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Merck

SML1540

SBI-0206965

≥98% (HPLC), serine/threonine autophagy-initiating kinases ULK1 and ULK2 inhibitor, powder

Synonym(s):

2-((5-Bromo-2-((3,4,5-trimethoxyphenyl)amino)pyrimidin-4-yl)oxy)-N-methylbenzamide

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$298.00

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About This Item

Empirical Formula (Hill Notation):
C21H21BrN4O5
CAS Number:
1884220-36-3
Molecular Weight:
489.32
UNSPSC Code:
12352200
PubChem Substance ID:
329825951
NACRES:
NA.77

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Product Name

SBI-0206965, ≥98% (HPLC)

Quality Level

100

Assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 20 mg/mL, clear

storage temp.

−20°C

SMILES string

BrC1=C(OC2=C(C(NC)=O)C=CC=C2)N=C(NC3=CC(OC)=C(OC)C(OC)=C3)N=C1

InChI

1S/C21H21BrN4O5/c1-23-19(27)13-7-5-6-8-15(13)31-20-14(22)11-24-21(26-20)25-12-9-16(28-2)18(30-4)17(10-12)29-3/h5-11H,1-4H3,(H,23,27)(H,24,25,26)

InChI key

NEXGBSJERNQRSV-UHFFFAOYSA-N

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This Item
SML0995SML2202S7071
SBI-0206965 ≥98% (HPLC)

Sigma-Aldrich

SML1540

SBI-0206965

GSK1838705A ≥98% (HPLC)

Sigma-Aldrich

SML0995

GSK1838705A

SGC-GAK-1 ≥98% (HPLC)

Sigma-Aldrich

SML2202

SGC-GAK-1

SD-208 ≥98% (HPLC), powder

Sigma-Aldrich

S7071

SD-208

assay

≥98% (HPLC)

assay

≥98% (HPLC)

assay

≥98% (HPLC)

assay

≥98% (HPLC)

form

powder

form

powder

form

powder

form

powder

Quality Level

100

Quality Level

100

Quality Level

-

Quality Level

100

storage temp.

−20°C

storage temp.

−20°C

storage temp.

2-8°C

storage temp.

2-8°C

solubility

DMSO: 20 mg/mL, clear

solubility

DMSO: 20 mg/mL, clear

solubility

DMSO: 2 mg/mL, clear

solubility

DMSO: >5 mg/mL

color

white to beige

color

white to light brown

color

white to beige

color

off-white to tan

Application

SBI-0206965 has been used to study its effect on the growth of cadmium-transformed prostate epithelial cells.[1]

Biochem/physiol Actions

SBI-0206965 is a potent and selective inhibitor of the serine/threonine autophagy-initiating kinases ULK1 and ULK2 with selectivity for ULK1.
SBI-0206965 is a potent and selective inhibitor of the serine/threonine autophagy-initiating kinases ULK1 and ULK2 with selectivity for ULK1. SBI-0206965 has an IC50 value of 108 nM for ULK1, compared to 711nM for ULK2. Tumor cells require autophagy to remove misfolded proteins or damaged cellular organelles. SBI-0206965 was shown to suppress autophagy induced by mTOR inhibition. mTOR signaling is often hyperactive in many tumors and can drive proliferation, so mTOR inhibitors are being investigated as anticancer agents. However, mTOR inhibition also results in activation of the ULK1-dependent autophagy survival response, and most results with mTOR inhibitors have been at best cytostatic. SBI-0206965 synergizes with mTOR inhibition to induce apoptosis and cell death.
Since most of the tumor cells survive on autophagy mechanism, inhibition of autophagy inducers Unc-51 (serine/threonine-protein kinase)-like autophagy activating kinase (ULK1 and ULK2) might be useful in cancer therapy.[2]

Pictograms

Exclamation mark
GHS07

Signal Word

Warning

Hazard Statements

H315,H319,H335

Hazard Classifications

Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3

Target Organs

Respiratory system

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
0000434453
0000434453
0000187831
0000062734
0000062735

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Structure and function of the ULK1 complex in autophagy.
Lin M G and James H H
Current Opinion in Cell Biology, 39, 61-68 (2016)
Venkatesh Kolluru et al.
Cancer letters, 408, 121-129 (2017-08-29)
Chronic exposure to cadmium is known to be a risk factor for human prostate cancer. Despite over-whelming evidence of cadmium causing carcinogenicity in humans, the specific underlying molecular mechanisms that govern metal-induced cellular transformation remain unclear. Acute exposure (up to
Marine Angé et al.
Scientific reports, 11(1), 13700-13700 (2021-07-03)
Sepsis capillary leak syndrome (SCLS) is an independent prognostic factor for poor sepsis outcome. We previously demonstrated that α1AMP-activated protein kinase (α1AMPK) prevents sepsis-induced vascular hyperpermeability by mechanisms involving VE-cadherin (VE-Cad) stabilization and activation of p38 mitogen activated protein kinase/heat
Cansu Karabiyik et al.
STAR protocols, 2(4), 100926-100926 (2021-11-13)
The regulation of lipid kinases has remained elusive given the difficulties of assessing changes in lipid levels. Here, we describe the isolation of protein and lipid kinases to determine the regulation of lipid kinases in vitro. This can be followed
Prajna Paramita Naik et al.
Life sciences, 264, 118722-118722 (2020-11-09)
Secretory clusterin (sCLU) plays an important role in tumor development and cancer progression. However, the molecular mechanisms and physiological functions of sCLU in oral cancer is unclear. We examined the impact of sCLU-mediated autophagy in cell survival and apoptosis inhibition
View All Related Papers

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