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).

(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.

JAK2-IN-14 is an orally effective JAK2 inhibitor with an IC50 of 2 nM. It exhibits selectivity for JAK2 over JAK1, JAK3, and TYK2 by factors of 89.5, 80.5, and 51 times, respectively. JAK2-IN-14 inhibits the STAT5 signaling pathway and can cause tumor cell cycle arrest and apoptosis (apoptosis). It is applicable in the research of myeloproliferative neoplasms (MPN).

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.

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.

Givinostat (ITF-2357) is an HDAC inhibitor with IC50 values of 198 nM for HDAC1 and 157 nM for HDAC3.

AK-2292 is a highly potent and selective STAT5A/B PROTAC protein degrader with a DC50 value of 0.10 μM that induces STAT5A/B protein degradation both in vitro and in vivo. AK-2292 can be used in research on acute myeloid leukemia and chronic myeloid leukemia.

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)

Abrocitinib (Standard) is a reference standard for research and analysis in studies involving Abrocitinib. Abrocitinib (PF-04965842) (PF-04965842) is a potent, specific and orally-active JAK1 inhibitor (IC50s: 29/803 nM for JAK1/2).

Pimozide (Standard) is a reference standard for research and analysis in studies involving Pimozide. 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.