1. GPCR/G Protein
  2. Ras

CID-1067700 

Cat. No.: HY-13452 Purity: 98.86%
Handling Instructions

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

For research use only. We do not sell to patients.

CID-1067700 Chemical Structure

CID-1067700 Chemical Structure

CAS No. : 314042-01-8

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 88 In-stock
Estimated Time of Arrival: December 31
5 mg USD 80 In-stock
Estimated Time of Arrival: December 31
10 mg USD 140 In-stock
Estimated Time of Arrival: December 31
50 mg   Get quote  
100 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

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

IC50 & 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].

Solvent & Solubility
In Vitro: 

DMSO : 75 mg/mL (192.07 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5610 mL 12.8048 mL 25.6095 mL
5 mM 0.5122 mL 2.5610 mL 5.1219 mL
10 mM 0.2561 mL 1.2805 mL 2.5610 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.40 mM); Clear solution

References
Cell Assay
[2]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[2]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

390.48

Formula

C₁₈H₁₈N₂O₄S₂

CAS No.

314042-01-8

SMILES

O=C(C1=C(NC(NC(C2=CC=CC=C2)=O)=S)SC3=C1CC(C)(C)OC3)O

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Purity: 98.86%

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Product Name:
CID-1067700
Cat. No.:
HY-13452
Quantity:

CID-1067700

Cat. No.: HY-13452