Inhibitors

Questiomycin A derivative 18 TFA exhibits antibacterial, anticancer properties and inhibits GRP78.

Benzovindiflupyr: a fungicide that inhibits SDH (IC50=5.2nM), halts S. sclerotiorum growth (EC50=0.011μg/ml), and protects crops like eggplants.

HBV-IN-34 (compound 17i) is a potent inhibitor of HBsAg production, demonstrating remarkable in vitro anti-HBV efficacy with EC50 values of 0.018 μM for HBV DNA

EGFR-IN-82 (Compound 8a) is a potent, orally active inhibitor of EGFR, exhibiting IC50 values of 0.09 nM for EGFR L858R/T790M/C797S and 0.06 nM for EGFR Del19/

Saxitoxinol is an analog of saxitoxin, a known voltage-gated sodium channel blocker.

Lp-PLA2-IN-12 (compound 19), an Lp-PLA2 inhibitor, is utilized in researching neurodegenerative diseases including Alzheimer's disease (AD), glaucoma, age-

FGFR1 inhibitor-10 (Compound 4i), with an IC50 of 28 nM, effectively inhibits FGFR1 phosphorylation.

Mavodelpar free acid (REN001 free acid) is an selective agonist of PPARδ.

Radafaxine hydrochloride is an inhibitor of DAT and NET transporters, and nAChR family modulator.

DprE1-IN-8 is a potent inhibitor of DprE1, exhibiting an IC50 of less than 0.75 μM.

ALPK1-IN-2 is a potent inhibitor of ALPK1 (α-kinase 1) (IC50: 95 nM). ALPK1-IN-2 inhibits NF-κB (IC50: 1.31 μM).

"PPARγ-IN-2 (Compound 5a), a PPARγ inhibitor, exhibits an EC50 of 0.106 μM in inhibiting TG accumulation in 3T3-L1 preadipocytes.

ALPK1-IN-1 (A001) strongly inhibits ALPK1, key for innate immunity & NF-κB signaling via TIFA/TRAF.

Lp-PLA2-IN-15 (example 2) is an inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2) with potential application in Alzheimer's disease research [1].

Compound A8, known as JAK2-IN-9, is a selective JAK2 inhibitor with an IC50 of 5 nM.

Estrogen Receptor Modulator 8 (compound 4) is an orally active inhibitor targeting Estrogen Receptor/ERR α with potent efficacy (IC50 = 0.437 nM in MCF-7 cells

Mal-cyclohexane-Gly-Gly-Phe-Gly-Exatecan is a linker molecule employed in the synthesis of antibody-drug conjugates (ADCs), demonstrating potent antitumor

DPP, a Platinum(IV) complex with a pterostilbene-derived axial ligand, inhibits the JAK2-STAT3 pathway in breast cancer (BC) cells, demonstrating

IDO/Tubulin-IN-2 inhibits TDO/tubulin, effective on U87, HepG2, A549, HCT-116, LO2 cancer cells; IC50 values 0.036-1.04 μM, boosts antitumor action.

S-72 acts as a microtubule polymerization inhibitor, effective in cell-free assays at concentrations of 1, 3, and 10 µM.

CYY292 is a chemical compound acting as an inhibitor of PDGFRα, PDGFRβ, FGFR1, -2, and -3, with respective IC50 values of 5.35, 4.6, 28, 28, and 78 nM.

SHP2-IN-14 (compound 27) is a potent, orally active allosteric inhibitor of SHP2, displaying strong anti-tumor activity with an IC50 of 7 nM.

Anti-MI/R injury agent 1 (compound 18), derived from Panaxatriol, represents an orally administered, potent agent against myocardial ischemia/reperfusion (MI/R

DiMal-O-CH2COOH is a cleavable linker utilized in antibody-drug conjugates (ADCs).

AEF0117 is a signaling inhibitor of CB1-SSi that inhibits cannabinoid self-administration and can be used to study cannabis withdrawal.

Igermetostat, an EZH2 inhibitor, is utilized both in vivo and in vitro for cancer research [1].

Compound I (S1P1 agonist 6) is an S1P1 agonist that mitigates autoimmune activity by inhibiting lymphocyte trafficking and has potential as an immunosuppressive

Mal-VC-PAB-PNP-CDN-A is a conjugate comprised of an agent and a linker, utilized in antibody-drug conjugates (ADC) [1] [2].

FLT3-IN-19 (Comp 50) is a potent, selective inhibitor of FLT3, demonstrating an IC50 value of 0.213 nM, and is applicable in research pertaining to acute

BBDDL2059 is a selective covalent inhibitor targeting EZH2, exhibiting an IC50 of 1.5 nM against the EZH2-Y641F mutant.

URAT1 Inhibitor 5 (compound 16) serves as a powerful inhibitor of URAT1 and is utilized in hyperuricemia research [1].

Antitumor Agent-104 (Compound 9) serves as an antineoplastic by impeding DNA repair mechanisms in tumor cells, primarily through the inhibition of PARP1 enzyme

Azilsartan medoxomil potassium (QR-01019K), an angiotensin II receptor antagonist, exhibits a potent and sustained antihypertensive effect, along with a more

Bi-Mc-VC-PAB-MMAE is an agent-linker conjugate for antibody-drug conjugates (ADCs), featuring the linker (Fmoc-Val-Cit-PAB) and the potent tubulin inhibitor (

MDL-811, an allosteric activator of SIRT6, markedly enhances the deacetylation of histone H3 at lysine residues 9, 18, and 56 (H3K9Ac, H3K18Ac, and H3K56Ac),

IDO1-IN-22 (Compound 3) is an inhibitor of IDO1, demonstrating potent activity with biochemical hIDO1 IC50 of 67.4 nM and HeLa hIDO1 IC50 of 17.6 nM.

JAK1-IN-10 (compound 9), a cyano-substituted cyclic hydrazine derivative, functions as a potent and selective inhibitor of JAK1 [1].

BCR-ABL-IN-8 (compound 26f) is a BCR-ABL inhibitor featuring a trimethoxy group [1].

Immune cell migration-IN-1 (compound 2) serves as a potent inhibitor of immune cell migration, with potential research applications for mitigating conditions

HBV-IN-38 (Example 193), an HBV DNA inhibitor with an EC50 value of ≤100 nM, serves as a research tool for investigating viral infections [1].

Civorebrutinib (WS-413) is an inhibitor of Bruton's tyrosine kinase that exhibits antineoplastic activity [1].

Antitumor Photosensitizer-1 (Compound 8) is a potent photosensitizer with remarkable photodynamic anti-tumor properties and minimal skin photo-toxicity,

Tibremciclib is a cyclin-dependent kinase 4 (CDK4) inhibitor that exhibits antineoplastic properties [1].

EST73502 is a compound that functions as a dual agonist for the μ-opioid receptor (MOR) and an antagonist for the σ1 receptor (σ1R). It is selective, orally active, and possesses the ability to penetrate the blood-brain barrier (BBB). The compound exhibits a Ki value of 64 nM for the MOR and 118 nM for the σ1R. Additionally, EST73502 demonstrates antinociceptive activity [1].

BET-IN-14 is a pan BET inhibitor with an IC50 of 5.35 nM, demonstrating oral activity and anticancer properties [1].

Py-MAA-Val-Cit-PAB-MMAE (AAJ8D6-PY-Val-Cit-MMAE) serves as an ADC linker for Zapadcine-3a, a broad-spectrum anti-TRAILR2 ADC with antineoplastic properties.

Syk-IN-8 (compound 19q) functions as a Syk inhibitor with demonstrated antiproliferative effects on a variety of hematological tumor cells.

RIOK2-IN-2 (8) functions as an inhibitor of RIOK2, exhibiting IC50 values of 3.02 μM in MKN-1 cells and 5.34 μM in MOLT4 cells [1].

Compound S6, Mc-Alanyl-Alanyl-Asparagine-PAB-MMAE, is a potent anticancer agent specifically activated by the tumor microenvironment; it demonstrates efficacy

Cap-dependent endonuclease-IN-9, a strong influenza inhibitor, shows low toxicity, good pharmacokinetics, and dynamic action.

CIAC001, a pyruvate kinase PKM2 inhibitor, exhibits anti-neuroinflammatory properties.

DiaFluo is a probe for protein S-sulfinylation from cells.

JAK1-IN-11 (compound 11) serves as a potent inhibitor of Janus kinases, exhibiting nanomolar inhibitory concentrations with IC50 values of 0.02 nM (JAK1) and 0.

TrkB-IN-1 is a potent, orally active agonist of the TrkB receptor, with favorable pharmacokinetic (PK) properties.

Compound 11, also known as Antitumor Photosensitizer-2, is a potent photosensitizer with remarkable photodynamic anti-tumor properties and minimal skin photo-

STAT3-IN-18 (compound SPP), a platinum (IV) complex featuring an axial ligand from sandalwood, suppresses the JAK2-STAT3 pathway in breast cancer (BC) cells and

JAK-IN-27, also known as compound 1, is an orally active, potent inhibitor of the JAKS family kinases, displaying inhibitory concentrations (IC50s) of 3.0 nM

BTK-IN-27 (example 8), a potent BTK inhibitor with an IC50 of 0.2 nM, demonstrates anti-proliferative effects in TMD8 cells with an IC50 of less than 5 nM.

LM2I, a derivative of Spinosyn A (SPA), serves both as an argininosuccinate synthase (ASS1) enzyme activator and a tumor inhibitor through direct interaction

Sakura 6, a synthetic serotonin transporter (SERT)-binding peptide, enhances the interaction between SERT and neuronal nitric oxide synthase.

VISTA-IN-2 (Compound 1) is a V-domain Ig suppressor of T-cell activation (VISTA) inhibitor that promotes the degradation of VISTA in cells via autophagy,

MOR Agonist-1 is a μ-opioid receptor (MOR) agonist noted for its potent analgesic properties and is utilized in research concerning pain and associated

Compound B12 (Antibacterial agent 157) is a fungicidal agent that can impact protein synthesis in Botrytis cinerea.

(αR)-Cyclopropaneacetamide-Exatecan (compound 2-A), an Exenotecan derivative, serves as a cytotoxic agent that effectively inhibits the proliferation of U87MG

FAP-IN-2 is a 99mTc-labeled, isonitrile-containing derivative of a fibroblast activation protein (FAPI) inhibitor suitable for tumor imaging [1].

Davelizomib is a proteasome inhibitor that exhibits antineoplastic activity [1].

APG-2449 is an orally active inhibitor targeting ALK, ROS1, and FAK, demonstrating antitumor efficacy in mouse models of non-small cell lung cancer (NSCLC) [1].

ATR-IN-24 (Compound 1) is an ATR inhibitor with demonstrated anticancer activity [1].

JAK-IN-34 (compound 11n) is a potent inhibitor of Janus kinases (JAKs), demonstrating IC50 values of 0.40 nM for JAK1, 0.83 nM for JAK2, 2.10 nM for JAK3,

Canlitinib, a tyrosine kinase inhibitor, holds potential for cancer research.

HPK1-IN-38 (compound 15) is an inhibitor of MAP4K1/HPK1, suitable for research into disorders related to HPK1 [1].

URAT1&XO Inhibitor 1 (compound 29) serves as a dual inhibitor with IC50 values of approximately 10 μM for URAT1 and 1.01 μM for Xanthine Oxidase.

Yhhu6669 is an anti-HBV agent that suppresses viral DNA and replication by promoting DNA-free capsid assembly, effectively reducing HBV DNA and HBcAg levels in

Lerzeparib is a PARP (ADP-ribose polymerase) inhibitor that exhibits antineoplastic activity [1].

ROCK2-IN-6 (Comp A) is a selective inhibitor of ROCK2, applicable in the study and treatment of ROCK-mediated, autoimmune, and inflammatory diseases [1].

JDB175, a selective BTK inhibitor with oral bioavailability, demonstrates excellent penetration through the blood-brain barrier.

SARS-CoV-2-IN-68 (compound 6C) is a covalent inhibitor of both SARS-CoV-2 PLpro and Mpro, exhibiting potent antiviral properties by targeting the Zn-finger

Compound Im (Insecticidal agent 6) is a potent inhibitor of insect ryanodine receptors (RyRs), exhibiting an EC50 of 0.6308 µM against S.

BTK-IN-25 (compound 71) is a potent BTK inhibitor, demonstrating an IC50 of 0.77 nM against BTK(C481S) and achieving an IC50 of 1 nM in DOHH2 cells [1].

FOXM1-IN-2, a FOXM1 inhibitor, exhibits antineoplastic activity [1].

PI3Kδ-IN-13 (compound 89), with an IC50 value of 2.6 nM, is an inhibitor of PI3Kδ, applicable for researching diseases involving cell proliferation, including

Xilmenolone acts as a positive allosteric modulator of the GABA_A receptor [1].

BET-IN-1 is a bromodomain inhibitor extracted from patent WO/2013024104A1 (example 2, plC50: 6.0 - 7.0).