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GAK

" in MedChemExpress (MCE) Product Catalog:

36

Inhibitors & Agonists

1

Peptides

2

Recombinant Proteins

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Click Chemistry

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-122186
    SGC-GAK-1
    2 Publications Verification

    		 Cyclin G-associated Kinase (GAK) Cancer
    SGC-GAK-1 is a potent, selective cyclin G-associated kinase (GAK) inhibitor with a Ki of 3.1 nM. SGC-GAK-1 is a chemical probe for GAK .
    SGC-GAK-1
  • HY-117626
    LP-935509
    1 Publications Verification

    		 AAK1 Cyclin G-associated Kinase (GAK) SARS-CoV Infection Neurological Disease Inflammation/Immunology
    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 Ki 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 .
    LP-935509
  • HY-136848
    SM1-71

    		MAP3K Src FGFR Ribosomal S6 Kinase (RSK) LIM Kinase (LIMK) Cancer
    SM1-71 (compound 5) is a potent TAK1 inhibitor, with a Ki of 160 nM, it also can covalently inhibit MKNK2, MAP2K1/2/3/4/6/7, GAK, AAK1, BMP2K, MAP3K7, MAPKAPK5, GSK3A/B, MAPK1/3, SRC, YES1, FGFR1, ZAK (MLTK), MAP3K1, LIMK1 and RSK2. SM1-71 can inhibit proliferation of multiple cancer cell lines .
    SM1-71
  • HY-148065
    FMF-06-098-1

    		PROTACs Wee1 CDK AAK1 ULK MELK Itk IRAK Ephrin Receptor FGFR MAP4K p38 MAPK Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    FMF-06-098-1 is a multi-target kinase PROTAC degrader. FMF-06-098-1 can be used to target degradation kinases which degrades AAK1, AΒL2, AURKA, AURKB, BUBIB, CDC7, CDK1, CDK12, CDK13, CDK2, CDK4, CDk6, CDK7, CDK9, CHEK1, CSNKID, EPHA1, PER, FGFR1, GAK, IRAK4, ITK, LIMK2, MAP4K2, MAP4K3, MAPK6, MAPK7, MARK4, MELK, PKN3, PLK4, PRKAA1, PTK2, PTK6, RPS6KA4, S1K2, STK35, TNK2, UHMK1, ULK1, and WEE1 .
    FMF-06-098-1
  • HY-124793
    GAK inhibitor 49
    1 Publications Verification

    		 Cyclin G-associated Kinase (GAK) Infection
    GAK inhibitor 49 is a potent, ATP-competitive and highly selective cyclin G associated kinase (GAK) inhibitor with a Ki of 0.54 nM and a cell IC50 of 56 nM. GAK inhibitor 49 also shows binding to RIPK2 .
    GAK inhibitor 49
  • HY-153385
    TMX1

    		Molecular Glues Epigenetic Reader Domain Cancer
    TMX1 is a covalent, selective BRD4 molecular glue degrader. TMX1 binds to the JQ1-binding site of BRD4BD2, forms covalent bonds with Cys58 of DCAF16 and Cys87 of GAK in a BRD4BD2-dependent template-assisted manner, stabilizes the BRD4-TMX1-DCAF16 ternary complex, and promotes the ubiquitination of BRD4 via the CRL4DCAF16 ubiquitin ligase complex. TMX1 induces selective degradation of BRD4, mild degradation of BRD2 and BRD3, as well as DCAF16-dependent cytotoxicity .
    TMX1
  • HY-15800A
    CZC-25146

    		TNK1 LRRK2 Neurological Disease Inflammation/Immunology
    CZC-25146 is a potent and orally active LRRK2 inhibitor with IC50 values of 4.76 nM and 6.87 nM for wild-type LRRK2 and G2019S LRRK2, respectively. CZC-25146 inhibits PLK4, GAK, TNK1, CAMKK2 and PIP4K2C as well. CZC-25146 prevents mutant LRRK2-induced injury of neurons in vitro. CZC-25146 exhibits relatively favorable pharmacokinetic properties in mice. CZC-25146 can increase normal α-1-antitrypsin (AAT) secretion and reduce inflammatory cytokines. CZC-25146 can be used to research Parkinson's disease and liver diseases .
    CZC-25146
  • HY-148061
    DB1113

    		PROTACs Bcr-Abl CDK Salt-inducible Kinase (SIK) Cyclin G-associated Kinase (GAK) MAP4K MAPKAPK2 (MK2) Ferroptosis ULK LIM Kinase (LIMK) Cancer
    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 .
    DB1113
  • HY-135871
    BMT-124110

    		AAK1 Neurological Disease
    BMT-124110 is a potent, selective AAK1 inhibitor with an IC50 of 0.9 nM. BMT-124110 shows antinociceptive activity. BMT-090605 inhibits BMP-2-inducible protein kinase (BIKE) and Cyclin G-associated kinase (GAK) with IC50s of 17 and 99 nM, respectively .
    BMT-124110
  • HY-101290A
    BMT-090605 hydrochloride

    		Cyclin G-associated Kinase (GAK) AAK1 Neurological Disease
    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 .
    BMT-090605 hydrochloride
  • HY-120179
    LP-922761
    1 Publications Verification

    		 AAK1 Neurological Disease
    LP-922761 is a potent, selective and orally active adapter protein-2 associated kinase 1 (AAK1) inhibitor with IC50s of 4.8 nM and 7.6 nM in enzyme and cell assays, respectively. LP-922761 also inhibits BMP-2-inducible protein kinase (BIKE) with an IC50 of 24 nM. LP-922761 exhibits no significant activity at cyclin G-associated kinase (GAK), opioid, adrenergic α2 or GABAa receptors .
    LP-922761
  • HY-171770
    dAurAB5

    		PROTACs Aurora Kinase AAK1 Cyclin G-associated Kinase (GAK) Mps1 FAK Cancer
    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) .
    dAurAB5
  • HY-148062
    RSS0680

    		PROTACs CDK AAK1 Cyclin G-associated Kinase (GAK) Salt-inducible Kinase (SIK) LIM Kinase (LIMK) Wee1 SnRK Others
    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].
    RSS0680
  • HY-169789
    PKN3-IN-1

    		PI3K Metabolic Disease Cancer
    PKN3-IN-1 (compound 16) inhibits PKN3 (serine/threonine protein kinase 3) and GAK (cyclin G-associated kinase) with IC50 of 0.014 μM and Ki of 0.0044 μM respectively. PKN3-IN-1 is a potential tool compound to study the cell biology of PKN3 and its role in pancreatic and prostate cancer and T-cell acute lymphoblastic leukemia .
    PKN3-IN-1
  • HY-148063
    DB0614

    		PROTACs AAK1 Aurora Kinase CaMK CDK Ferroptosis Salt-inducible Kinase (SIK) LIM Kinase (LIMK) ULK Metabolic Disease
    DB0614 is a PROTAC based on Cereblon ligand, which is a selective and potent targeted protein degrader of NEK9 inhibitor. DB0614 can degrade 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. DB0614 can be used for research of disease or disorder mediated by aberrant kinase activity .(Blue: Thalidomide-4-OH (HY-103596), Black: linker, Pink: FLT3-IN-17 (HY-148070))
    DB0614
  • HY-124793A
    GAK inhibitor 49 hydrochloride
    1 Publications Verification

    		 Cyclin G-associated Kinase (GAK) Infection
    GAK inhibitor 49 hydrochloride is a potent, ATP-competitive and highly selective cyclin G associated kinase (GAK) inhibitor with a Ki of 0.54 nM and a cell IC50 of 56 nM. GAK inhibitor 49 hydrochloride also shows binding to RIPK2 .
    GAK inhibitor 49 hydrochloride
  • HY-179717
    WZS0347

    		PROTACs Microphthalmia Associated Transcription Factor (MITF) Cancer
    WZS0347 is a MITF PROTAC degrader. WZS0347 effectively reduces the MITF protein levels in several melanoma cell lines, including B16F10, A375, and GAK. WZS0347 significantly inhibits the proliferation, migration, and invasion of melanoma cells. WZS0347 can be used for research on melanoma (Pink: MITF ligand: (HY-179718); Blue: CRBN ligand: (HY-131717); Black: linker: (HY-22391)) .
    WZS0347
  • HY-101290
    BMT-090605

    		AAK1 Cyclin G-associated Kinase (GAK) Neurological Disease
    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 .
    BMT-090605
  • HY-147761
    GAK inhibitor 2

    		Antibiotic Flavivirus Dengue Virus Infection
    GAK inhibitor 2 (Compound 14g) is a potent cyclin G-associated kinase (GAK) inhibitor with an IC50 of 0.024 μM. GAK inhibitor 2 shows antiviral activity with an EC50 of 1.049 μM against dengue virus (DENV) .
    GAK inhibitor 2
  • HY-P4443
    Ac-GAK-AMC

    		Fluorescent Dye Others
    Ac-GAK-AMC is a fluorescent substrate that can be used to measure protease activity. AMC (7-amino-4-methylcoumarin) is a fluorescent group. In the presence of protease, the protease will hydrolyze Ac-GAK-AMC into a fluorescent product .
    Ac-GAK-AMC
  • HY-159174
    EPHA2/A4/GAK-IN-1

    		Ephrin Receptor Cyclin G-associated Kinase (GAK) Dengue Virus Infection
    EPHA2/A4/GAK-IN-1 (compound 55) is a potent inhibitor of EPHA2/EPHA4 and GAK with KD 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 .
    EPHA2/A4/GAK-IN-1
  • HY-15800
    CZC-25146 hydrochloride

    		TNK1 LRRK2 Neurological Disease Inflammation/Immunology
    CZC-25146 hydrochloride is a potent LRRK2 inhibitor with IC50 values of 4.76 nM and 6.87 nM for wild-type LRRK2 and G2019S LRRK2, respectively. CZC-25146 hydrochloride inhibits PLK4, GAK, TNK1, CAMKK2 and PIP4K2C as well. CZC-25146 hydrochloride prevents mutant LRRK2-induced injury of neurons in vitro. CZC-25146 hydrochloride exhibits relatively favorable pharmacokinetic properties in mice. CZC-25146 hydrochloride can increase normal α-1-antitrypsin (AAT) secretion and reduce inflammatory cytokines. CZC-25146 hydrochloride can be used to research Parkinson's disease and liver diseases .
    CZC-25146 hydrochloride
  • HY-RS05236
    Gak Mouse Pre-designed siRNA Set A

    		Small Interfering RNA (siRNA) Others

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

    Gak Mouse Pre-designed siRNA Set A
    Gak Mouse Pre-designed siRNA Set A
  • HY-RS05235
    GAK Human Pre-designed siRNA Set A

    		Small Interfering RNA (siRNA) Others

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

    GAK Human Pre-designed siRNA Set A
    GAK Human Pre-designed siRNA Set A
  • HY-RS05237
    Gak Rat Pre-designed siRNA Set A

    		Small Interfering RNA (siRNA) Others

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

    Gak Rat Pre-designed siRNA Set A
    Gak Rat Pre-designed siRNA Set A
  • HY-135871A
    BMT-124110 formic

    		AAK1 Neurological Disease
    BMT-124110 formic is a potent, selective AAK1 inhibitor, with an IC50 of 0.9 nM. BMT-124110 shows antinociceptive activity. BMT-124110 formic inhibits BMP-2-inducible protein kinase (BIKE) and Cyclin G-associated kinase (GAK) with IC50s of 17 and 99 nM, respectively .
    BMT-124110 formic
  • HY-181169
    GAK-IN-3

    		Cyclin G-associated Kinase (GAK) Cancer
    GAK-IN-3 is a cyclin G-associated kinase (GAK) inhibitor with an IC50 of 207 nM and a Ki of 66 nM. GAK-IN-3 inhibits kinase activity in the nanomolar range by binding to GAK’s ATP-binding site. GAK-IN-3 acts as a cytotoxic agent that reduces viability of Ewing sarcoma cells. GAK-IN-3 can be used for the research of ewing sarcoma .
    GAK-IN-3
  • HY-174213
    AAK1-IN-7

    		AAK1 Cyclin G-associated Kinase (GAK) Infection
    AAK1-IN-7 (Compound 16) is a dual AAK1/GAK inhibitor (EC50 values are 40 and 80 nM, respectively). AAK1-IN-7 inhibits the phosphorylation of AP2-µ2 subunit at T156. AAK1-IN-7 has weak antiviral activity against RNA viruses .
    AAK1-IN-7
  • HY-174214
    AAK1-IN-8

    		AAK1 Cyclin G-associated Kinase (GAK) Infection
    AAK1-IN-8 (Compound 18) is a pan-NAK inhibitor. AAK1-IN-8 inhibits AAK1 and GAK (EC50 values are 50 and 190 nM, respectively). AAK1-IN-8 inhibits the phosphorylation of AP2-µ2 subunit at T156 .
    AAK1-IN-8
  • HY-120179A
    LP-922761 hydrate

    		AAK1 Neurological Disease
    LP-922761 hydrate is a potent, selective and orally active adapter protein-2 associated kinase 1 (AAK1) inhibitor with IC50s of 4.8 nM and 7.6 nM in enzyme and cell assays, respectively. LP-922761 hydrate also inhibits BMP-2-inducible protein kinase (BIKE) with an IC50 of 24 nM. LP-922761 hydrate shows less activity at cyclin G-associated kinase (GAK), opioid, adrenergic α2 or GABAa receptors .
    LP-922761 hydrate
  • HY-150782
    UNC-CA359

    		EGFR Cancer
    UNC-CA359 is a potent epidermal growth factor receptor (EGFR) inhibitor, with an IC50 value of 18 nM. UNC-CA359 exhibits strong anti-tumor activity, can be used to Chordoma research . UNC-CA359 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    UNC-CA359
  • HY-183100
    UNC8461

    		PROTACs IKK Apoptosis Cancer
    UNC8461 is a PROTAC and is negative control CRBN-recruiting PROTAC analog of UNC8209 (HY-183098). UNC8461 features a methyl group substitution on its CRBN ligand to disrupt CRBN binding. UNC8461 fails to reduce TBK1, AAK1, GAK, and AURKA protein levels in renal cancer cells. UNC8461 does not suppress 3-D soft agar colony formation in renal cancer cells, and exerts modest, partial inhibition on colony formation in some renal cancer cells .
    UNC8461
  • HY-181293
    PROTAC AAK1 degrader-1

    		PROTACs AAK1 Cancer
    PROTAC AAK1 degrader-1 (compound 14) is a selective PROTAC AAK1 degrader with a DC50 of <10 nM. PROTAC AAK1 degrader-1 does not significantly impact the levels of any other NAK family members, including BMP2K, GAK, and STK16. PROTAC AAK1 degrader-1 can be used in ovarian cancer research .
    PROTAC AAK1 degrader-1
  • HY-101290AR
    BMT-090605 hydrochloride (Standard)

    		Cyclin G-associated Kinase (GAK) Reference Standards AAK1 Neurological Disease
    BMT-090605 (hydrochloride) (Standard) is the analytical standard of BMT-090605 (hydrochloride) (HY-101290A). This product is intended for research and analytical applications. 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 .
    BMT-090605 hydrochloride (Standard)
  • HY-125142
    AP-24567

    		Ligands for Target Protein for PROTAC Cancer
    AP-24567 is a Ligands for Target Protein for PROTAC, which can be used for the synthesis of SB1-G-187 (HY-137342) .
    AP-24567
  • HY-183098
    UNC8209

    		PROTACs IKK Apoptosis Cancer
    UNC8209 is a selective PROTAC-based TANK-binding kinase 1 (TBK1) degrader. UNC8209 recruits cereblon (CRBN) to mediate ubiquitin-proteasome pathway-dependent TBK1 degradation and reduces AAK1, GAK, and AURKA abundance. UNC8209 suppresses tumor cell proliferation, impairs in vivo tumor growth, inhibits colony and clonogenic growth and enhances tumor cell sensitivity to TNFα or IFN-γ. UNC8209 modulates cell cycle and induces mild apoptosis. UNC8209 can be used for the research of clear cell renal cell carcinoma, non-small cell lung cancer, pancreatic ductal adenocarcinoma .
    UNC8209

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