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Cat. No. Product Name CAS No. Information
PC-43790

Napabucasin

83280-65-3

Napabucasin (BBI-608) is a potent small-molecule inhibitor of STAT3 that has a broad spectrum of activity against stemness-high cancer cells (IC50=0.5-1.5 uM); blocks spherogenesis of cancer stem cells (CSC), but not hematopoietic stem cells; significantly reduces the expression of various stemness genes, including Nanog, Sox2, and Oct4 (POU5F1); significantly inhibits PaCa-2 xenograft tumor growth, and inhibits cancer relapse and metastasis.

Colon Cancer

Phase 3 Clinical

PC-35089

PM-43I

PM-43I is a selective inhibitor of STAT5/6 Src Homology 2 (SH2) domain, binds recombinant STAT6 and STAT5B (IC50=1.8 and 3.8 uM) with much lower affinity for STAT3 (IC50=29.9 uM); potently inhibits both STAT5- and STAT6-dependent allergic airway disease in mice; PM-43I reverses preexisting allergic airway disease in mice with a minimum ED50 of 0.25 μg/kg.
PC-63206

KI16

1090696-43-7 KI16 is a novel small molecules that inhibit STAT3-dependent transcription and function, interacts with the STAT3 SH2 domain; inhibits STAT3 phosphorylation and transcriptional activity in response to IL6 stimulation, inhibits cell viability preferentially in STAT3-dependent cell lines.
PC-63081

PG-S3-001

2047372-50-7 PG-S3-001 is a small molecule STAT3 inhibitor that binds to STAT3 protein potently with Kd of 324 nM by surface plasmon resonance; shows no effect in a kinome screen (>100 cancer-relevant kinases); inhibits phosphorylation of STAT3 at Y705, inhibits patient-derived pancreatic cancer cell proliferation in vitro and in vivo in the low micromolar range; exhibits in vivo efficacy on pancreatic cancer xenografts.
PC-62863

NSC 368262

299421-08-2 NSC 368262 is a selective STAT3 inhibitor that alkylates Cys468 in Stat3, blocks the DNA-binding activity of phosphorylated Stat3 homodimers with IC50 of 10-50 uM, without inhibiting the DNA-binding of phosphorylated Stat1 homodimers; also disrupts the DNA-binding activity of Stat1/Stat3 heterodimers (IC50=50-100 uM), blocks accumulation of activated Stat3 in the nucleus in tumor cell lines, impressively inhibits tumor growth in mouse models.
PC-62576

QD 232

1527467-32-8 QD 232 is a novel quinazolinedione-based redox modulator that potently inhibits Src/FAK and STAT3 phosphorylation, decreasing pancreatic cancer cell viability and migration; arrests cell cycle progression and induces apoptosis at low micromolar concentrations, shows effectivity in drug-resistant cancer cell lines.
PC-62556

AC-4-130

1834571-82-2 AC-4-130 is a novel, potent STAT5 SH2 domain inhibitor, binds to and efficiently blocks STAT5 activation and subsequent transcriptional activity, shows high selectivity for STAT5 over STAT1 and STAT3; disrupts STAT5 activation, dimerization, nuclear translocation, and STAT5-dependent gene transcription; substantially impairs the proliferation and clonogenic growth of human AML cell lines and primary FLT3-ITD+ AML patient cells in vitro and in vivo; synergistically increases the cytotoxicity of the JAK1/2 inhibitor Ruxolitinib and the p300/pCAF inhibitor Garcinol in vivo.

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