PeptideDB

ZNL-05-044

ZNL-05-044

CAS No.:

ZNL-05-044 is a CDK11 inhibitor (antagonist) with IC50s of 0.23 μM and 0.27 μM for CDK11A and CDK11B, respectively, in
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ZNL-05-044 is a CDK11 inhibitor (antagonist) with IC50s of 0.23 μM and 0.27 μM for CDK11A and CDK11B, respectively, in NanoBRET experiments. ZNL-05-044 causes G2/M cell cycle arrest and impairs RNA splicing.

Physicochemical Properties


Molecular Formula C21H22CL2N6OS
Molecular Weight 477.41
Appearance White to off-white solid powder
HS Tariff Code 2934.99.9001
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)

Biological Activity


Targets IC50: 0.23 μM (CDK11A in NanoBRET assay), 0.27 μM (CDK11B in NanoBRET assay), 135 nM (CDK4/cyclin D1 in Adapta activity assay), 189 nM (CDK9/cyclin T1 in Adapta activity assay), 217 nM (CDK6/cyclin D1 in Adapta activity assay)[1] Kd: 69 nM (CDK11A in KdELECT assay)[1]
References

[1]. Synthesis and Structure-Activity relationships of cyclin-dependent kinase 11 inhibitors based on a diaminothiazole scaffold. Eur J Med Chem. 2022 Aug 5;238:114433.


Solubility Data


Solubility (In Vitro) DMSO :~100 mg/mL (~209.46 mM)
Solubility (In Vivo) Solubility in Formulation 1: ≥ 2.5 mg/mL (5.24 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 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 can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
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 (5.24 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.0946 mL 10.4732 mL 20.9464 mL
5 mM 0.4189 mL 2.0946 mL 4.1893 mL
10 mM 0.2095 mL 1.0473 mL 2.0946 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.