2. PI3K/Akt/mTOR Epigenetics
  3. PI3K Epigenetic Reader Domain
  4. SRX3212

SRX3212 is a potent PI3Kα/BRD4 inhibitor with human IC50 values of 22 nM, 3.7 nM, and 32 nM for PI3Kα, BRD4BD1, and BRD4BD2, respectively. SRX3212 inhibits PI3K kinase activity and blocks acetyllysine binding function of BRD4BD1 and BRD4BD2. SRX3212 can be used for the research of mantle cell lymphoma, colon carcinoma, neuroblastoma, prostate cancer[1].

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

SRX3212

SRX3212 Chemical Structure

CAS No. : 2735720-80-4

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SRX3212 Related Antibodies

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

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Description

SRX3212 is a potent PI3Kα/BRD4 inhibitor with human IC50 values of 22 nM, 3.7 nM, and 32 nM for PI3Kα, BRD4BD1, and BRD4BD2, respectively. SRX3212 inhibits PI3K kinase activity and blocks acetyllysine binding function of BRD4BD1 and BRD4BD2. SRX3212 can be used for the research of mantle cell lymphoma, colon carcinoma, neuroblastoma, prostate cancer[1].

IC50 & Target[1]

PI3Kα

22 nM (IC50)

BD1

3.7 nM (IC50)

BD2

32 nM (IC50)

In Vitro

SRX3212 potently inhibits purified BRD4BD1 (IC50 = 3.7 nM) and BRD4BD2 (IC50 = 32 nM) in an AlphaScreen displacement binding assay[1].
SRX3212 potently inhibits purified PI3Kα with an IC50 of 22 nM in a fluorescence-based kinase screening assay[1].
SRX3212 binds tightly to the hydrophobic pocket of purified BRD4BD1 via multiple conserved and unique interactions, acting as an acetyllysine mimetic to drive high binding potency[1].
SRX3212 (48 hours) potently inhibits viability of JeKo-1 (IC50 = 0.28 μM), Mino (IC50 = 0.44 μM), and Z138 (IC50 = 0.24 μM) mantle cell lymphoma cell lines, HCT116 colon carcinoma cells (IC50 = 1.3 μM), and SKNBE-2 neuroblastoma cells (IC50 = 3.2 μM), but does not inhibit PC3 prostate cancer cell viability[1].
SRX3212 (0.5-5 μM; 1 hour) inhibits PI3K activity in JeKo-1 mantle cell lymphoma cells[1].

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

SRX3212 Related Antibodies

Western Blot Analysis[1]

Cell Line: JeKo-1 mantle cell lymphoma cell line
Concentration: 0.5 μM; 1 μM; 2.5 μM; 5 μM
Incubation Time: 1 hour
Result: Caused a concomitant decrease in AKT phosphorylation at Ser473 with increasing concentrations, indicating reduced PI3K activity.
Molecular Weight

505.54

Formula

C26H23N3O6S
CAS No.
SMILES

O=C1C=C(N2CCOCC2)OC3=C1SC=C3C4=CC(C(NCC5=CC=CN=C5)=O)=C6OCCOC6=C4
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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SRX3212 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:

SRX32122735720-80-4SRX 3212SRX-3212PI3KEpigenetic Reader DomainPhosphoinositide 3-kinasecolon carcinomamantle cell lymphomaSer473BRD4 BD1prostate cancerBRD4 BD2PI3KαneuroblastomaAKTBRD4Inhibitorinhibitorinhibit

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