reversal

Sugammadex sodium (Org25969) , a synthetic derivative of γ-cyclodextrin, is a steroid-based neuromuscular blocker reversing agent.

Rubone (2'-Hydroxy-2,4,4',5,6'-pentamethoxychalcone), a natural product and a modulator of miR-34a (microRNA-34), upregulates miR-34a expression in a p53-dependent manner, which in turn downregulates the expression of downstream targets Bcl-2, cyclin-D1, CDK6, SIRT1, and FOXP1, thereby inhibiting tumor growth and reversal of hepatocellular carcinoma (HCC) and chemoresistance in prostate cancer.

1. Pristimerin (Celastrol methyl ester) has anticancer activity , treatment with Pristimerin may be a potential strategy for the suppression of hypoxia-induced metastasis through the reversal of hypoxia-induced stem cell characteristics and EMT in cancer cells. 2. Pristimerin down-regulates the expression of pro-inflammatory mediators through blocking of NF-κB activation by inhibiting interconnected ROS IKK NF-κB signaling pathways, can effectively inhibit both arthritic inflammation and cartilage and bone damage in the joints.

1-Methyladenine is a DNA alkylation product that undergoes damage reversal through oxidative demethylation for repair purposes.

Ciraparantag is an inhibitor of thrombin and factor Xa. Ciraparantag is a broad-spectrum reversal agent for anticoagulants, including unfractionated heparin, low-molecular-weight heparin, and certain direct oral anticoagulants.

Ciraparantag TFA is an inhibitor of thrombin and factor Xa. Ciraparantag is a broad-spectrum reversal agent for anticoagulants, including unfractionated heparin, low-molecular-weight heparin, and certain direct oral anticoagulants.

Ciraparantag acetate, an anticoagulant reversal agent, is a small molecule specifically designed to bind noncovalently by charge-charge interaction to unfractionated heparin and low-molecular-weight heparin. It shows binding characteristics that are similar to those of direct oral anticoagulants (DOACs).

Resorcinolnaphthalein is a specific enhancer of angiotensin-converting enzyme 2 (ACE2) (EC50 value of 19.5 μM).

ABCB1-IN-2 (compound 16q) is a functional inhibitor that directly binds and stabilizes the ABCB1 protein structure without altering its expression and subcellular localization. This compound enhances the sensitivity of MCF-7 ADR cells to paclitaxel (PTX) by increasing PTX accumulation and inhibiting the ABCB1-mediated accumulation and excretion of luciferin Rh123. As a potent ABCB1-mediated multidrug resistance (MDR) reversal agent, ABCB1-IN-2 effectively reverses MDR.

DOCP (2-((2,3-Bis(oleoyloxy)propyl)dimethylammonio)ethyl hydrogen phosphate) is a lipid characterized by an opposite charge orientation compared to traditional phosphatidylcholine (PC) lipids, featuring quaternary ammonium near the bilayer interface and phosphate groups projecting into the aqueous environment. This unique structure of iPC lipids presents an excellent opportunity to investigate the biophysical characteristics and biological activities influenced by the reversal of surface charges on bilayers.

Prenoverine is a diphenylmethanol derivative with effective multidrug resistance reversal activity.

Acerinol is an active ingredient from traditional Chinese medicinal herbs. It could be used as a cancer multidrug resistance reversal agent. Acerinol can significantly stimulate the activity of ABCB1 ATPase without affecting the expression of ABCB1 on nei

trans-Trimethoxyresveratrol (MR-3), a natural methoxylated analog of resveratrol, inhibits breast Y cell invasiveness by downregulation of PI3K Akt and Wnt β-catenin signaling cascades and reversal of epithelial-mesenchymal transition.

Simetride is used in the Reversal of resistance to vincristine in P388 leukemia.

Deacetylforskolin is a diterpene and a derivative of forskolin that has been found inC. forskohliiand has diverse biological activities.1,2,3,4It activates rat adipocyte adenylyl cyclase (IC50= 20 μM) and inhibits glucose transport in rat adipocyte plasma membranes.2Deactylforskolin (30-1,000 μg/kg) reduces blood pressure in spontaneously hypertensive rats.3It also attenuates hypercapnia-induced impairments in the passive avoidance response in mice.4 1.Gabetta, B., Zini, G., and Danieli, B.Minor Diterpenoids of Coleus forskohliiPhytochemistry28(3)859-862(1989) 2.Joost, H.G., Habberfield, A.D., Simpson, I.A., et al.Activation of adenylate cyclase and inhibition of glucose transport in rat adipocytes by forskolin analogues: structural determinants for distinct sites of actionMol. Pharmacol.33(4)449-453(1988) 3.Bhat, S.V., Dohadwalla, A.N., Bajwa, B.S., et al.The antihypertensive and positive inotropic diterpene forskolin: Effects of structural modifications on its activityJ. Med. Chem.26(4)486-492(1983) 4.McCulloch, A.J., Thomson, T.A., and Deacon, R.Hypoxic amnesia and its reversal with forskolinBiochem. Soc. Trans.17(1)212-213(1988)

Astragaloside II (Astrasieversianin VIII) is an effective MDR reversal agent and may be a potential adjunctive agent for hepatic cancer chemotherapy. Astragaloside II also induces osteogenic activities, differentiation, proliferation, and mineralization, through the bone morphogenetic protein-2 MAPK and Smad1 5 8 pathways.

1. Tectochrysin (Techtochrysine) has antioxidant effect. 2. Tectochrysin is promising inhibitors for the reversal of ABCG2-mediated drug transport. 3. Tectochrysin leads to apoptotic cell death in NSC-LC cells through activation of DR3 and Fas expression via inhibition of STAT3 phosphorylation.

Cinobufotalin is a main cardiac toxin in toad, it is a novel anti-HCC agent, it induces growth inhibition and apoptosis in cultured HCC cells through ceramide production. Cinobufotalin is also an effective reversal agent for the multidrug resistance of tu

Sugammadex is an agent for reversal of neuromuscular blockade by the agent rocuronium in general anaesthesia. It is the first selective relaxant binding agent (SRBA). Sugammadex is a modified γ-cyclodextrin, with a lipophilic core and a hydrophilic periph

1. Coptisine (Coptisin) treatment increases cell viability based on its reversal effect on the enhanced activity of Indoleamine 2, 3-dioxygenase . 2. Coptisine treats myocardial I R likely through suppressing myocardial apoptosis and inflammation by inhibiting the Rho ROCK pathway. 3. Coptisine is a potential anti-osteosarcoma drug candidate, via exerting a strong anti-osteosarcoma effect with very low toxicity . 4. Coptisine with a high dosage could inhibit cholesterol synthesis via suppressing the HMGCR expression and promoting the use and excretion of cholesterol via up-regulating LDLR and CYP7A1 expression. 5. Coptisine suppresses adhesion, migration and invasion of MDA-MB-231 breast cancer cells in vitro, the down-regulation of MMP-9 in combination with the increase of TIMP-1 possibly contributing to the anti-metastatic function for breast cancer.

OY-101, an orally active compound, serves as a potent and specific inhibitor of P-glycoprotein (P-gp). It has the capability to sensitize drug-resistant tumors and counteract tumor multidrug resistance efficiently. Compared to Tetrandrine [1], OY-101 demonstrates enhanced water-solubility, cytotoxicity, and reversal activity.

P-gp Inhibitor 3, an effective P-glycoprotein (P-gp) inhibitor, activates P-gp ATPase to inhibit P-gp's efflux function. It demonstrates a relatively stronger multidrug resistance (MDR) reversal ability, thereby enhancing the anti-tumor efficacy of Paclitaxel.

AcrB-IN-1 (Compound H6) is a potent inhibitor of AcrB, used to reverse bacterial multidrug resistance [1].

LL-37(17-32) is a biologically active peptide fragment derived from the C-terminal domain of human cathelicidin antimicrobial peptide. This segment reverses ABCG2-mediated multidrug resistance in cancer cell lines, highlighting its potential therapeutic role against drug resistance.