128 Results for "

blockade

" in MedChemExpress (MCE) Product Catalog:
Products (128)

128 Results for "blockade" in MCE Product Catalog:

35
35 Publications Verification
Art. -Nr.: HY-P9902A
Synonyms: MK-3475 (anti-PD-1); Lambrolizumab (anti-PD-1)

Target:  

PD-1/PD-L1

Forschungsgebiete:  

Cancer

Pembrolizumab (anti-PD-1) is a humanized IgG4 antibody and PD-1 inhibitor. Pembrolizumab produces PD-1 blockade, preventing PD-L1 and PD-L2 from connecting to PD-1. This avoids the uncontrolled regulation of T cells on cells that normally express PD-1 .
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15
15 Cited Publications
Art. -Nr.: HY-13650
CAS. Nr.: 165668-41-7
Reinheit:  99.80%
Synonyms: E 7070
Forschungsgebiete:  

Cancer

Indisulam (E 7070) is a carbonic anhydrase inhibitor with anticancer activity. Indisulam (E 7070) is a sulfonamide agent that targets the G1 phase of the cell cycle. Indisulam (E 7070) causes a blockade in the G1/S transition through inhibition of the activation of both CDK2 and cyclin E. Indisulam (E 7070) targets splicing by inducing RBM39 degradation via recruitment to DCAF15 .
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6
6 Cited Publications
Art. -Nr.: HY-16961
CAS. Nr.: 1123837-84-2
Synonyms: MGCD516; MG-516
Sitravatinib (MGCD516) is an orally bioavailable receptor tyrosine kinase (RTK) inhibitor with IC50s of 1.5 nM, 2 nM, 2 nM, 5 nM, 6 nM, 6 nM, 8 nM, 0.5 nM, 29 nM, 5 nM, and 9 nM for Axl, MER, VEGFR3, VEGFR2, VEGFR1, KIT, FLT3, DDR2, DDR1, TRKA, TRKB, respectively . Sitravatinib shows potent single-agent antitumor efficacy and enhances the activity of PD-1 blockade through promoting an antitumor immune microenvironment .
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4
4 Cited Publications
Art. -Nr.: HY-156677
CAS. Nr.: 2648257-56-9
Reinheit:  99.90%
Target:  

METTL3

Forschungsgebiete:  

Cancer

STC-15 is an orally active RNA methyltransferase METTL3 inhibitor with the activity of activating anti-tumor immunity and reshaping the tumor microenvironment. STC-15 inhibits tumor growth by activating anti-cancer immune responses associated with increased interferon signaling and synergizes with T-cell checkpoint blockade. STC-15 can be used in the study of proliferative diseases such as cancer and autoimmune diseases .
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3
3 Cited Publications
Art. -Nr.: HY-153346
CAS. Nr.: 2641998-63-0
Reinheit:  99.65%
Synonyms: RMC-6291
Target:  

Ras ERK Apoptosis

Forschungsgebiete:  

Cancer

Elironrasib is an orally active and covalent inhibitor of KRAS G12C(ON). Elironrasib forms a tri-complex within tumor cells between KRAS G12C(ON) and cyclophilin A (CypA). Thus, Elironrasib prevents KRAS G12C(ON) from signaling via steric blockade of RAS effector binding. Elironrasib inhibits ERK signaling and induced apoptosis in KRASG12C-mutant H358 cells. Elironrasib also inhibits the proliferation of KRAS G12C mutant cells with a median IC50 of 0.11 nM .
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2
2 Cited Publications
Art. -Nr.: HY-128679
CAS. Nr.: 1893397-65-3
Reinheit:  99.92%
Target:  

IKK

Forschungsgebiete:  

Cancer

TBK1/IKKε-IN-5 (compound 1) is an orally active TBK1 and IKKε dual inhibitor, with IC50 values of 1 and 5.6 nM, respectively. TBK1/IKKε-IN-5 enhances the blockade response to PD-1 and induces immune memory in rats when combines with anti-PD-L1. TBK1/IKKε-IN-5 can be used in cancer research, especially in tumour immunity .
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2
2 Cited Publications
Art. -Nr.: HY-B0653A
CAS. Nr.: 27262-48-2
Synonyms: (S)-(-)-Bupivacaine monohydrochloride
Levobupivacaine hydrochloride ((S)-(-)-Bupivacaine monohydrochloride) is a long-acting amide local agent that can suppress or relieve pain. Levobupivacaine hydrochloride exerts agent that can suppress or relieve pain. and analgesic effects through reversible blockade of neuronal sodium channel. Levobupivacaine hydrochloride can inhibit impulse transmission and conduction in cardiovascular and other tissues, possessing certain cardiac and CNS toxicity. Levobupivacaine hydrochloride is metabolized by hepatic cytochrome P450 (CYP450) enzymes in vivo. Levobupivacaine hydrochloride can also induce ferroptosis by miR-489-3p/SLC7A11 signaling in gastric cancer .
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2
2 Cited Publications
Art. -Nr.: HY-13954
CAS. Nr.: 870061-27-1
Reinheit:  98.08%
Target:  

P2X Receptor

A 839977 is a P2X7 selective antagonist; it blocks BzATP-evoked calcium influx at recombinant human, rat and mouse P2X7 receptors (IC50 values are 20 nM, 42 nM and 150 nM respectively) and reduces inflammatory and neuropathic pain in animal models; the antihyperalgesic effects of P2X7 receptor blockade are mediated by blocking the release of IL-1beta .
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2
2 Cited Publications
Art. -Nr.: HY-136310
CAS. Nr.: 2055405-95-1
Reinheit:  98.92%
Target:  

PI5P4K

Forschungsgebiete:  

Cancer

PIP4K-IN-a131 is PIP4K lipid kinases inhibitor, with IC50s of 1.9 μM and 0.6 μM for purified PIP4K2A and PIP4Ks, respectively. PIP4K-IN-a131 exhibits cancer-selective lethality via dual blockade of the lipid kinase PIP4Ks and mitotic pathways .
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2
2 Cited Publications
Art. -Nr.: HY-B0653
CAS. Nr.: 27262-47-1
Synonyms: (S)-(-)-Bupivacaine
Forschungsgebiete:  

Neurological Disease Cancer

Levobupivacaine ((S)-(-)-Bupivacaine) is a long-acting amide local agent that can suppress or relieve pain. Levobupivacaine exerts agent that can suppress or relieve pain. and analgesic effects through reversible blockade of neuronal sodium channel. Levobupivacaine can inhibit impulse transmission and conduction in cardiovascular and other tissues, possessing certain cardiac and CNS toxicity. Levobupivacaine is metabolized by hepatic cytochrome P450 (CYP450) enzymes in vivo. Levobupivacaine can also induce ferroptosis by miR-489-3p/SLC7A11 signaling in gastric cancer .
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1
1 Cited Publications
Art. -Nr.: HY-B0423
CAS. Nr.: 114-80-7
Synonyms: Eustigmin bromide; Neoserine bromide
Target:  

Cholinesterase (ChE)

Forschungsgebiete:  

Neurological Disease

Neostigmine (Eustigmin) Bromide is an orally active and reversible cholinesterase inhibitor that acts on myasthenia gravis to prolong and intensify the muscarinic and nicotinic effects of acetylcholine. Neostigmine Bromide can be used in anesthesia to reverse the neuromuscular blockade produced by competitive neuromuscular blockers .
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1
1 Cited Publications
Art. -Nr.: HY-129492
CAS. Nr.: 2041073-22-5
Reinheit:  99.78%
Target:  

DYRK GSK-3

Forschungsgebiete:  

Metabolic Disease

GNF4877 is a potent DYRK1A and GSK3β inhibitor with IC50s of 6 nM and 16 nM, respectively, which leads to blockade of nuclear factor of activated T-cells (NFATc) nuclear export and increased β-cell proliferation (EC50 of 0.66 μM for mouse β (R7T1) cells) .
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1
1 Cited Publications
Art. -Nr.: HY-N6636
CAS. Nr.: 4630-07-3
Valencene is a sesquiterpene that can be isolated from Cyperus rotundus. Valencene possesses antiallergic, antimelanogenesis, anti-infammatory, and antioxidant activitivies. Valencene inhibits the exaggerated expression of Th2 chemokines and proinflammatory chemokines through blockade of the NF-κB pathway. Valencene inhibits the production and expression of proinflammatory cytokines IL-1β and IL-6 in LPS-stimulated RAW 264.7 cells. Valencene can reduce atopic dermatitis symptoms and recover decreased expression of filaggrin in DNCB-sensitized mouse model .
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1
1 Cited Publications
Art. -Nr.: HY-B0292A
CAS. Nr.: 64228-81-5
Synonyms: BW-33A
Target:  

nAChR

Atracurium (BW-33A) besylate is a potent, competitive and non-depolarizing neuromuscular blocking agent. Atracurium besylate also is an AChR receptor antagonist. Atracurium besylate induces bronchoconstriction and neuromuscular blockade. Atracurium besylate promotes astroglial differentiation .
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1
1 Cited Publications
Art. -Nr.: HY-121276
CAS. Nr.: 2062-84-2
Reinheit:  ≥98.0%
Target:  

Dopamine Receptor

Forschungsgebiete:  

Neurological Disease

Benperidol is a relatively old antipsychotic agent. Benperidol is a butyrophenone antipsychotic, with the highest neuroleptic potency in terms of D2 receptor blockade .
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1
1 Cited Publications
Art. -Nr.: HY-141549
CAS. Nr.: 2305052-77-9
Reinheit:  99.56%
Forschungsgebiete:  

Inflammation/Immunology

BPK-21, an active acrylamide, suppresses T cell activation through blockade of ERCC3 function. BPK-21 specifically targets C342 in the helicase ERCC3 .
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1
1 Cited Publications
Art. -Nr.: HY-N2412
CAS. Nr.: 2345-17-7
Irisolidone is a major isoflavone found in Pueraria lobata flowers. Irisolidone exhibits potent hepatoprotective activity. Irisolidone shows the high efficacy for volume-regulated anion channels (VRAC) blockade (IC50=9.8 μM) .
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1
1 Cited Publications
Art. -Nr.: HY-12502
CAS. Nr.: 111011-63-3
Reinheit:  99.88%
Synonyms: NZ-105; (±)-Efonidipine
Efonidipine (NZ-105) is an orally active dual L-type and T-type calcium channel blocker (CCB) with IC50 values of 1.8 and 350 nM, respectively. Efonidipine inhibits SARS-CoV-2 main protease. Efonidipine modulates adrenal steroidogenesis by increasing the expression of steroidogenic acute regulatory protein (StAR), dbcAMP-or angiotensin II-induced StAR mRNA expression and DHEA-S production, while suppressing the biosynthesis of aldosterone and cortisol. Efonidipine reduces plasma aldosterone levels in vivo. Efonidipine improves cardiac function in heart failure models by inhibiting T-type calcium channels (via both tonic and use-dependent blockade), independently of blood pressure reduction. Efonidipine can be used for research in hypertension, heart failure, and disorders involving dysregulated steroid hormone synthesis .
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1
1 Cited Publications
Art. -Nr.: HY-12502A
CAS. Nr.: 111011-76-8
Reinheit:  99.28%
Synonyms: NZ-105 hydrochloride monoethanolate; (±)-Efonidipine hydrochloride monoethanolate
Efonidipine (NZ-105) hydrochloride monoethanolate is an orally active dual L-type and T-type calcium channel blocker (CCB) with IC50 values of 1.8 and 350 nM, respectively. Efonidipine hydrochloride monoethanolate inhibits SARS-CoV-2 main protease. Efonidipine hydrochloride monoethanolate modulates adrenal steroidogenesis by increasing the expression of steroidogenic acute regulatory protein (StAR), dbcAMP-or angiotensin II-induced StAR mRNA expression and DHEA-S production, while suppressing the biosynthesis of aldosterone and cortisol. Efonidipine hydrochloride monoethanolate reduces plasma aldosterone levels in vivo. Efonidipine hydrochloride monoethanolate improves cardiac function in heart failure models by inhibiting T-type calcium channels (via both tonic and use-dependent blockade), independently of blood pressure reduction. Efonidipine hydrochloride monoethanolate can be used for research in hypertension, heart failure, and disorders involving dysregulated steroid hormone synthesis .
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Art. -Nr.: HY-P99406
CAS. Nr.: 2213450-26-9
Synonyms: MCLA 158

Target:  

EGFR

Forschungsgebiete:  

Cancer

Petosemtamab (MCLA 158) is an anti- EGFR (Kd: 0.22 nM) and anti-LGR5 (Kd: 0.86 nM) monoclonal antibody (mAb). Petosemtamab leads to EGFR signaling blockade and receptor degradation in LGR5+ cancer cells. Petosemtamab can be used in the research of solid tumors, such as head and neck squamous cell carcinoma (HNSCC), metastatic colorectal cancer (CRC) .
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