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  3. HJB97

HJB97 

Cat. No.: HY-112429 Purity: 98.03%
Handling Instructions

HJB97 is a high-affinity BET inhibitor with Kis of 0.9±0.2 nM (BRD2 BD1), 0.27±0.09 nM (BRD2 BD2), 0.18±0.01 nM (BRD3 BD1), 0.21±0.03 nM (BRD3 BD2), 0.5±0.2 nM (BRD4 BD1), 1.0±0.1 nM (BRD4 BD2), respectively. HJB97 is employed for the design of potential PROTAC BET degrader. Antitumor activity.

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

HJB97 Chemical Structure

HJB97 Chemical Structure

CAS No. : 2093391-24-1

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 496 In-stock
Estimated Time of Arrival: December 31
5 mg USD 450 In-stock
Estimated Time of Arrival: December 31
10 mg USD 750 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2650 In-stock
Estimated Time of Arrival: December 31
100 mg USD 3950 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

HJB97 is a high-affinity BET inhibitor with Kis of 0.9±0.2 nM (BRD2 BD1), 0.27±0.09 nM (BRD2 BD2), 0.18±0.01 nM (BRD3 BD1), 0.21±0.03 nM (BRD3 BD2), 0.5±0.2 nM (BRD4 BD1), 1.0±0.1 nM (BRD4 BD2), respectively. HJB97 is employed for the design of potential PROTAC BET degrader. Antitumor activity[1].

IC50 & Target[1]

BRD2 BD1

0.9 nM (Ki)

BRD2 BD2

0.27 nM (Ki)

BRD3 BD1

0.18 nM (Ki)

BRD3 BD2

0.21 nM (Ki)

BRD4 BD1

0.5 nM (Ki)

BRD4 BD2

1.0 nM (Ki)

BRD2 BD1

3.1 nM (IC50)

BRD2 BD2

3.9 nM (IC50)

BRD3 BD1

6.6 nM (IC50)

BRD3 BD2

1.9 nM (IC50)

BRD4 BD1

7.0 nM (IC50)

BRD4 BD2

7.0 nM (IC50)

In Vitro

HJB97 is a highly potent and efficacious bomodomain and extra terminal (BET) inhibitor with IC50s of 3.1±0.7 nM (BRD2 BD1), 3.9±0.5 nM (BRD2 BD2), 6.6±0.2 nM (BRD3 BD1), 1.9±0.4 nM (BRD3 BD2), 7.0±0.6 nM (BRD4 BD1), 7.0±0.1 nM (BRD4 BD2)[1].
HJB97 (10-1000 nM, 4 days) potently inhibits cell growth in RS4;11 and MOLM-13 acute leukemia cell lines with IC50s of 24.1±5.3 nM and 25.6±1.9 nM[1].
HJB97 can effectively down-regulate the level of c-Myc at concentrations of 300-1000 nM in the RS4;11 cell line (treated for 24 h)[1].

Cell Viability Assay[1]

Cell Line: The human acute leukemia RS4;11 cell line; The human acute leukemia MOLM-13 cell line
Concentration: 10-1000 nM
Incubation Time: 4 days
Result: Achieved IC50s value of 24.1±5.3 nM and 25.6±1.9 nM in inhibition of the RS4;11 cell and MOLM-13 cell growth.

Western Blot Analysis[1]

Cell Line: RS4;11 cells
Concentration: 30, 100, 300, 1000 nM
Incubation Time: 24 h
Result: Down-regulated the level of c-Myc but at concentrations of 300-1000 nM in the RS4;11 cell line.
Molecular Weight

500.55

Formula

C₂₆H₂₈N₈O₃

CAS No.

2093391-24-1

SMILES

O=C(C1=NC(NC2=CC(C3CC3)=NN2CC)=C4C(NC5=C4C=C(OC)C(C6=C(C)ON=C6C)=C5)=N1)NC

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 : 30 mg/mL (59.93 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9978 mL 9.9890 mL 19.9780 mL
5 mM 0.3996 mL 1.9978 mL 3.9956 mL
10 mM 0.1998 mL 0.9989 mL 1.9978 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: ≥ 2.5 mg/mL (4.99 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.99 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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HJB97
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