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2-[[2-Ethoxy-4-(4-hydroxy-1-piperidinyl)phenyl]amino]-5,11-dihydro-5,11-dimethyl-6H-pyrimido[4,5-b][1,4]benzodiazepin-6-one, also known as XMD8-92, is a potent and selective ERK5 inhibitor with a Kd of 80 nM. It also inhibits DCAMKL2, TNK1, and Plk4 with less potency. XMD8-92 blocks ERK5 autophosphorylation, ERK5-mediated phosphorylation of promyelocytic leukemia protein (PML), and PML-dependent activation of p21. It is a BMK1 inhibitor and has been shown to block cellular BMK1 activation.

1234480-50-2

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1234480-50-2 Usage

Uses

Used in Pharmaceutical Industry:
XMD8-92 is used as an ERK5 inhibitor for its potential therapeutic applications in treating various diseases. It has been shown to inhibit AP-1 transcriptional activity induced by MEK5-activated ERK5, which plays a role in cell proliferation and survival. XMD8-92 is also used as a BMK1 inhibitor, which has potential applications in treating various diseases by blocking cellular BMK1 activation.
Used in Oncology Research:
XMD8-92 is used as an anticancer agent in lung and cervical tumor models. It has been shown to significantly suppress tumor growth and is well tolerated in animals. 2-[[2-Ethoxy-4-(4-hydroxy-1-piperidinyl)phenyl]amino]-5,11-dihydro-5,11-dimethyl-6H-pyrimido[4,5-b][1,4]benzodiazepin-6-one inhibits bFGF-induced angiogenesis in a Matrigel plug assay in mice and reduces tumor growth in a HeLa mouse xenograft model when administered at a dose of 50 mg/kg twice per day.
Used in Drug Discovery:
XMD8-92 is used as a research tool in drug discovery to identify and develop new therapeutic agents targeting ERK5 and other kinases. Its selectivity and potency make it a valuable compound for studying the role of these kinases in various diseases and for developing new drugs with improved efficacy and safety profiles.
Used in Biochemical Research:
XMD8-92 is used in biochemical research to study the mechanisms of action of ERK5 and other kinases. It can be used to investigate the role of these kinases in various cellular processes, such as cell proliferation, survival, and angiogenesis, and to identify potential therapeutic targets for the treatment of various diseases.
Overall, XMD8-92 is a versatile compound with potential applications in various fields, including pharmaceuticals, oncology research, drug discovery, and biochemical research. Its selectivity and potency make it a valuable tool for studying the role of ERK5 and other kinases in disease and for developing new therapeutic agents.

Check Digit Verification of cas no

The CAS Registry Mumber 1234480-50-2 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,2,3,4,4,8 and 0 respectively; the second part has 2 digits, 5 and 0 respectively.
Calculate Digit Verification of CAS Registry Number 1234480-50:
(9*1)+(8*2)+(7*3)+(6*4)+(5*4)+(4*8)+(3*0)+(2*5)+(1*0)=132
132 % 10 = 2
So 1234480-50-2 is a valid CAS Registry Number.

1234480-50-2 Well-known Company Product Price

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  • Sigma

  • (SML1382)  XMD8-92  ≥98% (HPLC)

  • 1234480-50-2

  • SML1382-5MG

  • 1,481.22CNY

  • Detail
  • Sigma

  • (SML1382)  XMD8-92  ≥98% (HPLC)

  • 1234480-50-2

  • SML1382-25MG

  • 5,961.15CNY

  • Detail

1234480-50-2SDS

SAFETY DATA SHEETS

According to Globally Harmonized System of Classification and Labelling of Chemicals (GHS) - Sixth revised edition

Version: 1.0

Creation Date: Aug 13, 2017

Revision Date: Aug 13, 2017

1.Identification

1.1 GHS Product identifier

Product name 2-[2-ethoxy-4-(4-hydroxypiperidin-1-yl)anilino]-5,11-dimethylpyrimido[4,5-b][1,4]benzodiazepin-6-one

1.2 Other means of identification

Product number -
Other names XMD8-92

1.3 Recommended use of the chemical and restrictions on use

Identified uses For industry use only.
Uses advised against no data available

1.4 Supplier's details

1.5 Emergency phone number

Emergency phone number -
Service hours Monday to Friday, 9am-5pm (Standard time zone: UTC/GMT +8 hours).

More Details:1234480-50-2 SDS

1234480-50-2Upstream product

1234480-50-2Downstream Products

1234480-50-2Relevant academic research and scientific papers

PYRIMIDO-DIAZEPINONE KINASE SCAFFOLD COMPOUNDS AND METHODS OF TREATING DISORDERS

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Page/Page column 54, (2010/08/04)

The present invention relates to novel pyrimido-diazepinone compounds, methods of modulating protein kinases, including MPSl (TTK), ERK5 (BMKl, MAPK7), polo kinase 1,2,3, or 4, Ackl, Ack2, AbI, DCAMKLl, ABLl, AbI mutants, DCAMKL2, ARK5, BRK, MKNK2, FGFR4,

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