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SEC inhibitor KL-2  (Synonyms: KL-2)

Cat. No.: HY-123972 Purity: 99.80%
SDS COA Handling Instructions

SEC inhibitor KL-2 (KL-2), a peptidomimetic lead compound, is a potent, selective super elongation complex (SEC) inhibitor and disrupts the interaction between the SEC scaffolding protein AFF4 and P-TEFb, resulting in impaired release of Pol II from promoter-proximal pause sites and a reduced average rate of processive transcription elongation. SEC inhibitor KL-2 exhibits an dose-dependent inhibitory effect on AFF4-CCNT1 interaction with a Ki of 1.50 μM.

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

SEC inhibitor KL-2 Chemical Structure

SEC inhibitor KL-2 Chemical Structure

CAS No. : 900308-51-2

Size Price Stock Quantity
1 mg USD 105 In-stock
5 mg USD 280 In-stock
10 mg USD 460 In-stock
25 mg USD 700 In-stock
50 mg USD 1050 In-stock
100 mg USD 1650 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

1 Publications Citing Use of MCE SEC inhibitor KL-2

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

SEC inhibitor KL-2 (KL-2), a peptidomimetic lead compound, is a potent, selective super elongation complex (SEC) inhibitor and disrupts the interaction between the SEC scaffolding protein AFF4 and P-TEFb, resulting in impaired release of Pol II from promoter-proximal pause sites and a reduced average rate of processive transcription elongation. SEC inhibitor KL-2 exhibits an dose-dependent inhibitory effect on AFF4-CCNT1 interaction with a Ki of 1.50 μM[1].

IC50 & Target

SEC[1]

In Vitro

SEC inhibitor KL-2 (20 μM, 6 hours) significantly slows Pol II transcription elongation rates and increases Pol II accumulation at promoter-proximal regions in HEK293T cells[1].
SEC inhibitor KL-2 (20 μM, 24 hours) significantly inhibits MYC transcriptional programs and RNA splicing-related gene expressions in HEK293T cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

SEC inhibitor KL-2 (10 mg/kg, i.p., once daily for 15 days) delays tumor growth and prolonged survival in the MDA231-LM2 xenograft tumor model in nude mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: MDA231-LM2 xenograft tumor model in nude mice[1]
Dosage: 10 mg/kg
Administration: Intraperitoneal injection (i.p.), once daily for 15 days
Result: Significantly delayed tumor growth and increased survival of mice.
Molecular Weight

333.74

Formula

C17H13ClFNO3

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(NC1=CC(Cl)=CC=C1C)/C(O)=C/C(C2=CC=C(F)C=C2)=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 : 83.33 mg/mL (249.69 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 2.9963 mL 14.9817 mL 29.9634 mL
5 mM 0.5993 mL 2.9963 mL 5.9927 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)

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Concentration
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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Volume (start)

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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    90% Corn Oil

    Solubility: ≥ 2.08 mg/mL (6.23 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

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: 99.80%

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 2.9963 mL 14.9817 mL 29.9634 mL 74.9086 mL
5 mM 0.5993 mL 2.9963 mL 5.9927 mL 14.9817 mL
10 mM 0.2996 mL 1.4982 mL 2.9963 mL 7.4909 mL
15 mM 0.1998 mL 0.9988 mL 1.9976 mL 4.9939 mL
20 mM 0.1498 mL 0.7491 mL 1.4982 mL 3.7454 mL
25 mM 0.1199 mL 0.5993 mL 1.1985 mL 2.9963 mL
30 mM 0.0999 mL 0.4994 mL 0.9988 mL 2.4970 mL
40 mM 0.0749 mL 0.3745 mL 0.7491 mL 1.8727 mL
50 mM 0.0599 mL 0.2996 mL 0.5993 mL 1.4982 mL
60 mM 0.0499 mL 0.2497 mL 0.4994 mL 1.2485 mL
80 mM 0.0375 mL 0.1873 mL 0.3745 mL 0.9364 mL
100 mM 0.0300 mL 0.1498 mL 0.2996 mL 0.7491 mL
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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:
SEC inhibitor KL-2
Cat. No.:
HY-123972
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