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C188-9

Catalog No. T4650 CAS 432001-19-9

Synonyms: TTI-101

C188-9 (TTI-101) is a Stat3 inhibitor with an IC50 of 4-7 μM.

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

C188-9, CAS 432001-19-9

Pack Size	Availability	Price/USD
1 mg	In stock	$ 38.00
2 mg	In stock	$ 54.00
5 mg	In stock	$ 89.00
10 mg	In stock	$ 125.00
25 mg	In stock	$ 263.00
50 mg	In stock	$ 418.00
100 mg	In stock	$ 625.00
500 mg	In stock	$ 1,330.00
1 mL * 10 mM (in DMSO)	In stock	$ 97.00

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Purity: 100%

Purity: 98.83%

Purity: 98.07%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	C188-9 (TTI-101) is a Stat3 inhibitor with an IC50 of 4-7 μM.
Targets&IC50	STAT3:4-7 μM
In vitro	For apoptosis studies, AML cell lines and primary samples are treated for 24 hours with C188-9, then apoptotic cells are quantified by FACS analysis for annexin V-labeled cells. The EC50s for apoptosis induction are quite variable, ranging from 6 μM to over 50 μM
In vivo	In an analysis of approximately 13,528 discernible genes, C188 influences the expression of 37 gene transcripts (17 downregulated and 20 upregulated, false discovery rate (fdr)<0.01, fold change≥1.5), including 7 known targets of STAT3. Conversely, C188-9 exhibits a broader impact, modifying the expression of 384 genes related to oncogenesis (95 down- and 289 up-regulated), 76 of which are regulated by STAT3 (38 down-regulated and 38 up-regulated). Notably, C188-9 treatment downregulates 24 out of 38 genes (63%) previously identified as upregulated by STAT3. Furthermore, C188-9 downregulates an additional 10 genes (fdr <0.01, fold change≥1.5) known to be upregulated by STAT1, suggesting that 83.3% (40 out of 48) of the genes downregulated by C188-9 are positively regulated by STAT1. This includes sixteen genes co-regulated by both STAT3 and STAT1. The findings suggest that C188-9's modulation of gene transcript levels in head and neck squamous cell carcinoma (HNSCC) tumors may be attributed to its dual influence on STAT3 and STAT1 pathways.

Synonyms	TTI-101
Molecular Weight	471.52
Formula	C27H21NO5S
CAS No.	432001-19-9

Storage

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

Solubility Information

DMSO: 62 mg/mL

References and Literature

1. edell MS, et al. Stat3 signaling in acute myeloid leukemia: ligand-dependent and -independent activation and induction of apoptosis by a novel small-molecule Stat3 inhibitor. Blood. 2011 May 26;117(21):5701-9. 2. Bharadwaj U, et al. Small-molecule inhibition of STAT3 in radioresistant head and neck squamous cell carcinoma. Oncotarget. 2016 May 3;7(18):26307-30. 3. He Q R, Tang J J, Chen Z F, et al. Natural Product Trienomycin A is a STAT3 pathway inhibitor that exhibits potent in vitro and in vivo efficacy against pancreatic cancer[J]. Authorea Preprints. 2020 4. Gu H, Chen C, Hao X, et al. MDH1-mediated malate-aspartate NADH shuttle maintains the activity levels of fetal liver hematopoietic stem cells[J]. Blood. 2021, 137(11): 1478-1490.

Citations

1. Gu H, Chen C, Hao X, et al. MDH1-mediated malate-aspartate NADH shuttle maintains the activity levels of fetal liver hematopoietic stem cells. Blood. 2020, 136(5): 553-571. 2. He, Qiu‐Rui, et al. The natural product trienomycin A is a STAT3 pathway inhibitor that exhibits potent in vitro and in vivo efficacy against pancreatic cancer. British Journal of Pharmacology. 178.12 (2021): 2496-2515. 3. Guan X, Yang J, Wang W, et al.Dual inhibition of MYC and SLC39A10 by a novel natural product STAT3 inhibitor derived from Chaetomium globosum suppresses tumor growth and metastasis in gastric cancer.Pharmacological Research.2023: 106703.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Anti-Cancer Active Compound Library Anti-Cancer Drug Library Drug Repurposing Compound Library Anti-Cancer Clinical Compound Library Anti-COVID-19 Compound Library Bioactive Compounds Library Max Immuno-Oncology Compound Library Target-Focused Phenotypic Screening Library Bioactive Compound Library

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Keywords

C188-9 432001-19-9 Apoptosis JAK/STAT signaling Stem Cells STAT C1889 TTI101 Inhibitor C188 9 C-188-9 TTI-101 inhibit TTI 101 inhibitor

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