0.0544 mL 0.2720 mL 0.5440 mL 1.3601 mL
50 mM 0.0435 mL 0.2176 mL 0.4352 mL 1.0881 mL
60 mM 0.0363 mL 0.1813 mL 0.3627 mL 0.9067 mL
80 mM 0.0272 mL 0.1360 mL 0.2720 mL 0.6800 mL
100 mM 0.0218 mL 0.1088 mL 0.2176 mL 0.5440 mL
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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.

Keywords:

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

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