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LCL161

Catalog No. T2080   CAS 1005342-46-0

LCL161, a SMAC mimetic, effectivity binds to and inhibits multiple IAPs (i.e. XIAP, c-IAP).

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LCL161 Chemical Structure
LCL161, CAS 1005342-46-0
Pack Size Availability Price/USD Quantity
2 mg In stock $ 63.00
5 mg In stock $ 97.00
10 mg In stock $ 129.00
25 mg In stock $ 198.00
50 mg In stock $ 297.00
100 mg In stock $ 479.00
1 mL * 10 mM (in DMSO) In stock $ 98.00
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Purity: 99.72%
Purity: 99.72%
Purity: 99.46%
Purity: 99.13%
Purity: 98%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description LCL161, a SMAC mimetic, effectivity binds to and inhibits multiple IAPs (i.e. XIAP, c-IAP).
Targets&IC50 XIAP (HEK293 cells):35 nM, CIAP1 (MDA-MB-231 cells):0.4 nM
Kinase Assay CYP3A activity is assessed using the probe reactions, midazolam-1′-hydroxylation and testosterone 6β-hydroxylation. For reversible inhibition, incubations (37°C, 10 min) are composed of (final concentrations): potassium phosphate buffer (100 mM, pH 7.4), β-NADPH (1 mM), magnesium chloride (5 mM), microsomal protein (0.025 mg/mL), probe substrate (1 μM midazolam or 25 μM testosterone), LCL161 (0, 0.5, 1, 5, 10, 25, 50, or 100 μM) and organic solvent (0.2% acetonitrile for midazolam, 0.2% methanol for testosterone). After a 3-minute preincubation, the reactions are initiated by addition of β-NADPH and terminated by addition of acetonitrile (two volumes). Reactions are previously shown to be linear with respect to time and protein concentration (results not shown) with midazolam and testosterone turnover of 8.7±1.3% (n=3) and 2.6±0.20%, respectively. Formation of 1′-hydroxymidazolam and 6β-hydroxytestosterone is determined by LC-MS/MS as described below[3].
Cell Research In vitro testing is performed using DIMSCAN (Only for Reference)
Molecular Weight 500.63
Formula C26H33FN4O3S
CAS No. 1005342-46-0

Storage

keep away from direct sunlight

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 93 mg/mL (185.8 mM)

Ethanol: 16 mg/mL (32 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

TargetMolReferences and Literature

1. Weisberg E, et al. Leukemia, 2010, 24(12), 2100-2109. 2. Houghton PJ, et al. Pediatr Blood Cancer, 2012, 58(4), 636-639. 3. Knights AJ, et al. Cancer Immunol Immunother, 2013, 62(2), 321-335. 4. Chen H, Li Y, Wu J, et al. RIPK3 collaborates with GSDMD to drive tissue injury in lethal polymicrobial sepsis[J]. Cell Death & Differentiation. 2020: 1-18.

TargetMolCitations

1. Chen H, Li Y, Wu J, et al. RIPK3 collaborates with GSDMD to drive tissue injury in lethal polymicrobial sepsis. Cell Death & Differentiation. 2020: 1-18

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Drug Repurposing Compound Library Anti-Cancer Clinical Compound Library Anti-Cancer Active Compound Library Anti-Cancer Drug Library Bioactive Compounds Library Max Autophagy Compound Library Anti-Breast Cancer Compound Library Anti-Fibrosis Compound Library NO PAINS Compound Library

Related Products

Related compounds with same targets
CUDC-427 Xevinapant AZD5582 AZD5582 acetate (1258392-53-8 free base) SM-164 Hydrochloride (957135-43-2 free base) Se-Methylselenocysteine SM-164 Anticancer agent 128

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Keywords

LCL161 1005342-46-0 Apoptosis IAP inhibit Inhibitor LCL-161 LCL 161 inhibitor

 

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