| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
RBM39 (RNA-binding motif protein 39); CRL4DCAF15 E3 ubiquitin ligase.
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|---|---|
| ln Vitro |
The EC50 values of WT and UBE2Mmut KBM7 cells are 3 and 8 µM, respectively, indicating that dCeMM1 (0-100 µM; 3 days) slows cell growth. RBM39 expression is downregulated in WT KBM7 cells by dCeMM1 (10 µM; 12, 16 h) [1].
dCeMM1 is a RBM39 glue degrader. It decreases the expression of RBM39 levels in wild-type KBM7 cells. It functions by re-directing the activity of the CRL4DCAF15 E3 ligase. As a molecular glue, it works by a different mechanism than PROTACs; it induces proximity between the E3 ligase and the target protein to promote RBM39 ubiquitination and degradation. |
| ln Vivo |
No specific in vivo activity has been reported for dCeMM1. Its potential in vivo effects are currently being studied, as it is primarily used as a tool compound in cell-based assays to study RBM39 biology and the mechanism of CRL4DCAF15-mediated degradation.
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| Enzyme Assay |
N/A; dCeMM1 is a molecular glue degrader, not a PROTAC. Its binding to the CRL4DCAF15 ligase complex and its ability to recruit RBM39 are typically assessed using cellular degradation assays rather than isolated enzyme/receptor binding studies. Biophysical methods such as surface plasmon resonance (SPR) can be used to measure its affinity for the ligase complex.
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: WT and UBE2Mmut KBM7 cells Tested Concentrations: 10 µM Incubation Duration: 12, 16 h Experimental Results: diminished the expression of RBM39 levels in WT KBM7 cells. The in vitro degradation activity of dCeMM1 is evaluated in RBM39-expressing cancer cell lines, such as KBM7 cells. Cells are treated with increasing concentrations of the compound (e.g., 1 nM to 10 uM) for a defined period, typically 4-24 hours. After treatment, cell lysates are prepared and RBM39 protein levels are measured by Western blotting to determine the DC50 (half-maximal degradation concentration). |
| Animal Protocol |
N/A; in vivo efficacy studies for dCeMM1 would typically be conducted in mouse xenograft models of cancers that are dependent on RBM39. The compound would be formulated in a suitable vehicle and administered via oral gavage, IP, or IV injection. Tumor growth inhibition, RBM39 degradation in tumor tissue, and overall animal health would be monitored.
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| ADME/Pharmacokinetics |
dCeMM1 has a molecular weight of 369.23, a molecular formula of C14H13BrN2O3S, and a purity of >98% or up to 99.5%. It is typically stored as a powder at -20degC for up to 3 years or in a solvent at -80degC for 6 months. It appears as a white to off-white solid powder and should be stored at 4degC.
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| Toxicity/Toxicokinetics |
This product is for research use only and is not intended for human or veterinary use. Standard safe handling practices for laboratory chemical reagents should be followed. Information concerning product stability, particularly in solution, has rarely been reported.
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| References | |
| Additional Infomation |
N'-(5-Bromo-2-hydroxybenzylidene)-4-methylbenzenesulfonohydrazide is an RBM39 collagen-degrading enzyme. dCeMM1 functions by redirecting the activity of the CRL4DCAF15 ligase. dCeMM1 reduces the expression level of RBM39 in wild-type KBM7 cells.
dCeMM1 is a chemical tool that has helped elucidate the mechanism of CRL4DCAF15-mediated degradation. Unlike PROTACs, which are bifunctional molecules, molecular glues like dCeMM1 are monovalent and induce degradation by altering the surface of an E3 ligase to recruit a new target. This compound is a valuable probe for studying RBM39 biology and validating it as a therapeutic target in cancer and other diseases. |
| Molecular Formula |
C14H13BRN2O3S
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|---|---|
| Molecular Weight |
369.23
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| Exact Mass |
367.983
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| CAS # |
118719-16-7
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| PubChem CID |
135541690
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| Appearance |
White to off-white solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
509.6±60.0 °C at 760 mmHg
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| Flash Point |
262.0±32.9 °C
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| Vapour Pressure |
0.0±1.4 mmHg at 25°C
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| Index of Refraction |
1.637
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| LogP |
4.53
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
21
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| Complexity |
455
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| Defined Atom Stereocenter Count |
0
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| SMILES |
BrC1=CC=C(O)C(/C=N/NS(C2=CC=C(C)C=C2)(=O)=O)=C1
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| InChi Key |
PBEIAQYKTXKQGF-CXUHLZMHSA-N
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| InChi Code |
InChI=1S/C14H13BrN2O3S/c1-10-2-5-13(6-3-10)21(19,20)17-16-9-11-8-12(15)4-7-14(11)18/h2-9,17-18H,1H3/b16-9+
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| Chemical Name |
N-[(E)-(5-bromo-2-hydroxyphenyl)methylideneamino]-4-methylbenzenesulfonamide
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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) |
DMSO :~100 mg/mL (~270.83 mM)
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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 | 2.7083 mL | 13.5417 mL | 27.0834 mL | |
| 5 mM | 0.5417 mL | 2.7083 mL | 5.4167 mL | |
| 10 mM | 0.2708 mL | 1.3542 mL | 2.7083 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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