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Results for "(+)-JQ1 PA" in MCE Product Catalog:

58

Inhibitors & Agonists

1

Dye Reagents

6

Peptides

5

Natural
Products

Cat. No. Product Name Target Research Areas
  • HY-112789
    (+)-JQ1 PA

    Epigenetic Reader Domain Cancer
    (+)-JQ1 PA is a derivative of the Bromodomain and extra-terminal (BET) inhibitor JQ1, with an IC50 of 10.4 nM.
  • HY-13030
    (+)-JQ-1

    JQ1

    Epigenetic Reader Domain Autophagy Ligand for Target Protein for PROTAC Cancer
    (+)-JQ-1 (JQ1) is a potent, specific, and reversible BET bromodomain inhibitor, with IC50s of 77 and 33 nM for the first and second bromodomain (BRD4(1/2)). (+)-JQ-1 also activates autophagy.
  • HY-78695
    JQ-1 (carboxylic acid)

    Epigenetic Reader Domain Cancer
    JQ-1 carboxylic acid is a (+)-JQ1 derivative (a BET bromodomain inhibitor). JQ-1 carboxylic acid can be uesd as a precursor to synthesize PROTACs, which targets BET bromodomains.
  • HY-13030A
    (R)-(-)-JQ1 Enantiomer

    Epigenetic Reader Domain Cancer
    (R)-(-)-JQ1 Enantiomer is the stereoisomer of (+)-JQ1. (+)-JQ1 potently decreases expression of both BRD4 target genes, whereas (R)-(-)-JQ1 Enantiomer has no effect.
  • HY-129917
    KB02-JQ1

    PROTAC Epigenetic Reader Domain Cancer
    KB02-JQ1 is a highly selective and PROTAC-based BRD4 degrader (molecular glue), but does not degrade BRD2 or BRD3. KB02-JQ1 promotes BRD4 degradation by covalently modifying DCAF16 (E3 ligase) and can improve the durability of protein degradation in biological systems. JQ1 binds ubiquitin E3 ligase ligand KB02 via a linker to form KB02-JQ1.
  • HY-130256
    β-NF-JQ1

    PROTAC Epigenetic Reader Domain Cancer
    β-NF-JQ1 is a PROTAC that recruits AhR E3 ligase to target proteins. β-NF-JQ1 is directed against bromodomain-containing (BRD) proteins using β-NF as an AhR ligand, induces the interaction of AhR and BRD proteins, and displays effective anticancer activity that correlated with protein knockdown activity.
  • HY-111823
    VH032 thiol

    VHL ligand 6

    Ligand for E3 Ligase Cancer
    VH032 thiol (VHL ligand 6) is a VHL ligand, which binds to pan-BET inhibitor JQ1 via a linker to form PROTAC.
  • HY-100696
    PNZ5

    Epigenetic Reader Domain Cancer
    PNZ5 is a potent and isoxazole-based pan-BET inhibitor with high selectivity and potency similar to the well-established (+)-JQ1, with a KD of 5.43 nM for BRD4(1).
  • HY-101838
    dBET1

    PROTAC Epigenetic Reader Domain Cancer
    dBET1 is a potent BRD4 protein degrader based on PROTAC technology with an EC50 of 430 nM. dBET1 is a PROTAC that composes of (+)-JQ1 (HY-13030) linked to NSC 527179 (HY-14658) with a linker.
  • HY-111875
    SNIPER(BRD)-1

    SNIPER Epigenetic Reader Domain Cancer
    SNIPER(BRD)-1, consists of an IAP antagonist LCL-161 derivative and a BET inhibitor, (+)-JQ-1, connected by a linker. SNIPER(BRD)-1 induces the degradation of BRD4 via the ubiquitin-proteasome pathway. SNIPER(BRD)-1 also degrades cIAP1 , cIAP2 and XIAP with IC50s of 6.8 nM, 17 nM, and 49nM, respectively.
  • HY-130842
    β-Naphthoflavone-CH2-Br

    β-NF-CH2-Br

    Ligand for E3 Ligase Cancer
    β-Naphthoflavone-CH2-Br (β-NF-CH2-Br) is an arylhydrocarbon receptor (AhR) ligand. β-Naphthoflavone-CH2-Br can be used to synthesize the PROTAC β-NF-JQ1(HY-130256).
  • HY-W007545
    NH2-PEG3

    PROTAC Linker 35

    PROTAC Linker Cancer
    NH2-PEG3 (PROTAC Linker 35) is a PROTAC linker, which belongs to a polyethylene glycol (PEG) linker. NH2-PEG3 (PROTAC Linker 35) can be used in the synthesis of the PROTAC (β-NF-JQ1).
  • HY-114407
    TD-428

    PROTAC Epigenetic Reader Domain Cancer
    TD-428 is a highly specific BRD4 degrader with a DC50 of 0.32 nM. TD-428 is a BET PROTAC, which comprises TD-106 (a CRBN ligand) linked to JQ1 (a BET inhibitor). TD-428 efficiently induce BET protein degradation.
  • HY-112544
    IK1 inhibitor PA-6

    PA-6

    Potassium Channel Cardiovascular Disease
    IK1 inhibitor PA-6 (PA-6), a pentamidine analogue, is a selective and potent IK1 (KIR2.x ion-channel-carried inward rectifier current) inhibitor, with IC50 values of 12-15 nM for human and mouse KIR2.x currents. IK1 inhibitor PA-6 (PA-6) elevates KIR2.1 protein expression and induces intracellular KIR2.1 accumulation. IK1 inhibitor PA-6 (PA-6) has the potential to treat atrial fibrillation and arrhythmia.
  • HY-10844
    Pretomanid

    PA-824; (S)-PA 824

    Bacterial Antibiotic Infection Cancer
    Pretomanid (PA-824) is an antibiotic used for the research of multi-drug-resistant tuberculosis affecting the lungs. Pretomanid exhibits a sub-micromolar MIC against M. tuberculosis (MTB). The MIC values of PA-824 against a panel of MTB pan-sensitive and Rifampin mono-resistant clinical isolates range from 0.015 to 0.25 µg/mL.
  • HY-130269
    β-Naphthoflavone-CH2-OH

    β-NF-CH2-OH

    Ligand for E3 Ligase Cancer
    β-Naphthoflavone-CH2-OH (β-NF-CH2-OH) is a ligand for arylhydrocarbon receptor (AhR) E3 ligase. β-Naphthoflavone-CH2-OH can be connected to the ligand for protein by a linker to form PROTACs or SNIPERs (e.g., β-naphthoflavone-JQ1) that recruit the AhR E3 ligase complex by incorporating AhR ligands into chimeric molecules. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins [1].
  • HY-108522
    PA452

    RAR/RXR Metabolic Disease
    PA452, retinoic X receptor (RXR) specific antagonist, inhibits the effect of Retinoic acid (RA) on Th1/Th2 development.
  • HY-133534
    PA-Nic TFA

    Others Others
    PA-Nic TFA is a photoactivatable nicotine, whcih can be photolyzed with ~405 nm laser flashes to efficiently release nicotine.
  • HY-P1580
    PA (224-233), Influenza

    Influenza Virus Infection
    PA (224-233), Influenza is a 10-aa peptide, a fragment of polymerase 2 protein in influenza A virus.
  • HY-133535
    PA-JF646-NHS

    Others
    PA-JF646-NHS, a photoactivatable fluorescent dye, is an NHS ester for coupling to primary amine groups. PA-JF646-NHS is non-fluorescent until activated at 365 nm. NHS ester can be converted to relevant substrate for use in self-labeling tag systems, e.g.HaloTag ® and SNAP-tag ®. PA-JF646-NHS is used for single molecule tracking and super resolution microscopy in live cells, specifically live cell sptPALM and fixed cell PALM. (λExcitation/emission~650/664 nm).
  • HY-W013549
    6-Aminopenicillanic acid

    6-APA

    Bacterial Infection
    6-Aminopenicillanic acid (6-APA) is an important precursor for the synthesis of -lactam antibiotics. 6-Aminopenicillanic acid is the main product of Penicillin G (PenG) hydrolyzed by penicillin acylase (PA).
  • HY-129968
    AM-Imidazole-PA-Boc

    PROTAC Linker Cancer
    AM-Imidazole-PA-Boc is an alkyl chain-based PROTAC linker can be used in the synthesis of PROTAC IRAK4 degrader-1 (HY-129966).
  • HY-N0842
    Bevirimat

    PA-457; MPC-4326; YK FH312

    HIV Infection
    Bevirimat (PA-457; MPC-4326; YK FH312) is an anti-HIV drug derived from a betulinic acid-like compound; is believed to inhibit HIV by a novel mechanism, so-called maturation inhibition.
  • HY-41919
    Mal-L-PA-NH-Boc

    mDPR(boc)

    ADC Linker Cancer
    Mal-L-PA-NH-Boc is a noncleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
  • HY-I0508
    Phthalic acid

    Others Others
    Phthalic acid is the final common metabolite of phthalic acid esters (PAEs). Phthalic acid can be used for the synthesis of synthetic agents, such as isophthalic acid (IPA), and terephthalic acid (TPA). Phthalic acid has applications in the preparation of phthalate ester plasticizers.
  • HY-N0478
    Neoline

    Bullatine B

    Others Neurological Disease
    Neoline, the active ingredient of processed aconite root (PA), alleviated oxaliplatin-induced peripheral neuropathy in mice. Neoline can be used as a marker compound to determine the quality of the PA products for the treatment of neuropathic pain.
  • HY-112684
    RO-7

    Influenza Virus Infection
    RO-7 is a next-generation polymerase (PA) endonuclease inhibitor of influenza A and B viruses.
  • HY-100152
    Beperidium iodide

    SX 810

    mAChR Inflammation/Immunology
    Beperidium iodide shows a competitive antagonistic effect against acetylcholine receptor with a pA2 of 7.93.
  • HY-101232
    Tiotidine

    ICI 125211

    Histamine Receptor Cardiovascular Disease
    Tiotidine (ICI 125211) is a potent and selective antagonist of histamine H2-receptor (pA2=7.3-7.8 for guinea-pig right atrium). Tiotidine has low affinity for both the H1 and the H3 receptors.
  • HY-110385
    cGAMP disodium

    Cyclic GMP-AMP disodium; 3',3'-cGAMP disodium

    Endogenous Metabolite Inflammation/Immunology
    cGAMP disodium (Cyclic GMP-AMP disodium) is the third cyclic dinucleotide (CDN) to be discovered in bacteria. cGAMP disodium is an effective adjuvant for sublingual vaccination capable of promoting broad immunity including serum anti-PA neutralizing and anti-PA SIgA responses in airway secretions.
  • HY-15010
    L-371,257

    Oxytocin Receptor Vasopressin Receptor Endocrinology
    L-371,257 is an orally bioavailable, non-blood-brain barrier penetrant, selective and competitive antagonist of oxytocin receptor (pA2=8.4) with high affinity at both the oxytocin receptor (Ki=19 nM) and vasopressin V1a receptor (Ki=3.7 nM).
  • HY-117319
    Indolmycin

    TAK-083; PA-155A

    Antibiotic Bacterial Infection Inflammation/Immunology
    Indolmycin (TAK-083), an antibiotic, is a competitive inhibitor of prokaryotic tryptophanyl-tRNA ligase (TrpS). Indolmycin (TAK-083) possesses both anti-viral and anti-bacterial activity.
  • HY-P1017
    MDL 29913

    Neurokinin Receptor Neurological Disease Cardiovascular Disease
    MDL 29913, a cyclic pseudopeptide, is a competitive NK2 tachykinin receptor selective antagonist, with a pA2 of 8.66.
  • HY-128780
    SPR206

    Bacterial Cancer Infection
    SPR206 is a polymyxin analogue and an important class of antibiotic for the treatment of bacterial infections due to multidrug resistant Gram-negative pathogen. The MIC values of SPR206 against Pseudomonas aeruginosa Pa14 (MIC value of for Pa14) and Acinetobacter baumannii NCTC13301 are 0.125 mg/L and 0.125 mg/L, respectively.
  • HY-17351
    Tezosentan

    RO 610612

    Endothelin Receptor Cancer Neurological Disease Cardiovascular Disease Endocrinology
    Tezosentan (RO 610612) is an endothelin (ET) receptor antagonist, with pA2s of 9.5, 7.7 for ETA and ETB receptors, respectively.
  • HY-U00355
    YM158 free base

    YM-57158

    Leukotriene Receptor Prostaglandin Receptor Inflammation/Immunology Endocrinology
    YM158 free base is a potent and selective LTD4 and TXA2 receptor antagonist with pA2 values of about 8.87 and 8.81, respectively.
  • HY-101336
    RS 17053 hydrochloride

    RS-17053

    Adrenergic Receptor Metabolic Disease Endocrinology
    RS 17053 hydrochloride is a potent and selective α1A adrenoceptor antagonist, with a pKi value of 9.1 in native cell membrane and a pA2 value of 9.8 in functional assays.
  • HY-128850
    N-Acetyl-D-mannosamine

    N-Acetylmannosamine; ManNAc

    Bacterial Neurological Disease
    N-Acetyl-D-mannosamine (ManNAc) is an essential precursor of N-acetylneuraminic acid (NeuAc), the specific monomer of bacterial capsular polysialic acid (PA). N-Acetyl-D-mannosamine (ManNAc) can be metabolized by GNE and GlcNAc 2-epimerase (Renin binding protein, RnBP), into ManNAc-6-phosphate and GlcNAc, respectively.  N-Acetyl-d-mannosamine (ManNAc) and its derivatives activates hypocretin (HCRT) gene expression in the orexin neurons, providing a potential model for the testing of a therapy for neural disorders.
  • HY-109025A
    Baloxavir

    Baloxavir acid; S-033447

    Influenza Virus Infection
    Baloxavir (Baloxavir acid) is a first-in-class, potent and selective cap-dependent endonuclease (CEN) inhibitor within the polymerase PA subunit of influenza A and B viruses. Baloxavir inhibits viral RNA transcription and replication and has potently antiviral activity.
  • HY-15895
    Aprocitentan

    ACT-132577

    Endothelin Receptor Cardiovascular Disease Endocrinology
    Aprocitentan (ACT-132577) is the major and pharmacologically active metabolite of Macitentan. Aprocitentan is dual ETA/ETB antagonist with IC50s of 3.4 nM and 987 nM, and pA2 valus of 6.7 and 5.5, respectively.
  • HY-N1919
    Ajmalicine

    Raubasine

    Adrenergic Receptor AChE Cardiovascular Disease Endocrinology
    Ajmalicine (Raubasine) is found in herbs of Catharanthus roseus, is an antihypertensive drug used in the treatment of high blood pressure, decreases peripheral resistance and blood pressure. Ajmalicine (Raubasine) is an adrenolytic drug which preferentially blocks alpha 1-adrenoceptor than alpha 2-adrenoceptor. Ajmalicine (Raubasine) is an reversible non-competitive nicotine receptor antagonist with an IC50 of 72.3 μM. Ajmalicine (Raubasine) acts preferentially at postsynaptic sites, competitively antagonizes the effect of noradrenaline on postsynaptic alpha-adrenoceptor with a pA2 value of 6.57, blocks the inhibitory effect of clonidine with an pA2 value of 6.2.
  • HY-125263
    OP-1074

    Estrogen Receptor/ERR Cancer
    OP-1074 is a pure antiestrogen and a selective ER degrader (PA-SERD), shows specific antiestrogenic activity for ERα and ERβ, inhibits 17β-estradiol (E2)-stimulated transcriptional activity with IC50 of 1.6 and 3.2 nM, respectively.
  • HY-P1320A
    [Nphe1]Nociceptin(1-13)NH2 TFA

    Opioid Receptor Inflammation/Immunology
    [Nphe1]Nociceptin(1-13)NH2, a novel nociceptin/orphanin FQ (NC) endogenous ligand, is a selective and competitive ociceptin receptor antagonist without any residual agonist activity. [Nphe1]nociceptin(1-13)NH2 binds selectively to recombinant nociceptin receptors (pKi=8.4) and antagonizes the inhibitory effects of nociceptin on cyclic AMP accumulation in CHO cells (pA2=6.0). [Nphe1]Nociceptin(1-13)NH2 has the potential to act as an analgesic agent.
  • HY-P1320
    [Nphe1]Nociceptin(1-13)NH2

    Opioid Receptor Inflammation/Immunology
    [Nphe1]Nociceptin(1-13)NH2, a novel nociceptin/orphanin FQ (NC) endogenous ligand, is a selective and competitive ociceptin receptor antagonist without any residual agonist activity. [Nphe1]nociceptin(1-13)NH2 binds selectively to recombinant nociceptin receptors (pKi=8.4) and antagonizes the inhibitory effects of nociceptin on cyclic AMP accumulation in CHO cells (pA2=6.0). [Nphe1]Nociceptin(1-13)NH2 has the potential to act as an analgesic agent.
  • HY-P1143
    [Des-His1,Glu9]-Glucagon amide

    Glucagon Receptor Metabolic Disease
    [Des-His1,Glu9]-Glucagon amide is a potent and peptide antagonist of the glucagon receptor, with a pA2 of 7.2. [Des-His1,Glu9]-Glucagon amide is potentially useful in the study of the pathogenesis of diabetes.
  • HY-15895S
    Aprocitentan D4

    ACT-132577 D4

    Endothelin Receptor Endocrinology Cardiovascular Disease
    Aprocitentan D4 (ACT-132577 D4) is a deuterium labeled Aprocitentan. Aprocitentan is a major and pharmacologically active metabolite of Macitentan. Aprocitentan is dual ETA/ETB antagonist with IC50s of 3.4 nM and 987 nM, and pA2 valus of 6.7 and 5.5, respectively.
  • HY-P1143A
    [Des-His1,Glu9]-Glucagon amide TFA

    Glucagon Receptor Metabolic Disease
    [Des-His1,Glu9]-Glucagon amide TFA is a potent and peptide antagonist of the glucagon receptor, with a pA2 of 7.2. [Des-His1,Glu9]-Glucagon amide TFA is potentially useful in the study of the pathogenesis of diabetes.
  • HY-100988
    Methylergometrine maleate

    Methylergonovine maleate; Ryegonovin; SPAmetrin F

    5-HT Receptor Neurological Disease
    Methylergometrine maleate (Methylergonovine maleate) is an ergot alkaloid and an active metabolite of Methysergide with vasoconstrictive and uterotonic activity. Methylergometrine maleate is a potent, selective and orally active 5-HT receptors antagonist with a pA2 value of 9.6. Methylergometrine maleate has antimigraine and dopaminergic activity. Methylergometrine maleate can used for the prevention and control of postpartum hemorrhage.
  • HY-19432
    UBP-282

    iGluR Neurological Disease
    UBP-282 is a potent, selective and competitive AMPA and kainate receptor antagonist. UBP-282 inhibits the fast component of the dorsal root-evoked ventral root potential (fDR-VRP) with an IC50 value of 10.3 μM. UBP-282 antagonizes kainate-induced depolarisations of dorsal roots with a pA2 value of 4.96.
  • HY-105189
    Meclinertant

    SR 48692

    Neurotensin Receptor Neurological Disease
    Meclinertant (SR 48692) is a potent, selective, nonpeptide and orally active neurotensin receptor 1 (NTS1) antagonist. In human colon carcinoma (HT-29) cells, Meclinertant competitively antagonizes neurotensin-induced intracellular Ca 2+ mobilization with a pA2 values of 8.13. Meclinertant has anxiolytic, anti-addictive and memory-impairing effects.
  • HY-76569
    Desfesoterodine

    PNU-200577; 5-Hydroxymethyl Tolterodine

    mAChR Neurological Disease
    Desfesoterodine (PNU-200577) is a potent and selective muscarinic receptor (mAChR) antagonist with a KB and a pA2 of 0.84 nM and 9.14, respectively. Desfesoterodine is a major pharmacologically active metabolite of Tolterodine (PNU-200583; HY-A0024) and Fesoterodine (HY-70053). Desfesoterodine improves cerebral infarction induced detrusor overactivity in rats.
  • HY-N0801
    Polygalacic acid

    MMP AChE Inflammation/Immunology Neurological Disease
    Polygalacic acid, is a triterpene, isolated from the root of Polygala tenuifolia Willd. Polygalacic acid inhibits MMP expression. Polygalacic acid may have a therapeutic effect in Osteoarthritis (OA) treatment [1]. Polygalacic acid exerts a significant neuroprotective effect on cognitive impairment, PA improves cholinergic system reactivity by inhibiting acetylcholinesterase (AChE) activity, increasing choline acetyltransferase (ChAT) activity, and elevating levels of acetylcholine (Ach) in the hippocampus and frontal cortex.
  • HY-100634
    4-Hydroxypropranolol hydrochloride

    (±)-4-hydroxy Propranolol hydrochloride

    Adrenergic Receptor Neurological Disease
    4-Hydroxypropranolol hydrochlorid is an active metabolite of Propranolol. 4-Hydroxypropranolol hydrochlorid is of comparable potency to Propranolol. 4-Hydroxypropranolol hydrochlorid inhibits β1- and β2-adrenergic receptors with pA2 values of 8.24 and 8.26, respectively. 4-Hydroxypropranolol hydrochlorid has intrinsic sympathomimetic activity, membrane stabilizing activity and potent antioxidant properties.
  • HY-101189
    JNJ-39758979

    Histamine Receptor Neurological Disease Endocrinology
    JNJ-39758979 is a selective, orally active, and high-affinity histamine H4 receptor antagonist with Kis of 12.5, 5.3, and 25 nM for human, mouse, and monkey histamine H4 receptor, respectively. JNJ-39758979 functionally antagonizes histamine-induced cAMP inhibition with a pA2 of 7.9 in transfected cells. JNJ-39758979 shows good anti-inflammatory and antipruritic activity.
  • HY-101189B
    JNJ-39758979 dihydrochloride

    Histamine Receptor Inflammation/Immunology
    JNJ-39758979 dihydrochloride is a selective, orally active, and high-affinity histamine H4 receptor antagonist, with Kis of 12.5, 5.3, and 25 nM for human, mouse, and monkey histamine H4 receptor, respectively. JNJ-39758979 dihydrochloride functionally antagonizes histamine-induced cAMP inhibition with a pA2 of 7.9 in transfected cells. JNJ-39758979 dihydrochloride shows good anti-inflammatory and antipruritic activity.
  • HY-100634S
    4-Hydroxypropranolol D7 hydrochloride

    (±)-4-hydroxy Propranolol D7 hydrochloride

    Adrenergic Receptor Neurological Disease
    4-Hydroxypropranolol D7 hydrochloride ((±)-4-hydroxy Propranolol D7 hydrochloride) is a deuterium labeled 4-Hydroxypropranolol hydrochloride. 4-Hydroxypropranolol hydrochlorid is an active metabolite of Propranolol, with potency comparable to Propranolol. 4-Hydroxypropranolol hydrochlorid inhibits β1- and β2-adrenergic receptors with pA2 values of 8.24 and 8.26, respectively. 4-Hydroxypropranolol hydrochlorid has intrinsic sympathomimetic activity, membrane stabilizing activity and potent antioxidant properties.
  • HY-101308
    MRS2179 tetrasodium

    P2Y Receptor Cardiovascular Disease
    MRS2179 tetrasodium is a competitive P2Y1 receptor antagonist, with a Kb of 102 nM and a pA2 of 6.99 for turkey P2Y1 receptor. MRS2179 tetrasodium is selective for P2Y1 over P2X1 (IC50=1.15 µM), P2X3 (12.9 µM), P2X2, P2X4, P2Y2, P2Y4, and P2Y6 receptors. MRS2179 tetrasodium inhibits platelet aggregation.
  • HY-10349
    WAY-100635

    5-HT Receptor Dopamine Receptor Neurological Disease
    WAY-100635 is a potent and selective 5-HT1A Receptor antagonist with a pIC50 of 8.87, an apparent pA2 of 9.71. WAY-100635 is a potent and selective 5-hydroxytryptamine 1A (5-HT1A) receptor antagonist with an IC50 value of 0.91 nM and Ki value of 0.39 nM. WAY-100635 has pIC50 values for 5-HT1A and α1-adrenergic receptors of 8.9 and 6.6, respectively. WAY-100635 is also a potent dopamine D4 receptor agonist.