Product Name :
CID-1067700
Description:
CID-1067700 (ML282) is a pan GTPase inhibitor, and competitively inhibits Ras-related in brain 7 (Rab7) with a Ki of 13 nM.
CAS:
314042-01-8
Molecular Weight:
390.48
Formula:
C18H18N2O4S2
Chemical Name:
5,5-dimethyl-2-[(phenylformamido)methanethioyl]amino-4H,5H,7H-thieno[2,3-c]pyran-3-carboxylic acid
Smiles :
CC1(C)CC2C(C(O)=O)=C(NC(=S)NC(=O)C3C=CC=CC=3)SC=2CO1
InChiKey:
ATSWBWHRHAQVFM-UHFFFAOYSA-N
InChi :
InChI=1S/C18H18N2O4S2/c1-18(2)8-11-12(9-24-18)26-15(13(11)16(22)23)20-17(25)19-14(21)10-6-4-3-5-7-10/h3-7H,8-9H2,1-2H3,(H,22,23)(H2,19,20,21,25)
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
CID-1067700 (ML282) is a pan GTPase inhibitor, and competitively inhibits Ras-related in brain 7 (Rab7) with a Ki of 13 nM.|Product information|CAS Number: 314042-01-8|Molecular Weight: 390.48|Formula: C18H18N2O4S2|Chemical Name: 5,5-dimethyl-2-[(phenylformamido)methanethioyl]amino-4H,5H,7H-thieno[2,3-c]pyran-3-carboxylic acid|Smiles: CC1(C)CC2C(C(O)=O)=C(NC(=S)NC(=O)C3C=CC=CC=3)SC=2CO1|InChiKey: ATSWBWHRHAQVFM-UHFFFAOYSA-N|InChi: InChI=1S/C18H18N2O4S2/c1-18(2)8-11-12(9-24-18)26-15(13(11)16(22)23)20-17(25)19-14(21)10-6-4-3-5-7-10/h3-7H,8-9H2,1-2H3,(H,22,23)(H2,19,20,21,25)|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: DMSO : 75 mg/mL (192.Oxacillin sodium salt In Vitro 07 mM; Need ultrasonic).Cromolyn GSK-3 |Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.PMID:32885679 |Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|In Vitro:|CID-1067700 (ML282) 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. 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.|In Vivo:|CID-1067700 (ML282; 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.|Products are for research use only. Not for human use.|
