Cyclin G-associated Kinase (GAK)

Auxilin 2

Cyclin G-associated kinase (GAK), also known as auxilin 2, is a cellular serine/threonine kinase. GAK was originally identified as an association partner of cyclin G and CDK5 (cyclin-dependent kinase 5). It is essential for clathrin trafficking, mediating binding of clathrin to the plasma membrane and the trans-Golgi network, and regulating receptor signalling by influencing trafficking downstream of clathrin-coated vesicles. GAK has been reported to phosphorylate the μ2 subunit of adaptor protein 1 and 2 (AP-1 and AP-2), thereby initiating a conformational change and enhancing their binding to sorting signals (in the form of tyrosineor dileucine-based motifs) within the cargo. In addition to its role in the cytoplasm, GAK has important functions in the nucleus. It is required for the maintenance of proper centrosome maturation and progression through mitosis. GAK plays a central role during development and GAK KO mice die early in gestation.

Cyclin G-associated Kinase (GAK) Related Products (26):

By Effects:	Inhibitors (14) Agonists (2) Degrader (1) Modulator (1)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-112486

TA-316		99.50%
TA-3166 (Megakaryocytes/platelets inducing agent) is a novel chemically synthesized c-MPL agonist (CMA) and thrombopoietin (TPO) receptor agonist. TA-316 enhances ex vivo platelet generation from human-induced pluripotent stem (iPS) cells.

HY-B0766

Bicyclol		99.91%
Bicyclol (SY801) is an orally active derivative of the traditional Chinese medicine Schisandra chinensis, which has antiviral, anti-inflammatory, immunomodulatory, antioxidant, anti-steatosis, anti-fibrotic and anti-tumor activities. Bicyclol regulates the expression of heat shock proteins and plays an anti-apoptosis role in hepatocytes. Bicyclol reduces the activation of NF-κB and the levels of inflammatory factors in hepatocytes infected with hepatitis C virus (HCV) by inhibiting the activation of the ROS-MAPK-NF-κB pathway, and prevents ferroptosis in acute liver injury. Bicyclol can change the expression of Mdr-1, GSH/GST and Bcl-2, increase the intracellular concentration of anticancer drugs, and sensitize drug-resistant cells to anticancer drugs. Bicyclol inhibits the proliferation of human malignant hepatoma cells by regulating the PI3K/AKT pathway and the Ras/Raf/MEK/ERK pathway. Bicyclol can be used in the study of chronic hepatitis, acute liver injury, nonalcoholic fatty liver disease, liver fibrosis and hepatocellular carcinoma.

HY-P990685

Romiplostim	Agonist	≥99.0%
Romiplostim is an Fc-peptide fusion protein mimetic of TPO (thrombopoietin protein) and also a c-Mpl agonist. Romiplostim binds to c-Mpl, stimulates megakaryocyte-mediated thrombopoiesis, and activates the same downstream signaling pathways as endogenous TPO. Romiplostim is applicable to research related to hematopoietic acute radiation syndrome and chronic immune thrombocytopenia.

HY-122186

SGC-GAK-1		99.92%
SGC-GAK-1 is a potent, selective cyclin G-associated kinase (GAK) inhibitor with a K_i of 3.1 nM. SGC-GAK-1 is a chemical probe for GAK.

HY-117626

LP-935509	Inhibitor	99.74%
LP-935509 is an orally active, potent, selective, ATP-competitive and brain-penetrant inhibitor of adaptor protein-2 associated kinase 1 (AAK1) with an IC₅₀ of 3.3 nM and a K_i of 0.9 nM, respectively. LP-935509 is also a potent inhibitor of BIKE (IC₅₀=14 nM) and a modest inhibitor of GAK (IC₅₀=320 nM). LP-935509 shows antinociceptive activity. LP-935509 can be used for neuropathic pain and SARS-CoV-2 research.

HY-171770

dAurAB5	Inhibitor	99.03%
dAurAB5 is a dual Aurora-A (DC₅₀ = 8.8 nM) and Aurora-B (DC₅₀ = 6.1 nM) PROTAC degrader. dAurAB5 induces degradation of Aurora-A and Aurora-B, reduces N-Myc levels, and decreases viability in IMR32 neuroblastoma cells. dAurAB5 downregulates the levels of AAK1, PTK2, GAK, and TTK. dAurAB5 can be used to study cancers such as neuroblastoma. (Pink: TTK ligand 2: HY-168542, Blue: Thalidomide-O-COOH: HY-103597, Black: 6-Aminocaproic acid: HY-B0236).

HY-101290A

BMT-090605 hydrochloride	Inhibitor	98.76%
BMT-090605 hydrochloride is a potent, selective the adapter protein-2 associated kinase 1 (AAK1) inhibitor with an IC₅₀ value of 0.6 nM. BMT-090605 hydrochloride shows antinociceptive activity. BMT-090605 hydrochloride inhibits BMP-2-inducible protein kinase (BIKE) and Cyclin G-associated kinase (GAK) with IC₅₀ values of 45 nM and 60 nM, respectively. BMT-090605 hydrochloride can be used for the research of neuropathic pain.

HY-148061

DB1113		99.86%
DB1113 (Example 24) is a bifunctional compound targeted protein degradation of kinases. DB1113 degrades 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. DB1113 can be used for research of disease or disorder mediated by aberrant kinase activity.

HY-148062

RSS0680		98.03%
RSS0680 is a small noncoding RNA (sRNA) targeting the mRNA ribosome binding site (RBS) and a PROTAC with protein kinase degradation activity (Pink: FLT3-IN-17 (HY-148070); Black: Linker (HY-W041970); Blue: E3 ligase Ligand (HY-112078)). RSS0680 competitively binds to RBS through the conserved CCUCCUCCC anti-Shine-Dalgarno (aSD) sequence and inhibits the translation initiation of target genes. RSS0680 can interact with the DUF1127 protein CcaF1, regulate its own stability and participate in bacterial oxidative stress defense, enhancing the host's resistance to heat shock and oxidative damage by affecting pathways such as C1 metabolism and pyruvate dehydrogenase complex. RSS0680 degrades AAK1, CDK1, CDK16, CDK2, CDK4, CDK6, EIF2AK4, GAK, LATSl, LIMK2, MAPK6, MAPKAPK5, MARK2, MARK4, MKNK2, NEK9, RPS6KB1, SIK2, SNRK, STK17A, STK17B, STK35, and WEEl. RSS0680 can be used to study diseases or disorders mediated by aberrant kinase activity and regulatory mechanisms of noncoding RNAs in α-proteobacteria[1][2].

HY-137342

SB1-G-187	Degrader	98.70%
SB1-G-187 is a multi-target kinase PROTAC degrader with activity against various kinases including GCK, YES1, IRAK1 and LYN. SB1-G-187 induces degradation of target kinases via a p97-dependent pathway, and forms ternary complexes with CRBN and specific functional kinases. SB1-G-187 can be used in tumor-related research. (Pink: multi-target kinase ligand (HY-125142); Blue: CRBN ligand (HY-A0003); Black: linker).

HY-N2128

Nigakinone		99.95%
Nigakinone is one of the most abundant alkaloids responsible for the major pharmacological activities of Kumu.

HY-112486G

TA-316 (GMP)	Agonist
TA-316 (GMP) is TA-316 (HY-112486) produced by using GMP guidelines. GMP grade small molecules can be used as auxiliary agents in cell therapy. TA-316 is a c-MPL agonist and a thrombopoietin (TPO) receptor agonist.

HY-18006

NKP608	Inhibitor	99.88%
NKP608 is a non-peptidic derivative of 4-aminopiperidine, a highly selective, orally active, neurokinin-1 (NK₁) receptor antagonist with IC₅₀ of 2.6 nM. NKP608 is active both in vitro and in vivo, showing extremely low affinity for NK₂, NK₃ receptors. NKP608 exerts its effects by blocking the NK₁ receptor, regulate cell proliferation and apoptosis, affect neurotransmitter functions and gastric mucosal repair mechanisms, and suppress the Wnt/β-catenin pathway in antitumor research. NKP608 is applicable to research related to various diseases, including cough, anxiety disorders, depression, gastric mucosal injury, and colorectal cancer.

HY-124793

GAK inhibitor 49		98.28%
GAK inhibitor 49 is a potent, ATP-competitive and highly selective cyclin G associated kinase (GAK) inhibitor with a K_i of 0.54 nM and a cell IC₅₀ of 56 nM. GAK inhibitor 49 also shows binding to RIPK2.

HY-114569

6-CEPN	Inhibitor	99.17%
6-CEPN is a RAS inhibitor. 6-CEPN can inhibit RAS activation by binding to Icmt binding sites. 6-CEPN has anticancer activity. 6-CEPN can block cancer cells in the G1 phase. 6-CEPN can induce autophagy and necrosis of Cancer cells (Icmt: isovalerylcysteine carboxymethyltransferase).

HY-124793A

GAK inhibitor 49 hydrochloride		99.52%
GAK inhibitor 49 hydrochloride is a potent, ATP-competitive and highly selective cyclin G associated kinase (GAK) inhibitor with a K_i of 0.54 nM and a cell IC₅₀ of 56 nM. GAK inhibitor 49 hydrochloride also shows binding to RIPK2.

HY-172394

ZSNI-21	Inhibitor
ZSNI-21 is a ADAM17/HDAC2 inhibitor with ADAM17 IC₅₀ 0.939 μM and HDAC2 IC₅₀ 0.844 μM. ZSNI-21 regulates the expression of apoptosis-related proteins (Bax, Bcl-2) and Cyclin D1, and induces apoptosis.. ZSNI-21 can be used for the research of hepatocellular carcinoma, breast cancer, and non-small cell lung cancer.

HY-114214

CKD-712	Inhibitor
CKD-712 is an orally active multi-target tetrahydroisoquinoline derivatived and a potent inhibitor of the NF-κB pathway. CKD-712 selectively inhibits MMP-9 with no effect on MMP-2, downregulates the expression of TNF-α, IL-6, cyclin A, cyclin B, CDK-1 and other proteins, and activates the PI3K/Akt signaling pathway. CKD-712 blocks the activation and nuclear translocation of NF-κB, downregulates inflammatory factors and pro-tumor metastatic proteins, and induces G2/M phase arrest in tumor cells and thereby inhibits the invasion of cancer cells. CKD-712 can be used for the research of sepsis, myocardial ischemia-reperfusion injury and non-small cell lung cancer.

HY-159174

EPHA2/A4/GAK-IN-1	Inhibitor
EPHA2/A4/GAK-IN-1 (compound 55) is a potent inhibitor of EPHA2/EPHA4 and GAK with K_D values of 180.5 nM for EPHA2 and 19.2 nM for GAK, respectively. EPHA2/GAK-IN-1 shows an extrapolated half-life time of 4.6 h in a microsomal stability assay. EPHA2/GAK-IN-1 shows antiviral activity and prevents dengue virus infection of Huh7 liver cells.

HY-101290

BMT-090605	Inhibitor	98.27%
BMT-090605 is a potent, selective the adapter protein-2 associated kinase 1 (AAK1) inhibitor with an IC₅₀ value of 0.6 nM. BMT-090605 shows antinociceptive activity. BMT-090605 inhibits BMP-2-inducible protein kinase (BIKE) and Cyclin G-associated kinase (GAK) with IC₅₀ values of 45 nM and 60 nM, respectively. BMT-090605 can be used for the research of neuropathic pain.

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