idh1 inhibitor 1

IDH1 Inhibitor 1 is an orally bioavailable, brain-penetrant, and selective mutant IDH1 inhibitor (IC50s: 0.021 μM, 0.045 μM, and 2.52 μM for IDH1R132H, IDH1R132C, and IDH1WT).

Mutant IDH1 inhibitor is an effective inhibitor of mutant IDH1 R132H (IC50: < 72 nM).

IDH1 Inhibitor 2 (compound 13) is a potent IDH1 inhibitor through direct covalent modification of His315, with an IC50 of 110 nM.

IDH1 Inhibitor 3 is a mutant isocitric dehydrogenase 1 (IDH1) inhibitor (IC50: 45 nM for IDH1R132H).

WT IDH1 Inhibitor 2 is a wild-type isocitrate dehydrogenase 1 (WT IDH1) inhibitor (IC50: 120 nM) and is a mutant R132H IDH1 inhibitor, an isoform of GSK321 with wild-type cross-reactivity.

IDH1 Inhibitor 7 is an IDH1 inhibitor with an IC 50 of less than 100 nM .

IDH1 Inhibitor 5 (compound 2) is an IDH1 (isocitrate dehydrogenase 1) inhibitor with an IC50 of 64.4 nM for MOG cells and an IC50 of 34.9 nM for wild-type IDH1 glioma cells expressing exogenous mutant IDH1 R132H protein.

IDH1 Inhibitor 9 (compound 11S) (2, 4, 8, 10 µM) induces apoptosis and causes cell cycle arrest in the S phase in a dose-dependent manner.

(S,R)-WT IDH1 Inhibitor 2 is a selective and potent mutant IDH1 inhibitor that inhibits R132G (IC50: 2.9 nM), R132C (IC50: 3.8 nM), R132H (IC50: 4.6 nM) and WT IDH1 (IC50: 46 nM) with 100-fold higher selectivity than IDH2. 100-fold higher selectivity than IDH2. (S,R)-WT IDH1 Inhibitor 2 is investigated in acute myeloid leukemia (AML) and other cancers for its ability to induce intracellular 2-HG reduction, failure of myeloid differentiation block, and induction of granulocyte differentiation at the level of leukemia mother cells and more immature stem cells.

Necrostatin-1 (Nec-1) is a specific RIP1 inhibitor and necrotic apoptosis inhibitor, which inhibits TNF-α-induced necrotic apoptosis and also inhibits IDO.

Aldose reductase-IN-1 (AT-001) is a aldose reductase inhibitor (IC50: 28.9 pM).

Shield-1 is a specific, high-affinity and cell-permeant ligand of FK506-binding protein-12 (FKBP), and reverses the instability by binding to mutated FKBP (mtFKBP), allowing conditional expression of mtFKBP-fused proteins. Shield-1 can stabilize the entir

Werner syndrome RecQ helicase-IN-1 is a potent Werne r syndrome RecQ DNA deconjugase (WRN) inhibitor that can be used to study cancers such as colon and stomach cancer.

Mdivi-1 (Mitochondrial division inhibitor 1) is a mitochondrial division inhibitor that inhibits DRP1 and Dynamin I (IC50=1-10 μM). Mdivi-1 inhibits mitochondrial autophagy.

(+)-JQ-1 (JQ1) is a specific, reversible BET bromine domain inhibitor that targets BRD4 (1 2) with IC50 values of 77 33 nM. (+)-JQ-1 induces cell autophagy and inhibits cell proliferation.

CD38 inhibitor 1 is an inhibitor of CD38. For hCD38 and mouse CD38, the IC50s are 7.3 nM and 1.9 nM.

SETDB1-TTD-IN-1 is a potent, selective, and endogenous binder-competitive inhibitor of SETDB1-TTD with a Kd of 88 nM.

T3Inh-1 is an effective and selective inhibitor of ppGalNAc-T3 with an IC50 of 7 µM. T3Inh-1 prevents breast cancer cells. T3Inh-1 reduces FGF23 hormone levels in both tissue cells and mice, without causing any toxic side effects.

1-N-Methyl-4-mercaptohistidine disulfide is a potential Duchenne chloroplast coupling factor 1 redox regulator, an oxidized form of ochratoxin A, that inhibits light-triggered CF1 ATPase activity.

Spautin-1 is an autophagy inhibitor that suppresses the deubiquitination activity of ubiquitin-specific peptidase USP10 and USP13. Spautin-1 inhibits UPR and exhibits preferential cytotoxicity in glucose-starved cancer cells.

PROTAC BRD4 ligand-1, a component of Protac GNE-987, is a ligand for BRD4 and acts as an inhibitor of BET.

diABZI STING agonist-1 (Tautomerism) (diABZI STING agonist (Compound 3)) is a selective stimulator of interferon genes (STING) receptor agonist, with EC50s of 130, 186 nM for human and mouse, respectively.

Liproxstatin-1 is a potent and selective inhibitor of ferroptosis (IC50=22 nM). Liproxstatin-1 protects cells from ferroptosis induced by ferroptosis inducers (e.g., Erastin, RSL3).

Kv3 modulator 1 is a voltage-gated potassium channel Kv3 modulator that can be used to study neurologic-level diseases.

rel-5-(4-Chloro-2-fluorophenyl)-2,3-dimethyl-7-[(2R,4S)-tetrahydro-2-(1-methyl-1H-pyrazol-4-yl)-2H-pyran-4-yl]pyrido[3,4-b]pyrazine has an EC50 value of ≤ 0.05 μM and an E.max value of > 250 μM for TREM2.

GLP-1(7-36) amide (MKC 253) is a peptide hormone released from intestinal L-cells upon nutrient intake. It binds to the GLP-1 receptor in the pancreas, enhancing insulin secretion from pancreatic β-cells and increasing insulin expression, thereby exhibiting antidiabetic effects.

Ferrostatin-1 (Fer-1) is a potent and selective inhibitor of ferroptosis. Ferrostatin-1 potently inhibits Erastin-induced ferroptosis in HT-1080 cells with an EC50 of 60 nM. Ferrostatin-1 also exhibits antioxidant and antifungal activities.

Pam3CSK4 TFA (Pam3Cys-Ser-(Lys)4 TFA) is an agonist of toll-like receptor 1 2 (TLR1 2) (EC50 of 0.47 ng mL for human TLR1 2).

AZD 1775 Linker Conjugate 1 TFA is a compound involved in ubiquitinase-targeted chimeric assays

iGP-1 is a mitochondrial sn-glycerol 3-phosphate dehydrogenase (mGPDH) inhibitor that can be used to study obesity.

GSK-3 inhibitor 1 is a GSK-3 inhibitor.

Akt3 degrader 1 is a specific Akt3 degrader with anticancer and antiproliferative activity that inhibits tumor growth in mice.Akt3 degrader 1 is used in the study of non-small cell lung cancer and pancreatic cancer.

hSMG-1 inhibitor 11j is a pyrimidine derivative. hSMG-1 inhibitor 11j is a potent and selective inhibitor of hSMG-1, IC50 = 0.11 nM. hSMG-1 inhibitor 11j exhibits >455-fold selectivity for hSMG-1 over mTOR (IC50=50 nM), PI3Kα γ (IC50=92 60 nM) and CDK1 CDK2 (IC50=32 7.1 μM). hSMG-1 inhibitor 11j can be used for the research of cancer.

RAS GTPase inhibitor 1 is a RAS GTPase inhibitor with potential antitumor activity.

DHODH-IN-1 is a potent dihydroorotate dehydrogenase (DHODH) inhibitor with IC50 of 25 nM. DHODH-IN-1 is an inhibitor of the pyrimidine biosynthetic pathway.

4-(2-chloro-4-methoxy-5-methylphenyl)-N-[(1A)-2-cyclopropyl-1-(3-fluoro-4-methylphenyl)ethyl]-5-methyl-N-(2-propyn-1-yl)-2-thiazolamine is an enantiomeric counterpart of SSR-125543. SSR-125543 is a potent CRF-R1 antagonist with Ki = 1.0 nM for human CRF-R1.

Chymase-IN-1 is a selective, orally active inhibitor of human mast cell chymase (IC50: 29 nM).

EGFR-IN-1 hydrochloride is an irreversible and specific inhibitor of L858R T790M mutant EGFR, with 100-fold selectivity over wild-type EGFR. It exhibits potent antitumor and antiproliferative activity in H1975 cells and mutant HCC827 cells with IC50s of 4 and 28 nM, respectively.

Collagen proline hydroxylase inhibitor-1 exhibits antifibroproliferative activity.

DA-3003-1 (DA-3003-1) is a membrane-permeable, potent and selective Cdc25 dual specificity phosphatase inhibitor with antitumor activity that inhibits Cdc25B2, Cdc25A, Cdc25B2 and Cdc25C.

MC-1-F2 is a direct FOXC2 inhibitor with anticancer activity, inhibits cancer stem cell (CSC) characteristics, and reduces the invasive ability of castration-resistant prostate cancer (CRPC) cell lines. MC-1-F2 can be used to study prostate cancer.

Adenosine antagonist-1 acts as an adenosine A3 receptor (AA3R) antagonist.

1-PeCSO is isolated from onion or garlic bulbs. It acts as a key compound in garlic greening and reacts with lachrymatory factor synthase.

ZINC40099027 is a specific adhesion plaque kinase (FAK) activator that promotes gastric mucosal repair in persistent aspirin-associated gastric injury through activation of adhesion plaque kinase, activates human adhesion plaque kinase by accelerating the enzyme activity of the structural domain of FAK kinase, activates cytosolic FAK, and promotes intestinal epithelial wound closure.

5-HT6 7 antagonist 1 is a dual 5-HT6 7 2A and D2 receptor antagonist used in the study of dementia and Alzheimer's disease.

GPAT-IN-1 is a glycerol 3-phosphate acyltransferase (GPAT) inhibitor, which can be used to study obesity and diabetes.

Xanthine oxidase-IN-1 is an effective inhibitor of xanthine oxidase with an IC50 value of 6.5 nM. It plays a central role in purine catabolism through the degradation of bioactive nucleotides facilitated by nucleic acid and nucleotide intermediates.

Hepcidin antagonist-1 is an iron-modulating antagonist.Hepcidin antagonist-1 can be used to study metabolic disorders such as iron-deficiency diseases and anemia.