Art. -Nr.: HY-173274

CB039

Name: CB039
Brand: MedChemExpress
SKU: HY-173274
Price: 490.00 USD
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CB039 is a RBM39 molecular glue degrader with an IC₅₀ of 36.7 nM against HCT-116 cells. CB039 induces RBM39 degradation in a dose- and time-dependent manner. This process depends on the Cullin-RING E3 ubiquitin ligase complex (CRL) and proteasome, and promotes the recruitment of RBM39 to the DCAF15-DDB1 complex with an IC₅₀ of 594 nM. CB039 causes abnormal RNA splicing, reduces CEP192 protein levels, induces G2/M phase cell cycle arrest and mitotic spindle disorder. CB039 can be used in studies on RBM39-targeted protein degradation and colorectal cancer-related mechanisms.

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Reinheit: 98.10%
CAS. Nr.: 3056259-55-0
Formel: C₂₃H₂₃N₅O₅S
Molecular Weight:481.52

Speicherung:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

CB039 Chemical Structure

CAS. Nr.: 3056259-55-0

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

RBM39

Cellular Effect

Cell Line	Type	Value	Description	References
HCT-116	IC50	36.7 nM	Antiproliferative activity against human HCT-116 colon cancer cells assessed as reduction in cell viability incubated for 4 days by Cell Counting Kit-8 assay. Antiproliferative activity against human HCT-116 colon cancer cells assessed as reduction in cell viability incubated for 4 days by Cell Counting Kit-8 assay.	40107850

In Vitro

CB039 (4 days) potently inhibits the proliferation of HCT-116 colon cancer cells, with an IC₅₀ value of 36.7 nM^[1].
CB039 (1 μM; 24 h) reduces the levels of at least 103 proteins by 2-fold or more in proteomic analysis of HCT-116 cells, among which RBM39 is the most significantly downregulated protein; CB039 also decreases the protein levels of CEP192, CENPI, KNL1 and RTTN in a dose-dependent manner^[1].
CB039 (0.1 or 1 μM; 24 h) dose-dependently induces RBM39 degradation in HCT-116 cells, with the residual RBM39 level at 1 μM reaching approximately 21% of that in the vehicle control, while the DCAF15 protein level remains essentially unchanged^[1].
CB039 (1 μM; 1-48 h) induces time-dependent degradation of RBM39 in HCT-116 cells. Obvious degradation is observed within 3-6 h and continues to increase up to 48 h^[1].
CB039 displaces Probe-3 in a competitive fluorescence polarization assay containing RBM39, DCAF15-DDB1 and Probe-3, with an IC₅₀ of 594 nM, which supports that CB039 promotes the recruitment of RBM39 to the DCAF15-DDB1 complex^[1].
CB039 (1-10 μM; 12 h) induces abnormal RNA splicing in HCT-116 cells, leading to an approximately 3- to 30-fold increase in intron-retaining transcripts of CUL4A, NCKAP1L and PRPF38A, and an approximately 10-fold decrease in the normal exon 8-exon 9 transcript of ZNF207^[1].
CB039 (0.1-10 μM; 12 h) dose-dependently induces CEP192 exon 42 skipping in HCT-116 cells; at 1 or 10 μM, it also increases CEP192 exon 42 skipping transcripts and decreases normal exon 41-42-43 transcripts in K562, MV4-11, HL-60, Kasumi-1, MOLM-13, CEM/C1 and RS4;11 cells^[1].
CB039 (5 μM; 48 h) induces G2/M phase arrest in HCT-116 cells, increasing the proportion of G2/M phase cells to 60%; at 1 μM, it also exerts a time-dependent effect, with the proportions of G2/M phase cells reaching 33%, 58% and 66% at 24, 48 and 72 h, respectively^[1].
CB039 (1 μM; 48 h) induces abnormal mitotic spindles and chromosome condensation/segregation failure in HCT-116 cells, reducing the proportion of normal mitotic cells to 0.8% and increasing the proportion of abnormal mitotic cells to 21.8%^[1].

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

Real Time qPCR^[1]

Cell Line:

HCT-116 colon cancer cells
Concentration:

1, 5, 10 μM
Incubation Time:

12 h
Result:

Increased intron-retaining CUL4A, NCKAP1L and PRPF38A transcripts and decreased normal ZNF207 transcripts.

Cell Cycle Analysis^[1]

Cell Line:

HCT-116 colon cancer cells
Concentration:

0.1-5 μM (48 h); 1 μM (24 h, 48 h, 72 h)
Incubation Time:

24 h, 48 h, 72 h
Result:

Increased the proportion of HCT-116 cells in the G2/M phase to 60% after treatment with 5 μM for 48 h.
Increased the G2/M phase fraction to 33% at 24 h, 58% at 48 h, and 66% at 72 h after treatment with 1 μM.
Induced negligible apoptosis after 48 h treatment.

Immunofluorescence^[1]

Cell Line:

HCT-116 colon cancer cells
Concentration:

1 μM
Incubation Time:

48 h
Result:

Induced disorganized spindle structures, characterized by random microtubule distribution around condensed, undivided chromosomes.
Reduced the percentage of cells with normal mitosis to 0.8%, compared to 17.2% in the vehicle control group.
Increased the percentage of defective mitotic cells to 21.8%, compared to 0.3% in the vehicle control group.

Western Blot Analysis^[1]

Cell Line:

HCT-116 colon cancer cells
Concentration:

1 μM
Incubation Time:

1-48 h
Result:

Time-dependently degraded RBM39, with substantial degradation within 3-6 h.

Parmacokinetics

Species	Dose	Route	C_max	AUC_0-t
Mice^[1]	15 mg/kg	p.o.	2120.77 ng/mL	3482

In Vivo

CB039 (50-150 mg/kg; p.o.; twice daily/once daily; 14 consecutive days) administered orally at 150 mg/kg once daily inhibits subcutaneous HCT-116 xenograft tumor growth by 72% in female BALB/c nude mice^[1].

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

Animal Model:

BALB/c nude (female, 3-4 weeks old)^[1]
Dosage:

50 mg/kg; 150 mg/kg
Administration:

p.o.; twice daily; 14 consecutive days (50 mg/kg); p.o.; once daily; 14 consecutive days (150 mg/kg)
Result:

Inhibited tumor growth by 72% compared to the vehicle group.

Chemical Information

CAS. Nr. 3056259-55-0
Appearance Solid
Molecular Weight 481.52
Formel C₂₃H₂₃N₅O₅S
Color White to off-white
SMILES

CC1=C2C(NC=C2C#N)=C(C=C1)NS(C3=CC=CC(NC(C(N4[C@H](CCC4)CO)=O)=O)=C3)(=O)=O
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (207.68 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.0768 mL

10.3838 mL

20.7676 mL

5 mM

0.4154 mL

2.0768 mL

4.1535 mL

10 mM

0.2077 mL

1.0384 mL

2.0768 mL

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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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 (5.19 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

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.

Protocol 2

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

Solubility: ≥ 2.5 mg/mL (5.19 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.19 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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (283 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Lyu X, et al. Synthesis of an RBM39 Degrader That Downregulates CEP192 and Induces Disorganized Spindle Structures. Journal of medicinal chemistry. 2025 Apr 10;68(7):7807-7826. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.0768 mL	10.3838 mL	20.7676 mL	51.9189 mL
	5 mM	0.4154 mL	2.0768 mL	4.1535 mL	10.3838 mL
	10 mM	0.2077 mL	1.0384 mL	2.0768 mL	5.1919 mL
	15 mM	0.1385 mL	0.6923 mL	1.3845 mL	3.4613 mL
	20 mM	0.1038 mL	0.5192 mL	1.0384 mL	2.5959 mL
	25 mM	0.0831 mL	0.4154 mL	0.8307 mL	2.0768 mL
	30 mM	0.0692 mL	0.3461 mL	0.6923 mL	1.7306 mL
	40 mM	0.0519 mL	0.2596 mL	0.5192 mL	1.2980 mL
	50 mM	0.0415 mL	0.2077 mL	0.4154 mL	1.0384 mL
	60 mM	0.0346 mL	0.1731 mL	0.3461 mL	0.8653 mL
	80 mM	0.0260 mL	0.1298 mL	0.2596 mL	0.6490 mL
	100 mM	0.0208 mL	0.1038 mL	0.2077 mL	0.5192 mL

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CB039

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

CB039 Related Classifications

HY-173274 Related Classifications

Bioz