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Pathways Recommended: Protein Tyrosine Kinase/RTK
Results for "

degradable kinases

" in MedChemExpress (MCE) Product Catalog:

85

Inhibitors & Agonists

1

Peptides

2

Natural
Products

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-148066
    DB0662

    		Others Others
    DB0662 is a compound for kinase-targeted protein degradation and can be used in studies of diseases mediated by abnormal kinase activity, as well as for the identification of degradable kinases and optimal kinases .
    DB0662
  • HY-148062
    RSS0680

    		PROTACs CDK AAK1 Cyclin G-associated Kinase (GAK) Salt-inducible Kinase (SIK) LIM Kinase (LIMK) Wee1 Others
    RSS0680 (Example 22) is a bifunctional compound targeted protein degradation of kinases. 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 for research of disease or disorder mediated by aberrant kinase activity .
    RSS0680
  • HY-148061
    DB1113

    		PROTACs Bcr-Abl CDK Salt-inducible Kinase (SIK) Cyclin G-associated Kinase (GAK) MAP4K MAPKAPK2 (MK2) Ferroptosis ULK LIM Kinase (LIMK) Others
    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-146231A
    SS47 TFA

    		MAP4K PROTACs Inflammation/Immunology Cancer
    SS47 TFA, a PROTAC-based HPK1 degrader, exerts proteasome-mediated HPK1 degradation. The degradation of HPK1 via SS47 also significantly enhances the in vivo antitumor efficacy of BCMA CAR-T cell research. HPK1, an immunosuppressive regulatory kinase, is a promising target for cancer immunotherapies . SS47 (TFA) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    SS47 TFA
  • HY-111870
    PROTAC RIPK degrader-6

    		PROTACs RIP kinase Cancer
    PROTAC RIPK degrader-6 (example 1) is a Cereblon-based PROTAC targeting RIP Kinase degradation wherein the RIP2 kinase inhibitor is linked via a linker to a cereblon binder .
    PROTAC RIPK degrader-6
  • HY-112557
    PROTAC TBK1 degrader-2

    		PROTACs IKK Cancer
    PROTAC TBK1 degrader-2 is a Ligands for Target Protein for PROTAC. PROTAC TBK1 degrader-2 is a potent degrader based on the serine/threonine kinase TANK-binding kinase 1 (TBK1) (DC50=15 nM; Kd=4.6 nM) with a maximum efficiency of 96%. PROTAC TBK1 degrader-2 also targets to IkB kinase IKKε (IC50=8.7 nM), with low selectivity over TBK1 (IC50=1.3 nM) .
    PROTAC TBK1 degrader-2
  • HY-137343
    DB-0646

    		PROTACs Cancer
    DB-0646, a PROTAC, is a multi-kinase degrader .
    DB-0646
  • HY-157767
    Abd110

    		PROTACs ATM/ATR Cancer
    Abd110 (compound 42i) is a Lenalidomide-based PROTAC ATR kinase degrader. Abd110 selectively decreases ATR and phospho-ATR without affecting related kinases ATM and DNA-PKcs .
    Abd110
  • HY-148065
    FMF-06-098-1

    		PROTACs Cancer
    FMF-06-098-1 is a multitargeted depressant. 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-163295
    BTK degrader-1

    		ADC Cytotoxin Btk Cancer
    BTK degrader-1 (compound 1) is a Bruton’s tyrosine kinase (BTK) bifunctional degrader that can be conjugated with CD79b. BTK degrader-1 (compound 1) has anti-tumor effect .
    BTK degrader-1
  • HY-155582
    BLK degrader 1

    		Others Cancer
    BLK degrader 1 (compound 9) is a selective degrader of B-lymphoid tyrosine kinase (BLK). BLK degrader 1 shows anticancer activity in several B-lymphoid cell lines .
    BLK degrader 1
  • HY-168057
    PROTAC CDK2 Degrader-1

    		PROTACs CDK Cancer
    PROTAC CDK2 Degrader-1 (Compound 41) is a PROTAC degrader for cyclin-dependent kinase 2 (CDK2). PROTAC CDK2 Degrader-1 inhibits the phosphorylation of RB protein in CDK2 dependent cell line OVCAR3 with an IC50 of 100-500 nM .
    PROTAC CDK2 Degrader-1
  • HY-139315
    PROTAC IRAK4 degrader-4

    		PROTACs IRAK Cancer
    PROTAC IRAK4 degrader-4 is a Cereblon-based PROTAC as interleukin-1 receptor-associated kinase 4 (IRAK4) degrader extracted from patent US20190192668A1, compound I-127 .
    PROTAC IRAK4 degrader-4
  • HY-139317
    PROTAC IRAK4 degrader-6

    		PROTACs IRAK Cancer
    PROTAC IRAK4 degrader-6 is a Cereblon-based PROTAC as interleukin-1 receptor-associated kinase 4 (IRAK4) degrader extracted from patent US20190192668A1, compound I-172 .
    PROTAC IRAK4 degrader-6
  • HY-143905
    PROTAC TTK degrader-2

    		PROTACs Cancer
    PROTAC TTK degrader-2 is a potent TTK (threonine tyrosine kinase) PROTAC degrader, with DC50 values of 3.1 and 12.4 nM in COLO-205 and HCT-116 cell, respectively. PROTAC TTK degrader-2 exhibits target degradation and anticancer efficacy in a xenograft mouse model of COLO-205 human colorectal cancer cells .
    PROTAC TTK degrader-2
  • HY-143904
    PROTAC TTK degrader-1

    		PROTACs Cancer
    PROTAC TTK degrader-1 is a potent TTK (threonine tyrosine kinase) PROTAC degrader, with DC50 values of 1.7 and 5.8 nM in COLO-205 and HCT-116 cell, respectively. PROTAC TTK degrader-1 exhibits target degradation and anticancer efficacy in a xenograft mouse model of COLO-205 human colorectal cancer cells .
    PROTAC TTK degrader-1
  • HY-161633
    PROTAC EGFR degrader 11

    		PROTACs EGFR FAK Cancer
    PROTAC EGFR degrader 11 (Compound B71) is a PROTAC degrader for epidermal growth factor receptor (EGFR), with DC50 <100 nM. PROTAC EGFR degrader 11 binds CRBN-DDB1 with a Ki of 36 nM. PROTAC EGFR degrader 11 degrades EGFR, focal adhesion kinase (FAK), and RSK1, inhibits the proliferation of BaF3 wild type and EGFR mutants, with IC50 <100 nM.
    PROTAC EGFR degrader 11
  • HY-161632
    PROTAC EGFR degrader 10

    		PROTACs EGFR FAK Cancer
    PROTAC EGFR degrader 10 (Compound B56) is a PROTAC degrader for epidermal growth factor receptor (EGFR), with DC50 <100 nM. PROTAC EGFR degrader 10 binds CRBN-DDB1 with a Ki of 37 nM. PROTAC EGFR degrader 10 degrades EGFR, focal adhesion kinase (FAK), and RSK1, inhibits the proliferation of BaF3 wild type and EGFR mutants, with IC50 <150 nM .
    PROTAC EGFR degrader 10
  • HY-136010
    RIP2 Kinase Inhibitor 4

    		RIP kinase PROTACs Inflammation/Immunology
    RIP2 Kinase Inhibitor 4 is a potent and selective RIPK2 PROTAC. RIP2 Kinase Inhibitor 4 effectively degrades RIPK2 (pIC50 of 8) and inhibits the release of related TNF-α .
    RIP2 Kinase Inhibitor 4
  • HY-161709
    FLT3/CDKs ligand-1

    		Ligands for Target Protein for PROTAC FLT3 CDK Cancer
    FLT3/CDKs ligand-1 (Compound 14) is a ligand for target protein, which promotes the degradation of cyclin-dependent kinase (CDK) and the FMS-like tyrosine kinase 3 (FLT3), inhibits FLT3/CDK related proliferations and survivals of leukemia cells. LT3/CDKs ligand-1 can be used for synthesis of PROTAC FLT3/CDKs degrader-1 (HY-161708) .
    FLT3/CDKs ligand-1
  • HY-111866
    PROTAC RIPK degrader-2

    		PROTACs RIP kinase Metabolic Disease Cancer
    PROTAC RIPK degraders -2 is a non-peptide PROTAC based on von Hippel-Lindau and targets serine-threonine kinase RIPK2, which is highly selective to the degradation of RIPK2. PROTAC RIPK degrader-2 acts as an activator to increase cell death and activate ion channels in cancer cells. PROTAC RIPK degrader-2 also can inhibit protein interactions, such as receptors and ligands, involved in a variety of diseases, such as cancer and diabetes .
    PROTAC RIPK degrader-2
  • HY-112156
    MS4077

    		PROTACs Anaplastic lymphoma kinase (ALK) Cancer
    MS4077 is an anaplastic lymphoma kinase (ALK) PROTAC (degrader) based on Cereblon ligand, with a Kd of 37?nM for binding affinity to ALK .
    MS4077
  • HY-112155
    MS4078
    2 Publications Verification

    		 PROTACs Anaplastic lymphoma kinase (ALK) Cancer
    MS4078 is an anaplastic lymphoma kinase (ALK) PROTAC (degrader) based on Cereblon ligand, with a Kd of 19?nM for binding affinity to ALK .
    MS4078
  • HY-143882
    MS5033

    		PROTACs Akt Cancer
    MS5033 is a potent PROTAC-based AKT (protein kinase B) degrader, with a DC50 of 430 nM in PC3 cells .
    MS5033
  • HY-151110
    PROTAC CDK12/13 Degrader-1

    		PROTACs CDK Cancer
    PROTAC CDK12/13 Degrader-1 (7f) is a highly selective cell cycle protein-dependent kinase CDK12/CDK13 dual degrader with the DC50 values of 2.2 nM and 2.1 nM, respectively. PROTAC CDK12/13 Degrader-1 has anti-proliferative activity and can be used in breast cancer research .
    PROTAC CDK12/13 Degrader-1
  • HY-137488
    PROTAC BRAF-V600E degrader-2

    		PROTACs Raf Cancer
    PROTAC BRAF-V600E degrader-2 (compound 12) is a potent BRAF-V600E degrader with Kds of 14.4 nM and 9.5 nM for BRAF and BRAF-V600E, respectively. PROTAC BRAF-V600E degrader-2 selectively degraded the kinase domain of BRAF-V600E but not the wild-type BRAF. PROTAC BRAF-V600E degrader-2 inhibits melanoma cell growth .
    PROTAC BRAF-V600E degrader-2
  • HY-151110A
    PROTAC CDK12/13 Degrader-1 TFA

    		PROTACs CDK Cancer
    PROTAC CDK12/13 Degrader-1 (7f) TFA is a highly selective cell cycle protein-dependent kinase CDK12/CDK13 dual degrader with the DC50 values of 2.2 nM and 2.1 nM, respectively. PROTAC CDK12/13 Degrader-1 TFA has anti-proliferative activity and can be used in breast cancer research .
    PROTAC CDK12/13 Degrader-1 TFA
  • HY-161708
    PROTAC FLT3/CDKs degrader-1

    		PROTACs CDK FLT3 Cancer
    PROTAC FLT3/CDKs degrader-1 (Compound C3) is a degrader for cyclin-dependent kinases (DC50 is 18.73 nM for CDK2) and the FMS-like tyrosine kinase 3 (FLT3). PROTAC FLT3/CDKs degrader-1 induces differentation of HL-60 (72.77% differentation at 6.25 nM), inhibits proliferation of AML cells, with IC50s of 2.9-37 nM. PROTAC FLT3/CDKs degrader-1 is potential for ameliorating acute myeloid leukemia. (Pink: ligand for target protein FLT3/CDKs ligand-1 (HY-161709); Black: linker (HY-W012935); Black: ligand for E3 ligase Thalidomide 5-fluoride (HY-W087383))
    PROTAC FLT3/CDKs degrader-1
  • HY-149917
    ITK degrader 1

    		PROTACs Itk Cancer
    ITK degrader 1 is a highly selective degrader of interleukin-2-inducible T-cell kinase (ITK; DC50=3.6 nM in vivo in mice). ITK degrader 1 induces rapid, and prolonged ITK degradation and suppresses IL-2 secretion (EC50=35.2 nM, Jurkat cells) stimulated by anti-CD3 antibodyin vivo. ITK degrader 1 also shows good plasma exposure levels .
    ITK degrader 1
  • HY-163814
    CDK2 degrader 1

    		PROTACs CDK Cancer
    CDK2 degrader 1 (Compound 3) is an orally active cyclin-dependent kinase 2 (CDK2) degrader based on PROTAC technology. CDK2 degrader 1 binds to cereblon to induce ubiquitination and subsequent proteasomal degradation of the CDK2. CDK2 degrader 1 is used in the research of a wide range of cancers (Red: spiro[3.3]heptan-2- ylmethyl carbonochloridate; Blue: N,N-diisopropylethylamine; Black: linker) .
    CDK2 degrader 1
  • HY-129966
    PROTAC IRAK4 degrader-1
    1 Publications Verification

    		 PROTACs IRAK Cancer
    PROTAC IRAK4 degrader-1 is a Cereblon-based PROTAC interleukin-1 receptor-associated kinase 4 (IRAK4) degrader extracted from patent US20190192668A1 Compound I-210, makes <20%, >20-50%, and >50% IRAK4 degradation at 0.01, 0.1, and 1 μM in OCI-LY-10 cells, respectively .
    PROTAC IRAK4 degrader-1
  • HY-137341
    SK-3-91

    		PROTACs Cancer
    SK-3-91 is a PROTAC-type multi-kinase degrader that can jointly induce the degradation of the largest number of unique kinases (more than 125 unique kinases) . SK-3-91 induces protein degradation through the ubiquitin biotinylation (E-STUB) pathway and consists of the target protein ligand (red part) TAE648 (HY-169396), the E3 ubiquitin ligase ligand (blue part) Thalidomide-NH-CH2-COOH (HY-131717) and the PROTAC linker (Bromo-PEG1-C2-azide) (HY-140819). The E3 ligase ligand and linker can form a conjugate (HY-169397).
    SK-3-91
  • HY-169072
    PROTAC MLKL Degrader-2

    		PROTACs Mixed Lineage Kinase Cancer
    PROTAC MLKL Degrader-2 (compound MP-1) is a PROTAC targeting MLKL (Mixed Lineage Kinase). PROTAC MLKL Degrader-2 is composed of PROTAC target protein ligand PROTAC MLKL Degrader-2 (HY-169072) (red part), E3 ligase ligand Thalidomide (HY-14658) (blue part) and PROTAC Linker N-Methylpiperazine (HY-78871) (black part), among which the conjugate of E3 ubiquitin ligase ligand + Linker is Thalidomide-N-methylpiperazine (HY-169074) [1] .
    PROTAC MLKL Degrader-2
  • HY-129967
    PROTAC IRAK4 ligand-1

    		Ligands for Target Protein for PROTAC Cancer
    PROTAC IRAK4 ligand-1 is a synthetic ligand for interleukin-1 receptor-associated kinase 4 (IRAK4). PROTAC IRAK4 ligand-1 can be used in the synthesis of PROTAC IRAK4 degrader-1 (HY-129966) .
    PROTAC IRAK4 ligand-1
  • HY-137340
    WH-10417-099

    		PROTACs Cancer
    WH-10417-099 is a CRBN-type PROTAC multi-kinase degrader that can jointly induce the degradation of the largest number of unique kinases (more than 125 unique kinases). WH-10417-099 induces protein degradation through the ubiquitin biotinylation (E-STUB) pathway and consists of the target protein ligand (red part) PI3Kγ ligand 1 (HY-168319), the E3 ubiquitin ligase ligand (blue part) Thalidomide 4-fluoride (HY-41547) and the PROTAC linker (black part) Amino-PEG5-C2-acid (HY-115384). The E3 ligase ligand and linker can form a conjugate Pomalidomide 4'-PEG5-acid (HY-131647).
    WH-10417-099
  • HY-112273
    CD532

    		Aurora Kinase Cancer
    CD532 is a potent Aurora A kinase inhibitor with an IC50 of 45 nM. CD532 has the dual effect of blocking Aurora A kinase activity and driving degradation of MYCN. CD532 also can directly interact with AURKA and induces a global conformational shift. CD532 can be used for the research of cancer .
    CD532
  • HY-112273A
    CD532 hydrochloride

    		Aurora Kinase Cancer
    CD532 hydrochloride is a potent Aurora A kinase inhibitor with an IC50 of 45 nM. CD532 hydrochloride has the dual effect of blocking Aurora A kinase activity and driving degradation of MYCN. CD532 hydrochloride also can directly interact with AURKA and induces a global conformational shift. CD532 hydrochloride can be used for the research of cancer .
    CD532 hydrochloride
  • HY-143275
    HL-8

    		PI3K Cancer
    HL-8 is a PROTAC molecule targeting PI3K kinase. HL-8 has a significant and complete degradation effect on PI3K kinase at a concentration of 10 μM within 8 h. HL-8 has the potential for the research of cancer diseases .
    HL-8
  • HY-130665
    TL12-186
    1 Publications Verification

    		 PROTACs CDK Cancer
    TL12-186 is a Cereblon-dependent multi-kinase PROTAC degrader. Multi-kinases include CDK, BTK, FLT3, Aurora kinases, TEC, ULK, ITK, et al. TL12-186 inhibits CDK2/cyclin A (IC50=73 nM) and CDK9/cyclin T1 (IC50=55 nM) .
    TL12-186
  • HY-P10438
    Tat-braftide

    		Raf Cancer
    Tat-braftide is a peptide inhibitor designed to block the dimerization of BRAF, thereby inhibiting its kinase activity. The destruction of BRAF dimer by Tat-braftide makes BRAF protein more susceptible to proteasome degradation, directly inhibits the activity of BRAF kinase, and reduces the activation of MAPK signaling pathway. Tat-braftide can be used for the role of RAF kinase in MAPK signaling pathway and for the study of BRAF mutant cancers .
    Tat-braftide
  • HY-145320
    TMX-4113

    		Molecular Glues Phosphodiesterase (PDE) Casein Kinase Cancer
    TMX-4113 is a degrader of phosphodiesterase 6D (PDE6D) and casein kinase 1α (CK1α). TMX-4113 can be used for the research of cancer .
    TMX-4113
  • HY-145322
    TMX-4116

    		Casein Kinase Molecular Glues Cancer
    TMX-4116 is a casein kinase 1α (CK1α) degrader. TMX-4116 shows the degradation preference for CK1α with DC50s less than 200 nM in MOLT4, Jurkat, and MM.1S cells. TMX-4116 can be used for the research of multiple myeloma .
    TMX-4116
  • HY-163144
    DAS-5-oCRBN

    		PROTACs Src Cancer
    DAS-5-oCRBN is a selective and potent PROTAC degrader of c-Src kinase. DAS-5-oCRBN has antiproliferative activity in both c-Src-dependent cell lines .
    DAS-5-oCRBN
  • HY-132296
    GSK215

    		FAK PROTACs Cancer
    GSK215 is a potent and selective PROTAC focal adhesion kinase (FAK) degrader with a pDC50 of 8.4. GSK215 is designed by a binder for the VHL E3 ligase and the FAK inhibitor VS-4718. GSK215 induces rapid and prolonged FAK degradation, giving a long-lasting effect on FAK levels and a marked pharmacokinetic/pharmacodynamics (PK/PD) disconnect .
    GSK215
  • HY-130770
    Ald-CH2-PEG3-CH2-Boc

    		PROTAC Linkers Cancer
    Ald-CH2-PEG3-CH2-Boc is a PEG- and Alkyl/ether-based PROTAC linker can be used in the synthesis of SGK3 kinase PROTAC degrader .
    Ald-CH2-PEG3-CH2-Boc
  • HY-100932
    ML-9
    4 Publications Verification

    		 Myosin Cancer
    ML-9 is a selective and potent inhibitor of Akt kinase, inhibits myosin light-chain kinase (MLCK) and stromal interaction molecule 1 (STIM1) activity . ML-9 inhibits inhibits MLCK, PKA and PKC activity with Ki values of 4, 32 and 54?μM, respectively . ML-9 induces autophagy by stimulating autophagosome formation and inhibiting their degradation .
    ML-9
  • HY-141796
    MS67

    		Histone Methyltransferase PROTACs Cancer
    MS67 is a potent and selective WD40 repeat domain protein 5 (WDR5) degrader with a Kd of 63 nM. MS67 is inactive against other protein methyltransferases, kinases, GPCRs, ion channels, and transporters. MS67 shows potent acticancer effects .
    MS67
  • HY-137677B
    GTPγS tetralithium

    Guanosine 5'-[γ-thio]triphosphate tetralithium

    		 GLUT Others
    GTPγS (tetralithium) (Guanosine 5'-[γ-thio]triphosphate (tetralithium)) is a G-protein activator that protects proteins from proteolytic degradation, stimulates GLUT4 translocation in a tyrosine kinase-dependent manner, stimulate phospholipases and induce actin polymerization. GTPγS (tetralithium) to couple with G- protein α, to study its effect on kinase activity. GTPγS (tetralithium) acts as a component of lysis buffer .
    GTPγS tetralithium
  • HY-164487
    JBJ-08-178-01

    		EGFR Cancer
    JBJ-08-178-01 is a mutant-selective tyrosine kinase inhibitor against human epidermal growth factor receptor 2 (HER2) with an antitumoral activity. JBJ-08-178-01 reduces both the kinase activity and protein levels of HER2 by inducing proteasomal degradation of the receptor in lung cancer. JBJ-08-178-01 is promising for research of non-small-cell lung cancer .
    JBJ-08-178-01
  • HY-123919
    TL13-112
    1 Publications Verification

    		 PROTACs Anaplastic lymphoma kinase (ALK) Cancer
    TL13-112 is a potent and selective ALK-PROTAC degrader and inhibits ALK activity with an IC50 value of 0.14 nM. TL13-112 also prompts the degradation of additional kinases including Aurora A, FER, PTK2 and RPS6KA1 with IC50 values of 8550 nM, 42.4 nM, 25.4 nM, and 677 nM, respectively. TL13-112 is comprised of the conjugation of Ceritinib?(HY-15656) and the Cereblon ligand of Pomalidomide (HY-10984) .
    TL13-112

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