2. Epigenetics Apoptosis PI3K/Akt/mTOR Cell Cycle/DNA Damage Cytoskeleton
  3. Epigenetic Reader Domain Apoptosis AMPK c-Myc PAK Bcl-2 Family
  4. XY221

XY221 (Compound 16o) selectively inhibits BRD4 BD2, with an IC50 of 5.8 nM. XY221 demonstrates high pan-BD2 selectivity (667-fold over BRD4 BD1) and BRD4 BD2 domain selectivity (9−32-fold over BRD2/3/T BD2). XY221 induce Apoptosis in MV4-11 cells and shows anticancer activity .

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

XY221 Chemical Structure

XY221 Chemical Structure

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XY221 Related Antibodies

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Description

XY221 (Compound 16o) selectively inhibits BRD4 BD2, with an IC50 of 5.8 nM. XY221 demonstrates high pan-BD2 selectivity (667-fold over BRD4 BD1) and BRD4 BD2 domain selectivity (9−32-fold over BRD2/3/T BD2). XY221 induce Apoptosis in MV4-11 cells and shows anticancer activity [1].

IC50 & Target

BRD4 BD1

3869 nM (IC50)

BRD4 BD2

5.8 nM (IC50)

BRD3 BD2

70.98 nM (Ki)

In Vitro

XY221 inhibits BRD4 BD2, BRD3 BD2, BRD2 BD2, BRDT BD2 and BRD4 BD1 with IC50s of 5.8, 70.98, 53.47, 183, 3869 nM, respectively[1].
XY221 (72 h) inhibits MV4−11, LNCaP, HL-7702 cells proliferation with IC50s of 0.51, 0.68, 47.7 μM, respectively[1].
XY221 (500-2000 nM, 72 h) significantly induces antiproliferative activity and apoptosis in MV4−11 cell line[1].
XY221 (1-10 μM, 2h) displays long T1/2 (>120 min) in RLM (rat liver microsomes) and T1/2 (>120 min) in HLM (human liver microsomes)[1].
XY221 (500-2000 nM, 72h) inhibits target genes p21 ,ODC1, BRD4 and the phosphorylation of AKT and AMPK in MV4−11 cells[1].
. XY221 (2 μM, 72h) suppresses oncogene MYC and its target gene p21 and cell-cycle-related gene BCL-2 at mRNA level in MV4−11 cells[1].

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

XY221 Related Antibodies

Western Blot Analysis[1]

Cell Line: MV4−11 cells
Concentration: 500, 2000 nM
Incubation Time: 24-72 h
Result: Inhibited target genes p21 ,ODC1, BRD4 and the phosphorylation of AKT and AMPK.

Real Time qPCR[1]

Cell Line: MV4−11 cells
Concentration: 2 μM
Incubation Time: 72 h
Result: Inhibited target genes p21 ,ODC1, BRD4 and the phosphorylation of AKT and AMPK.
Suppressed oncogene MYC and its target gene p21 and cell-cycle-related gene BCL-2 at mRNA level.
In Vivo

Intravenous (iv) and Oral (po) Pharmacokinetic Parameters for XY221 in Rats

route Cmax(μg/L) Tmax(h) AUC(0-t)(μg/L・h) AUC(0-∞)(μg/L・h) T1/2(h) CI(L/h/kg) F (%)
iv (5 mg/kg) 9790 0.03 4291 4294 1.35 1.21
po (25 mg/kg) 567 3.67 2811 2816 2.13 13.1

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

559.63

Formula

C32H34FN3O5
SMILES

O=C1C2=C(OC(C3=C(COC)N=C(CC)N3)=C2)C(C4=CC(C(C)(O)C)=CC=C4OC5=C(C)C=C(F)C=C5C)=CN1C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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XY221 Related Classifications

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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:

XY221XY 221XY-221Epigenetic Reader DomainApoptosisAMPKc-MycPAKBcl-2 FamilyAMP-activated protein kinaseMycp21 activated kinasesantiproliferationantileukemiaacute myeloid leukemiaprostate cancer,Inhibitorinhibitorinhibit

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