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HJB97

Name: HJB97
Brand: TargetMol
SKU: T15484
Rating: 4.5 (1 reviews)

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Catalog No. T15484Cas No. 2093391-24-1

HJB97 is used for the design of potential PROTAC BET degrader. It also has antitumor activity. HJB97 is a high-affinity inhibitor of BET (Kis: 0.9 nM (BRD2 BD1), 0.27 nM (BRD2 BD2), 0.18 nM (BRD3 BD1), 0.21 nM (BRD3 BD2), 0.5 nM (BRD4 BD1), 1.0 nM (BRD4 BD2), respectively).

HJB97

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Catalog No. T15484Cas No. 2093391-24-1

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Appearance:Solid

Color:Yellow

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Product Introduction

Bioactivity

Description	HJB97 is used for the design of potential PROTAC BET degrader. It also has antitumor activity. HJB97 is a high-affinity inhibitor of BET (Kis: 0.9 nM (BRD2 BD1), 0.27 nM (BRD2 BD2), 0.18 nM (BRD3 BD1), 0.21 nM (BRD3 BD2), 0.5 nM (BRD4 BD1), 1.0 nM (BRD4 BD2), respectively).
Targets&IC50	BRD4 BD2:1.0nM, BRD4 BD2:7.0nM, BRD3 BD1:0.18nM, BRD3 BD1:6.6nM, BRD2 BD1:0.9(ki), BRD2 BD1:3.1nM, BRD3 BD2:0.21nM, BRD3 BD2:1.9nM, Plusmn:0.01 nM （ki）, Plusmn:0.03 nM （ki）, Plusmn:0.09 nM (ki), Plusmn:0.1 nM （ki）, Plusmn:0.2 nM, Plusmn:0.2 nM (ki), Plusmn:0.4 nM, Plusmn:0.5 nM, Plusmn:0.6 nM, Plusmn:0.7 nM, BRD2 BD2:0.27nM(ki), BRD2 BD2:3.9nM, BRD4 BD1:0.5nM, BRD4 BD1:7.0nM
In vitro	HJB97 is a highly potent BET inhibitor with IC50 values of 3.1 nM (BRD2 BD1), 3.9 nM (BRD2 BD2), 6.6 nM (BRD3 BD1), 1.9 nM (BRD3 BD2), and 7.0 nM for both BRD4 BD1 and BD2. At concentrations of 300-1000 nM, HJB97 effectively down-regulates c-Myc levels in RS4;11 cell lines within 24 hours. Additionally, HJB97 (10-1000 nM over 4 days) significantly inhibits cell growth in RS4;11 and MOLM-13 acute leukemia cell lines, with IC50 values of 24.1 nM and 25.6 nM, respectively[1].

Chemical Properties

Molecular Weight	500.55
Formula	C₂₆H₂₈N₈O₃
Cas No.	2093391-24-1
Smiles	CCn1nc(cc1Nc1nc(nc2[nH]c3cc(-c4c(C)noc4C)c(OC)cc3c12)C(=O)NC)C1CC1
Relative Density.	1.52 g/cm3 (Predicted)

Storage & Solubility Information

Storage

store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 27 mg/mL (53.94 mM), Sonication is recommended.

H2O: insoluble

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween-80+45% Saline: 2 mg/mL (4 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.9978 mL	9.9890 mL	19.9780 mL	99.8901 mL
5 mM	0.3996 mL	1.9978 mL	3.9956 mL	19.9780 mL
10 mM	0.1998 mL	0.9989 mL	1.9978 mL	9.9890 mL
20 mM	0.0999 mL	0.4995 mL	0.9989 mL	4.9945 mL
50 mM	0.0400 mL	0.1998 mL	0.3996 mL	1.9978 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc