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SR

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183

Inhibitors & Agonists

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3

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Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-18345
    SR 49059
    1 Publications Verification

    Vasopressin Receptor Cardiovascular Disease Endocrinology
    SR 49059 (SR-49059) is a potent, orally active, selective vasopressin V1a antagonist with a Ki vaule of 1.4 nM .
    SR 49059
  • HY-13751

    Sigma Receptor Inflammation/Immunology
    SR-31747 is a sigma ligand with immunosuppressive and anti-inflammatory properties. SR-31747 blocks cell proliferation by inhibiting sterol isomerase .
    SR-31747
  • HY-145409

    Epigenetic Reader Domain Cancer
    SR-0813 is a potent and selective ENL/AF9 YEATS domain inhibitor. SR-0813 has IC50 and EC50 values of 25 nM and 205 nM for ENL YEATS domain, respectively. SR-0813 has IC50 and EC50 values of 311 nM and 76 nM (CETSA) for AF9 YEATS domain, respectively. SR-0813 binds MAP3K19 with over 100-fold lower affinity (Kd=3.5 μM) than ENL YEATS (Kd=30 nM). SR-0813 can be used for the research of acute leukemia .
    SR-0813
  • HY-100277
    Mifobate
    1 Publications Verification

    SR-202

    PPAR Metabolic Disease
    Mifobate (SR-202) is a potent and specific PPARγ antagonist. Mifobate (SR-202) selectively inhibits Thiazolidinedione (TZD)-induced PPARγ transcriptional activity (IC50=140 μM). Mifobate (SR-202) does not affect basal or ligand-stimulated transcriptional activity of PPARα, PPARβ, or the farnesoid X receptor (FXR). Mifobate (SR-202) shows antiobesity and antidiabetic effects .
    Mifobate
  • HY-106716

    Others Neurological Disease
    SR 41378 is an orally active aminopyrazine derivative. SR 41378 has anticonvulsant, antianxiety and hypnotic activities .
    SR 41378
  • HY-105259

    Renin Cardiovascular Disease
    SR 43845 is a renin inhibitor. SR 43845 decreases blood pressure and inhibits plasma renin activity. SR 43845 can be used for hypertension research .
    SR 43845
  • HY-149292

    Casein Kinase Cancer
    SR-4133 is a potent and highly CK1ε selective inhibitor with an IC50 of 58 nM. SR-4133 binds to the ATP-binding site of CK1ε. SR-4133 displays nanomolar growth inhibition of bladder cancer cells, and inhibits the phosphorylation of 4E-BP1 .
    SR-4133
  • HY-120853

    Others Others
    SR-4326 is an active compound.
    SR-4326
  • HY-120144

    Others Neurological Disease
    SR-8993 is a highly selective nociceptin receptor agonist that can penetrate the blood-brain barrier and has the activity of reducing alcohol intake and relieving withdrawal anxiety. SR-8993 has shown mild anxiolytic effects in animal models and can effectively reverse anxiety caused by acute alcohol withdrawal. SR-8993 further reduces restricted drinking, operant responses for alcohol, and increased drinking induced by long-term intermittent exposure to alcohol. SR-8993 also reduces stress- and cue-related alcohol-seeking relapse .
    SR-8993
  • HY-P2130

    Renin Cardiovascular Disease
    SR 42128 is a potent renin inhibitor. SR 42128 potently inhibits primate renins whereas other animal renins are much less inhibited .
    SR 42128
  • HY-135674

    p38 MAPK TNF Receptor Inflammation/Immunology Cancer
    SR-318 is a potent and highly selective p38 MAPK inhibitor with IC50s of 5 nM, 32 nM and 6.11 μM for p38α, p38β and p38α/β, respectively. SR-318 potently inhibits the TNF-α release in whole blood with an IC50 of 283 nM. SR-318 has anti-cancer and anti-inflammatory activity .
    SR-318
  • HY-120542

    PPAR Metabolic Disease
    SR 1824 is a non-agonist PPARγ ligand that blocks Cdk5-mediated phosphorylation. SR 1824 has anti-diabetic effects .
    SR 1824
  • HY-13300
    SR-3677
    1 Publications Verification

    ROCK Autophagy Cancer
    SR-3677 is a potent and selective ROCK-II inhibitor with an IC50 of ~3 nM.
    SR-3677
  • HY-12829

    JNK Neurological Disease
    SR-3306 is a selective, potent, highly brain penetrant JNK inhibitor.
    SR-3306
  • HY-101454
    SR0987
    2 Publications Verification

    ROR Inflammation/Immunology Cancer
    SR0987, a SR1078 analog, is a RORγt agonist, with an EC50 of 800 nM. SR0987 increases IL17 expression while repressing the expression of PD-1 .
    SR0987
  • HY-108907

    Casein Kinase Cancer
    SR-1277 is a potent, selective and ATP competitive CK1δ/ε inhibitor, with IC50s of 49 nM and 260 nM, respectively. SR-1277 also inhibits FLT3, CDK4/cyclin D1, CDK6/cyclin D3 and CDK9/cyclin K, with IC50s of 305 nM, 1340 nM, 311 nM and 109 nM, respectively. SR-1277 can be used for the research of cancer .
    SR-1277
  • HY-122681

    Opioid Receptor Neurological Disease
    SR-16435 is a nociceptin/orphanin FQ (NOP)/μ-opioid receptor partial agonist, with high binding affinity (NOP receptor Ki=7.49; μ-Opioid receptor Ki=2.70). SR-16435 can relieve pain .
    SR-16435
  • HY-107596

    JNK Others
    SR-3576 is a highly potent and selective JNK3 inhibitor with an IC50 of 7 nM .
    SR-3576
  • HY-117248

    JNK p38 MAPK Neurological Disease
    SR-3737 is a JNK3 and p38 inhibitor (IC50: 12 and 3 nM) .
    SR-3737
  • HY-120785A

    ROR Inflammation/Immunology
    SR1555 hydrochloride is the hydrochloride salt form of SR1555 (HY-120785). SR1555 hydrochloride is an inverse agonist for retinoic acid receptor-related orphan nuclear receptor γ (RORγ) with an IC50 of 1 μM. SR1555 hydrochloride inhibits the development and function of pro-inflammatory TH17 cell, increases the frequency of anti-inflammatory T regulatory (Treg) cells. SR1555 hydrochloride can be used for research about autoimmune diseases .
    SR1555 hydrochloride
  • HY-115881

    PROTACs Cancer
    SR-1114 is a first-in-class PROTAC ENL degrader. SR-1114 elicits rapid, CRBN-dependent degradation of ENL with DC50s of 150 nM, 311 nM, and 1.65 μM in MV4;11 , MOLM-13, and OCI/AML-2 cells, respectively .
    SR-1114
  • HY-13751A

    Sigma Receptor Inflammation/Immunology
    SR-31747 free base is a sigma ligand with immunosuppressive and anti-inflammatory properties. SR-31747 blocks cell proliferation by inhibiting sterol isomerase .
    SR-31747 free base
  • HY-156458

    REV-ERB Inflammation/Immunology
    SR-29065 is a selective REV-ERBα agonist, can be used for autoimmune disorders research .
    SR-29065
  • HY-W841840

    Sirtuin Neurological Disease Cancer
    SR94, a SR17 derivative, is a SIRT2 inhibitor that contains an arbitrary 6-member ring and different R2 groups. SR94 is promising for research of cancer, ischemia-reperfusion and neurodegenerative diseases .
    SR94
  • HY-15870
    SR 11302
    5 Publications Verification

    AP-1 Inflammation/Immunology Cancer
    SR 11302 is an activator protein-1 (AP-1) transcription factor inhibitor. SR 11302 is a retinoid that specifically inhibits AP-1 activity without activating the transcription of retinoic acid response element (RARE) .
    SR 11302
  • HY-107664

    Neurotensin Receptor Neurological Disease
    SR 142948 is an orally active and selective non-peptide neurotensin receptor (NT) antagonist with IC50s of 1.19 nM, 0.32 nM, 3.96 nM in h-NTR1-CHO cells, HT-29 cells, and adult rat brain, respectively. SR 142948 antagonizes NT-induced inositol monophosphate formation in HT-29 cells with an IC50 of 3.9 nM. SR 142948 blocks hypothermia, analgesia and steering behavior induced by NT in vivo. SR 142948 shows blood-brain permeability and can be used in study of psychiatric disorders .
    SR 142948
  • HY-107664A

    Neurotensin Receptor Neurological Disease
    SR 142948 dihydrochloride is an orally active and selective non-peptide neurotensin receptor (NT) antagonist with IC50s of 1.19 nM, 0.32 nM, 3.96 nM in h-NTR1-CHO cells, HT-29 cells, and adult rat brain, respectively. SR 142948 dihydrochloride antagonizes NT-induced inositol monophosphate formation in HT-29 cells with an IC50 of 3.9 nM. SR 142948 dihydrochloride blocks hypothermia, analgesia and steering behavior induced by NT in vivo. SR 142948 dihydrochloride shows blood-brain permeability and can be used in study of psychiatric disorders .
    SR 142948 dihydrochloride
  • HY-131454
    SR-717
    10+ Cited Publications

    STING Inflammation/Immunology Cancer
    SR-717 is a non-nucleotide STING agonist with EC50s of 2.1 μM and 2.2 μM in ISG-THP1 (WT) and ISG-THP1 cGAS KO (cGAS KO) cell lines, respectively. SR-717 is a stable cyclic guanosine monophosphate-adenosine monophosphate (cGAMP) mimetic. Antitumor activity .
    SR-717
  • HY-13300A

    ROCK Autophagy Cancer
    SR-3677 dihydrochloride (compound 5) is a potent and selective ROCK-I and ROCK-II inhibitor with an IC50 values of 56 nM and 3 nM .
    SR-3677 dihydrochloride
  • HY-117413

    ULK Cancer
    SR-17398 is an inhibitor for Unc-51-Like Kinase 1 (ULK1) with an IC50 of 22.4 μM .
    SR-17398
  • HY-130250
    SR-4835
    10+ Cited Publications

    CDK Apoptosis Cancer
    SR-4835 is a potent, highly selective and ATP competitive dual inhibitor of CDK12/CDK13 (CDK12: IC50=99 nM, Kd=98 nM; CDK13: Kd=4.9 nM). SR-4835 acts in synergy with DNA-damaging chemotherapy and PARP inhibitors and provokes triple-negative breast cancer (TNBC) cell death .
    SR-4835
  • HY-161362

    PI3K Cancer
    SR-3-65 (compound 6) is a Indisulam (HY-13650) derivative,and inhibits the migration of gastric cancer cells. SR-3-65 attenuates PI3K/AKT/GSK-3β/β-catenin signaling pathway .
    SR-3-65
  • HY-118961

    Kinesin Cancer
    SR31527 chloride is a potent KIFC1 inhibitor with an IC50 value of 6.6 µM. SR31527 chloride decreases cell viability and colony formation .
    SR31527 chloride
  • HY-117516

    REV-ERB Neurological Disease Metabolic Disease
    SR10067 is a potent, selective and brain penetrant REV-ERB agonist. SR10067 has high affinity for Rev-Erbβ and Rev-Erbα with IC50 values of 160 nM and 170 nM, respectively. SR10067 can be used for the research of metabolic diseases and neuropsychiatric disorders .
    SR10067
  • HY-11077

    Cholecystokinin Receptor Metabolic Disease Endocrinology
    SR 146131 is a potent, orally available, and selective nonpeptide (cholecystokinin 1) receptor agonist.
    SR 146131
  • HY-136909

    Calcium Channel Cardiovascular Disease
    SR33805 is a potent Ca 2+ channel antagonist, with EC50s of 4.1 nM and 33 nM in depolarized and polarized conditions, respectively. SR33805 blocks L-type but not T-type Ca 2+ channels. SR33805 can be used for the research of acute or chronic failing hearts .
    SR33805
  • HY-123936

    NF-κB IKK Neurological Disease Inflammation/Immunology
    SR12343, an IKK/NF-κB inhibitor, is a NF-κB essential modulator (NEMO)-binding domain (NBD) mimetic. SR12343 inhibits TNF-α- and LPS-induced NF-κB activation by blocking the interaction between IKKβ and NEMO, with an IC50 of 37.02 μM for TNF-α-mediated NF-κB activation. SR12343 suppresses LPS-induced acute pulmonary inflammation in mice. SR12343 can be used for research of inflammatory and degenerative diseases .
    SR12343
  • HY-120456

    Opioid Receptor Neurological Disease
    SR16835 has high affinity for both NOPr and MOPr, with full agonist activity for NOPr and partial agonist activity for MOPr. SR16835 has no analgesic effect .
    SR16835
  • HY-14415
    SR8278
    5+ Cited Publications

    REV-ERB Neurological Disease Metabolic Disease
    SR8278 is a REV-ERBα antagonist and inhibits the REV-ERBα transcriptional repression activity with an EC50 of 0.47 μM. SR8278 is used to regulate the metabolism in organisms and study biological rhythm. SR8278 also can be used for the research of Duchenne muscular dystrophy and Alzheimer's disease .
    SR8278
  • HY-100011
    SR-3029
    2 Publications Verification

    Casein Kinase Cancer
    SR-3029 is a potent and ATP competitive CK1δ and CK1ε inhibitor, with IC50s of 44 nM and 260 nM, respectively, and Kis of 97 nM for both kinases.
    SR-3029
  • HY-131454A

    STING Inflammation/Immunology Cancer
    SR-717 free acid is a non-nucleotide STING agonist with EC50s of 2.1 μM and 2.2 μM in ISG-THP1 (WT) and ISG-THP1 cGAS KO (cGAS KO) cell lines, respectively. SR-717 free acid is a stable cyclic guanosine monophosphate-adenosine monophosphate (cGAMP) mimetic. Antitumor activity .
    SR-717 free acid
  • HY-112247

    PPAR Metabolic Disease
    SR 16832 is a dual site covalent PPARγ inhibitor that acts at orthosteric and allosteric sites .
    SR 16832
  • HY-107610

    Leukotriene Receptor Inflammation/Immunology
    SR2640 (hydrochloride) is a potent and selective competitive leukotriene D4/leukotriene E4 antagonist. SR2640 can be used for researching the role of leukotrienes in human asthma .
    SR2640 hydrochloride
  • HY-121974

    Others Neurological Disease
    SR14150 is a partial agonist of the NOP receptor with high affinity. The biological activity of SR14150 makes it potentially useful for the development of a new generation of multi-target opioids designed to simultaneously improve analgesia and reduce side effects. The activity of SR14150 and its interaction with other opioid receptors may provide new inhibitory options for the management of chronic pain .
    SR14150
  • HY-B0209
    Metolazone
    1 Publications Verification

    SR-720-22

    Thrombin Cardiovascular Disease
    Metolazone (SR-720-22) is primarily used to treat congestive heart failure and high blood pressure.
    Metolazone
  • HY-124767

    Others Neurological Disease
    SR 142948A is a non-peptide neuropeptide neuropeptin (NT) receptor antagonist. SR 142948A is able to bind to neuropeptin receptors, especially with high affinity for NT1 and NT2 receptors. SR 142948A is mainly used to study the role of neuropeptide in the neurotransmitter system, especially the dopamine system .
    SR 142948A
  • HY-120785

    ROR Inflammation/Immunology
    SR1555 is a specific retinoic acid receptor-related orphan nuclear receptor γ (RORγ) inverse agonist with an IC50 value of 1 μM. SR1555 not only inhibits TH17 cell development and function but also increases the frequency of T regulatory cells, as well as inhibits the expression of IL-17. SR1555 can be used for researching autoimmune diseases .
    SR1555
  • HY-107679

    nAChR Neurological Disease
    SR 16584 is a selective antagonist of α3β4 nAChR with an IC50 of 10.2 μM .
    SR 16584
  • HY-12483

    PPAR Metabolic Disease
    SR1664 is a PPARγ antagonist. SR1664 binds to PPARγ and potently inhibits Cdk5-mediated PPARγ phosphorylation (IC50=80 nM; Ki= 28.67 nM) .
    SR1664
  • HY-160162

    PPAR Metabolic Disease
    SR 11023 is an orally active antagonist of PPARγ, with the IC50 value of 109 nM that plays an important role in diabetic research .
    SR 11023

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