2. Epigenetics PROTAC
  3. PROTACs Histone Acetyltransferase
  4. JET-209

JET-209 is a potent CBP/p300 PROTAC degrader, with DC50 values of 0.05 nM and 0.2 nM for CBP and p300. JET-209 demonstrates remarkable anti-tumor activity against various acute leukemia cell lines and effectively inhibits tumor growth in xenograft tumor models. JET-209 can be used for the study of acute leukemia (Pink: CBP/p300 ligand (HY-175620); Blue: CRBN ligand (HY-132248); Black: Linker; CBP/p300 ligand + Linker (HY-175621)).

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

JET-209

JET-209 Chemical Structure

CAS No. : 3033714-58-5

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
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5 mg In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

JET-209 Related Antibodies

Top Publications Citing Use of Products

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CBP/p300 GCN5/PCAF TIP60 MOZ/MORF HBO1

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

JET-209 is a potent CBP/p300 PROTAC degrader, with DC50 values of 0.05 nM and 0.2 nM for CBP and p300. JET-209 demonstrates remarkable anti-tumor activity against various acute leukemia cell lines and effectively inhibits tumor growth in xenograft tumor models. JET-209 can be used for the study of acute leukemia (Pink: CBP/p300 ligand (HY-175620); Blue: CRBN ligand (HY-132248); Black: Linker; CBP/p300 ligand + Linker (HY-175621))[1].

IC50 & Target[1]

CBP

0.05 nM (DC50)

p300

0.2 nM (DC50)

Cereblon

 

In Vitro

JET-209 exhibits strong antiproliferative activity against MV4;11 (IC50 = 0.04 nM), HL-60 (IC50 = 0.54 nM), MOLM-13 (IC50 = 2.3 nM) and RS4;11 cells (IC50 = 0.1 nM)[1].
JET-209 (1 nM- 1 μM, 24 h) effectively induces G1 phase arrest in RS4;11 cells[1].
FIP22 (1 nM- 1 μM, 8 h) potently and effectively suppresses the expression ofMYC and MYB genes in the RS4;11 cell line[1].

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

JET-209 Related Antibodies

Cell Cycle Analysis[1]

Cell Line: RS4;11 cells
Concentration: 1, 10, 100, 1000 nM
Incubation Time: 24 h
Result: Effectively induced G1 arrest at concentrations as low as 1 nM.

RT-PCR[1]

Cell Line: RS4;11 cells
Concentration: 1, 10, 100, 1000 nM
Incubation Time: 8 h
Result: Effectively suppressed the expression ofMYC and MYB genes.
In Vivo

JET-209 (1-3 mg/kg, i.p., single dose) effectively depletes CBP/p300 proteins in RS4;11 xenograft tumors in mice[1].
JET-209 (0.3-3 mg/kg, i.p., for 2 weeks) achieves strong tumor inhibition in RS4;11 and MV4;11 xenograft tumor mice models[1].

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

Animal Model: RS4;11 cells xenograft model established in female immunodeficient (SCID) mice[1]
Dosage: 1 and 3 mg/kg
Administration: Intraperitoneal injection (i.p.), single dose, twice a week (1 mg/kg) or once a week (3 mg/kg) for 2 weeks
Result: Completely eliminated the CBP/p300 protein in the tumor within 3 to 6 hours at a single administration, and the protein level returned to normal 24 hours later.
Achieved 81% long-term tumor growth inhibition with continuous administration at 3 mg/kg.
Animal Model: MV4;11 cells xenograft model established in female immunodeficient (SCID) mice[1]
Dosage: 0.3 and 1 mg/kg
Administration: Intraperitoneal injection (i.p.), 0.3 mg/kg once daily 5 days a week for 2 weeks or 1 mg/kg three times a week for 2 weeks
Result: Demonstrated potent anti-tumor activity and has good safety profile.
Molecular Weight

821.92

Formula

C46H47N9O6
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

CC(N1CCC2=C(C(C3=CC=CC4=C3C=NC(C5=CN=C(C=C5)C(NC6CCN(CC6)C7=CC8=C(C(N(C8)C9CCC(NC9=O)=O)=O)C=C7)=O)=C4)=NN2C%10CCOCC%10)C1)=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 (121.67 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 1.2167 mL 6.0833 mL 12.1666 mL
5 mM 0.2433 mL 1.2167 mL 2.4333 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 (3.04 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (3.04 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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
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 1.2167 mL 6.0833 mL 12.1666 mL 30.4166 mL
5 mM 0.2433 mL 1.2167 mL 2.4333 mL 6.0833 mL
10 mM 0.1217 mL 0.6083 mL 1.2167 mL 3.0417 mL
15 mM 0.0811 mL 0.4056 mL 0.8111 mL 2.0278 mL
20 mM 0.0608 mL 0.3042 mL 0.6083 mL 1.5208 mL
25 mM 0.0487 mL 0.2433 mL 0.4867 mL 1.2167 mL
30 mM 0.0406 mL 0.2028 mL 0.4056 mL 1.0139 mL
40 mM 0.0304 mL 0.1521 mL 0.3042 mL 0.7604 mL
50 mM 0.0243 mL 0.1217 mL 0.2433 mL 0.6083 mL
60 mM 0.0203 mL 0.1014 mL 0.2028 mL 0.5069 mL
80 mM 0.0152 mL 0.0760 mL 0.1521 mL 0.3802 mL
100 mM 0.0122 mL 0.0608 mL 0.1217 mL 0.3042 mL
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JET-209 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:

JET-2093033714-58-5JET209JET 209PROTACsHistone AcetyltransferaseHATsHATLeukemiacancerMV4;11HL-60MOLM-13LenalidomidebromodomainGNE-207Inhibitorinhibitorinhibit

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