dual-specificity

GNF4877 is a potent inhibitor of DYRK1A and GSK3β (IC50s: 6 nM and 16 nM, respectively), resulting in the blockade of nuclear export of nuclear factor of activated T-cells (NFATc) and increased β-cell proliferation.

BCI hydrochloride ((E)-BCI hydrochloride) is a selective dual-specificity phosphatase 6 (DUSP6) inhibitor that inhibits RANKL-mediated osteoclastogenesis and attenuates oophorectomy-induced bone loss.BCI hydrochloride has anti-inflammatory activity, reduces reactive oxygen species (ROS) production, and partially reverses AE-induced bone loss. BCI hydrochloride has anti-inflammatory activity and can reduce reactive oxygen species (ROS) production, partially reverse AE-induced cytotoxicity, and increase ERK activity, which can be used to study inflammatory diseases.

DA-3003-1 (DA-3003-1) is a membrane-permeable, potent and selective Cdc25 dual specificity phosphatase inhibitor with antitumor activity that inhibits Cdc25B2, Cdc25A, Cdc25B2 and Cdc25C.

Harmine (Telepathine) is an alkaloid isolated from seeds of Peganum harmala.

Abemaciclib (LY2835219) is a dual inhibitor of CDK4 6 (IC50=2 10 nM) with selectivity and specificity. Abemaciclib has antitumor activity and is used to treat advanced or metastatic breast cancer.

AZ191(IC50 of 17 nM) is an effective and specific DYRK1B inhibitor. The specificity of AZ191 for DYRK1B is about 5- and 110-fold greater over DYRK1A and DYRK2, respectively.

Aclacinomycin A (Aclarubicin) hydrochloride is a fluorescent molecule and the first described non-peptidic inhibitor with discrete specificity for the CTRL (chymotrypsin-like) activity of the 20S proteasome. Additionally, it is a dual inhibitor of topoisomerase I and II.

BCI ((E)-BCI) is an allosteric inhibitor of dual-specificity phosphatases (DUSP), with EC50 values of 13.3 μM for DUSP6 and 8.0 μM for DUSP1 in cells, and does not inhibit DUSP5.

DYRKs-IN-1 has antitumor activity. DYRKs-IN-1 is a potent DYRKs (Dual-specificity tyrosine-phosphorylation-regulated kinases) inhibitor with IC50s of 9 nM and 5 nM for DYRK1B and DYRK1A, respectively.

(E Z)-BCI (NSC-150117), a dual-specificity phosphatase 6 (DUSP6) inhibitor with anti-inflammatory properties, reduces LPS-induced inflammatory mediators and ROS production in macrophage cells by activating the Nrf2 signaling axis and inhibiting the NF-κB pathway.

LDN-192960 hydrochloride is an inhibitor of Dual-specificity Tyrosine-regulated Kinase 2 (DYRK2) and Haspin, with IC50 values of 48 nM and 10 nM, respectively.

NSC305787 hydrochloride ((Rac)-NSC305787 hydrochloride is a cell membrane permeable and selective and potent small molecule dual inhibitor of Cdc25 dual specificity phosphatase and EZR that displays antitumor activity in pancreatic cancer cells and inhibits Cdc25B2, Cdc25A, Cdc25B2 and Cdc25C.NSC 663284 inhibits NSD2 (IC50 of 170 nM) enzyme activity.

AZ-Dyrk1B-33 (3-(2-Methyl-4-pyrimidinyl)-1-(phenylmethyl)-1H-pyrrolo[2,3-c]pyridine) is a potent and selective Dyrk1B kinase inhibitor with an IC50 of 7 nM.

CLK-IN-T3 is an inhibitor of CLK1, CLK2, and CLK3 with IC50s of 0.67, 15, and 110 nM. CLK-IN-T3 exhibits anti-cancer activity.

GSK-626616 is a potent and orally bioavailable DYRK3 inhibitor (IC50: 0.7 nM). It inhibits other members of the DYRK family with similar potency. GSK-626616 is a potential therapy for the treatment of anemia.

NSC-87877 is an effective inhibitor of Shp2 and Shp1 protein tyrosine phosphatases (IC50=0.318 μM, 0.355 μM of shp2 and shp1, respectively).It also inhibits dual-specificity phosphatase 26 (DUSP26).

Dyrk1A-IN-11 (compound 166) is an effective inhibitor targeting dual-specificity tyrosine phosphorylation-regulated 1A (DYRK1A) with an EC50 of 0.0021 µM. Additionally, this compound inhibits the phosphorylation of Tau (Thr212) with an EC50 of 0.0361 µM.

Dyrk1A-IN-12 (compound S43) is an inhibitor of dual specificity tyrosine phosphorylation regulated kinase 1A (Dyrk1A). It has an IC50 of 95 nM for inhibiting Dyrk1A. The compound demonstrates antiviral activity against EV-A71 (Enterovirus A71) with an EC50 of 4.4 μM, a CC50 of 12.8 μM, and a selectivity index (SI) of 2.9. Additionally, Dyrk1A-IN-12 exhibits potent inhibitory effects on the herpes simplex virus (HSV).

ID-8, a DYRK inhibitor, sustains embryonic stem cell self-renewal in long-term culture.

Harmine hydrochloride (telepathine hydrochloride) is extracted from Peganum Harmala Genus.

GNF2133 is an effective and selective inhibitor of DYRK1A with IC50s of 6.2 nM. GNF2133 can be used in studies about type 1 diabetes.

MLS-0437605 is a potent and selective inhibitor of dual-specificity phosphatase 3 (DUSP3), with an IC50 of 3.7 μM. It exhibits higher selectivity towards DUSP3 in comparison to DUSP22 and other protein tyrosine phosphatases (PTPs).

F1063-0967 is a Dual-specificity phosphatase 26 (DUSP26) inhibitor with an IC50 of 11.62 μM.

Protein kinase inhibitors 1 is a novel inhibitor of HIPK2 with an IC50 of 74 nM and Kd of 9.5 nM.