2. Cell Cycle/DNA Damage Stem Cell/Wnt Immunology/Inflammation
  3. Casein Kinase Wee1 IKZF Family
  4. SB-405483

SB-405483 is a CRBN orthosteric ligand bindign enhancer. SB-405483 potentiates degradation of CRBN substrates including CK1α, Wee1, IKZF1/3. SB-405483 stabilizes CRBN and reduces CRBN autoubiquitination. SB-405483 can be used for the research of cancer, such as multiple myeloma and acute myeloid leukemia.

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

SB-405483

SB-405483 Chemical Structure

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
25 mg In-stock
50 mg In-stock
100 mg In-stock
250 mg In-stock
1 g In-stock
5 g   Get quote  
10 g   Get quote  

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SB-405483 Related Antibodies

Top Publications Citing Use of Products

View All Casein Kinase Isoform Specific Products:

View All Isoforms
CK1 CK2

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PKMYT1

View All IKZF Family Isoform Specific Products:

View All Isoforms
IKZF1 IKZF2 IKZF3 IKZF4

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

SB-405483 is a CRBN orthosteric ligand bindign enhancer. SB-405483 potentiates degradation of CRBN substrates including CK1α, Wee1, IKZF1/3. SB-405483 stabilizes CRBN and reduces CRBN autoubiquitination. SB-405483 can be used for the research of cancer, such as multiple myeloma and acute myeloid leukemia[1].

IC50 & Target[1]

CK1α

 

IKZF1

 

IKZF3

 

In Vitro

SB-405483 (2.5-25 μM) binds the recombinant human CRBN/DDB1 complex with a binding potency of 25 ± 0.9 μM and exhibits highly synergistic binding with the lenalidomide-Alexa647 probe[1].
SB-405483 (25 μM) potentiates the binding of multiple orthosteric CRBN ligands to the recombinant human CRBN/DDB1 complex, as shown by 8.96- to 43.7-fold decreases in their IC50 values, with no effect on mezigdomide binding[1].
SB-405483 (0.1-25 μM; 1 h) stabilizes endogenous CRBN in MM.1S cells in a dose-dependent manner, with enhanced stabilization when co-treated with Lenalidomide (HY-A0003)[1].
SB-405483 (0.1-10 μM) inhibits autoubiquitination of endogenous Flag-tagged CRBN in HEK293T cells in a dose-dependent manner[1].
SB-405483 (10 μM; 0.5-24 h) potentiates DEG-47-mediated degradation of endogenous CK1α in MOLM-13 cells[1].
SB-405483 (10 μM; 24 h) potentiates DEG-47-mediated degradation of Wee1 in A2780 Wee1-HiBiT cells and MOLM-13 cells[1].
SB-405483 (10 μM; 24 h) inhibits DEG-47-mediated degradation of IKZF1/3(ZF2)-GFP and IKZF2(ZF2)-GFP in HEK293T reporter cells after 24 h[1].
SB-405483 (10 μM; 24 h) modestly potentiates DEG-47-mediated degradation of SALL4(ZF1,2)-GFP in U937 Cas9 cells[1].

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

SB-405483 Related Antibodies

Western Blot Analysis[1]

Cell Line: Human acute myeloid leukemia MOLM-13 cells
Concentration: 10 μM
Incubation Time: 0.5, 1, 2, 4, 6, 24 h
Result: Decreased the DC50 of DEG-47 from 21 nM to 5 nM in a GFP-CK1α reporter assay after 24 h.
Reduced CK1α expression.
Molecular Weight

360.37

Formula

C20H16N4O3
Appearance

Solid

Color

White to light yellow

SMILES

O=C(NC1=CC=C(C#N)C=C1O)NC2=NC=CC=C2OCC3=CC=CC=C3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (69.37 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 2.7749 mL 13.8746 mL 27.7493 mL
5 mM 0.5550 mL 2.7749 mL 5.5499 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 (stored under nitrogen). 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
×
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    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (6.94 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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).

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

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: 99.33%

SDS (252 KB)

COA (249 KB) HNMR (222 KB) LCMS (389 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 (stored under nitrogen). 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 2.7749 mL 13.8746 mL 27.7493 mL 69.3731 mL
5 mM 0.5550 mL 2.7749 mL 5.5499 mL 13.8746 mL
10 mM 0.2775 mL 1.3875 mL 2.7749 mL 6.9373 mL
15 mM 0.1850 mL 0.9250 mL 1.8500 mL 4.6249 mL
20 mM 0.1387 mL 0.6937 mL 1.3875 mL 3.4687 mL
25 mM 0.1110 mL 0.5550 mL 1.1100 mL 2.7749 mL
30 mM 0.0925 mL 0.4625 mL 0.9250 mL 2.3124 mL
40 mM 0.0694 mL 0.3469 mL 0.6937 mL 1.7343 mL
50 mM 0.0555 mL 0.2775 mL 0.5550 mL 1.3875 mL
60 mM 0.0462 mL 0.2312 mL 0.4625 mL 1.1562 mL
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SB-405483 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:

SB-405483SB405483SB 405483Casein KinaseWee1IKZF FamilyIkaros zinc finger protein familyIKZF2human embryonic kidney cellsCK1αmultiple myeloma cellsCereblon (CRBN)BRD4IKZF1/3FKBP12GSPT1Inhibitorinhibitorinhibit

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