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relatively selective

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40

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3

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Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-100024
    NTRC 0066-0

    		Mps1 Cancer
    NTRC 0066-0 is a selective threonine tyrosine kinase (TTK) inhibitor (IC50=0.9 nM). NTRC 0066-0 can be used for the research of cancer .
    NTRC 0066-0
  • HY-101836
    DKM 2-93
    4 Publications Verification

    		 E1/E2/E3 Enzyme Cancer
    DKM 2-93 is a relatively selective inhibitor of UBA5 with an IC50 of 430 μM.
    DKM 2-93
  • HY-143585
    CDK9-IN-14

    		CDK Cancer
    CDK9-IN-14 is a potent and selective CDK9 inhibitor with IC50 of 6.92 nM. CDK9-IN-14 has a relatively strong inhibitory effect on MV4;11 cells and in vivo tumor models, and has a good selectivity and a low toxicity and few side effects .
    CDK9-IN-14
  • HY-N2333
    Resiniferatoxin
    1 Publications Verification

    (+)-Resiniferatoxin

    		 TRP Channel Cardiovascular Disease Cancer
    Resiniferatoxin ((+)-Resiniferatoxin), is a selective agonist of transient receptor potential vanilloid 1 (TRPV1) receptor agonist. Resiniferatoxin can be isolated from the Euphorbia resinifera plant. Resiniferatoxin eliminates TRPV1+ primary sensory afferents and blunt cardiac sympathetic afferent reflex for a relatively long period .
    Resiniferatoxin
  • HY-10791
    Ritanserin
    3 Publications Verification

    R 55667

    		 5-HT Receptor Histamine Receptor Dopamine Receptor Adrenergic Receptor Neurological Disease
    Ritanserin (R 55667) is a highly potent, relatively selective, orally active, long acting antagonist of 5-HT2 receptor, with an IC50 of 0.9 nM, less active on Histamine H1, Dopamine D2, Adrenergic α1, Adrenergic α2 receptors .
    Ritanserin
  • HY-14200A
    (S)-Rasagiline mesylate

    TVP1022 mesylate; S-PAI mesylate

    		 Monoamine Oxidase Neurological Disease
    (S)-Rasagiline (TVP1022) mesylate is the relatively inactive S-enantiomer form of Rasagiline mesylate. Rasagiline mesylate is a highly potent selective irreversible MAO inhibitor with IC50s of 4.43 nM and 412 nM for rat brain MAO B and A activity, respectively .
    (S)-Rasagiline mesylate
  • HY-W184837
    m-Nisoldipine

    KR-1008

    		 Calcium Channel Cardiovascular Disease
    m-Nisoldipine (KR-1008) is a dihydropyridine calcium antagonist that can significantly increase cardiac output and heart index, significantly reduce the negative inotropic effect on the myocardium, and has a relatively high selectivity for the thoracic aorta. m-Nisoldipine can be used in the research of cardiovascular diseases .
    m-Nisoldipine
  • HY-147537
    Antileishmanial agent-9

    		Parasite Infection
    Antileishmanial agent-9 (compound 16c) has potent and selective activity against Leishmania donovani (L. donovani) with an IC50 value of 4.01 μM. Antileishmanial agent-9 has relatively low cytotoxicity in L-6 cells (IC50 = 40.1 μM) .
    Antileishmanial agent-9
  • HY-147536
    Antileishmanial agent-8

    		Parasite Infection
    Antileishmanial agent-8 (compound 18) has potent and selective activity against Leishmania donovani (L. donovani) with an IC50 value of 5.64 μM. Antileishmanial agent-8 has relatively low cytotoxicity in L-6 cells (IC50=73.9 μM) .
    Antileishmanial agent-8
  • HY-146104
    Antimycobacterial agent-1

    		Bacterial Infection
    Antimycobacterial agent-1 (compound 33) has selectively antimycobacterial activity against Mycobacterium tuberculosis (M. tuberculosis) H37Ra with a MIC value of 1 μg/ml. Antimycobacterial agent-1 has relatively low cytotoxicity in normal cells (Vero cells IC50 = 143.2 μg/ml) .
    Antimycobacterial agent-1
  • HY-112780
    UC2288
    5 Publications Verification

    		 MDM-2/p53 Apoptosis Cancer
    UC2288 is a potent and orally active p21 attenuator (relatively selective activity for p21), which is synthesized based Sorafenib (HY-10201). UC2288 potently inhibits cancer cell growth by inducing apoptosis. UC2288 has no inhibition of VEGFR2 and Raf kinases even at 10 μM .
    UC2288
  • HY-10514
    BX795
    Maximum Cited Publications
    30 Publications Verification

    		 PDK-1 IKK Autophagy Cancer
    BX795 is a potent and selective inhibitor of PDK1, with an IC50 of 6 nM. BX795 is also a potent and relatively specific inhibitor of TBK1 and IKKε, with an IC50 of 6 and 41 nM, respectively. BX795 blocks phosphorylation of S6K1, Akt, PKCδ, and GSK3β, and has lower selectivity over PKA, PKC, c-Kit, GSK3β etc. BX795 modulates autophagy .
    BX795
  • HY-16712
    LDN-214117
    1 Publications Verification

    		 TGF-β Receptor Cancer
    LDN-214117 is an orally active ALK2 inhibitor with well-tolerated and good brain penetration. LDN-214117 has a high selectivity and low cytotoxicity for ALK2 with an IC50 value of 24 nM. LDN-214117 also is a specific bone morphogenetic proteins (BMPs) signaling inhibitor and has relatively selective inhibition for BMP6 with an IC50 value of 100 nM. LDN-214117 can be used for the research of fibrodysplasia ossificans progressiva (FOP), diffuse intrinsic pontine glioma (DIPG) .
    LDN-214117
  • HY-101311
    UPF-523

    AIDA

    		 mGluR Inflammation/Immunology Cancer
    UPF-523 (AIDA), a rigid (carboxyphenyl) glycine derivative, is a relatively potent and selective antagonist of group I metabotropic glutamate receptors (mGlu1a) with an IC50 of 214 μM. But UPF-523 has no effect on group II (mGlu2), group III (mGlu4) receptors or ionotropic glutamate receptors. UPF-523 has the potential for the research of the acute arthritis .
    UPF-523
  • HY-10791R
    Ritanserin (Standard)

    		5-HT Receptor Histamine Receptor Dopamine Receptor Adrenergic Receptor Neurological Disease
    Ritanserin (Standard) is the analytical standard of Ritanserin. This product is intended for research and analytical applications. Ritanserin (R 55667) is a highly potent, relatively selective, orally active, long acting antagonist of 5-HT2 receptor, with an IC50 of 0.9 nM, less active on Histamine H1, Dopamine D2, Adrenergic α1, Adrenergic α2 receptors .
    Ritanserin (Standard)
  • HY-116871
    YKL-1-116

    		CDK Cancer
    YKL-1-116 is a selective and covalent inhibitor of Cdk7. YKL-1-116 does not target Cdk9, Cdk12, or Cdk13. YKL-1-116 is more potent than THZ1 (HY-80013) toward both Cdk7 WT and Cdk7 as, although Cdk7 as is relatively resistant to this compound as well .
    YKL-1-116
  • HY-14200
    (S)-Rasagiline
    1 Publications Verification

    TVP1022; S-PAI

    		 Monoamine Oxidase Neurological Disease
    (S)-Rasagiline (TVP1022) is the relatively inactive S-enantiomer form of Rasagiline. Rasagiline is a highly potent selective irreversible MAO inhibitor with IC50s of 4.43 nM and 412 nM for rat brain MAO B and A activity, respectively . (S)-Rasagiline is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    (S)-Rasagiline
  • HY-167688
    GSK-1562590

    		Endogenous Metabolite Cardiovascular Disease
    GSK-1562590 is a uropeptide-II receptor antagonist with high affinity and selectivity. GSK-1562590 exhibits significant antagonistic activity in multiple bioassays and, in contrast, displays relatively sustained receptor binding times. GSK-1562590 can inhibit human urinary peptide-II-induced aortic contraction in rats in experiments, and its effect can last for at least 24 hours .
    GSK-1562590
  • HY-150582
    c-Met-IN-14

    		c-Met/HGFR c-Kit FLT3 Apoptosis Cancer
    c-Met-IN-14 (compound 26af) is a selective inhibitor of c-Met kinase from N-sulfonylamidine-based derivatives, with an IC50 value of 2.89 nM. c-Met-IN-14 shows anticancer activity by blocking phosphorylation of c-Met, and arrests cell cycle at G2/M phase. c-Met-IN-14 induces apoptosis of A549 cells in a dose-dependent manner .
    c-Met-IN-14
  • HY-149262
    CLK1-IN-3

    		CDK DYRK Autophagy Cancer
    CLK1-IN-3 (compound 10ad) is a potent and selective Clk1 inhibitor, with an IC50 of 5 nM and over 300-fold selectivity for Dyrk1A. CLK1-IN-3 also shows a relatively potent inhibition against Clk2 and Clk4, with IC50 values of 42 and 108 nM, respectively. CLK1-IN-3 potently induces autophagy in vitro. CLK1-IN-3 can be used for acute liver injury (ALI) research .
    CLK1-IN-3
  • HY-W011266
    JNJ-10198409
    1 Publications Verification

    		 PDGFR Cancer
    JNJ-10198409 is a relatively selective, orally active, and ATP competitive PDGF-RTK (platelet-derived growth factor receptor tyrosine kinase) inhibitor (IC50=2 nM). It is a dual-mechanism, antiangiogenic, and tumor cell antiproliferative agent. JNJ-10198409 has good activity against PDGFR-β kinase (IC50=4.2 nM) and PDGFR-α kinase (IC50=45 nM) .
    JNJ-10198409
  • HY-146226
    Viral 2C protein inhibitor 1

    		Enterovirus Infection
    Viral 2C protein inhibitor 1 (compound 6aw) is a potent and broad-spectrum enterovirus antiviral agent, inhibiting viral 2C protein. Viral 2C protein inhibitor 1 inhibits multiple strains of EV-D68, EV-A71 and CVB3 with EC50s of 0.1~3.6 µM, and exhibits high selectivity index and relatively low cytotoxicity .
    Viral 2C protein inhibitor 1
  • HY-167952
    mTOR inhibitor-25

    		PI3K Cancer
    mTOR inhibitor-25 is an enzyme inhibitor that is more selective than PI3K and has good anticancer activity. mTOR inhibitor-25 shows strong inhibitory effects on mTOR and may be used to study leukemia, skin cancer, breast cancer, lung cancer and colon cancer. mTOR inhibitor-25 showed excellent activity in cell proliferation experiments, but its inhibitory ability on PI3K was relatively weak .
    mTOR inhibitor-25
  • HY-12383S
    Pelubiprofen-13C,d3

    		Isotope-Labeled Compounds COX Neurological Disease Inflammation/Immunology
    Pelubiprofen- 13C,d3 is the 13C- and deuterium labeled Pelubiprofen. Pelubiprofen, an orally active and non-steroidal anti-inflammatory drug, is a member of the 2-arylpropionic acid family and has relatively selective effects on COX-2 activity. Pelubiprofen inhibits COX activity and the transforming growth factor-β activated kinase 1-IκB kinase β-NF-κB pathway, and has significant anti-inflammatory and analgesic effects .
    Pelubiprofen-13C,d3
  • HY-125856A
    Milvexian TFA

    BMS-986177 TFA; JNJ-70033093 TFA

    		 Factor Xa Cardiovascular Disease
    Milvexian TFA (BMS-986177 TFA) is a factor XIa inhibitor with biological activity to prevent venous thromboembolism. Milvexian TFA was effective in reducing the occurrence of venous thromboembolism in patients undergoing knee replacement surgery. Milvexian TFA has good selectivity and shows significant inhibitory effects on plasma kallikrein and trypsin. Milvexian TFA has a bioavailability of 32%, which means it has a high absorption rate in the body. Milvexian TFA showed a relatively low risk of bleeding in clinical trials .
    Milvexian TFA
  • HY-146352
    HIV-1 inhibitor-28

    		HIV Infection Inflammation/Immunology
    HIV-1 inhibitor-28 (compound 14j2) is a highly potent and selective HIV-1 inhibitor with an EC50 of 58 nM for WT HIV-1 strain and an IC50 of 3.37 μM for HIV-1 WT reverse transcription (RT). HIV-1 inhibitor-28 exhibits relatively low cytotoxicity in MT-4 cells (CC50 = 38.6 μM). HIV-1 inhibitor-28 can be used for researching AIDS .
    HIV-1 inhibitor-28
  • HY-16940
    24(S)-Hydroxycholesterol

    24S-OHC; 24S-HC; Cerebrosterol

    		 LXR iGluR Endogenous Metabolite Metabolic Disease
    24(S)-Hydroxycholesterol (24S-OHC), the major brain cholesterol metabolite, plays an important role to maintain homeostasis of cholesterol in the brain. 24(S)-Hydroxycholesterol (24S-OHC) is one of the most efficient endogenous LXR agonist known and is present in the brain and in the circulation at relatively high levels. 24(S)-Hydroxycholesterol (24S-OHC) is a very potent, direct, and selective positive allosteric modulator of NMDARs with a mechanism that does not overlapthat of other allosteric modulators .
    24(S)-Hydroxycholesterol
  • HY-109968A
    Irdabisant hydrochloride

    CEP-26401 hydrochloride

    		 Histamine Receptor Neurological Disease
    Irdabisant (CEP-26401) hydrochloride is a selective, orally active and blood-brain barrier (BBB) penetrant histamine H3 receptor (H3R) inverse agonist/inverse agonist with Ki values of 7.2 nM and 2.0 nM for rat H3R and human H3R, respectively. Irdabisant hydrochloride has relatively low inhibitory activity against hERG current with an IC50 of 13.8 μM. Irdabisant hydrochloride has cognition-enhancing and wake-promoting activities in the rat social recognition model. Irdabisant hydrochloride can be used to research schizophrenia or cognitive impairment .
    Irdabisant hydrochloride
  • HY-109968
    Irdabisant

    CEP-26401

    		 Histamine Receptor Neurological Disease
    Irdabisant (CEP-26401) is a selective, orally active and blood-brain barrier (BBB) penetrant histamine H3 receptor (H3R) inverse agonist/inverse agonist with Ki values of 7.2 nM and 2.0 nM for rat H3R and human H3R, respectively. Irdabisant has relatively low inhibitory activity against hERG current with an IC50 of 13.8 μM. Irdabisant has cognition-enhancing and wake-promoting activities in the rat social recognition model. Irdabisant can be used to research schizophrenia or cognitive impairment .
    Irdabisant
  • HY-15746A
    Dobutamine

    		Adrenergic Receptor Cardiovascular Disease Endocrinology Cancer
    Dobutamine is a synthetic catecholamine that acts on α1-AR, β1-AR, β2-AR (α-1, β-1 andβ-2 adrenoceptors). Dobutamine is a selective β1-AR agonist, relatively weak activity at α1-AR and β2-AR. Dobutamine can increase cardiac output and correct hypoperfusion .
    Dobutamine
  • HY-15746
    Dobutamine hydrochloride
    3 Publications Verification

    		 Adrenergic Receptor Cardiovascular Disease Endocrinology Cancer
    Dobutamine hydrochloride is a synthetic catecholamine that acts on α1-AR, β1-AR, β2-AR (α-1, β-1 andβ-2 adrenoceptors). Dobutamine hydrochloride is a selective β1-AR agonist, relatively weak activity at α1-AR and β2-AR. Dobutamine hydrochloride can increase cardiac output and correct hypoperfusion .
    Dobutamine hydrochloride
  • HY-16950A
    (E/Z)-4-Hydroxytamoxifen
    1 Publications Verification

    Afimoxifene; 4-OHT

    		 Estrogen Receptor/ERR Adhesion G Protein-coupled Receptors (AGPCRs) Drug Metabolite Metabolic Disease Cancer
    (E/Z)-4-Hydroxytamoxifen (Afimoxifene) is a racemic compound of (Z)-4-Hydroxytamoxifen and (E)-4-Hydroxytamoxifen isomers. (E/Z)-4-Hydroxytamoxifen is a selective estrogen receptor modulator with mixed estrogenic and antiestrogenic activity, which is also an active metabolite of Tamoxifen (HY-13757A). (E/Z)-4-Hydroxytamoxifen is an agonist of the G protein-coupled estrogen receptor (GPER) with relatively low affinity (100-1000 nM). (E/Z)-4-Hydroxytamoxifen is promising for research of cyclical mastalgia, such as breast pain, tenderness, and nodularity .
    (E/Z)-4-Hydroxytamoxifen
  • HY-168953
    Lysosomal P-gp targeted agent 1

    		P-glycoprotein Apoptosis Bcl-2 Family Reactive Oxygen Species (ROS) Caspase Cancer
    Lysosomal P-gp targeted agent 1 (Compound 14) is an anti-tumor agent targeting lysosomal P-glycoprotein (Pgp). Lysosomal P-gp targeted agent 1 is selectively transported into lysosomes by overexpressed Pgp, release nitric oxide (NO) to generate reactive oxygen species (ROS), resulting in lysosomal membrane permeabilization (LMP) and inducing apoptosis. Lysosomal P-gp targeted agent 1 can overcome P-glycoprotein-mediated drug resistance and lead to cell cycle arrest, but relatively low toxicity to normal cells. Lysosomal P-gp targeted agent 1 has antitumor activity, significantly inhibits tumor volume .
    Lysosomal P-gp targeted agent 1
  • HY-15746B
    Dobutamine tartrate

    		Adrenergic Receptor Cardiovascular Disease Endocrinology Cancer
    Dobutamine tartrate is a synthetic catecholamine that acts on α1-AR, β1-AR, β2-AR (α-1, β-1 andβ-2 adrenoceptors). Dobutamine tartrate is a selective β1-AR agonist, relatively weak activity at α1-AR and β2-AR. Dobutamine tartrate can increase cardiac output and correct hypoperfusion .
    Dobutamine tartrate
  • HY-15746S1
    (rac)-Dobutamine-d6 hydrochloride

    		Isotope-Labeled Compounds Adrenergic Receptor Cardiovascular Disease Endocrinology
    (rac)-Dobutamine-d6 (hydrochloride) is a labelled racemic Dobutamine hydrochloride. Dobutamine hydrochloride is a synthetic catecholamine that acts on α1-AR, β1-AR, β2-AR (α-1, β-1 andβ-2 adrenoceptors). Dobutamine hydrochloride is a selective β1-AR agonist, relatively weak activity at α1-AR and β2-AR. Dobutamine hydrochloride can increase cardiac output and correct hypoperfusion .
    (rac)-Dobutamine-d6 hydrochloride
  • HY-15746S
    (rac)-Dobutamine-d4 hydrochloride

    		Isotope-Labeled Compounds Adrenergic Receptor Cardiovascular Disease Endocrinology
    (rac)-Dobutamine-d4 (hydrochloride) is a labelled racemic Dobutamine hydrochloride. Dobutamine hydrochloride is a synthetic catecholamine that acts on α1-AR, β1-AR, β2-AR (α-1, β-1 andβ-2 adrenoceptors). Dobutamine hydrochloride is a selective β1-AR agonist, relatively weak activity at α1-AR and β2-AR. Dobutamine hydrochloride can increase cardiac output and correct hypoperfusion .
    (rac)-Dobutamine-d4 hydrochloride
  • HY-174445
    C199

    		PROTACs Histone Methyltransferase Apoptosis Cancer
    C199 is a PROTAC degrader targeting PRMT4 (DC50 = 106 nM). C199 shows high selectivity for PRMT4 over other protein arginile methyltransferases. C199 exhibits strong cell degradation ability. C199 induces apoptosis in MM cell lines. C199 efficiently clears PRMT4 protein via the VHL-proteasome pathway. C199 has a relatively long half-life and shows strong anti-multiple myeloma (MM) tumor activity (Pink: Target protein ligand (HY-111109); Blue: E3 ligase ligand (HY-112078), E3 ligase ligand + linker (HY-174474); black: Linker) .
    C199
  • HY-176735
    FLT3/IRAK4-IN-1

    		IRAK FLT3 Apoptosis Cancer
    FLT3/IRAK4-IN-1 is a selective FLT3/IRAK4 inhibitor with the remarkable activity towards FLT3-WT (IC50 = 1.95 nM), FLT3-D835Y (IC50 = 3.22 nM) and IRAK4 (IC50 = 53.72 nM). LT3/IRAK4-IN-1 has relatively low toxicity to normal bone marrow cells, can effectively promote cell apoptosis, and has the potential to overcome drug resistance. FLT3/IRAK4-IN-1 can be used for research on acute myeloid leukemia (AML) .
    FLT3/IRAK4-IN-1
  • HY-15746R
    Dobutamine hydrochloride (Standard)

    		Reference Standards Adrenergic Receptor Cardiovascular Disease Endocrinology Cancer
    Dobutamine (hydrochloride) (Standard) is the analytical standard of Dobutamine (hydrochloride). This product is intended for research and analytical applications. Dobutamine hydrochloride is a synthetic catecholamine that acts on α1-AR, β1-AR, β2-AR (α-1, β-1 andβ-2 adrenoceptors). Dobutamine hydrochloride is a selective β1-AR agonist, relatively weak activity at α1-AR and β2-AR. Dobutamine hydrochloride can increase cardiac output and correct hypoperfusion .
    Dobutamine hydrochloride (Standard)
  • HY-16950AR
    (E/Z)-4-Hydroxytamoxifen (Standard)

    Afimoxifene (Standard); 4-OHT (Standard)

    		 Reference Standards Estrogen Receptor/ERR Endogenous Metabolite Cancer
    (E/Z)-4-Hydroxytamoxifen (Standard) is the analytical standard of (E/Z)-4-Hydroxytamoxifen. This product is intended for research and analytical applications. (E/Z)-4-Hydroxytamoxifen (Afimoxifene) is a racemic compound of (Z)-4-Hydroxytamoxifen and (E)-4-Hydroxytamoxifen isomers. (E/Z)-4-Hydroxytamoxifen is a selective estrogen receptor modulator with mixed estrogenic and antiestrogenic activity, which is also an active metabolite of Tamoxifen (HY-13757A). (E/Z)-4-Hydroxytamoxifen is an agonist of the G protein-coupled estrogen receptor (GPER) with relatively low affinity (100-1000 nM). (E/Z)-4-Hydroxytamoxifen is promising for research of cyclical mastalgia, such as breast pain, tenderness, and nodularity .
    (E/Z)-4-Hydroxytamoxifen (Standard)

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