CID-1067700

Modify Date: 2026-07-09 15:04:58

CID-1067700 Structure
CID-1067700 structure
Common Name CID-1067700
CAS Number 314042-01-8 Molecular Weight 390.477
Density 1.4±0.1 g/cm3 Boiling Point N/A
Molecular Formula C18H18N2O4S2 Melting Point N/A
MSDS USA Flash Point N/A

 Use of CID-1067700


CID-1067700 is a pan GTPase inhibitor, and competitively inhibits Ras-related in brain 7 (Rab7) with a Ki of 13 nM.

 Names

Name 2-(benzoylcarbamothioylamino)-5,5-dimethyl-4,7-dihydrothieno[2,3-c]pyran-3-carboxylic acid
Synonym More Synonyms

 CID-1067700 Biological Activity

Description CID-1067700 is a pan GTPase inhibitor, and competitively inhibits Ras-related in brain 7 (Rab7) with a Ki of 13 nM.
Related Catalog
Target

Ki: 13 nM (Rab7)[1]

In Vitro CID-1067700 is a pan GTPase inhibitor, and competitively inhibits Rab7 with a Ki of 13 nM. CID-1067700 shows inhibitory activity against nucleotide binding by Rab7, with Kds of 100 nM and 40 nM for BODIPY-GTP and BODIPY-GDP, respectively. With increasing concentration, CID-1067700 causes strong inhibition on binding of the BODIPY-linked nucleotides, with EC50 values of 11.22 ± 1.34 nM for BODIPY-GTP and 20.96 ± 1.34 nM for BODIPY-GDP and calculated Ki values of 12.89 nM and 19.70 nM respectively. CID-1067700 (10 μM) has no effect on the rate of release of bound BODIPY-linked nucleotide by wild type Rab7 under equilibrium binding conditions[1]. CID-1067700 (0-40 μM) inhibits Rab7 activity, NF-κB activation as well as AID induction in B cells. Furthermore, CID-1067700 binds Rab7 with a high affinity (EC50: 10-20 nM), and blocks Class switch DNA recombination (CSR) in B cells via targeting Rab7[2].
In Vivo CID-1067700 (16 mg/kg, i.p.) prevents disease development in lupus-prone mice by Rab7 inhibition, and reduces IgG-IC deposition in MRL/Faslpr/lpr mice. CID-1067700 also targets B cells and specifically impairs the CSR machinery in vivo[2].
Cell Assay To treat human and mouse B cells in vitro with the Rab7 inhibitor, CID-1067700 is diluted in DMSO and added to cell cultures to the final concentration of 40 μM. CID-1067700 or DMSO is added either at the time when B cell stimulation started, or 66 h after B cells are stimulated with LPS plus IL-4, TGF-β, anti-δ/dex and RA, for analysis of plasma cell survival[2].
Animal Admin Mice[2] For in vivo treatment, CID-1067700 dissolved in DMSO (stock concentration 40 mM, 16 mg/mL) is diluted with the solvent to the final volume of 50 μL and injected intraperitoneally (i.p.) once per week at the dose of 16 mg/kg body weight. C57, MRL/Faslpr/lpr and C57/Sle1Sle2Sle3 mice injected i. p. with the vehicle DMSO (50 μL). For survival studies and skin lesion analyses, MRL/Faslpr/lpr mice are treated with nil or CID-1067700 for 10 weeks and maintained until moribund (e.g., showing signs of severe loss of mobility, hunched back, piloerection, ruffled fur, dyspnea, gasping and weight loss), at which point they are euthanized[2].
References

[1]. Agola JO, et al. A competitive nucleotide binding inhibitor: in vitro characterization of Rab7 GTPase inhibition. ACS Chem Biol. 2012 Jun 15;7(6):1095-108.

[2]. Lam T, et al. Small Molecule Inhibition of Rab7 Impairs B Cell Class Switching and Plasma Cell Survival To Dampen the Autoantibody Response in Murine Lupus. J Immunol. 2016 Nov 15;197(10):3792-3805.

 Chemical & Physical Properties

Density 1.4±0.1 g/cm3
Molecular Formula C18H18N2O4S2
Molecular Weight 390.477
Exact Mass 390.070801
PSA 158.52000
LogP 4.76
Index of Refraction 1.681
InChIKey ATSWBWHRHAQVFM-UHFFFAOYSA-N
SMILES CC1(C)Cc2c(sc(NC(=S)NC(=O)c3ccccc3)c2C(=O)O)CO1
Storage condition 2-8℃

 Safety Information

RIDADR NONH for all modes of transport

 CID-1067700Bioassay

View more

Name: Luminescence-based cell-based primary high throughput screening assay to identify ago...
Source: The Scripps Research Institute Molecular Screening Center
Target: mu-type opioid receptor isoform MOR-1 [Homo sapiens]
External Id: OPRM1-OPRD1_AG_LUMI_1536_1X%ACT PRUN
Name: Primary qHTS assay for inhibitors of alpha-synuclein gene (SNCA) expression
Source: NCGC
External Id: SNCA-p-activity-luciferase
Name: Fluorescence-based cell-based primary high throughput screening assay to identify ago...
Source: The Scripps Research Institute Molecular Screening Center
Target: muscarinic acetylcholine receptor M1 [Homo sapiens]
External Id: CHRM1_AG_FLUO8_1536_1X%ACT PRUN
Name: Quantitative High-Throughput drug screen in 47 multiple myeloma cell lines against th...
Source: NCGC
Target: N/A
External Id: s-my-keats_OPM1-m4-1
Name: Quantitative High-Throughput drug screen in 47 multiple myeloma cell lines against th...
Source: NCGC
Target: N/A
External Id: s-my-OC1MY5-m4-1
Name: Quantitative High-Throughput drug screen in 47 multiple myeloma cell lines against th...
Source: NCGC
Target: N/A
External Id: s-my-KMS_34-m4-1
Name: Quantitative High-Throughput drug screen in 47 multiple myeloma cell lines against th...
Source: NCGC
Target: N/A
External Id: s-my-keats_L363-m4-1
Name: Quantitative High-Throughput drug screen in 47 multiple myeloma cell lines against th...
Source: NCGC
Target: N/A
External Id: s-my-keats_OCIMY7-m4-1
Name: Quantitative High-Throughput drug screen in 47 multiple myeloma cell lines against th...
Source: NCGC
Target: N/A
External Id: s-my-MM1R-m4-1
Name: Quantitative High-Throughput drug screen in 47 multiple myeloma cell lines against th...
Source: NCGC
Target: N/A
External Id: s-my-mm1s-m4-1
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 Synonyms

2-{[(benzoylamino)carbonothioyl]amino}-5,5-dimethyl-4,7-dihydro-5H-thieno[2,3-c]pyran-3-carboxylic acid
cc-692
2-[(Benzoylcarbamothioyl)amino]-5,5-dimethyl-4,7-dihydro-5H-thieno[2,3-c]pyran-3-carboxylic acid
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