| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| ln Vitro |
KI-DX-014 (pre-incubated with DDX21-FL for 30 minutes at room temperature, then incubated with RNA for 1 hour at room temperature) inhibited the interaction of full-length DDX21 with 7SK-SL4 RNA and 7SK-SL1 RNA, with IC50 values of 3.31 μM and 3.79 μM, respectively [1]. KI-DX-014 inhibited the interaction of DDX21-HC+CTD with 7SK-SL4 RNA, with an IC50 value of 10.28 μM [1]. KI-DX-014 inhibited the interaction of DDX21-CTD with 7SK-SL4 RNA, with an IC50 value of 13.64 μM [1]. KI-DX-014 (10-100 μM; 1 hour) at concentrations of 10, 50, and 100 μM attenuated the ATPase activity of full-length DDX21 stimulated by 7SK-SL4 in a dose-dependent manner [1]. KI-DX-014 (10–100 μM; 1 h) at concentrations of 10, 50, and 100 μM at dose-dependent concentrations at which the ATPase activity of full-length DDX21 stimulated by U15 was attenuated[1]. KI-DX-014 (10–100 μM; 30 cycles at 4 °C (1 min on, 3 min off)) at concentrations of 10, 50, and 100 μM at dose-dependent concentrations at which the release of P-TEFb from the 7SK snRNP complex was inhibited from DDX21 at dose-dependent concentrations at which the release was attenuated[1].
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| ln Vivo |
KI-DX-014 (2.5-10 μM; microinjection; single-cell single-dose) can induce dose-dependent developmental defects and reduce phosphorylation of RNA polymerase II CTD serine 2 and serine 5 in zebrafish embryos by inhibiting DDX21-dependent P-TEFb release [1].
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| Animal Protocol |
Animal/Disease Models:Zebrafish embryos (wild-type, 1-2 cell stage) [1]
Dose: 2.5 μM; 5 μM; 10 μM< Route of Administration: Microinjection; single administration at 1 cell stage Experimental Results: Dose-dependent larval deformities, including body curvature and facial developmental defects, were induced. The survival rate of embryos in the treated group was slightly lower at 24 hours post-fertilization compared to the vector control group. A dose-dependent decrease in the phosphorylation levels of RNA polymerase II CTD serine 2 and serine 5 was detected by Western blot. |
| References |
| Molecular Formula |
C17H22N4O3
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|---|---|
| Molecular Weight |
330.38
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| CAS # |
1309288-83-2
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| Appearance |
Colorless to light yellow oil
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| SMILES |
COC1=CC=C(C=C1)N2N=CC(CN3CCC(C(O)=O)(C3)N)=C2C
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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 Note: 请将本产品存放在密封保护的环境中，避免受潮。 |
| 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 (~302.68 mM; with sonication)
H2O : ~100 mg/mL (~302.68 mM; with sonication) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.57 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution.
For example, if 1 mL of working solution is to be prepared, you canAdd 100 μL of DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and adjust the volume to 1 mL. Preparation of physiological saline: Dissolve 0.9 g of sodium chloride in double-distilled water and dilute to 100 mL to obtain clear physiological saline. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.57 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), Clear solution. For example, if 1 mL of working solution is to be prepared, you canAdd 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. Preparation of 20% SBE-β-CD saline (4°C, store for one week): Dissolve 2 g of SBE-β-CD powder in 10 mL of saline until completely dissolved and clear. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.57 mM)(saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.0268 mL | 15.1341 mL | 30.2682 mL | |
| 5 mM | 0.6054 mL | 3.0268 mL | 6.0536 mL | |
| 10 mM | 0.3027 mL | 1.5134 mL | 3.0268 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.
Products are for research use only; We do not sell to patients
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