|
T15422 |
GSK-626616
|
|
DYRK
|
|
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. |
|
T6257 |
AZ191
|
|
DYRK
|
|
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. |
|
T14364 |
AZ-Dyrk1B-33
|
3-(2-Methyl-4-pyrimidinyl)-1-(phenylmethyl)-1H-pyrrolo[2,3-c]pyridine |
DYRK
|
|
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. |
|
TQ0111 |
LDN-192960
|
|
DYRK
,
Haspin Kinase
|
|
LDN-192960 is a potent inhibitor of Haspin and DYRK2 (IC50s: 10 nM and 48 nM). |
|
T2431 |
ID-8
|
ID8 |
DYRK
|
|
ID-8, a DYRK inhibitor, sustains embryonic stem cell self-renewal in long-term culture. |
|
T11447 |
GNF4877
|
|
GSK-3
,
DYRK
|
|
GNF4877 is a potent DYRK1A and GSK3β inhibitor (IC50s: 6 nM and 16 nM). It leads to blockade of nuclear factor of activated T-cells (NFATc) nuclear export and increased β-cell proliferation cells. |
|
T14980 |
CLK-IN-T3
|
|
DYRK
,
CDK
|
|
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. |
|
T40187 |
GNF2133
|
|
DYRK
|
|
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. |
|
T4636 |
Protein kinase inhibitors 1
|
|
Others
,
DYRK
|
|
Protein kinase inhibitors 1 is a novel inhibitor of HIPK2 with an IC50 of 74 nM and Kd of 9.5 nM. |
|
T62096 |
Dyrk1A/α-synuclein-IN-1
|
|
|
|
Dyrk1A/α-synuclein-IN-1 (Compound b1) is a dual inhibitor of Dyrk1A (IC50: 177 nM) and α-synuclein aggregation (IC50: 10.5 μM). CNS permeability and neuroprotective activity. |
|
T62226 |
Dyrk1A/α-synuclein-IN-2
|
|
|
|
Dyrk1A/α-synuclein-IN-2 (Compound b20) is a dual inhibitor of Dyrk1A and α-synuclein aggregation that acts on α-synuclein (IC50: 7.8 μM). Dyrk1A/α-synuclein-IN-2 has a high predictive CNS permeability and neuroprotective... |
|
T11132 |
DYRKs-IN-1
|
|
DYRK
|
|
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. |
|
T60334 |
DYRK1-IN-1
|
|
|
|
DYRK1-IN-1 is a highly selective and ligand-efficient DYRK1A inhibitor. DYRK1-IN-1 inhibits DYRK1A phosphorylation activity with an IC 50 value of 220 nM. DYRK1-IN-1 exhibits good permeability and cellular activity witho... |
|
T27226 |
DYRKi
|
|
|
|
DYRKi is a nontoxic, DYRK1-selective inhibitor. |
|
T62414 |
Dyrk1A-IN-1
|
|
|
|
Dyrk1A-IN-1 is a triple inhibitor of Dyrk1A kinase activity, aggregation of tau and α-syn oligomers, with an IC50 value of 119 nM for Dyrk1A kinase. |
|
T62043 |
Dyrk1A/B-IN-1
|
|
|
|
Dyrk1A/B-IN-1 (compound 3n) is a potent, selective and cell-permeable inhibitor of DYRK1A and DYRK1B. Dyrk1A/B-IN-1 inhibits DYRK1A and DYRK1B with Kis of 67.8 nM and 237.9 nM, and IC 50 s of 1.1 μM and 0.8 μM, respectiv... |
|
T72242 |
DYRKs-IN-1 hydrochloride
|
|
|
|
DYRKs-IN-1 hydrochloride is a potent inhibitor of Dual-specificity tyrosine-phosphorylation-regulated kinases (DYRKs), exhibiting IC50 values of 5 nM and 8 nM for DYRK1A and DYRK1B, respectively. This compound demonstrat... |
|
T11133 |
DYRKs-IN-2
|
|
DYRK
|
|
DYRKs-IN-2 has antitumor activity. DYRKs-IN-2 is a potent DYRKs inhibitor with IC50s of 30.6 nM and 12.8 nM for DYRK1B and DYRK1A, respectively. |
|
T63440 |
Dyrk1A-IN-2
|
|
|
|
Dyrk1A-IN-2 is a DYRK1A inhibitor (EC50: 37 nM). dyrk1A-IN-2 exhibits efficient promotion of human β-cell replication, as well as low cytotoxicity. |
|
T61739 |
Dyrk1A-IN-5
|
|
|
|
Dyrk1A-IN-5 (compound 5j) is a highly potent and selective inhibitor of DYRK1A, exhibiting an IC50 of 6 nM. It dose-dependently diminishes the phosphorylation of Thr434 in SF3B1, with an IC50 of 0.5 μM. Moreover, Dyrk1A-... |
|
T60824 |
Dyrk1A-IN-3
|
|
|
|
Dyrk1A-IN-3 (Compound 8b) is a highly selective inhibitor of dual-specificity tyrosine-regulated kinase 1A (DYRK1A). Dyrk1A-IN-3 has high binding affinity of DYRK1A with an IC 50 of 76 nM. Dyrk1A-IN-3 can be used in neur... |
|
T60867 |
Dyrk1A-IN-4
|
|
|
|
Dyrk1A-IN-4 (compound 48) is a potent and orally active DYRK1A and DYRK2 dual inhibitor with anticancer effects. The IC50 values of Dyrk1A-IN-4 for DYRK1A and DYRK2 are 2 nM and 6 nM, respectively [1]. |
|
T23186 |
ProINDY
|
Pro-indy |
DYRK
|
|
ProINDY (Pro-indy) is a potent DYRK inhibitor that activates NFAT for the study of Down syndrome. |
|
T36707 |
ML 315
|
|
DYRK
,
CDK
|
|
ML 315 is a selective Clk and DYRK inhibitor with potential anticancer activity for the study of neurological disorders. |
|
T15204 |
EHT 1610
|
EHT 5372 |
GSK-3
,
NF-κB
,
Tyrosinase
,
DYRK
,
CDK
|
|
EHT 1610 (EHT 5372) is a potent inhibitor of DYRK, with an IC50 of 0.36 nM and 0.59 nM for DYRK1A and DYRK1B, respectively. EHT 1610 has an inhibitory effect on leukemia, regulating cell cycle and inducing cell apoptosis... |
|
T76409 |
Woodtide
|
|
|
|
Woodtide, a substrate for the DYRK (DYRK) family of kinases, is designed based on the sequence surrounding the DYRK phosphorylation site in FKHR [1] [2]. |
|
T36689 |
KuWal151
|
|
|
|
Potent and selective CLK inhibitor (IC50 values are 28, 88 and 510 nM for CLK4, 1 and 2, respectively). Exhibits no significant activity at CLK3, DYRK, CDK or GSK3 at a concentration of 10 μM. Inhibits growth of a range ... |
|
T79562 |
Leucettinib-92
|
|
CDK
|
|
Leucettinib-92 (compound 92) is a kinase inhibitor selective for DYRK/CLK families, displaying IC50 values of 147 nM (CLK1), 39 nM (CLK2), 5.2 nM (CLK4), 0.8 μM (CLK3), 124 nM (DYRK1A), 204 nM (DYRK1B), 0.16 μM (DYRK2), ... |
