XX-650-23
Based on 1 Customer Validation
XX-650-23 is a potent CREB inhibitor. XX-650-23inhibits CREB function through disruption of CBP-CREB interaction. XX-650-23 can be used for AML research.
For research use only. We do not sell to patients.
- Purity: 99.90%
- CAS No.: 117739-40-9
- Formula: C18H12N2O2
- Molecular Weight:288.30
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Bone marrow cell | IC50 |
>10 μM
Compound: 3; XX-650-23
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Cytotoxicity against human bone marrow cells incubated for 3 days by CellTiter-Glo luminescent assay
Cytotoxicity against human bone marrow cells incubated for 3 days by CellTiter-Glo luminescent assay
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[PMID: 31253529] |
| HEK293 | IC50 |
4.03 μM
Compound: 3; XX-650-23
|
Inhibition of KIX-RLucN fused CBP (unknown origin) binding to KID-RLucC fused CREB (unknown origin) transfected in human HEK293 cells preincubated with compound 30 mins before before forskolin addition and measured after 90 mins in presence of coelenteraz
Inhibition of KIX-RLucN fused CBP (unknown origin) binding to KID-RLucC fused CREB (unknown origin) transfected in human HEK293 cells preincubated with compound 30 mins before before forskolin addition and measured after 90 mins in presence of coelenteraz
|
[PMID: 31253529] |
| HL-60 | IC50 |
1.58 μM
Compound: 3; XX-650-23
|
Cytotoxicity against human HL60 cells incubated for 3 days by CellTiter-Glo luminescent assay
Cytotoxicity against human HL60 cells incubated for 3 days by CellTiter-Glo luminescent assay
|
[PMID: 31253529] |
| KG-1 | IC50 |
1.23 μM
Compound: 3; XX-650-23
|
Cytotoxicity against human KG1 cells incubated for 3 days by CellTiter-Glo luminescent assay
Cytotoxicity against human KG1 cells incubated for 3 days by CellTiter-Glo luminescent assay
|
[PMID: 31253529] |
XX-650-23 (870 nM-2.3 μM; 48 hours) inhibits AML cell growth, the IC50 values are 870 nM, 910 nM, 2.0 μM and 2.3 μM for HL-60, KG-1, MOLM-13, and MV-4-11,respectively[1]. XX-650-23( 5 μM; 6 or 24 hours) causes a specific decrease in H3K27 acetylation and is not a general inhibitor of acetyltransferase activity[1]. XX-650-23 (2 μM; 72 hours) elicits apoptosis through the intrinsic apoptosis pathway, with activation of caspase-3 and detectable caspase-9 cleavage. It also leads to the downregulation of Mcl-1 and bcl-2[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 117739-40-9
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Appearance Solid
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Molecular Weight 288.30
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Formula C18H12N2O2
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Color Off-white to yellow
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SMILES
O=C(C1=C(C=C2C=CC=CC2=C1)O)NC3=CC=C(C=C3)C#N
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (346.86 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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Data Sheet (272 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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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 | 3.4686 mL | 17.3430 mL | 34.6861 mL | 86.7152 mL |
| 5 mM | 0.6937 mL | 3.4686 mL | 6.9372 mL | 17.3430 mL | |
| 10 mM | 0.3469 mL | 1.7343 mL | 3.4686 mL | 8.6715 mL | |
| 15 mM | 0.2312 mL | 1.1562 mL | 2.3124 mL | 5.7810 mL | |
| 20 mM | 0.1734 mL | 0.8672 mL | 1.7343 mL | 4.3358 mL | |
| 25 mM | 0.1387 mL | 0.6937 mL | 1.3874 mL | 3.4686 mL | |
| 30 mM | 0.1156 mL | 0.5781 mL | 1.1562 mL | 2.8905 mL | |
| 40 mM | 0.0867 mL | 0.4336 mL | 0.8672 mL | 2.1679 mL | |
| 50 mM | 0.0694 mL | 0.3469 mL | 0.6937 mL | 1.7343 mL | |
| 60 mM | 0.0578 mL | 0.2891 mL | 0.5781 mL | 1.4453 mL | |
| 80 mM | 0.0434 mL | 0.2168 mL | 0.4336 mL | 1.0839 mL | |
| 100 mM | 0.0347 mL | 0.1734 mL | 0.3469 mL | 0.8672 mL |