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

A126326

A409220

AZD1480

≥98%, 10mM in DMSO

B345013

B421120

BMS 911543

≥98%, 10mM in DMSO

C127224

M408149

CYT387

≥98%, 10mM in DMSO

F413789

F420902

GLPG-0634

≥98%, 10mM in DMSO

R126338

R409244

INCB018424

≥98%, 10mM in DMSO

J339604

J422387

JAK2 Inhibitor V

≥98%, 10mM in DMSO

P108001

P580488

Piceatannol

≥98%, 10mM in DMSO

T126330

F408078

TG101348

≥98%, 10mM in DMSO

E129454

T408126

Tofacitinib Citrate

≥99%, 10mM in DMSO

A126525

A408508

Tyrphostin AG490

≥98%, 10mM in DMSO

J126663

J422462

JANEX-1

≥98%, 10mM in DMSO


Inhibitors of STAT signaling:


Aladdin catalog

Product name

Purity

C110682

C295384 

C423884 

Carboplatin

≥98%,≥99.95% metals basis,10mM in Water

D135631 

C580352

Corosolic acid

≥98%, 10mM in DMSO

C101973 

C101974 

C408350

Cryptotanshinone

analytical standard ≥98%,≥98%, 10mM in DMSO

D299451 

D117978

Demethoxycurcumin

≥95%,analytical standard ≥98%

E107404 

E107403 

E409009

Epigallocatechin gallate

≥98%,analytical standard,10mM in DMSO

S171302 

S107347 

S425032

Sesamin

≥98%,analytical standard, 10mM in DMSO

S125098 

S408543

Sorafenib

≥99%, 10mM in DMSO

S111997 

S140384 

D424040

DL-Sulforaphane

≥95%,≥70%,10mM in DMSO

T109794 

T109795 

T424804

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/

Categories: Technical articles

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