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CCF642

Catalog No. T6800 CAS 346640-08-2

Synonyms: AC1LYELL

CCF642 (AC1LYELL) is a novel PDI-inhibiting compound with antimyeloma activity.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

CCF642, CAS 346640-08-2

Pack Size	Availability	Price/USD
1 mg	In stock	$ 30.00
2 mg	In stock	$ 43.00
5 mg	In stock	$ 77.00
10 mg	In stock	$ 105.00
25 mg	In stock	$ 207.00
50 mg	In stock	$ 369.00
100 mg	In stock	$ 531.00
500 mg	In stock	$ 1,180.00
1 mL * 10 mM (in DMSO)	In stock	$ 64.00

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Purity: 98.82%

Purity: 97.12%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	CCF642 (AC1LYELL) is a novel PDI-inhibiting compound with antimyeloma activity.
Targets&IC50	PDI:2.9 μmol/L
In vitro	In vitro, CCF642 inhibits PDI reductase activity about 100-fold more potently than the structurally distinct established inhibitors PACMA 31 and LOC14. Computational modeling suggests a novel covalent binding mode in active-site CGHCK motifs. CCF642 causes acute ER stress in multiple myeloma cells accompanied by apoptosis-inducing calcium release[1].
In vivo	CCF642 displays potent efficacy in an aggressive syngeneic mouse model of multiple myeloma and prolongs the lifespan of C57BL/KaLwRij mice engrafted with 5TGM1-luc myeloma, an effect comparable to the first-line multiple myeloma therapeutic bortezomib[1].
Kinase Assay	Inhibition of CB-839 on rHu-GAC: The enzymatic activity is measured in assay buffer containing 50 mM Tris-Acetate pH 8.6, 150 mM K2HPO4 , 0.25 mM EDTA, 0.1 mg/mL bovine serum albumin, 1 mM DTT, 2 mM NADP+ and 0.01% Triton X-100. To measure inhibition, the inhibitor (prepared in DMSO) is first pre-mixed with glutamine and glutamate dehydrogenase (GDH) and reactions are initiated by the addition of rHu-GAC. Final reactions contains 2 nM rHu-GAC, 10 mM glutamine, 6 units/mL GDH and 2% DMSO. Generation of NADPH is monitored by fluorescence (Ex340/Em460 nm) every minute for 15 minutes on a SpectraMax M5e plate reader. Relative fluorescence units (RFU) are converted to units of NADPH concentration (μM) using a standard curve of NADPH. Each assay plate incorporates control reactions that monitores the conversion of glutamate (1 to 75 μM) plus NADP+ to α-ketoglutarate plus NADPH by GDH. Under these assay conditions, up to 75 μM glutamate is stoichiometrically converts to α-ketoglutarate/NADPH by GDH. Initial reaction velocities are calculated by fitting the first 5 minutes of each progress curve to a straight line. Inhibition curves are fitted to a four-parameter dose response equation of the form: % activity = Bottom + (Top-Bottom)/(1+10^((LogIC50-X)*HillSlope)).

Synonyms	AC1LYELL
Molecular Weight	378.45
Formula	C15H10N2O4S3
CAS No.	346640-08-2

Storage

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

Solubility Information

DMSO: 7.6 mg/mL (20 mM)

References and Literature

1. Vatolin S, et al. Cancer Res. 2016, 76(11):3340-50.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Bioactive Compounds Library Max Hematonosis Compound Library Endoplasmic Reticulum Stress Compound Library Bioactive Compound Library Covalent Inhibitor Library Anti-Metabolism Disease Compound Library

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

CCF642 346640-08-2 Others calcium Inhibitor PDI apoptosis isomerases disulfide CCF 642 myeloma AC1LYELL protein multiple release CCF-642 stress inhibit anti-multiple inhibitor

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