JAK/STAT Inhibitors
JAK/STAT Inhibitors
The Janus kinase (JAK) and signal transducer and activator of transcription (STAT) proteins form a critical signaling cascade that conveys extracellular signals across the plasma membrane and into the nucleus, where they modulate gene transcription. This pathway regulates key biological processes, including cell proliferation, differentiation, survival, and host defense. While broadly expressed, JAK/STAT signaling is particularly prominent in immune cells, where it mediates the actions of cytokines, interferons, and growth factors.
Within the nucleus, STAT proteins function as transcription factors by binding to promoter regions of DNA and driving the expression of downstream genes. Dysregulation of this process is implicated in numerous diseases. For example, constitutive activation of STAT3 and STAT5 has been documented in several cancers, leading to persistent signaling activity and uncontrolled gene transcription.
Upstream, JAK proteins act as receptor-associated kinases that phosphorylate and activate STATs following ligand binding to transmembrane receptors. Gain-of-function mutations in JAK genes have been strongly associated with hematologic malignancies, including essential thrombocythemia, myelofibrosis, and various forms of leukemia.
Inhibitors of JAK signaling:
| Aladdin catalog | Product name | Purity |
AZD1480 | ≥98%, 10mM in DMSO | |
BMS 911543 | ≥98%, 10mM in DMSO | |
CYT387 | ≥98%, 10mM in DMSO | |
GLPG-0634 | ≥98%, 10mM in DMSO | |
INCB018424 | ≥98%, 10mM in DMSO | |
JAK2 Inhibitor V | ≥98%, 10mM in DMSO | |
Piceatannol | ≥98%, 10mM in DMSO | |
TG101348 | ≥98%, 10mM in DMSO | |
Tofacitinib Citrate | ≥99%, 10mM in DMSO | |
Tyrphostin AG490 | ≥98%, 10mM in DMSO | |
JANEX-1 | ≥98%, 10mM in DMSO |
Inhibitors of STAT signaling:
Aladdin catalog | Product name | Purity |
Carboplatin | ≥98%,≥99.95% metals basis,10mM in Water | |
Corosolic acid | ≥98%, 10mM in DMSO | |
Cryptotanshinone | analytical standard ≥98%,≥98%, 10mM in DMSO | |
Demethoxycurcumin | ≥95%,analytical standard ≥98% | |
Epigallocatechin gallate | ≥98%,analytical standard,10mM in DMSO | |
Sesamin | ≥98%,analytical standard, 10mM in DMSO | |
Sorafenib | ≥99%, 10mM in DMSO | |
DL-Sulforaphane | ≥95%,≥70%,10mM in DMSO | |
Tanshinone IIA | analytical standard ≥99%,≥98%,10mM in DMSO |
References:
1. Yu H, Pardoll D, Jove R. Nat Rev Cancer. 2009 Nov;9(11):798-809.
2.Berger A, Sexl V, Valent P, et al. Oncotarget. 2014 Oct 30;5(20):9564-76.
3. Vainchenker W, Constantinescu SN. Oncogene. 2013 May 23;32(21):2601-13.
4. Villarino AV, Kanno Y, Ferdinand JR, et al. J Immunol. 2015 Jan 1;194(1):21-7.
Aladdin: https://www.aladdinsci.com/
