A RARβ antagonist
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LE 135

Item No. 14415

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-(7,8,9,10-tetrahydro-5,7,7,10,10-pentamethyl-5H-benzo[e]naphtho[2,3-b][1,4]diazepin-13-yl)-benzoic acid
CAS Number
155877-83-1
Molecular Formula
C29H30N2O2
Formula Weight
438.6
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 5 mg/mlDMSO: 12.5 mg/mlDMSO:PBS(pH7.2) (1:1): 0.5 mg/mlEthanol: 1.1 mg/ml
λmax
267, 399 nm
SMILES
CC1(C)C2=C(C=C(N(C)C(C=CC=C3)=C3C(C4=CC=C(C(O)=O)C=C4)=N5)C5=C2)C(C)(C)CC1
InChi Code
InChI=1S/C29H30N2O2/c1-28(2)14-15-29(3,4)22-17-25-23(16-21(22)28)30-26(18-10-12-19(13-11-18)27(32)33)20-8-6-7-9-24(20)31(25)5/h6-13,16-17H,14-15H2,1-5H3,(H,32,33)
InChi Key
YZZAIQOVMHVWBS-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $36

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    5 mg

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    10 mg

    $153

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    Cayman Chemical
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    Product Description

    LE 135 is a retinoic acid receptor (RAR) antagonist that displays moderate selectivity for RARβ over RARα (Kis = 0.22 and 1.4 μM, respectively).1,2 LE 135 inhibits retinoic acid-induced transcriptional activation of RARβ (>70% inhibition at 10 μM), but not RARα, RARγ or retinoid X receptor α.1 It has been shown to inhibit retinoid Am80-induced differentiation of human promyelocytic leukemia cells, HL-60, with an IC50 value of 0.2 μM.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Li, Y., Hashimoto, Y., Agadir, A., et al. Identification of a novel class of retinoic acid receptor ß-selective retinoid antagonists and their inhibitory effects on AP-1 activity and retinoic acid-induced apoptosis in human breast cancer cells. The Journal of Biological Chemisty 274 (22), 15360-15366 (1999).

    2. Eyrolles, L., Kagechika, H., Kawachi, E., et al. Retinobenzoic Acids. 6. Retinoid antagonists with a heterocyclic ring. J. Med. Chem. 37, 1508-1517 (1994).

    3. Umemiya, H., Fukasawa, H., Ebisawa, M., et al. Regulation of retinoidal actions by diazepinylbenzoic acids. Retinoid synergists which activate the RXR-RAR heterodimers. J. Med. Chem. 40(26), 4222-4234 (1997).