1. Protein Tyrosine Kinase/RTK Cell Cycle/DNA Damage Neuronal Signaling
  2. DYRK CDK Tau Protein
  3. DYRK2-IN-2 hydrochloride

DYRK2-IN-2 hydrochloride is a selective DYRK2 inhibitor with an IC50 of 40.3 nM. DYRK2-IN-2 hydrochloride shows weaker inhibitory activity against DYRK1A (IC50 = 1842 nM), DYRK1B (IC50 = 1335 nM), DYRK4 (IC50 = 1931 nM), DYRK3 (IC50 = 112 nM) and CLK (IC50 = 540-6496 nM). DYRK2-IN-2 hydrochloride inhibits the phosphorylation of Thr212 in Tau protein. DYRK2-IN-2 hydrochloride is applicable for neuronal research.

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DYRK2-IN-2 hydrochloride

DYRK2-IN-2 hydrochloride Chemical Structure

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Description

DYRK2-IN-2 hydrochloride is a selective DYRK2 inhibitor with an IC50 of 40.3 nM. DYRK2-IN-2 hydrochloride shows weaker inhibitory activity against DYRK1A (IC50 = 1842 nM), DYRK1B (IC50 = 1335 nM), DYRK4 (IC50 = 1931 nM), DYRK3 (IC50 = 112 nM) and CLK (IC50 = 540-6496 nM). DYRK2-IN-2 hydrochloride inhibits the phosphorylation of Thr212 in Tau protein. DYRK2-IN-2 hydrochloride is applicable for neuronal research[1].

IC50 & Target[1]

DYRK2

40.3 nM (IC50)

DYRK1A

1842 nM (IC50)

DYRK1B

1335 nM (IC50)

DYRK4

1931 nM (IC50)

DYRK3

112 nM (IC50)

CLK1

1128 nM (IC50)

CLK2

4290 nM (IC50)

CLK3

6496 nM (IC50)

CLK4

536.9 nM (IC50)

In Vitro

DYRK2-IN-3 (Compound C17) (up to 10 μM) hydrochloride potently and selectively inhibits recombinant DYRK2 with an IC50 of 0.0403 μM; it shows weak activity against other kinases of the DYRK and CLK families, and no activity against CDK5/p25, CK1ε or GSK3β[1].
DYRK2-IN-3 (1-30 μM; 6 h) hydrochloride potently and dose-dependently inhibits Thr212-Tau phosphorylation in SH-SY5Y cells expressing 4R-Tau[1].
DYRK2-IN-3 (48 h) hydrochloride exhibits cytotoxicity against HT22 cells, with an IC50 of 14.7 μM following 48 h of exposure[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: SH-SY5Y cells expressing human 4R-Tau
Concentration: 1-30 μM
Incubation Time: 6 h
Result: Efficiently and dose-dependently inhibited phosphorylation of Tau at the Thr212 site.
Induced a distinct second band in total Tau staining at the highest tested concentration.
Molecular Weight

420.95

Formula

C21H25ClN2O3S

Appearance

Solid

SMILES

COC1=CC2=C(SC[C@H]3CCNC3)C4=C(N=C2C=C1)C(CO)=CC(OC)=C4.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Purity & Documentation
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
DYRK2-IN-2 hydrochloride
Cat. No.:
HY-402805A
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