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  3. KH-4-43

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

For research use only. We do not sell to patients.

KH-4-43 Chemical Structure

KH-4-43 Chemical Structure

CAS No. : 2813310-07-3

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 638 In-stock
Solution
10 mM * 1 mL in DMSO USD 638 In-stock
Solid
5 mg USD 580 In-stock
10 mg USD 950 In-stock
50 mg   Get quote  
100 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

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Description

KH-4-43 is an inhibitor of E3 CRL4. KH-4-43 inhibits E3 CRL4's core ligase complex and exhibits anticancer activity. KH-4-43 has a binding Kd to E3 ROC1-CUL4A CTD or the highly related ROC1-CUL1 CTD at 83 nM or 9.4 μM, respectively[1].

Molecular Weight

422.74

Formula

C19H10ClF3N2O4

CAS No.
Appearance

Solid

Color

Off-white to yellow

SMILES

O=C1C2=CC=C(C(O)=C2OC(C(F)(F)F)=C1C3=CN(C4=CC=C(C=C4)Cl)N=C3)O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (236.55 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.91 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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

Purity: 99.99%

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 2.3655 mL 11.8276 mL 23.6552 mL 59.1380 mL
5 mM 0.4731 mL 2.3655 mL 4.7310 mL 11.8276 mL
10 mM 0.2366 mL 1.1828 mL 2.3655 mL 5.9138 mL
15 mM 0.1577 mL 0.7885 mL 1.5770 mL 3.9425 mL
20 mM 0.1183 mL 0.5914 mL 1.1828 mL 2.9569 mL
25 mM 0.0946 mL 0.4731 mL 0.9462 mL 2.3655 mL
30 mM 0.0789 mL 0.3943 mL 0.7885 mL 1.9713 mL
40 mM 0.0591 mL 0.2957 mL 0.5914 mL 1.4785 mL
50 mM 0.0473 mL 0.2366 mL 0.4731 mL 1.1828 mL
60 mM 0.0394 mL 0.1971 mL 0.3943 mL 0.9856 mL
80 mM 0.0296 mL 0.1478 mL 0.2957 mL 0.7392 mL
100 mM 0.0237 mL 0.1183 mL 0.2366 mL 0.5914 mL
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KH-4-43 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
KH-4-43
Cat. No.:
HY-148602
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