KH-4-43 is an inhibitor of E3 CRL4. KH-4-43 inhibits the core ligase complex of E3 CRL4 and exhibits anticancer activity. KH-4-43 binds to E3 ROC1-CUL4A CTD or the highly related ROC1-CUL1 CTD with Kd of 83 nM or 9.4 μM, respectively.

Physicochemical Properties

Molecular Formula	C19H10CLF3N2O4
Molecular Weight	422.74
CAS #	2813310-07-3
Appearance	Off-white to yellow 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

References

[1].Targeting Cullin-RING E3 Ubiquitin Ligase 4 by Small Molecule Modulators. J Cell Signal. 2021;2(3):195-205.

Solubility Data

Solubility (In Vitro)

DMSO :~100 mg/mL (~236.55 mM; with sonication)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.5 mg/mL (5.91 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 can add 100 μL of 25.0 mg/mL clear DMSO stock solution and add it to 400 μL PEG300 and mix well. Then add 50 μL Tween-80 to the above system and mix well. Then continue to add 450 μL of physiological saline to make up to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.3655 mL	11.8276 mL	23.6552 mL
	5 mM	0.4731 mL	2.3655 mL	4.7310 mL
	10 mM	0.2366 mL	1.1828 mL	2.3655 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.