stat5β

STAT5-IN-1 (STAT5 Inhibitor) is a cell-permeable inhibitor which suppresses Stat5 via binding to the SH2 domain.

Stafib-1 is a selective inhibitor of STAT5β targeting SH2 domain with an IC50 of 154 nM and a Ki of 44 nM.

Fedratinib (TG-101348) (TG101348) is an ATP-competitive inhibitor of JAK2 (IC50: 3 nM) with significantly less potent activity against JAK3.

Cenisertib is A potent ATP-competitive multi-kinase inhibitor, showing inhibitory effects on the activity of Aurora-kinase-A/B, ABL1, AKT, STAT5, FLT3, as well as kinase inhibitors of FER and its homolog. Cenisertib inhibits the growth of tumor mast cells (MCS) by inhibiting the activity of several different molecular targets. Cenisertib also inhibits tumor growth in pancreatic, breast, colon, ovarian and lung cancer and leukemia in xenograft models.

Stafib-2 is a potent and selective inhibitor of the transcription factor STAT5b, with IC50 values of 82 nM and 1.7 μM for STAT5b and STAT5a, respectively. Stafib-2 has poor cell permeability.

Nifuroxazide (Diarlidan) is an orally available and cell-permeable nitrofuran-based antidiarrheal agent. It has the inhibitory effect against the activation of cellular STAT1/3/5 transcription.

HODHBt is a STAT5-SUMO protein-protein interaction inhibitor.

AS2863619 free base enables the conversion of antigen-specific effector/memory T cells into Foxp3+ regulatory T (Treg) cells. It is a potent, orally active CDK8 and CDK19 inhibitor (IC50s: 0.61 nM and 4.28 nM). STAT5 activation enhanced by AS2863619 free base inhibition of CDK8/19, which consequently activates the Foxp3 gene.

Pimozide D4 is a deuterium labeled Pimozide.

STAT5-IN-2 is an inhibitor of STAT5 with antileukemic effects (EC50s: 9 μM and 5 μM in K562 and KU812 cells, respectively).

SH-4-54 is a most potent, small molecule, nonphosphorylated STAT3 inhibitor.

AS2863619 is an oral inhibitor of cyclin-dependent kinase 8 (CDK8) and CDK19. Inhibition of CDK8/19 can enhance the activation of STAT5, thereby activating the Foxp3 gene. It can convert antigen-specific effector/memory T cells into Foxp3+ regulatory T cells to study various immune diseases.

NS-3-008 hydrochloride (NS-3-008 HCl) is a transcriptional G0/G1 switch 2 (G0s2) inhibitor( IC50 of 2.25 μM).

BD750 is an effective immunosuppressant and a JAK3/STAT5 inhibitor, inhibits IL-2-induced JAK3/STAT5-dependent T cell proliferation(IC50 of 1.5 μM and 1.1 μM in mouse and human T cells, respectively)

Fedratinib hydrochloride hydrate (SAR 302503 hydrochloride hydrate) is a potent, selective, ATP-competitive and orally active JAK2 inhibitor.

CMD178 (TFA) is a lead peptide that consistently reduces the expression of Foxp3 and STAT5 induced by IL-2/s IL-2Rα signaling.

STAT5-IN-3 (Compound 14a) is a STAT5 inhibitor with anticancer properties. It works by blocking the tyrosine phosphorylation of STAT5A/5B at the Y694/699 sites, significantly reducing the expression of the STAT5B protein. This leads to the inhibition of downstream gene transcription, thereby preventing the proliferation and survival of leukemia cells. Additionally, STAT5-IN-3 has significant potential in overcoming chemotherapy resistance.

PF-05221304 (NSC-170984) is an orally active, liver-targeted inhibitor of acetyl-CoA carboxylase (ACC), a rate-limiting enzymes for fatty acid synthesis.

SD-436 is a selective and highly efficient STAT3 PROTAC degrader (DC50 = 0.5 μM), with an IC50 of 19 nM for STAT3, significantly higher than for STAT1/4/5/6. SD-436 depletes STAT3 and induces tumour regression in mouse leukaemia and lymphoma xenograft models.

IST5-002 (N6-Benzyladenosine-5'-phosphate) is a selective Stat5a/b inhibitor with anticancer activity that inhibits the transcriptional activity of Stat5a/b and induces apoptosis and death of prostate cancer cells and chronic myelogenous leukemia (CML) cells, which can be used for cancer research.

CDK8-IN-4k is a potent and highly selective CDK8 inhibitor, with no apparent potential for time-dependent CYP3A4 inhibition.

BP-1-108 is a potent and selective STAT5 inhibitor.

AK-2292 is a potent and selective STAT5 PROTAC degrader with a DC50 of 0.10 μM. It induces degradation of STAT5A/B proteins in vitro and in vivo and can cause tumor regression in acute myeloid leukemia and chronic myeloid leukemia xenograft mouse models [1] [2].

Stafia-1 is a potent STAT5a inhibitor (IC50=22.2 μM), displaying high selectivity over STAT5b and other STAT family members.