Home JAK/STAT STAT inhibitor C188-9 For research use only.

C188-9

Synonyms: TTI 101

C188-9 (TTI 101) is a potent inhibitor of STAT3 that binds to STAT3 with high affinity (KD=4.7±0.4 nM). C188-9 is well tolerated in mice, shows good oral bioavailability, and is concentrated in tumors.

C188-9 Chemical Structure

C188-9 Chemical Structure

CAS No. 432001-19-9

Purity & Quality Control

C188-9 Related Products

Signaling Pathway

STAT Signaling Pathways

STAT Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Y79 Function assay 10 μM 28684419
SK-N-DZ Function assay 10 μM 28684419
Huh7 Cell viability assay 48 h IC50=11.27 μM 28533225
PLC/PRF/5 Cell viability assay 48 h IC50=11.83 μM 28533225
HepG2 Cell viability assay 48 h IC50=10.19 μM 28533225
SCC-35 Cell growth assay 0/0.1/0.3/1/3/10/100 μM 36 h IC50=10.8 ± 0.0 μM 27027445
SCC-61 Cell growth assay 0/0.1/0.3/1/3/10/100 μM 36 h IC50=14.8 ±2.9 μM 27027445
UM-SCC-17B Cell growth assay 0/0.1/0.3/1/3/10/100 μM 36 h IC50=0.7 ± 0.6 μM 27027445
HN30 Cell growth assay 0/0.1/0.3/1/3/10/100 μM 36 h IC50=4.4 ± 0.1 μM 27027445
A549 Function assay 2.5 h decreased pSTAT3 levels in a concentration-dependent manner starting at concentrations as low as 3 nM 26410177
Kasumi-1 Function assay IC50=4.5 μM 21447830
THP-1 Function assay IC50=4.8 μM 21447830
GDM-1 Function assay IC50=5.0 μM 21447830
NB-1 Function assay IC50=8.3 μM 21447830
HL-60 Function assay IC50=5.3 μM 21447830
KG-1 Function assay IC50=4.1 μM 21447830
K562 Apoptosis assay induction of apoptosis with an EC50 of 43.6 μM 21447830
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells 29435139
Click to View More Cell Line Experimental Data

Biological Activity

Description C188-9 (TTI 101) is a potent inhibitor of STAT3 that binds to STAT3 with high affinity (KD=4.7±0.4 nM). C188-9 is well tolerated in mice, shows good oral bioavailability, and is concentrated in tumors.
Targets
STAT3 [1]
(Cell-free)
4.7 nM(Kd)
In vitro
In vitro C188-9 is a small-molecule inhibitor of Stat3 that targets the phosphotyrosyl peptide binding site within the Stat3 Src homology 2 (SH2) domain with Ki 136 nM. It does not inhibit upstream Jak or Src kinases[1].
Cell Research Cell lines HNSCC cell line, UM-SCC-17B
Concentrations 0, 0.1, 0.3, 1, 3, 10, 30 μM
Incubation Time 24 h
Method

UM-SCC-17B cells were incubated with various doses (0/0.1/0.3/1/3/10/30μM) of C188 or C188-9 for 24 hrs.
Experimental Result Images Methods Biomarkers Images PMID
Western blot p-STAT3 / STAT3 / CEBPδ / Myostatin / p-Akt / Akt 24011072
Immunofluorescence VE-cadherin / β-catenin non-phosphorylated β-Catenin 26948077
In Vivo
In vivo Treatment of nude mice bearing xenografts of UM-SCC-17B, a radioresistant HNSCC line, with C188-9, but not C188, prevented tumor xenograft growth. C188-9 was well tolerated in mice, showed good oral bioavailability, and was concentrated in tumors[2].
Animal Research Animal Models CD2F1 female mice received isogenic C26 tumor cell via s.c injection
Dosages 12.5 mg/kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 471.52 Formula

C27H21NO5S
CAS No. 432001-19-9 SDF Download C188-9 SDF
Smiles COC1=CC=C(C=C1)S(=O)(=O)NC2=CC(=C(C3=CC=CC=C32)O)C4=C(C=CC5=CC=CC=C54)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 94 mg/mL ( (199.35 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 2 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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