Home Cart Sign in  
Chemical Structure| 1619994-68-1 Chemical Structure| 1619994-68-1

Structure of GSK2801
CAS No.: 1619994-68-1

Chemical Structure| 1619994-68-1

*Storage: {[sel_prStorage]}

*Shipping: {[sel_prShipping]}

,{[proInfo.pro_purity]}

GSK2801 inhibits BAZ2 family of bromodomain-containing proteins BAZ2A (Kd = 260 nM) and BAZ2B (Kd= 140 nM, IC50 = 9-350 nM).

4.5 *For Research Use Only !

{[proInfo.pro_purity]}
Cat. No.: {[proInfo.prAm]} Purity: {[proInfo.pro_purity]}

Change View

Size Price VIP Price

US Stock

Global Stock

In Stock
{[ item.pr_size ]} Inquiry {[ getRatePrice(item.pr_usd,item.pr_rate,item.mem_rate,item.pr_is_large_size_no_price, item.vip_usd) ]}

US Stock: ship in 0-1 business day
Global Stock: ship in 5-7 days

  • {[ item.pr_size ]}

In Stock

- +

Please Login or Create an Account to: See VIP prices and availability

US Stock: ship in 0-1 business day
Global Stock: ship in 2 weeks

  • 1-2 Day Shipping
  • High Quality
  • Technical Support
Product Citations

Alternative Products

Product Details of GSK2801

CAS No. :1619994-68-1
Formula : C20H21NO4S
M.W : 371.45
SMILES Code : O=C(C)C1=CC(C2=C(S(=O)(C)=O)C=CC=C2)=C3N1C=CC(OCCC)=C3
MDL No. :MFCD26142953
InChI Key :KHWCPNJRJCNVRI-UHFFFAOYSA-N
Pubchem ID :73010930

Safety of GSK2801

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Related Pathways of GSK2801

epigenetics

Isoform Comparison

Biological Activity

Target
  • bromodomain

    BAZ2A, Kd:257 nM

    BAZ2B, Kd:136 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
Prostate cancer cell 22Rv1 ≥5μM GSK2801 significantly reduced growth rate of 22Rv1 cells at the highest concentrations tested without affecting viability PMC10464297
Prostate cancer cell PC3 ≥5μM GSK2801 significantly reduced growth rate of PC3 cells at the highest concentrations tested without affecting viability PMC10464297
Huh7 cells 10 µM Inhibition of HDV replication PMC6972770
HepaRG cells 10 µM 8 days Inhibition of HDV replication PMC6972770
WHIM12 10 μM 96 hours Evaluate the synergistic anti-proliferative effect of GSK2801 with BET inhibitor JQ1 PMC6610760
SUM-159 10 μM 96 hours Evaluate the synergistic anti-proliferative effect of GSK2801 with BET inhibitor JQ1 PMC6610760
MDA-MB-231 10 μM 96 hours Evaluate the synergistic anti-proliferative effect of GSK2801 with BET inhibitor JQ1 PMC6610760
HCC1806 10 μM 96 hours Evaluate the synergistic anti-proliferative effect of GSK2801 with BET inhibitor JQ1 PMC6610760
8505C-PTX 20 μM 72 hours Evaluate the effect of GSK2801 on cell viability, showing limited effect when used alone but significant decrease in cell viability when combined with paclitaxel PMC10054879
SW1736-PTX 20 μM 72 hours Evaluate the effect of GSK2801 on cell viability, showing limited effect when used alone but significant decrease in cell viability when combined with paclitaxel PMC10054879
SUM-159 10 µM 72 hours To evaluate the anti-proliferative activity of GSK2801 on SUM-159 cells, results showed limited efficacy when used alone but synergistic effects when combined with JQ1. PMC9173973
HCC-1806 10 µM 72 hours To evaluate the anti-proliferative activity of GSK2801 on HCC-1806 cells, results showed limited efficacy when used alone but synergistic effects when combined with JQ1. PMC9173973
MDA-MB-231 10 µM 72 hours To evaluate the anti-proliferative activity of GSK2801 on MDA-MB-231 cells, results showed limited efficacy when used alone but synergistic effects when combined with JQ1. PMC9173973

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
CD1 mice Oral and intraperitoneal 30 mg/kg Assessed the pharmacokinetic properties of GSK2801 in mice. Results showed that GSK2801 had reasonable in vivo exposure after oral dosing, with modest clearance and reasonable plasma stability. PMC4770311

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.69mL

0.54mL

0.27mL

13.46mL

2.69mL

1.35mL

26.92mL

5.38mL

2.69mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

Historical Records

Categories