Home Cart Sign in  
Chemical Structure| 1268524-70-4 Chemical Structure| 1268524-70-4

Structure of (+)-JQ1
CAS No.: 1268524-70-4

Chemical Structure| 1268524-70-4

*Storage: {[sel_prStorage]}

*Shipping: {[sel_prShipping]}

,{[proInfo.pro_purity]}

(+)-JQ-1 (JQ1) is a potent, specific, and reversible BET bromodomain inhibitor, with IC50s of 77 and 33 nM for the first and second bromodomains (BRD4(1/2)). It also activates autophagy.

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

Product Citations

Chrysanthi Kagiou ; Jose A. Cisneros ; Jakob Farnung ; Joanna Liwocha ; Fabian Offensperger ; Kevin Dong , et al.

Abstract: Targeted degradation (TPD) relies on small molecules to recruit proteins to E3 ligases to induce their ubiquitylation and degradation by the . Only a few of the approximately 600 human E3 ligases are currently amenable to this strategy. This limits the actionable target space and clinical opportunities and thus establishes the necessity to expand to additional ligases. Here we identify and characterize SP3N, a specific degrader of the prolyl isomerase FKBP12. SP3N features a minimal design, where a known FKBP12 ligand is appended with a flexible alkylamine tail that conveys degradation properties. We found that SP3N is a precursor and that the alkylamine is metabolized to an active aldehyde species that recruits the SCFFBXO22 ligase for FKBP12 degradation. Target engagement occurs via covalent adduction of Cys326 in the FBXO22 C-terminal domain, which is critical for ternary complex formation, ubiquitylation and degradation. This mechanism is conserved for two recently reported alkylamine-based degraders of NSD2 and XIAP, thus establishing alkylamine tethering and covalent hijacking of FBXO22 as a generalizable TPD strategy.

Purchased from AmBeed:

Alternative Products

Product Details of (+)-JQ1

CAS No. :1268524-70-4
Formula : C23H25ClN4O2S
M.W : 456.99
SMILES Code : O=C(OC(C)(C)C)C[C@H]1C2=NN=C(C)N2C3=C(C(C)=C(C)S3)C(C4=CC=C(Cl)C=C4)=N1
MDL No. :MFCD22683748
InChI Key :DNVXATUJJDPFDM-KRWDZBQOSA-N
Pubchem ID :46907787

Safety of (+)-JQ1

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H332-H335
Precautionary Statements:P261-P280-P305+P351+P338

Related Pathways of (+)-JQ1

epigenetics

Isoform Comparison

Biological Activity

Target
  • BET

    BRD4 (1), IC50:77 nM

    BRD4 (2), IC50:33 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
Adult rat ventricular fibroblasts (ARVFs) 10μM to 5nM 72 h JQ1 inhibited TGF-β1-stimulated α-SMA signal with an IC50 of 94nM. PMC7310347
Adult rat ventricular fibroblasts (ARVFs) 500nM 72 h JQ1 significantly reduced basal and TGF-β-mediated collagen gel contraction and profoundly reduced α-SMA protein expression. PMC7310347
KP-4 cells 500 nM 9 h JQ1 increased LC3II levels, indicating that JQ1 activates autophagy by inhibiting BRD4 PMC5446411
NMC 797 cells 500 nM 48 h JQ1 induces differentiation in NMC cells, characterized by changes in cell morphology and increased keratin expression PMC3010259
U2OS cells 500 nM JQ1 competitively binds to BRD4, leading to its displacement from nuclear chromatin as demonstrated by FRAP experiments PMC3010259
JJN3 0.5 μM 72 h JQ1 upregulated the expression of MICA in JJN3 cells. PMC5131470
ARP-1 0.5 μM 72 h JQ1 upregulated the expression of MICA in ARP-1 cells. PMC5131470
U266 0.5 μM 72 h JQ1 upregulated the expression of MICA in U266 cells. PMC5131470
RPMI-8226 0.5 μM 72 h JQ1 upregulated the expression of MICA in RPMI-8226 cells. PMC5131470
SKO-007(J3) 0.5 μM 72 h JQ1 upregulated the expression of MICA in SKO-007(J3) cells, enhancing their sensitivity to NK cell-mediated cytotoxicity. PMC5131470
Cortical neurons 250 nM 10 min JQ1 pretreatment blocked the rapid induction of Arc, Fos, and Nr4a1 after TTX withdrawal PMC4752120
Cortical neurons 250 nM 10 min JQ1 pretreatment blocked the BDNF-induced increase in transcription of Arc, Fos, and Nr4a1 PMC4752120
C2C12 cells 200 nM 24 h JQ1 treatment prevented H2O2-induced oxidative stress, restored LC3II abundance, and reduced p62 levels. PMC7705749
H2081 cells 1 µM 48 h JQ1 significantly reduced ASCL1 and IGFBP5 expression, while having no effect on IGFBP3 expression. PMC6642156

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice NMC 797 xenograft model Intraperitoneal injection 50 mg/kg Once daily for 4 days JQ1 significantly reduces tumor growth, induces keratin expression, and inhibits tumor proliferation PMC3010259
Mice Adult male mice Intraperitoneal injections 50 mg/kg Daily for one week or three weeks JQ1 treatment affected memory formation and decreased seizure susceptibility in mice PMC4752120
Mice Mdx mouse model Intraperitoneal injection 20 mg/kg Once daily for two weeks JQ1 treatment reduced muscle damage and inflammation in mdx mice, improving muscle function. PMC7705749
Mice ASCL1High SCLC xenograft model Intraperitoneal injection 25 mg/kg Every other day, continuous treatment Combination treatment of JQ1 and BMS-754807 significantly inhibited tumor growth, while monotherapy with either JQ1 or BMS-754807 had limited effects. PMC6642156

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.19mL

0.44mL

0.22mL

10.94mL

2.19mL

1.09mL

21.88mL

4.38mL

2.19mL

References

 

Historical Records

Categories