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Kinase selectivity profile

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19

Inhibitors & Agonists

1

Screening Libraries

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-122051
    AC1903
    1 Publications Verification

    		 TRP Channel Metabolic Disease
    AC1903 is a specific and selective inhibitor of TRPC5 and has podocyte-protective properties. AC1903 does no effects on TRPC4 or TRPC6 currents and shows no off-target effects in kinase profiling assays. AC1903 suppresses severe proteinuria and prevents podocyte loss in focal segmental glomerulosclerosis (FSGS) rat model .
    AC1903
  • HY-112613
    UCB9608
    1 Publications Verification

    		 PI4K Inflammation/Immunology
    UCB9608 is a potent, selective and orally active PI4KIIIβ inhibitor, with an IC50 of 11 nM, selective over PI3KC2 α, β, and γ lipid kinases. UCB9608 improves metabolic stability and exhibits excellent pharmacokinetic profile, acts as a potent immunosuppressive agent .
    UCB9608
  • HY-14362
    GSK-25

    		ROCK Ribosomal S6 Kinase (RSK) Cardiovascular Disease
    GSK-25 is a potent, selective and orally bioavailable ROCK1 inhibitor (IC50=7 nM). GSK-25 maintains good selectivity against a panel of 31 kinases (>100 fold), as well as RSK1 and p70S6K (RSK1: IC50=398 nM, p70S6K: IC50=1 μM). GSK-25 inhibits P450 profile (IC50s of 2.5, 5.2, 2.5 µM for CYP2C9, CYP2D6, CYP3A4, respectively) .
    GSK-25
  • HY-103266
    TC-A 2317 hydrochloride

    		Aurora Kinase Cancer
    TC-A 2317 hydrochloride is an orally active Aurora A kinase inhibitor (Ki=1.2 nM). TC-A 2317 hydrochloride exhibits excellent selectivity to Aurora B kinase (Ki=101 nM) and other 60 kinases, good cell permeability and good PK profile. Antitumor activity .
    TC-A 2317 hydrochloride
  • HY-131335
    p38α inhibitor 2

    		p38 MAPK Inflammation/Immunology
    p38α inhibitor 2 is a highly potent and selective p38α MAPK inhibitor, with a pIC50 of 9.6. p38α inhibitor 2 inhibits the hERG ion channel (IC50=27 μM) and shows a promising selectivity profile when tested in a panel of 51 other protein kinases (<30% inhibition at 10 μM concentration) and a panel of 141 other biological targets .
    p38α inhibitor 2
  • HY-178980
    APL-5125

    		Casein Kinase Cancer
    APL-5125 (Compound 61f) is a potent, selective and orally active ATP-competitive CK2α inhibitor with an IC50 of 0.348 nM and a Ki of 0.095 nM. APL-5125 binds to CK2α in a bivalent manner, simultaneously interacting with the ATP-binding site and the αD pocket. APL-5125 exhibits antitumor activity and can be used for the research of cancer, such as colon cancer .
    APL-5125
  • HY-146697
    IHMT-TRK-284

    		Trk Receptor c-Fms PDGFR Bcr-Abl c-Kit Apoptosis Cancer
    IHMT-TRK-284 (Compound 34) is a potent, orally active type II TRK kinase inhibitor with IC50 values of 10.5, 0.7, and 2.6 nM to TRKA, B, and C respectively. IHMT-TRK-284 displays great selectivity profile in the kinome and good in vivo antitumor efficacies .
    IHMT-TRK-284
  • HY-150537
    AChE/GSK-3β-IN-1

    		Cholinesterase (ChE) GSK-3 Microtubule/Tubulin ROS Kinase Neurological Disease
    AChE/GSK-3β-IN-1 (compound GT15) is a potent, dual AChE/GSK-3β inhibitor with IC50 values of 1.2, 149.8 and 22.4 nM for hAChE , hBChE and hGSK-3β, respectively. AChE/GSK-3β-IN-1 penetrates the blood-brain barrier (BBB). AChE/GSK-3β-IN-1 has high kinase selectivity profiles for the CMGC kinase family. AChE/GSK-3β-IN-1 occupies the ATP binding site of DYRK1A. AChE/GSK-3β-IN-1 inhibits ROS expression and reduces oxidative stress. AChE/GSK-3β-IN-1 can be used for Alzheimer’s disease research .
    AChE/GSK-3β-IN-1
  • HY-155804
    RIP1 kinase inhibitor 8

    		Necroptosis RIP kinase Inflammation/Immunology
    RIP1 kinase inhibitor 8 (Compound 77) is a potent and highly selective dihydropyrazole (DHP) RIP1 kinase inhibitor with an IC50 of 20 nM. RIP1 kinase inhibitor 8 prevents necrotic cell death. RIP1 kinase inhibitor 8 shows a favorable pharmacokinetic profile in multiple species .
    RIP1 kinase inhibitor 8
  • HY-156793
    hRIO2 kinase ligand-1

    		PKC Others
    hRIO2 kinase ligand-1 (compound 9) is a ligand of hRIO2 kinase, with a Kd value of 520 nM .
    hRIO2 kinase ligand-1
  • HY-164041
    Staurosporine-Boc

    		PKC Others
    Staurosporine-Boc, a natural product isolated from the actinomyces Streptomyces staurosporeus, is a potent non-selective inhibitor of protein kinase. Staurosporine-Boc inhibits a variety of protein kinases, including protein kinase C (PKC), tyrosine kinase, and serine/threonine kinase. Because of its broad inhibition profile, Staurosporine-Boc is widely used as a tool compound in biological research, especially when studying cell signaling pathways .
    Staurosporine-Boc
  • HY-149099
    RET-IN-22

    		RET Cancer
    RET-IN-22 (compound 17b) is a potent, selective and orally active RET inhibitor with an IC50 of 20.9 nM and 18.3 nM for wild-type RET and RET-V804M, respectively. RET-IN-22 shows highly selective profile to most kinases, especially to EGFR and VEGFR2. RET-IN-22 has anticancer effects .
    RET-IN-22
  • HY-16636
    ML337

    		mGluR Neurological Disease
    ML337 is a selective and brain-penetrant negative allosteric modulator of mGlu3, with an IC50 of 593 nM. ML337 possesses a favorable dystrophia myotonica protein kinase (DMPK) and ancillary pharmacology profile . ML337 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    ML337
  • HY-151156
    EGFR/HER2-IN-6

    		EGFR Apoptosis Cancer
    EGFR/HER2-IN-6 (compound 43) is an EGFR/HER2 and DHFR inhibitor. EGFR/HER2-IN-6 inhibits EGFR kinase, HER2 kinase and DHFR with IC50s of 0.122, 0.078 and 0.585 μM, respectively. EGFR/HER2-IN-6 shows anticancer activity against several cancer cell lines with high safety profile and selectivity indices. EGFR/HER2-IN-8 can be used for the research of cancer .
    EGFR/HER2-IN-6
  • HY-151161
    EGFR/HER2-IN-8

    		EGFR Cancer
    EGFR/HER2-IN-8 (compound 34) is a EGFR/HER2 and DHFR inhibitor. EGFR/HER2-IN-8 inhibits EGFR kinase, HER2 kinase and DHFR with IC50s of 0.45, 0.244 and 5.669 μM, respectively. EGFR/HER2-IN-8 shows anticancer activity against several cancer cell lines with high safety profile and selectivity indices. EGFR/HER2-IN-8 can be used for the research of cancer .
    EGFR/HER2-IN-8
  • HY-170958
    Scr-IN-1

    		Src Apoptosis Cancer
    Scr-IN-1 (Compound 4e) is a Tyrosine kinase inhibitor. Scr-IN-1 inhibits HCT-116 cells and MIA-PaCa-2 cells with IC50s of 0.16 μM and 1.16 μM, respectively. Scr-IN-1 displays selectivity profile on HCT-116 cells and MIA-PaCa-2 cells with SI > 625 and SI > 86, respectively. Scr-IN-1 induces Apoptosis in HCT-116 colon cancer cell and does not cause any change in the rate of necrotic cells. Scr-IN-1 is a novel SRC kinase inhibitor candidate for HCT-116 cells. Scr-IN-1 is potential for cancer research .
    Scr-IN-1
  • HY-180574
    TSL2109

    		DYRK Cancer
    TSL2109 is an orally active and selective DYRK2 and CDK4/6 inhibitor with an IC50 value of 22 nM for DYRK2. TSL2109 exhibits high kinase selectivity over 93%. TSL2109 arrests cell cycle and induces apoptosis in virto. TSL2109 effectively overcomes Enzalutamide (HY-70002) resistance by suppressing tumor growth in vivo and virto. TSL2109 also shows CDK4/6 inhibitor resistance.TSL2109 demonstrates safety profile. TSL2109 can be used for prostate cancer research and breast cancer [1][2].
    TSL2109
  • HY-179633
    ZLMT-72

    		CDK Apoptosis DNA/RNA Synthesis Bcl-2 Family IAP Cancer
    ZLMT-72 is an orally active dual CDK2 and CDK9 inhibitor with IC50s of 0.741 nM and 1.03 nM, respectively. ZLMT-72 shows good selectivity in kinase profiling andcholinesterase inhibition activity. ZLMT-72 has strong antiproliferative effects in the colorectal cancer (CRC) cell line HCT116 (GI50 < 0.1 nM). ZLMT-72 induces apoptosis by inhibiting thephosphorylation of retinoblastoma and RNA polymerase II, resulting in downregulation of antiapoptotic proteins (Mcl-1 and XIAP). ZLMT-72 can be used for the study of colorectal cancer (CRC) .
    ZLMT-72
  • HY-180523
    PKM2-IN-13

    		Pyruvate Kinase Apoptosis Reactive Oxygen Species (ROS) Caspase Cancer
    PKM2-IN-13 is a selective PKM2 inhibitor inhibiting PKM2 with an IC50 value of 55.13 μM. PKM2-IN-13 exhibits broad-spectrum anticancer activity with low toxicity to normal cells. PKM2-IN-13 induces apoptosis by elevated ROS levels and activation of caspases 3/7, and interacts with and inhibits the glycolytic activity of Pyruvate Kinase M2 in virto. PKM2-IN-13 demonstrates a favorable safety profile with no significant adverse effects in vivo. PKM2-IN-13 can be used for oral squamous cell carcinoma (OSCC), colon carcinoma, breast cancer and melanoma research .
    PKM2-IN-13

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