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SML1272

Sigma-Aldrich

I-BET762

≥98% (HPLC)

Synonym(s):

(4S)- 6-(4-Chlorophenyl)-N-ethyl-8-methoxy-1-methyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine-4-acetamide, GSK525762, GSK525762A, I-BET

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5 MG
¥1,438.55
25 MG
¥5,801.75

¥1,438.55

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5 MG
¥1,438.55
25 MG
¥5,801.75

About This Item

Empirical Formula (Hill Notation):
C22H22ClN5O2
CAS Number:
1260907-17-2
Molecular Weight:
423.90
MDL number:
MFCD22417091
UNSPSC Code:
12352200
PubChem Substance ID:
329825759
NACRES:
NA.77

¥1,438.55

Please contact Customer Service for Availability
Request a Bulk Order

Quality Level

100

Assay

≥98% (HPLC)

form

powder

optical activity

[α]/D +80 to +90°, c = 0.3 in methanol

drug control

regulated under CDSA - not available from Sigma-Aldrich Canada

color

white to beige

solubility

DMSO: 10 mg/mL, clear

storage temp.

2-8°C

SMILES string

CCNC(C[C@@H]1N=C(C2=CC=C(Cl)C=C2)C3=CC(OC)=CC=C3N4C1=NN=C4C)=O

InChI

1S/C22H22ClN5O2/c1-4-24-20(29)12-18-22-27-26-13(2)28(22)19-10-9-16(30-3)11-17(19)21(25-18)14-5-7-15(23)8-6-14/h5-11,18H,4,12H2,1-3H3,(H,24,29)/t18-/m0/s1

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Show Differences

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This Item
SML1605401010SML1406
I-BET762 ≥98% (HPLC)

SML1272

I-BET762

OTX015 ≥98% (HPLC)

SML1605

OTX015

I-BET A cell-permeable benzodiazepine compound that binds the tandem bromodomains of BET (bromodomain and extra terminal domain) family members BRD2 (1-473), BRD3 (1-434), and BRD4 (1-477) with high affinity.

401010

I-BET

油菜素唑 ≥98% (HPLC)

SML1406

油菜素唑

assay

≥98% (HPLC)

assay

≥98% (HPLC)

assay

≥98% (HPLC)

assay

≥98% (HPLC)

drug control

regulated under CDSA - not available from Sigma-Aldrich Canada

drug control

-

drug control

-

drug control

-

Quality Level

100

Quality Level

100

Quality Level

100

Quality Level

100

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

−20°C

storage temp.

2-8°C

solubility

DMSO: 10 mg/mL, clear

solubility

DMSO: 20 mg/mL, clear

solubility

DMSO: 50 mg/mL

solubility

DMSO: 5 mg/mL, clear (warmed)

Biochem/physiol Actions

I-BET762 (GSK525762) is a selective inhibitor of bromodomain and extra terminal (BET) domain proteins BRD2, BRD3 and BRD4 with IC50 values of 32.5–42.5 nM and no interaction with other bromodomain-containing proteins. I-BET mimicks acetylated histone, preventing the protein-protein interaction between acetyl-lysines and the BET reader protein. This was shown to block expression of inflammatory genes in activated macrophages and confer protection against endotoxic shock and bacterial sepsis. I-BET762 also showed potent anti-myeloma activity in vitro and in vivo.
I-BET762 is a selective inhibitor of bromodomain and extra terminal (BET) domain proteins; synthetic histone mimic.
I-BET762 possesses anti-inflammatory property by controlling the pro-inflammatory gene expression.[1] I-BET762 hinders the MYC (proto-oncogene) expression in cellular models. This action of I-BET762 might serve as an effective therapy in treating prostate cancer.[2]

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

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    Certificates of Analysis (COA)

    Lot/Batch Number
    0000179114
    0000166781
    0000179114
    0000166781
    0000101605

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    Inhibition of BET bromodomain proteins as a therapeutic approach in prostate cancer.
    Wyce A, et al.
    Oncotarget, 4(12), 2419-2419 (2013)
    Bromodomains: are readers right for epigenetic therapy?.
    Conway S J.
    ACS Medicinal Chemistry Letters, 3(9), 691?694-691?694 (2012)
    Laura Helminen et al.
    Nucleic acids research, 52(2), 625-642 (2023-11-28)
    Treatment of prostate cancer relies predominantly on the inhibition of androgen receptor (AR) signaling. Despite the initial effectiveness of the antiandrogen therapies, the cancer often develops resistance to the AR blockade. One mechanism of the resistance is glucocorticoid receptor (GR)-mediated
    Francesco Paolo Fiorentino et al.
    International journal of molecular sciences, 21(24) (2020-12-20)
    Small cell lung cancer (SCLC) is an aggressive type of lung cancer with high mortality that is caused by frequent relapses and acquired resistance. Despite that several target-based approaches with potential therapeutic impact on SCLC have been identified, numerous targeted
    Brian Krug et al.
    Cancer cell, 35(5), 782-797 (2019-05-16)
    High-grade gliomas defined by histone 3 K27M driver mutations exhibit global loss of H3K27 trimethylation and reciprocal gain of H3K27 acetylation, respectively shaping repressive and active chromatin landscapes. We generated tumor-derived isogenic models bearing this mutation and show that it
    View All Related Papers

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