Salt-inducible Kinase (SIK) Inhibitor

Salt-inducible Kinase (SIK) Inhibitors (33):

Cat. No.	Product Name	Effect	Purity

HY-15776

HG-9-91-01	Inhibitor	99.77%
HG-9-91-01 is a potent and highly selective salt-inducible kinase (SIK) inhibitor with IC₅₀s of 0.92 nM, 6.6 nM and 9.6 nM for SIK1, SIK2 and SIK3 respectively.

HY-101147

YKL-05-099	Inhibitor	99.76%
YKL-05-099 is a salt-inducible kinase (SIK) inhibitor. YKL-05-099 binds to SIK1 and SIK3 with IC₅₀s of ~10 and ~30 nM, respectively. YKL-05-099 has slightly less potent SIK2-inhibitory (IC₅₀=40 nM).

HY-157442

GLPG3312	Inhibitor	98.63%
GLPG3312 (Compound 28) is an orally active SIK inhibitor with IC₅₀ values of 2.0 nM, 0.7 nM and 0.6 nM for SIK1, SIK2 and SIK3, respectively. GLPG3312 exhibits anti-inflammatory and immunomodulatory activity in vitro on human primary myeloid cells and in vivo in mouse models. GLPG3312 has good oral bioavailability and can be used for research on inflammatory and immune diseases.

HY-150203

GLPG3970	Inhibitor	99.70%
GLPG3970 (compound 88) is a first-in-class SIK2/SIK3 inhibitor. GLPG3970 can be used for the research of inflammation and autoimmune disease.

HY-120877

MRT199665	Inhibitor	99.85%
MRT199665 is a potent and ATP-competitive, selective MARK/SIK/AMPK inhibitor with IC₅₀s of 2/2/3/2 nM, 10/10 nM, and 110/12/43 nM for MARK1/MARK2/MARK3/MARK14, AMPKα1/AMPKα2, and SIK1/SIK2/SIK3, respectively. MRT199665 causes apoptosis in MEF2C-activated human acute myeloid leukemias (AML) cells. MRT199665 inhibits the phosphorylation of SIK substrate CRTC3 at S370.

HY-164534

SIK2/3-IN-2	Inhibitor
SIK2/3-IN-2 (compound 12, compound I-200) is a potent SIK2/3 inhibitor (SIK2 IC₅₀ = 65 nM, SIK3 IC₅₀ = 14 nM). SIK2/3-IN-2 is also a p21-activated protein kinase (PAK) 1 inhibitor with a K_i of 20.7 nM. SIK2/3-IN-2 can be used for hyperproliferative diseases and cancer research, such as Paclitaxel (HY-B0015)-resistant ovarian cancer.

HY-101149

YKL-05-093	Inhibitor
YKL-05-093 is a salt-induced kinase (SIK) inhibitor (SIK2: K_d = 7.1 nM). YKL-05-093 reduces the phosphorylation level of HDAC4/5/CRTC2, inhibits SOST expression, and stimulates RANKL expression in vitro and in vivo. YKL-05-093 can be used in research on bone diseases.

HY-182804

SIK2/3-IN-3	Inhibitor
SIK2/3-IN-3 (Example 15) is a potent, selective SIK2/3 inhibitor that exhibits preferential inhibitory activity against SIK2 (IC₅₀ = 10.3 nM) and SIK3 (IC₅₀ = 0.8 nM) over SIK1 (IC₅₀ = 801 nM). SIK2/3-IN-3 can be used for the study of inflammatory diseases.

HY-120856

ARN-3236	Inhibitor	99.66%
ARN-3236 is an oral active and selective inhibitor of salt-inducible kinase 2 (SIK2), with IC₅₀s of <1 nM, 21.63 nM and 6.63 nM for SIK2, SIK1 and SIK3, respectively. Has anti-cancer activity.

HY-129141

YKL-06-062	Inhibitor	99.44%
YKL-06-062 is a second-generation salt-inducible kinase (SIK) inhibitor with an IC₅₀ of 2.12 nM/1.40 nM/2.86 nM for SIK1, SIK2 and SIK3, respectively.

HY-120056

YKL-06-061	Inhibitor	99.82%
YKL-06-061 is a potent, selective, second-generation salt-inducible kinase (SIK) inhibitor with IC₅₀ values of 6.56 nM/1.77 nM/20.5 nM for SIK1/2/3, respectively.

HY-N1570

Pterosin B	Inhibitor	99.98%
Pterosin B is an orally active indanone. Pterosin B can be obtained from Pteridium aquilinum. Pterosin B is a Sik3 signaling inhibitor. Pterosin B inhibits Klf5 expression and reduces β-amyloid deposition. Pterosin B prevents chondrocyte hypertrophy and osteoarthritis in mice. Pterosin B inhibits cardiomyocyte hypertrophy, improves cognitive impairment, and lowers blood glucose. Pterosin B can be used in research on arthritis, Alzheimer's disease, pathological cardiac hypertrophy and diabetes.

HY-138001

WH-4-025	Inhibitor	99.31%
WH-4-025 is a Salt-inducible kinase (SIK) inhibitor (WO2016023014 A2).

HY-139253

MRIA9	Inhibitor	98.88%
MRIA9, a chemical probe, is an ATP-competitive, pan Salt-Inducible kinase (SIK) and PAK2/3 inhibitor, with IC₅₀ values of 516 nM, 180 nM and 127 nM for SIK1, SIK2 and SIK3, respectively.

HY-163743

SIC-19	Inhibitor	98.00%
SIC-19 is a SIK2 inhibitor and promotes SIK2 protein degradation via the ubiquitination pathway. SIC-19 inhibits cancer cell growth and sensitizes cells to PARP inhibitors (Such as Olaparib (HY-10162)), as well as in ovarian cancer organoids and xenograft models.

HY-159657

PF-07899895	Inhibitor	98.83%
PF-07899895 (Compound 34) is a SIK inhibitor, with IC₅₀ values of 1.2 nM, 0.9 nM, and 1.8 nM against SIK1, SIK2, and SIK3, respectively. PF-07899895 modulates the anti-inflammatory cytokine IL-10 in immune cells. PF-07899895 is applicable to research related to inflammatory diseases.

HY-175479

GLPG4970	Inhibitor	99.60%
GLPG4970 is a potent, selective and orally active salt-inducible kinase 2/3 (SIK2/SIK3) dual inhibitor with IC₅₀ values of 0.3 nM and 0.7 nM. GLPG4970 has weak inhibition of hERG channel with an IC₅₀ of 29 μM. GLPG4970 can decrease TNFα release and increase IL-10 release GLPG4970 can be used for the researches of inflammation and immunology, such as colitis.

HY-120877A

(R)-MRT199665	Inhibitor	98.70%
(R)-MRT199665 is an isomer of MRT199665 (HY-120877). MRT199665 is a potent and ATP-competitive, selective MARK/SIK/AMPK inhibitor with IC₅₀s of 2/2/3/2 nM, 10/10 nM, and 110/12/43 nM for MARK1/MARK2/MARK3/MARK14, AMPKα1/AMPKα2, and SIK1/SIK2/SIK3, respectively. MRT199665 causes apoptosis in MEF2C-activated human acute myeloid leukemias (AML) cells. MRT199665 inhibits the phosphorylation of SIK substrate CRTC3 at S370.

HY-RS12917

SIK3 Human Pre-designed siRNA Set A	Inhibitor
SIK3 Human Pre-designed siRNA Set A contains three designed siRNAs for SIK3 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

HY-173191

SK-124	Inhibitor
SK-124 is an orally active, selective SIK2/SIK3 inhibitor. SK-124 inhibits SIK2 and SIK3. SK-124 increases P1NP and CTX. SK-124 increases bone formation and bone mass.

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