2. PROTAC Stem Cell/Wnt JAK/STAT Signaling
  3. PROTACs STAT
  4. AK-1690

AK-1690 is a selective PROTAC degrader targeting STAT6 (DC50=1 nM) with a Ki of 6 nM against human STAT6. AK-1690 degrades STAT6 via the interaction of STAT6 with cereblon and a ubiquitin-like process. AK-1690 effectively depletes STAT6 protein in mouse liver and lung tissues, and is applicable to research related to leukemia, Hodgkin's lymphoma, follicular lymphoma, etc..

(Pink: STAT6 ligand (HY-169182); Blue: Cereblon ligand (HY-131318); Black: linker (HY-W459522)).

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

AK-1690

AK-1690 Chemical Structure

CAS No. : 2984505-88-4

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Based on 1 publication(s) in Google Scholar

AK-1690 Related Antibodies

Top Publications Citing Use of Products

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STAT3 STAT5 STAT6 STAT1

  • Biological Activity

  • Purity & Documentation

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  • Customer Review

Description

AK-1690 is a selective PROTAC degrader targeting STAT6 (DC50=1 nM) with a Ki of 6 nM against human STAT6. AK-1690 degrades STAT6 via the interaction of STAT6 with cereblon and a ubiquitin-like process. AK-1690 effectively depletes STAT6 protein in mouse liver and lung tissues, and is applicable to research related to leukemia, Hodgkin's lymphoma, follicular lymphoma, etc.[1].
(Pink: STAT6 ligand (HY-169182); Blue: Cereblon ligand (HY-131318); Black: linker (HY-W459522)).

IC50 & Target

STAT6

1 nM (DC50)

Cereblon

 

In Vitro

AK-1690 potently induces STAT6 degradation in MV4;11 cells with a DC50 of 1 nM (12 h), and effectively induces STAT6 degradation in human peripheral blood mononuclear cells (PBMCs) with a DC50 of 80 nM (18 h)[1].
AK-1690 (0-10 μM; 24 h) effectively depletes total STAT6 and phosphorylated STAT6 in L1236 cells, with no impact on other STAT proteins even at concentrations as high as 10 μM[1].
AK-1690 (1 μM; 0-60 min, 120 min) exhibits excellent microsomal and plasma stability in humans, mice, rats, dogs, and monkeys, with a T1/2 value > 120 min (except for a T1/2 of 63 min in monkey microsomes)[1].

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

AK-1690 Related Antibodies

Western Blot Analysis[2]

Cell Line: L1236 Hodgkin’s lymphoma cells (with activated STAT6)
Concentration: Up to 10 μM
Incubation Time: 24 h
Result: Induced dose-dependent depletion of both total STAT6 and pSTAT6Y641 proteins; showed no effect on other STAT members up to 10 μM.
In Vivo

AK-1690 (200 mg/kg; i.p.; single dose) effectively depletes STAT6 protein in mouse liver and lung tissues for up to 24 hours[2].

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

Animal Model: Balb/c mouse model (female)[2]
Dosage: 200 mg/kg
Administration: i.p.; single dose
Result: Depleted STAT6 by >90% in liver tissue at 2, 6, and 24 h time points; depleted STAT6 by >70%, >90%, and >70% in lung tissue at 2, 6, and 24 h time points, respectively.
Molecular Weight

1016.05

Formula

C51H56F2N5O11PS
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

FC(C1=CC=C2C(C=C(C(N[C@@H](C(C)(C)C)C(N3[C@H](C(N4C[C@@H](C5=CC=CC=C5)OCC4)=O)C[C@H](OCCCCCC#CC6=CC=CC7=C6CN(C(CC8)C(NC8=O)=O)C7=O)C3)=O)=O)S2)=C1)(P(O)(O)=O)F
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (98.42 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 0.9842 mL 4.9210 mL 9.8420 mL
5 mM 0.1968 mL 0.9842 mL 1.9684 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 (protect from light, stored under nitrogen). 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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Volume
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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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C2

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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    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (2.46 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 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 (25.0 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).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

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: 99.91%

SDS (252 KB)

COA (252 KB) HNMR (366 KB) RP-HPLC (261 KB)

Handling Instructions (2659 KB)
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 (protect from light, stored under nitrogen). 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 0.9842 mL 4.9210 mL 9.8420 mL 24.6051 mL
5 mM 0.1968 mL 0.9842 mL 1.9684 mL 4.9210 mL
10 mM 0.0984 mL 0.4921 mL 0.9842 mL 2.4605 mL
15 mM 0.0656 mL 0.3281 mL 0.6561 mL 1.6403 mL
20 mM 0.0492 mL 0.2461 mL 0.4921 mL 1.2303 mL
25 mM 0.0394 mL 0.1968 mL 0.3937 mL 0.9842 mL
30 mM 0.0328 mL 0.1640 mL 0.3281 mL 0.8202 mL
40 mM 0.0246 mL 0.1230 mL 0.2461 mL 0.6151 mL
50 mM 0.0197 mL 0.0984 mL 0.1968 mL 0.4921 mL
60 mM 0.0164 mL 0.0820 mL 0.1640 mL 0.4101 mL
80 mM 0.0123 mL 0.0615 mL 0.1230 mL 0.3076 mL
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AK-1690 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.

Keywords:

AK-16902984505-88-4AK1690AK 1690PROTACsSTATlymphomaMV4;11 cellshodgkin's lymphomaSTAT6leukemiamouse liverfollicular lymphomamouse lungneddylationcereblonInhibitorinhibitorinhibit

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