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PI3K/Akt/mTOR signalingSIK
Salt-inducible kinases (SIKs) belong to AMP-activated protein kinase (AMPK) family, and functions mainly involve in regulating energy response-related physiological processes, such as gluconeogenesis and lipid metabolism. The SIK family comprises three isoforms, namely, SIK1, SIK2, and SIK3, all of which may act as metabolic transmitters. SIKs have shown self-phosphorylation, and play an important role in regulating adrenocortical function under the stimulation of high salt or adreno-cortico-tropic-hormone (ACTH).
GLPG3970
T733842403733-82-2In house
GLPG3970 GLPG3970 is a novel orally available selective dual SIK2/SIK3 inhibitor.GLPG3970 has potential anti-inflammatory activity for the study of autoimmune diseases.
- $60
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GLPG3312
T865092340388-72-7
GLPG3312 is a selective and potent pan-SIK inhibitor with the advantage of oral activity, with IC50=0.6-2.0 nM for SIK1, SIK2 and SIK3, and exhibits anti-inflammatory and immunomodulatory activity in both human primary myeloid cells and mouse models.
- $158
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YKL-06-062
T172722172617-16-0In house
YKL-06-062 is a second-generation salt-inducible kinase (SIK) inhibitor that targets SIK1, SIK2, and SIK3, with IC50 values of 2.12 nM, 1.40 nM, and 2.86 nM, respectively.
- $93
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HG-9-91-01
Cited
T45991456858-58-4
HG-9-91-01 (SIK inhibitor 1) is a potent and highly selective salt-inducible kinase (SIKs) inhibitor with IC50s of 0.92 nM, 6.6 nM and 9.6 nM for SIK1, SIK2 and SIK3respectively.
- $76
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CitedRSS0680
T746432769753-48-0
RSS0680 is a protein kinase degrader that degrades a variety of kinases and can be used to study diseases caused by kinase abnormalities.
- $399
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YKL-06-061
T55762172617-15-9
YKL-06-061 is a selective salt-inducible kinase (SIK) inhibitor with IC50 values of 6.56 nM 1.77 nM 20.5 nM for SIK1 2 3, respectively.
- $30
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WH-4-025
T92191876463-35-2
WH-4-025 is a Salt-inducible kinase (SIK) inhibitor that targets the SIK family of proteins.
- $34
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YKL-05-099 Cited
T172711936529-65-5
YKL-05-099 is a salt-inducible kinase (SIK) inhibitor. It can inhibit the activity of SIK1 (IC50: 10 nM) and SIK3 (IC50: 30 nM), and has a slightly weaker inhibitory effect on SIK2 (IC50: 40 nM). [1]
- $68
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CitedMRT 67307 dihydrochloride
T369941781882-89-0In house
MRT 67307 dihydrochloride is a dual inhibitor of the IKKε and TBK-1 with IC50s of 160 and 19 nM, respectively. MRT67307 dihydrochloride also inhibits ULK1 and ULK2 with IC50s of 45 and 38 nM, respectively. MRT67307 dihydrochloride also blocks autophagy in cells.
- $52
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ARN-3236 Cited
T59931613710-01-2
ARN-3236 is an orally active and selective inhibitor of salt-inducible kinase 2 (SIK2), with IC50 values of <1 nM for SIK2, 21.63 nM for SIK1, and 6.63 nM for SIK3. ARN-3236 exhibits anti-cancer activity.
- $55
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CitedPterosin B
T1257634175-96-7
Pterosin B is a salt-inducible kinase 3 (Sik3) signaling inhibitor widely found in leaves and shoots of green plants.Pterosin B promotes the expression of G6pc, protects against Ang II-induced cardiomyocyte hypertrophy, and acts through the regulation of the expression level of NAD(P)H oxidase 2/4.
- $149
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Phanginin A
T730741011528-58-7In house
Phanginin A, a natural product discovered in Caesalpinia sappan Linn, activates SIK1 and inhibits gluconeogenesis in mouse primary hepatocytes. Phanginin A increases PDE4 activity and suppresses the hepatic cAMP/PKA/CREB pathway, improving metabolic disorders in ob/ob mice. It may be used in studies of type 2 diabetes.
- $1,400
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MRT199665
T161421456858-57-3In house
MRT199665 is an effective and ATP-competitive, selective MARK SIK AMPK inhibitor (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 suppresses the phosphorylation of S
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DB1113
T746422769753-53-7
DB1113 (Example 24) is a bifunctional compound designed for the targeted degradation of various kinases, including ABL1, ABL2, BLK, CDK11B, CDK4, CSK, EPHA3, FER, GAK, LIMK1, MAP3K20, MAP4K1, MAP4K2, MAP4K3, MAP4K5, MAPK14, MAPK7, MAPK8, MAPK9, MAPKAPK2, MAPKAPK3, NLK, PDIK1L, PTK2B, RIPK1, RPS6KA1, RPS6KA3, SIK2, SIK3, STK35, TNK2, and ULK1. This capability positions DB1113 as a valuable tool for research into diseases or disorders associated with aberrant kinase activity [1].
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MRIA9
T368912750707-05-0
MRIA9, an ATP-competitive inhibitor targeting pan Salt-Inducible Kinases (SIK) and PAK2 3, demonstrates IC50 values of 516 nM, 180 nM, and 127 nM for SIK1, SIK2, and SIK3, respectively [1].
- $598
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DB0614
T746442769753-47-9
DB0614 (Example 21) is a bifunctional compound designed for the targeted degradation of kinases, effectively breaking down AAK1, AURKA, BMP2K, CAMKK1, CDK16, CML, CDK6, EIF2AK2, FER, GAK, LCK, LIMK2, MAP3KH, MAPK8, MAPK9, NEK9, PLK4, PTK2B, SIK2, STK17A, STK17B, ULK1, ULK3, and WEE1. This compound has potential applications in research on diseases or disorders caused by aberrant kinase activity [1].
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SIK2-IN-3
T2077162810809-10-8
SIK2-IN-3 is an orally active selective inhibitor of SIK1/2 with IC50 values of 0.128/0.084 μM. It hinders the phosphorylation of CRTC3 and suppresses the production of pro-inflammatory factors in myeloid cells. Additionally, SIK2-IN-3 alleviates systemic and tissue inflammatory responses in a mouse anti-CD40 colitis model.
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SIC-19
T88487713112-69-7
SIC-19, a SIK2 inhibitor, functions by promoting the degradation of SIK2 protein via the ubiquitination pathway. It inhibits the growth of cancer cells and sensitizes cells, ovarian cancer organoids, and xenograft models to PARP inhibitors (such as Olaparib).
- $1,520
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SIK2/3-IN-1
T2066383038863-24-7
SIK2/3-IN-1 (Compound 7S) is an orally active and selective inhibitor of SIK2/3. It significantly inhibits tumor growth without causing weight loss in the MV4-11 AML mouse CDX model. SIK2/3-IN-1 is applicable for research in MEF2C-dependent acute myeloid leukemia.
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SIKs-IN-1
T787622927557-06-8
SIKs-IN-1 (compound 8h), a pyrimidine-5-carboxamide derivative, functions as an inhibitor of Salt-inducible kinases (SIKs), which play a role in M1 M2 macrophage polarization linked to inflammation. By inhibiting SIK activity, this compound increases anti-inflammatory cytokine IL-10 and decreases pro-inflammatory cytokine IL-12, demonstrating significant anti-inflammatory efficacy in a DSS-induced colitis model [1].
- $1,520
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