stat5-in-2

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

WP1066 is a inhibitor of JAK2 (IC50: 2.30 μM) and STAT3 (IC50: 2.43 μM) in HEL cells; shows activity to JAK2, STAT3 5, and ERK1 2, not JAK1 and JAK3. WP1066 has been used in trials studying the treatment of Melanoma, Brain Cancer, Solid Tumors, and Central Nervous System Neoplasms.

Pimozide (R6238) is a diphenylbutylpiperidine derivative and a dopamine antagonist with the antipsychotic property. Pimozide selectively inhibits type 2 dopaminergic receptors in the central nervous system (CNS), thereby decreasing dopamine neurotransmission and reducing the occurrence of the motor and vocal tics and delusions of parasitosis. In addition, this agent antagonizes alpha-adrenergic and 5-HT2 receptors.

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)

(R)-2-Phenylmorpholine is a fragment molecule that is commonly used in organic synthesis and can be involved in the synthesis of STAT5 6 PROTAC degraders or inhibitors.

Tyk2-IN-22 (Compound A8) is a selective inhibitor of tyrosine kinase 2 (Tyk2), effectively inhibiting Tyk2, JAK1, and JAK3 with IC50 values of 9.7 nM, 148.6 nM, and 883.3 nM, respectively. Additionally, Tyk2-IN-22 suppresses downstream STAT5 phosphorylation.

MS-1020 is a JAK3 and STAT3 inhibitor. MS-1020 selectively blocks constitutively-active JAK3 and consistently suppressed interleukin-2-induced JAK3/STAT5 signalling. MS-1020 potently inhibits persistently-active STAT3 in a cell type-specific manner.

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].