KH-4-43

Name: KH-4-43
Brand: Tocris Bioscience
SKU: 8091

Tocris Bioscience, part of Bio-Techne | Catalog # 8091

COA / SDS

Selective CUL4 inhibitor

Key Product Details

Description:	Selective CUL4 inhibitor
Chemical Name:	3-[1-(4-Chlorophenyl)-1H-pyrazol-4-yl]-7,8-dihydroxy-2-(trifluoromethyl)-4H-1-benzopyran-4-one
Purity:	≥98% (HPLC)
Molecular Weight:	422.74

View Full Technical Details for KH-4-43

Technical Data
Citations

Biological Activity for KH-4-43

KH-4-43 is a selective CUL4 inhibitor (Kd = 83 nM). KH-4-43 inhibits the ubiquitination of CK1α by CRL4CRBN in vitro. Treatment of cells with KH-4-43 causes accumulation of the E3 CRL4 substrate CDT1. KH-4-43 suppresses the growth of human tumor xenografts in mice.

Licensing Information

Sold under license from Icahn School of Medicine at Mount Sinai.

Technical Data for KH-4-43

M. Wt	422.74
Formula	C₁₉H₁₀ClF₃N₂O₄
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	2813310-07-3
PubChem ID	164603779
InChi Key	KDPAGFLLKCODNF-UHFFFAOYSA-N
Smiles	O=C1C2=CC=C(C(O)=C2OC(C(F)(F)F)=C1C3=CN(C4=CC=C(C=C4)Cl)N=C3)O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for KH-4-43

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	ethanol	8.45	20 with gentle warming
	DMSO	21.14	50

Preparing Stock Solutions for KH-4-43

The following data is based on the product molecular weight 422.74.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.5 mM	4.73 mL	23.66 mL	47.31 mL
2.5 mM	0.95 mL	4.73 mL	9.46 mL
5 mM	0.47 mL	2.37 mL	4.73 mL
25 mM	0.09 mL	0.47 mL	0.95 mL

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References for KH-4-43

References are publications that support the biological activity of the product.

Wu Inhibitors of cullin-RING E3 ubiquitin ligase 4 with antitumor potential. Proc.Natl.Acad.Sci.U.S.A. 2021 PMID: 33602808