A BET family protein inhibitor
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PLX51107

Item No. 30742

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[6-(3,5-dimethyl-4-isoxazolyl)-1-[(1S)-1-(2-pyridinyl)ethyl]-1H-pyrrolo[3,2-b]pyridin-3-yl]-benzoic acid
CAS Number
1627929-55-8
Molecular Formula
C26H22N4O3
Formula Weight
438.5
Purity
≥98%
Formulation (Request formulation change)
A solid
λmax
227, 251, 305 nm
SMILES
C[C@@H](C1=NC=CC=C1)N2C=C(C3=CC=C(C(O)=O)C=C3)C4=NC=C(C5=C(C)ON=C5C)C=C42
InChi Code
InChI=1S/C26H22N4O3/c1-15-24(17(3)33-29-15)20-12-23-25(28-13-20)21(18-7-9-19(10-8-18)26(31)32)14-30(23)16(2)22-6-4-5-11-27-22/h4-14,16H,1-3H3,(H,31,32)/t16-/m0/s1
InChi Key
AMSUHYUVOVCWTP-INIZCTEOSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

    $63

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    1 mg

    $105

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    5 mg

    $303

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    Cayman Chemical
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    Product Description

    PLX51107 is a bromodomain and extra terminal domain (BET) family protein inhibitor.1 It binds to bromodomain 1 (BD1) in bromodomain-containing protein 2 (BRD2), BRD3, BRD4, and BRDT (Kds = 1.6, 2.1, 1.7, and 5 nM, respectively), as well as BD2 (Kds = 5.9, 6.2, 6.1, and 120 nM, respectively). It also binds to the bromodomains of CBP and p300 (Kds = ~100 nM for both). PLX51107 (0.1-10 µM) inhibits CpG-induced proliferation of primary chronic lymphocytic leukemia (CLL) cells. In vivo, PLX51107 (0.5-10 mg/kg) inhibits Ba/F3 cell-induced splenomegaly in mice. It also reduces tumor volume and increases survival in YUMM3.3 and D4M3.A mouse syngeneic B-RAFV600E mutant melanoma models.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Ozer, H.G., El-Gamal, D., Powell, B., et al. BRD4 profiling identifies critical chronic lymphocytic leukemia oncogenic circuits and reveals sensitivity to PLX51107, a novel structurally distinct BET Inhibitor. Cancer Discov. 8(4), 458-477 (2018).

    2. Erkes, D.A., Field, C.O., Capparelli, C., et al. The next-generation BET inhibitor, PLX51107, delays melanoma growth in a CD8-mediated manner. Pigm. Cell Melanoma R. 32(5), 687-696 (2019).