ChemicalBook CAS DataBase List 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

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

Product Name4-(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
CAS155877-83-1
CBNumberCB8162724
MFC29H30N2O2
MW438.56
MDL NumberMFCD06798318
MOL File155877-83-1.mol
MSDS FileSDS

Chemical Properties

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
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)
InChIKey	YZZAIQOVMHVWBS-UHFFFAOYSA-N
SMILES	N1(c2c(cc5c(c2)C(CCC5(C)C)(C)C)N=C(c4c1cccc4)c3ccc(cc3)C(=O)O)C
UNSPSC Code	12352200
NACRES	NA.77

Safety

Symbol(GHS)

Signal word

Warning

Hazard statements

H315-H319

Precautionary statements

P264-P280-P302+P352-P305+P351+P338-P332+P313-P337+P313

Hazard Codes

Risk Statements

36/38

Safety Statements

WGK Germany

Storage Class

11 - Combustible Solids

Hazard Classifications

Eye Irrit. 2
Skin Irrit. 2

NFPA 704:

	0
2		0

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 Price

Product number	Packaging	Price	Product description	Buy
Sigma-Aldrich SML0809	5mg	$111	LE 135 ≥98% (HPLC)	Buy
Sigma-Aldrich SML0809	25mg	$418	LE 135 ≥98% (HPLC)	Buy
Cayman Chemical 14415	1mg	$36	LE 135 ≥98%	Buy
Cayman Chemical 14415	5mg	$110	LE 135 ≥98%	Buy
Cayman Chemical 14415	10mg	$153	LE 135 ≥98%	Buy

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 Chemical Properties,Usage,Production

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.

Uses

LE 135 has been used for in vitro islet treatment.

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

References

[1] Y LI. Identification of a novel class of retinoic acid receptor beta-selective retinoid antagonists and their inhibitory effects on AP-1 activity and retinoic acid-induced apoptosis in human breast cancer cells.[J]. The Journal of Biological Chemistry, 1999, 274 22: 15360-15366. DOI: 10.1074/jbc.274.22.15360
[2] LAURENCE EYROLLES. Retinobenzoic Acids. 6. Retinoid Antagonists with a Heterocyclic Ring[J]. Journal of Medicinal Chemistry, 1994, 37 10: 1508-1517. DOI: 10.1021/jm00036a017
[3] HIROKI UMEMIYA. Regulation of Retinoidal Actions by Diazepinylbenzoic Acids. 1 Retinoid Synergists Which Activate the RXRRAR Heterodimers[J]. Journal of Medicinal Chemistry, 1997, 40 26: 4222-4234. DOI: 10.1021/jm9704309

Preparation Products And Raw materials

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 Suppliers

Supplier	Tel	Email	Country	ProdList	Advantage
TargetMol Chemicals Inc.	+1-781-999-5354; +17819995354	marketing@targetmol.com	United States	32467	58
Hubei Ipure Biology Co., Ltd	+8613367258412	ada@ipurechemical.com	China	10236	58
Nantong HI-FUTURE Biology Co., Ltd.	+undefined18051384581	sales@chemhifuture.com	China	3135	58
Aladdin Scientific		tp@aladdinsci.com	United States	57505	58
J & K SCIENTIFIC LTD.	18210857532; 18210857532	jkinfo@jkchemical.com	China	96815	76
3B Pharmachem (Wuhan) International Co.,Ltd.	821-50328103-801 18930552037	3bsc@sina.com	China	15838	69
Nanjing Chemlin Chemical Co., Ltd	025-83697070 13770331960	info@chemlin.com.cn	China	16059	64
Bide Pharmatech Ltd.	400-400-164-7117 18317119277	product02@bidepharm.com	China	39999	60
Sigma-Aldrich	021-61415566 800-8193336	orderCN@merckgroup.com	China	51395	80
EMMX Biotechnology LLC	888-539-0666	info@emmx.com	United States	8447	60

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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 Spectrum

155877-83-1, 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 ACIDRelated Search

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