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

Synonym(s):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;LE-135

CAS NO.：155877-83-1
Empirical Formula: C29H30N2O2
Molecular Weight: 438.56
MDL number: MFCD06798318
SAFETY DATA SHEET (SDS)
Update Date: 2024-11-11 17:44:06

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 Structural

What is 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?

Description

LE 135 is a retinoic acid receptor (RAR) antagonist that displays moderate selectivity for RARβ over RARα (K_is = 0.22 and 1.4 μM, respectively). LE 135 inhibits retinoic acid-induced transcriptional activation of RARβ (>70% inhibition at 10 μM), but not RARα, RARγ or retinoid X receptor α. 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.

The Uses of 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

LE 135 has been used for in vitro islet treatment.

What are the applications of Application

LE 135 is a retinoic acid receptor antagonist

Definition

ChEBI: 4-(5,7,7,10,10-pentamethyl-8,9-dihydronaphtho[2,3-b][1,4]benzodiazepin-13-yl)benzoic acid is a dibenzodiazepine.

Biological Activity

Retinoic acid antagonist; displays moderate selectivity for RAR β over RAR α (Ki values are 0.22 and 1.4 μ M respectively). Highly selective over RAR γ and RXR α . Inhibits human HL-60 leukemia cell differentiation induced by Am80 (IC 50 = 150 nM).

Biochem/physiol Actions

LE135 is a retinoic acid receptor (RAR) antagonist with selectivity for RARβ (Ki = 220 nM) over RARα (Ki = 1.4 μM). LE135 inhibits retinoic acid-induced transcriptional activation of RARβ (>70% inhibition at 10 μM), but not RARα, RARγ or retinoid X receptor α (RXRα). There is high interest in retinoic acid receptors for cancer and for differentiation studies. LE135 has been shown to inhibit retinoid Am80-induced differentiation of human promyelocytic leukemia HL-60 cells with an IC50 value of 0.2 μM. LE135 has been used to study the role of a retinoic acid receptor-β (RARβ) on the differentiation of mesenchymal stem cells, and was found to inhibit the neuronal differentiation promoting effects of all-trans retinoic acid (ATRA) on mesenchymal stem cells.

storage

Store at +4°C

Properties of 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

Boiling point:	601.3±55.0 °C(Predicted)
Density	1.17±0.1 g/cm3(Predicted)
storage temp.	2-8°C
solubility	DMSO: soluble15mg/mL, clear
pka	3.02±0.10(Predicted)
form	powder
color	yellow to orange

Safety information for 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

Signal word	Warning
Pictogram(s)	Exclamation Mark Irritant GHS07
GHS Hazard Statements	H315:Skin corrosion/irritation H319:Serious eye damage/eye irritation
Precautionary Statement Codes	P264:Wash hands thoroughly after handling. P264:Wash skin thouroughly after handling. P280:Wear protective gloves/protective clothing/eye protection/face protection. P302+P352:IF ON SKIN: wash with plenty of soap and water. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing. P332+P313:IF SKIN irritation occurs: Get medical advice/attention. P337+P313:IF eye irritation persists: Get medical advice/attention.

Computed Descriptors for 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

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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

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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

Synonym(s):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;LE-135

What is 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?

Description

The Uses of 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

What are the applications of Application

Definition

Biological Activity

Biochem/physiol Actions

storage

Properties of 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

Safety information for 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

Computed Descriptors for 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

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