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TK inhibitor

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47

Inhibitors & Agonists

1

Biochemical Assay Reagents

1

Peptides

3

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Products

1

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-151483
    TK-129

    		Wnt Histone Demethylase Cardiovascular Disease
    TK-129 is an orally active, low-toxicity, potent KDM5B inhibitor (with high affinity; IC50=44 nM). TK-129 exerts cardioprotective effects by inhibiting KDM5B and blocking the KDM5B-associated Wnt pathway. TK-129 reduces ang II-induced activation of cardiac fibroblasts in vitro and reduces isoprenaline-induced myocardial remodelling and fibrosis in vivo. TK-129 can be used in studies of cardiovascular disease .
    TK-129
  • HY-122903A
    (-)-TK216

    		DNA/RNA Synthesis Cancer
    (-)-TK216 is an enantiomer of TK216 (HY-122903). TK216 is an orally active and potent E26 transformation specific (ETS) inhibitor. (-)-TK216 has anti-cancer activity .
    (-)-TK216
  • HY-161927
    EGFR-TK-IN-4

    		EGFR Apoptosis Cancer
    EGFR-TK-IN-4 (compound 10k) is a potent and selective EGFR-TK inhibitor. EGFR-TK-IN-4 can induce apoptosis . EGFR-TK-IN-4 has antitumor activity .
    EGFR-TK-IN-4
  • HY-122903B
    (+)-TK216

    		DNA/RNA Synthesis Others
    (+)-TK216 is an enantiomer of TK216 (HY-122903). TK216 is an orally active and potent E26 transformation specific (ETS) inhibitor .
    (+)-TK216
  • HY-122903
    TK216
    Maximum Cited Publications
    6 Publications Verification

    		 DNA/RNA Synthesis Cancer
    TK216 is an orally active and potent E26 transformation specific (ETS) inhibitor . TK216 directly binds EWS-FLI1 and inhibits EWS-FLI1 protein interactions. TK216 blocks the binding between EWS-FLI1 and RNA helicase A. TK216 has anticancer activity .
    TK216
  • HY-117523
    (Z)-RG-13022

    (Z)-Tyrphostin RG13022

    		 EGFR Cancer
    (Z)-RG-13022 is a tyrosine kinase (TK) inhibitor, which inhibits preferentially the TK activity of the EGF receptor and inhibits EGF-stimulated growth of cultured cells. (Z)-RG-13022 exerts an IC50 of 11 μM for DNA synthesis in the HN5 cells, which is 3 times more potent than (E)-RG-13022 (IC50=38 μM). (Z)-RG-13022 can be used for research of breast cancer cells .
    (Z)-RG-13022
  • HY-173573
    TK-684

    		Apoptosis SHP2 Cancer
    TK-684 is a potent and selective allosteric SHP2 inhibitor with IC50 values of 2.1, ＞1000 nM for SHP2 WT, SHP22 PTP, respectively. TK-684 inhibits cell proliferation and induces apoptosis. TK-684 decreases the protein expression of p-AKT, p-ERK .
    TK-684
  • HY-158762
    TK-642

    		SHP2 Cancer
    TK-642 is a highly active, selective, orally activity SHP2 inhibitor based on pyrazole and pyrazine (IC50=2.7 nmol/L). TK-642 can effectively inhibit the proliferation of esophageal carcinoma cells and induce cell apoptosis. TK-642 can be used in the study of esophageal cancer .
    TK-642
  • HY-158018
    EGFR-TK-IN-2

    		EGFR Cancer
    EGFR-TK-IN-2 (compound 10b) is EGFR-TK inhibitor with the IC50 of 0.16 μM. EGFR-TK-IN-2 inhibits cell growth .
    EGFR-TK-IN-2
  • HY-173571
    TK-685

    		SHP2 Apoptosis Cancer
    TK-685 is an orally active, selective, and allosteric SHP2 inhibitor with an IC50 of 2.1 nM. TK-685 inhibits esophageal cancer cell proliferation and induced apoptosis by targeting SHP2-mediated AKT and ERK signaling pathways .
    TK-685
  • HY-W008907
    5'-O-Tritylthymidine

    5-OTT

    		 Apoptosis Cancer
    5'-O-Tritylthymidine is an inhibitor of TK-2 and inhibits angiogenesis . 5'-O-Tritylthymidine targets FAK-Mdm-2 interactions, decreasing cell viability and increasing apoptosis.
    5'-O-Tritylthymidine
  • HY-163860
    EGFR-TK-IN-3

    		EGFR Cancer
    EGFR-TK-IN-3 (3) is an EGFR TK inhibitor, with an IC50 of 2.33 μM against Erlotinib (HY-50896)-resistant A549 cells .
    EGFR-TK-IN-3
  • HY-112889
    Oxythiamine diphosphate

    		Transketolase Metabolic Disease
    Oxythiamin diphosphate is a potent transketolase (TK) inhibitor .
    Oxythiamine diphosphate
  • HY-112889B
    Oxythiamine diphosphate ammonium
    1 Publications Verification

    		 Transketolase Metabolic Disease
    Oxythiamin diphosphate ammonium is a potent transketolase (TK) inhibitor .
    Oxythiamine diphosphate ammonium
  • HY-151259
    TK4b

    		JAK Cancer
    TK4b is a Janus kinase (JAK) inhibitor with the IC50 values of 19.40 nM and 18.42 nM for JAK2 and JAK3, respectively. TK4b can be used in lymphoid-derived diseases and leukemia cancer research .
    TK4b
  • HY-151258
    TK4g

    		JAK Cancer
    TK4g is a Janus kinase (JAK) inhibitor with the IC50 values of 12.61 nM and 15.80 nM for JAK2 and JAK3, respectively. TK4g can be used in lymphoid-derived diseases and leukemia cancer research .
    TK4g
  • HY-P1079
    ω-Agatoxin TK

    		Calcium Channel Neurological Disease
    ω-Agatoxin TK, a peptidyl toxin of the venom of Agelenopsis aperta, is a potent and selective P/Q type Ca 2+ channel blocker. ω-Agatoxin TK inhibits the high K + depolarisation-induced rise in internal Ca 2+ in cerebral isolated nerve endings with an IC50 of of 60 nM. ω-Agatoxin TK has no effect on L-type, N-type, or T-type calcium channels .
    ω-Agatoxin TK
  • HY-117143
    TK05
    1 Publications Verification

    		 Glutathione S-transferase Inflammation/Immunology
    TK05 is a potent and selective inhibitor of leukotriene C4 synthase (LTC4S) with an IC50 of 95 nM .
    TK05
  • HY-144441
    NSC81111

    		EGFR Cancer
    NSC81111 is a potent and orally active EGFR-TK inhibitor with an IC50 of 0.15 nM. NSC81111 has anticaner effects .
    NSC81111
  • HY-147303
    Sacibertinib

    		Trk Receptor EGFR Cancer
    Sacibertinib is a tyrosine kinase (Trk) inhibitor with EC50 value of 110 nM and 244 nM for EGFR-TK phosphorylation and HER2, respectively. Antineoplastic activity .
    Sacibertinib
  • HY-146472
    EGFR-IN-52

    		EGFR Apoptosis Cancer
    EGFR-IN-52 (Compound 4) is a potent EGFR inhibitor with IC50 values of 0.358, 86.02 and 432.67 µM against EGFR, EGFR L858R-TK and EGFR T790M-TK, respectively. EGFR-IN-52 shows cytotoxic activity against cancer cell lines and induces apoptosis .
    EGFR-IN-52
  • HY-146471
    EGFR-IN-51

    		EGFR Apoptosis Cancer
    EGFR-IN-51 (Compound 6) is a potent EGFR inhibitor with IC50 values of 0.493, 102.60 and 461.63 µM against EGFR, EGFR L858R-TK and EGFR T790M-TK, respectively. EGFR-IN-51 shows cytotoxic activity against cancer cell lines and induces apoptosis .
    EGFR-IN-51
  • HY-169436
    Lon-TK

    		PD-1/PD-L1
    Lon-TK is a glycolysis inhibitor + linker conjugate of LTB (HY-169434). LTB is an intelligent responsive prodrug that connects Lonidamine (Lon) (HY-B0486) and a PD-L1 inhibitor (BMS-1, HY-19991) through a thioketal linker. It significantly inhibits the glycolytic metabolism of tumor cells and blocks the PD-1/PD-L1 immune escape pathway. Lon-TK shows potential for application in photodynamic-enhanced immunotherapy research .
    Lon-TK
  • HY-157526
    EGFR-TK-IN-1

    		EGFR Apoptosis Cancer
    EGFR-TK-IN-1 (compound 7o) is a potent mutant EGFR inhibitor with IC50 of 8.5 nM an 9.3 nM against EGFR L858R/T790M and EGFR Del19.EGFR-TK-IN-1 showes strong antiproliferative effects against EGFR mutant-driven non-small cell lung cancer (NSCLC) cells and induces cell apoptosis .
    EGFR-TK-IN-1
  • HY-144444
    NSC381467

    		EGFR Cancer
    NSC381467 is a potent and orally active inhibitor of EGFR tyrosine kinase (EGFR-TK). NSC381467 has strong antiproliferative activities. NSC381467 has the potential for the research of cancer diseases .
    NSC381467
  • HY-144445
    NSC114126

    		EGFR Cancer
    NSC114126 is a potent and orally active inhibitor of EGFR tyrosine kinase (EGFR-TK). NSC114126 has strong antiproliferative activities. NSC114126 has the potential for the research of cancer diseases .
    NSC114126
  • HY-155358
    Os30

    		EGFR Apoptosis Cancer
    Os30, a potent fourth-generation EGFR inhibitor, is a potent EGFRC797S-TK inhibitor with IC50 values of 18 nM and 113 nM for EGFRDel19/T790M/C797S TK and EGFRL858R/T790M/C797S TK, respectively. Os30 can suppress EGFR phosphorylation, arrest at G1 phase and induce the apoptosis of KC-0116 (BaF3-EGFRDel19/T790M/C797S) cells. Os30 shows potent antitumor efficacy on non-small cell lung cancer (NSCLC) with EGFmRC797S mutation .
    Os30
  • HY-107430B
    Oxythiamine chloride

    Hydroxythiamine chloride

    		 Apoptosis Cancer
    Oxythiamine (Hydroxythiamine) chloride, an analogue of anti-metabolite, can suppress the non-oxidative synthesis of ribose and induce cell apoptosis. Oxythiamine is a thiamine antagonist and inhibits transketolase (TK). Oxythiamine chloride inhibits cancer cell apoptosis and inhibits cell proliferation .
    Oxythiamine chloride
  • HY-107430
    Oxythiamine
    2 Publications Verification

    Hydroxythiamin

    		 Apoptosis Endogenous Metabolite Cancer
    Oxythiamine (Hydroxythiamin), an analogue of anti-metabolite, can suppress the non-oxidative synthesis of ribose and induce cell apoptosis. Oxythiamine is a thiamine antagonist and inhibits transketolase (TK). Oxythiamine inhibits cancer cell apoptosis and inhibits cell proliferation .
    Oxythiamine
  • HY-107430A
    Oxythiamine chloride hydrochloride
    2 Publications Verification

    Hydroxythiamine chloride hydrochloride

    		 Apoptosis Endogenous Metabolite Cancer
    Oxythiamine (Hydroxythiamine) chloride hydrochloride, an analogue of anti-metabolite, can suppress the non-oxidative synthesis of ribose and induce cell apoptosis. Oxythiamine chloride hydrochloride is a thiamine antagonist and inhibits transketolase (TK). Oxythiamine chloride hydrochloride inhibits cancer cell apoptosis and inhibits cell proliferation .
    Oxythiamine chloride hydrochloride
  • HY-16339
    N3PT
    1 Publications Verification

    N3-pyridyl thiamine

    		 Transketolase Cancer
    N3PT (N3-pyridyl thiamine) is a potent and selective transketolase inhibitor. N3PT is pyrophosphorylated and then binds to transketolase with an Kd value of 22 nM (Apo-TK, transketolase lacking bound thiamine) .
    N3PT
  • HY-144760
    EGFR-IN-3

    		EGFR Apoptosis Cancer
    EGFR-IN-3 (Compound 4c) is a potent EGFR inhibitor with an IC50 of 0.32 µM against EGFRwt-TK. EGFR-IN-3 shows cytotoxic activity against cancer cell lines and induces apoptosis .
    EGFR-IN-3
  • HY-151604
    Transketolase-IN-3

    		Transketolase Others
    Transketolase-IN-3 is a potent transketolase (TK) inhibitor. Transketolase-IN-3 has herbicidal activity and has inhibitory effects against Digitaria sanguinalis (DS) and Amaranthus retroflexus (AR). Transketolase-IN-3 can be used for the research of herbicides .
    Transketolase-IN-3
  • HY-149846
    SIQ17

    		EGFR Cancer
    SIQ17 is an EGFR inhibitor that inhibits its activity by occupying the ATP-binding site, with IC50 of 0.62 nM. SIQ17 shows more effective EGFR-TK inhibitory activity compared to the known inhibitor Erlotinib (HY-50896) (IC50 of ∼20 nM). SIQ17 can be used for cancer research
    SIQ17
  • HY-173314
    EGFR-IN-155

    		EGFR Apoptosis Cancer
    EGFR-IN-155 (compound 13a) is an EGFR inhibitor with IC50 values of 0.14 nM and 0.18 nM against EGFR TK and EGFR L858R, respectively. EGFR-IN-155 inhibits tumor growth, causes a cell cycle arrest at S phase, and and induces cell apoptosis .
    EGFR-IN-155
  • HY-163311
    Transketolase-IN-6

    		Transketolase Others
    Transketolase-IN-6 (Compound 6bj) is a herbicide lead compound. Transketolase-IN-6 displays a highly inhibitory effect with the root inhibition of about 80% against Amaranthus retroflexus and Setaria viridis. Transketolase-IN-6 is a potent transketolase (TK) inhibitor .
    Transketolase-IN-6
  • HY-107430R
    Oxythiamine (Standard)

    Hydroxythiamin (Standard)

    		 Reference Standards Apoptosis Endogenous Metabolite Cancer
    Oxythiamine (Standard) is the analytical standard of Oxythiamine. This product is intended for research and analytical applications. Oxythiamine (Hydroxythiamin), an analogue of anti-metabolite, can suppress the non-oxidative synthesis of ribose and induce cell apoptosis. Oxythiamine is a thiamine antagonist and inhibits transketolase (TK). Oxythiamine inhibits cancer cell apoptosis and inhibits cell proliferation[1][2][3].
    Oxythiamine (Standard)
  • HY-149889
    EGFR-IN-78

    		Apoptosis EGFR Cancer
    EGFR-IN-78 (compound A5)，a 2-aminopyrimidine derivative，is a reversible inhibitor of EGFR C797S-TK，and also an inducer of apoptosis. EGFR-IN-78 shows anti-proliferative activity，inhibits EGFR phosphorylation and arrests cell cycle at G2/M phase .
    EGFR-IN-78
  • HY-118304
    AKN-028

    		FLT3 Apoptosis Caspase Cancer
    AKN-028, a novel tyrosine kinase (TK) inhibitor, is a potent, orally active FMS-like receptor tyrosine kinase 3 (FLT3) inhibitor with an IC50 value of 6 nM. AKN-028 inhibits FLT3 autophosphorylation. AKN-028 induces dose-dependent cytotoxic response (mean IC50=1 μM). AKN-028 induces apoptosisby activation of caspase 3. AKN-028 can be used in research of acute myeloid leukemia (AML) .
    AKN-028
  • HY-118304B
    AKN-028 acetate

    		FLT3 Apoptosis Caspase Cancer
    AKN-028 acetate, a novel tyrosine kinase (TK) inhibitor, is a potent, orally active FMS-like receptor tyrosine kinase 3 (FLT3) inhibitor with an IC50 value of 6 nM. AKN-028 acetate inhibits FLT3 autophosphorylation. AKN-028 acetate induces dose-dependent cytotoxic response (mean IC50=1 μM). AKN-028 acetate induces apoptosisby activation of caspase 3. AKN-028 acetate can be used in research of acute myeloid leukemia (AML).
    AKN-028 acetate
  • HY-170761
    KEAP1-NRF2 PPI-IN-1

    		Keap1-Nrf2 Cancer
    KEAP1-NRF2 PPI-IN-1 (compound 23) is an inhibitor targeting the KEAP1-NRF2 interaction. KEAP1-NRF2 PPI-IN-1 has IC50 values of 136 nM and 62 nM in the DNA damage assays of human TK6 and insect SF9 cell lines, respectively .
    KEAP1-NRF2 PPI-IN-1
  • HY-158016
    Antiproliferative agent-49

    		EGFR Apoptosis Cancer
    Antiproliferative agent-49 (Compound 5a) is a EGFR-TK inhibitor with an IC50 of 0.09 μM. Antiproliferative agent-49 is a anti-proliferative agent. Antiproliferative agent-49 displays good activities against HER3 and HER4 with IC50 values 0.18 and 0.37 µM. Antiproliferative agent-49 induces mitochondrial apoptotic pathway and increased accumulation of ROS .
    Antiproliferative agent-49
  • HY-149022
    HSV-1/HSV-2-IN-1

    		HSV Orthopoxvirus Infection
    HSV-1/HSV-2-IN-1 (compound 7d) is a HSV-1 and HSV-2 inhibitor, with EC50s of 7.6, 7.6, 4, and 12 μM for HSV-1 (KOS), HSV-2 (G), HSV-1 TK - KOS ACV r and vaccinia virus in human embryonic lung fibroblast cell cultures .
    HSV-1/HSV-2-IN-1
  • HY-118304A
    AKN-028 TFA

    		FLT3 Apoptosis Caspase Cancer
    AKN-028 TFA, a novel tyrosine kinase (TK) inhibitor, is a potent, orally active FMS-like receptor tyrosine kinase 3 (FLT3) inhibitor with an IC50 value of 6 nM. AKN-028 TFA inhibits FLT3 autophosphorylation. AKN-028 TFA induces dose-dependent cytotoxic response (mean IC50=1 μM). AKN-028 TFA induces apoptosisby activation of caspase 3. AKN-028 TFA can be used in research of acute myeloid leukemia (AML) .
    AKN-028 TFA
  • HY-172897
    EGFR/DHFR-IN-2

    		EGFR Dihydrofolate reductase (DHFR) Apoptosis Cytochrome P450 Cancer
    EGFR/DHFR-IN-2 (9b) is a dual h-DHFR/EGFR TK inhibitor, with IC50 values of 0.192 μM and 0.109 μM for h-DHFR and EGFR, respectively. EGFR/DHFR-IN-2 (9b) halts the cell cycle at the G1/S phase and induces apoptosis. EGFR/DHFR-IN-2 (9b) is a potential inhibitor of CYP2C9 and CYP3A4. EGFR/DHFR-IN-2 (9b) can be used in the cancer research .
    EGFR/DHFR-IN-2
  • HY-146138
    EGFR-IN-57

    		EGFR VEGFR Casein Kinase Topoisomerase Microtubule/Tubulin Apoptosis Cancer
    EGFR-IN-57 (Compound 25a) is a potent, orally active EGFR-TK inhibitor with an IC50 of 0.054 µM. EGFR-IN-57 also inhibits VEGFR-2, CK2α, topoisomerase IIβ and tubulin polymerization with IC50 values of 0.087, 0.171, 0.13 and 3.61 µM, respectively. EGFR-IN-57 induces cell cycle arrest at G2/M and pre-G1 phases. EGFR-IN-57 induces cancer cell apoptosis .
    EGFR-IN-57
  • HY-17422S1
    Acyclovir-d4

    Aciclovir-d4; Acycloguanosine-d4

    		 Isotope-Labeled Compounds HSV Bacterial Apoptosis Antibiotic Infection Cancer
    Acyclovir-d4 is the deuterium labeled Acyclovir. Acyclovir (Aciclovir) is a guanosine analogue and an orally active antiviral agent. Acyclovir inhibits HSV-1 (IC50 of 0.85 μM), HSV-2 (IC50 of 0.86 μM) and varicella-zoster virus. Acyclovir can be phosphorylated by viral thymidine kinase (TK), and Acyclovir triphosphate interferes with viral DNA polymerization through competitive inhibition with guanosine triphosphate and obligatory chain termination . Acyclovir prevents bacterial infections during induction therapy for acute leukaemia .
    Acyclovir-d4

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