1. Metabolic Enzyme/Protease
  2. E1/E2/E3 Enzyme
  3. WSB1 Degrader 1

WSB1 Degrader 1 

Cat. No.: HY-141482 Purity: 99.93%
Handling Instructions

WSB1 Degrader 1 is a poten and orally active WSB1 (WD repeat and SOCS box-containing 1) degrader. WSB1 Degrader 1 has anticancer metastatic effects.

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

WSB1 Degrader 1 Chemical Structure

WSB1 Degrader 1 Chemical Structure

CAS No. : 2306039-66-5

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 330 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 330 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 300 In-stock
Estimated Time of Arrival: December 31
10 mg USD 480 In-stock
Estimated Time of Arrival: December 31
25 mg USD 950 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1450 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2250 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

WSB1 Degrader 1 is a poten and orally active WSB1 (WD repeat and SOCS box-containing 1) degrader. WSB1 Degrader 1 has anticancer metastatic effects[1].

In Vitro

WSB1 Degrader 1 (compound 4; 0.25-2500 nM; 2-24 hours; H1299-WSB1 cells) treatment indues WSB1 degradation in time-dependent and dose-dependent manners[1].
WSB1 Degrader 1 (compound 4) exhibits potent antimigration efficacy in both KHOS and H460 cell lines with IC50 values of 39.1 μM and 24.47 μM, respectively[1].
WSB1 Degrader 1 (compound 4) significantly inhibits cancer cell migration under normoxia and hypoxia in KHOS cells. WSB1 Degrader 1 (5 μM) treatment elevates the levels of the RhoGDI2 protein in KHOS cells under hypoxia[1].
The wound-healing of H1299-WSB1 cells is significantly inhibited by treating with WSB1 Degrader 1. WSB1 Degrader 1 can only block the wound-healing capability of wild-type A2780 (A2780-WT) cells but not the A2780-WSB1/KO cells[1].

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

Western Blot Analysis[1]

Cell Line: H1299-WSB1 cells
Concentration: 0.25 nM, 2.5 nM, 25 nM, 250 nM, 2500 nM
Incubation Time: 2 hours, 4 hours, 6 hours, 8 hours, 12 hours, 24 hours
Result: Induced WSB1 degradation in time-dependent and dose-dependent manners.
In Vivo

WSB1 Degrader 1 (compound 4; 100 mg/kg; p.o.; daily; for 28 days) treatment can effectively inhibit the pulmonary metastasis of cancer cells[1].
In rats, after 100 mg/kg oral dosing or 160 mg/kg intraperitoneal dosing of WSB1 Degrader 1 (compound 4), the two ways of administration are observed with quick absorption (Tmax), but the former dosing displayed a fast clearance (T1/2). Moreover, Cmax and AUC0-t values of WSB1 Degrader 1 in oral or intraperitoneal dosing groups showed acceptable blood exposure[1].

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

Animal Model: Balb/c (nu/nu) mice bearing highly metastatic 4T1 breast cancer cells[1].
Dosage: 100 mg/kg/day
Administration: p.o.; daily; for 28 days
Result: Effectively inhibited the pulmonary metastasis of cancer cells.
Molecular Weight

334.41

Formula

C₂₁H₂₂N₂O₂

CAS No.
SMILES

NC1=NC(C2=CC=C(OC)C(C)=C2)=C(C3=CC=C(OC)C(C)=C3)C=C1

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 : 25 mg/mL (74.76 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.9903 mL 14.9517 mL 29.9034 mL
5 mM 0.5981 mL 2.9903 mL 5.9807 mL
10 mM 0.2990 mL 1.4952 mL 2.9903 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: ≥ 2.08 mg/mL (6.22 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

WSB1 Degrader 1E1/E2/E3 EnzymeE1 activating enzymeE2 conjugating enzymeE3 ligating enzymeUbiquitin activating enzymeUbiquitin conjugating enzymeUbiquitin ligasemetastasisWSB1anticancerRhoGDI2oralInhibitorinhibitorinhibit

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Product Name:
WSB1 Degrader 1
Cat. No.:
HY-141482
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