cdk4 in 1

CDK4 inhibitor is a novel and specific CDK4/Cyclin D1 inhibitor with an IC50 of 10 nM; 1500 and 500 fold than CDK1/Cyclin B (IC50>15 uM) and CDK2/Cyclin A (IC50=5.265 uM) respectively.

CDK4/6/1 Inhibitor (Crozbaciclib) is a type of CDK4/6 inhibitor (IC50s: 3 and 1 nM). CDK4/6 inhibitor is a class of compounds used for the treatment of some types of hormone receptor positive, HER2-negative breast cancer, which can block the process of breast cancer cell division and reproduction.

PROTAC CDK4 6 degrader 1 (Compound 7f) is a dual degrader of CDK4 and CDK6, with DC50 values of 10.5 nM and 2.5 nM, respectively. This compound effectively inhibits proliferation in Jurkat cells (IC50 of 0.18 μM), induces cell cycle arrest during the G1 phase, and triggers cell apoptosis (apoptosis). It features a pink ligand for target protein YY173, a black linker, and a blue ligand for E3 ligase.

SHP2 CDK4-IN-1 (compound 10) is a dual inhibitor targeting SHP2 and CDK4, with oral activity and high potency, showing IC50 values of 4.3 nM for SHP2 and 18.2 nM for CDK4. It induces G0 G1 arrest, inhibits proliferation of TNBC cell lines, and demonstrates significant antitumor efficacy in the EMT6 syngeneic mouse model. This compound is valuable for research into triple-negative breast cancer (TNBC) [1].

HEMTAC CDK4 6 degrader 1 is a PROTAC connected by ligands for HSP90 and CDK4 6 with a ( K_d ) value of 35.7 μM. It induces CDK4 6 degradation in B16F10 melanoma cells, arrests the cell cycle at the G0 G1 phase, and induces apoptosis. HEMTAC CDK4 6 degrader 1 can be used in cancer research [1].

FLT3 CDK4-IN-1 is a highly selective, potent, orally active dual inhibitor of FLT3 (IC50: 7 nM) and CDK4 (IC50: 11 nM), demonstrating significant anti-tumor effects in vivo and anti-proliferative effects on certain cancer cells.

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.

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.

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.

MitoBloCK-6 is an effective inhibitor of Erv1/ALR with IC50 values of 900 nM and 700 nM, respectively. Additionally, MitoBloCK-6 inhibits Erv2 (IC50=1.4 μM). It induces apoptosis in hESCs by promoting the release of cytochrome c.

Piperazine,1-(4-fluorophenyl)-4-[(3,4,5-trimethoxyphenyl)methyl]- is a piperazine derivative with anti-SARS-CoV-2 activity.

(Z)-2-fluoro-1,3-bis(4-methoxyphenyl)prop-2-en-1-one is a screening compound and can be used in new drug development related research.

N-Boc-4-pentyne-1-amine is an alkyl chain-based PROTAC linker compound used in the synthesis of PROTAC MG-277 [1].

Trans-2-butene-1,4-dicarboxylic acid (3-Hexenedioic Acid) is a normal human unsaturated dicarboxylic acid metabolite with increased excretion in patients with Dicarboxylic aciduria caused by fatty acid metabolism disorders The urinary excretion of Trans-2-butene-1,4-dicarboxylic acid is increased in conditions of augmented mobilization of fatty acids or inhibited fatty acid oxidation.

3-Morpholino-1-(4-(2-oxopiperidin-1-yl)phenyl)-5,6-dihydropyridin-2(1H)-one shows antitumor activity in a human colon cancer cell line and may be used to combat thrombosis.

4-Methyl-1-phenyl-2-pentanone (Benzyl isobutyl ketone) is a volatile flavor compound utilized as a food additive.

4-(Imidazol-1-yl)phenol is a potent signal enhancer in horseradish peroxidase (HRP)–luminol chemiluminescence (CL) immunoassays [1].

Compound Fr12729 is a useful organic compound for research related to life sciences. The catalog number is Fr12729 and the CAS number is 4727-72-4.

4-(1-Phenylethyl)resorcinol (4-(1-Phenylethyl)benzene-1,3-diol) is a skin brightening agent that is a cosmetic additive. It works by inhibiting melanin production, reducing the appearance of dark spots, hyperpigmentation and uneven skin tone, and brightening the skin tone to reduce dullness.4-(1-Phenylethyl)resorcinol is generally regarded as safe in the cosmetic industry, and is widely used in several countries and regions.

4-Nitroquinoline 1-oxide (4-NQO) is a chemical carcinogen that induces mutations in bacteria, fungi, and animals through the formation of large amounts of purine adducts.

1-(4-AMinophenyl)-5,6-dihydro-3-(4-Morpholinyl)-2(1h)-pyridinone has broad-spectrum antifungal activity with inhibitory effects on Candida albicans, Aspergillus niger, Pseudomonas aeruginosa and Staphylococcus aureus.

6-(4-methylpiperazin-1-yl)-4-o-tolylnicotinamide can be used in the synthesis of befetupitant and netupitant.

1-(4-FLUORO-PHENYL)-BUTAN-1-ONE is a useful organic compound for research related to life sciences. The catalog number is T3679 and the CAS number is 582-83-2.

1-(3,5-Dichloro-4-fluorophenyl)-2,2,2-trifluoroethanone (sarolaner) is an intermediate of Sarolaner.

2-Chloro-1-(4-fluorobenzyl)benzimidazole is an inhibitor of aldose reductase (ALR2).

4-Diethylamino-2-butyn-1-ol is used as pharmaceutical intermediates.

1-{1H-pyrrolo[2,3-d]pyrimidin-4-yl}piperazine dihydrochloride (1-PPZ-DHC) is a compound used as a molecular structural unit. It is an analog of the natural product piperazine and has a wide range of biological activities, including anti-inflammatory, anti-tumor and antibacterial activities. It has also been studied for the treatment of neurological disorders such as Alzheimer's and Parkinson's.

Ethyl 1-(4-methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxylate has an inhibitory effect on coagulation factor Xa, and it can be used in the study of thrombophlebitis, atherosclerosis, cerebral embolism, stroke and pulmonary embolism.

((3S,5R)-5-((1H-1,2,4-Triazol-1-yl)methyl)-5-(2,4-difluorophenyl)tetrahydrofuran-3-yl)methyl 4-methylbenzenesulfonate is a pharmaceutical intermediate used in the synthesis of posaconazole with anticancer activity.

1-(4-chloro-3-(trifluoromethyl)phenyl)-3-(7-(1-methyl-1H-pyrazol-4-yl)-2,3,4,9-tetrahydro-1H-carbazol-3-yl)urea, a TNF-α agonistic compound, could induce cells to secrete TNF- α.

3- Phenyl- N- [1- (phenylmethyl) - 4- piperidinyl] -tricyclo[3.3.1.13, 7] decane- 1- carboxamide with antiviral activity against Ebola virus that targets the surface-exposed glycoprotein and inhibits viral entry into host cells. In vitro studies in Vero cells revealed the compound inhibits the viral replication with EC50 of 0.38 μM.

4-(benzyloxy)benzene-1-sulfonamide is inhibitor of human recombinant CA-7.

[4-(4-phenylpiperazin-1-yl)oxan-4-yl]methanamine is a piperazine derivative that is a partial agonist at serotonin and dopamine receptors, making it a candidate for the treatment of psychiatric disorders such as depression and schizophrenia.

Dynorphin A (1-10) acetate is an endogenous opioid neuropeptide, binds to extracellular loop 2 of the κ-opioid receptor. Dynorphin A (1-10) also blocks NMDA-activated current with an IC50 of 42.0 μM.

1-[2,4-Dihydroxy-6-methoxy-3-(3-methyl-2-buten-1-yl)phenyl]-3-(4-hydroxyphenyl)-2-propen-1-one (Xanthohumol) , prenylchacone flavonoid, is a natural product with multi-biofunctions purified from Hops Humulus lupulus,is effective against HIV-1 and might serve as an interesting lead compound. It may represent a novel chemotherapeutic agent for HIV-1 infection.

4-Cyclohexyl-1-phenylthiosemicarbazide is employed as an intermediate.

N-[1-(Aminocarbonyl)-4-[(2-chloro-1-iminoethyl)amino]butyl]benzamide is a racemic form of Cl-amidine (S enantiomer). Cl-amidine is an orally active peptidylarginine deminase (PAD) inhibitor.

2,5-Morpholinedione, 4-methyl-6-(1-methylethyl)-3-(phenylmethyl)- is the trans structure of Lateritin.

1-(4-Carbethoxyphenyl)-piperazin is used as a reagent for enzymes and chemical synthesis, as a model substrate for enzyme studies, and as a ligand for receptor binding assays.

Cyclopenta[c][1]benzopyran-8-ol, 1,2,3,3a,4,9b-hexahydro-4-(4-hydroxyphenyl)-, (3aR,4S,9bS)-rel- is an estrogen receptor beta (ERβ) agonist.

N-Cyclohexyl-4-[1-(1-piperazinyl)-2,6-naphthyridin-3-yl]-2-pyridinamine is a novel 2,6-naphthyridine identified by high throughput screen (HTS) as a dual protein kinase C/D (PKC/PKD) inhibitor[1].

(3Z)-1-methyl-3-[2-(4-methylphenyl)-2-oxo-ethylidene]piperazin-2-one is a chemical agent.

The compound inhibits Ras function and therefore inhibits the abnormal growth of cells.

Benzonitrile, 4-[[5-cyclopropyl-3-methyl-1-[(methylsulfonyl)methyl]-1H-pyrazol-4-yl]oxy]-2,6-dimethyl- is a progesterone receptor antagonist with antiprogestin effects.

Acth (1-4) acetate is the ACTH N-terminal tetrapeptide.

Pim-1 kinase inhibitor 4 is a potent Pim-1 kinase inhibitor with an IC50 value of 17.01 nM.Pim-1 kinase inhibitor 4 also possesses antioxidant activity and potential anticancer activity, and inhibits DPPH.Pim-1 kinase inhibitor 4 promotes apoptosis and inhibits the growth of PC-3 cells with an IC50 value of 16 nM. Pim-1 kinase inhibitor 4 promotes apoptosis and inhibits PC-3 cell growth with an IC50 of 16 nM. Pim-1 kinase inhibitor 4 can be used in prostate cancer research.

2H-Naphth[2′,1′:4,5]indeno[1,2-d][1,3]dioxole, pregn-4-ene-3,20-dione deriv showed high local anti-inflammatory potency and high lung selectivity when tested on Sprague Dawley rats.

6-chloro-1-ethyl-7-(4-methylpiperazin-1-yl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid is a compound used as a molecular structural unit for pefloxacin impurities.