cdk4/6-in-6

CDK4/6-IN-6 is a potent CDK4/CDK6 inhibitor with Ki of 0.6 nM and 13.9 nM for CDK4/Cyclin D1 and CDK6/Cyclin D3, respectively.

CDK4/6-IN-5 is a highly effective inhibitor of CDK4 and CDK6, with Ki values of 0.2 and 4.4 nM for CDK4/Cyclin D1 and CDK6/Cyclin D3, respectively (WO2019207463A1, example A93).

CDK4/6-IN-17 (compound 12) is an orally bioavailable inhibitor of CDK4/6, demonstrating potent activity with IC50 values between 10-100 nM in BE(2) cells. It has shown efficacy in inhibiting tumor growth in the COLO205 xenograft model [1].

CDK4/6-IN-7, a highly potent and selective orally active inhibitor of CDK4/6, demonstrates impressive inhibition activity with IC50 values of 1.58 nM and 4.09 nM respectively. This compound is particularly valuable for breast cancer research [1].

CDK4/6-IN-10 is a selective, potent, orally active inhibitor of CDK4 (IC50: 22 nM) and CDK6 (IC50: 10 nM) with antitumour effects. CDK4/6-IN-10 has potential for studies in multiple myeloma (MM).

CDK4/6-IN-12 is a potent cyclin-dependent kinase 4/6 (CDK4/6) inhibitor. CDK4/6-IN-12 has enzymatic inhibitory activity against CDK4 and CDK6 with IC 50 of 592.3 nM and 3090 nM, respectively. CDK4/6-IN-12 can be used in the cancer research[1].

CDK4/6-IN-8 (Compound 7p) is a selective inhibitor of CDK4 (IC50=5.01 nM) and CDK6 (IC50=3.97 nM).

CDK4/6-IN-15, an orally active and selective inhibitor of CDK4/6, effectively halts the growth of cancer cells by arresting the cell cycle at the G1 phase and inhibiting the phosphorylation of the retinoblastoma tumor suppressor protein (Rb) at S780, as well as suppressing E2 factor (E2F)-regulated gene expression.

CDK4/6-IN-9 (compound 10) is a selective inhibitor of CDK4/6, capable of acting on CDK6/cyclin D1 (IC50: 905 nM). CDK4/6-IN-9 has potential research value in multiple myeloma (MM).

CDK4/6-IN-3 is a brain-penetrant CDK4/CDK6 inhibitor (Kis: <0.3 nM and 2.2 nM) used for the treatment of glioblastoma. It inhibits CDK1 with a Ki of 110 nM.

CDK4/6-IN-14 is a potent, highly selective inhibitor of Cyclin-Dependent Kinases 4 and 6 (CDK4/6), demonstrating inhibition concentrations (IC50s) of 10 nM and 16 nM, respectively. It possesses over 60-fold greater selectivity for CDK4/6 compared to CDKs 1, 2, 7, and 9, and exhibits significant selectivity against a panel of 205 other kinases.

CDK4/6-IN-11 is a potent PROTAC CDK4/6 degrader.

CDK4/6-IN-2 is a potent CDK4 and CDK6 inhibitor (IC50s: 2.7 and 16 nM).

Compounds 10B and 10C, functioning as cdk4/6 inhibitors, demonstrated low nanomolar activity, optimal antiproliferative effects, excellent metabolic properties, and acceptable pharmacokinetics targeting cdk4/6.

(9α,13α,14α)-4-Hydroxy-3,7-dimethoxy-7,8-didehydromorphinan-6-one is a major mechanism of Sinomenine. Sinomenine is an alkaloid derived from the Chinese herb Sinomenium acutum (Thunb.) Rehd. et Wils. (9α,13α,14α)-4-Hydroxy-3,7-dimethoxy-7,8-didehydromorphinan-6-one exhibits anti-inflammation effects.

2,4-Diamino-6-hydroxypyrimidine (DAHP) (DAHP) is a selective, specific inhibitor of GTP cyclohydrolase I, the rate limiting step for de novo pterin synthesis

6-Methoxyflavanone (6-MeOF) is A positive allosteric modulator of the GABA response of human recombinant GABA A receptor, with antianxiety and anti-inflammatory activity, and can be used to reduce cisplatin induced neuropathic pain.

4-Methyl-6-Methoxycoumarin is a natural product isolated from Eupatorium pauciflorum.

6-Aminocaproic acid (EACA) is an antifibrinolytic agent that acts by inhibiting plasminogen activators which have fibrinolytic properties.

Pinocembrin 7-O-[3''-O-galloyl-4'',6''-hexahydroxydiphenoyl]-β-D-glucoside can moderately inhibit α-amylase activity, with the IC50 value of 0.03 umol/ml.

4-Hydroxy-6-methylcoumarin (4-HMC) is a naturally occurring phenolic compound, a derivative of coumarin, found in a variety of plants, fungi, and bacteria. It has anti-inflammatory and anti-tumor activity.4-HMC is used as a flavoring agent, preservative and antioxidant in the food industry.

[6]-Gingerol ((S)-(+)-[6]Gingerol), an antioxidant, protects HL-60 cells from oxidative stress. It has protective effects for Yous tumors in the pancreas, ovaries, breast tissue, the bowel, among other tissues.

6-Bromoindole-3-carboxylic acid (ZINC2547985) is a marine derived natural products found in Pseudosuberites hyalinus.

2',4,4',6'-Tetramethoxychalcone (2',4,4',6'-TETRAMETHOXY) is a natural product.

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.

Deslorelin acetate(57773-65-6 free base) is a gonadotropin releasing hormone super-agonist (GnRH agonist)

2-Furoyl-LIGRLO-amide TFA(729589-58-6 free base) is a potent and selective protease-activated receptor 2 (PAR2) agonist.

CEP-28122 mesylate salt (1022958-60-6 free base) is a highly selective orally active ALK inhibitor (IC50: 1.9 nM in an enzyme-based TRF assay).

1-Ethyl-6-aminouracil (6-AMINO-1-ETHYL-1H-PYRIMIDINE-2,4-DIONE) is an intermediate in the synthesis of a series of new substituted Xanthines which have high affinity and selectivity for the human adenosine A2B receptors.

6-Bromoindole-3-acetonitrile (2-(6-bromo-1H-indol-3-yl)acetonitrile) is a marine derived natural products found in Pseudosuberites hyalinus.

Pep2-EVKI acetate is a cell-permeable peptide. Pep2-EVKI acetate interferes the interaction between protein interacting with C-kinase (PICK1) and GluR2 AMPA receptor subunits.

4-Amino-6-(trifluoromethyl)benzene-1,3-disulfonamide (4-Amino-6-(trifluoromethyl)benzene-1,3-d) is a carbonic anhydrase inhibitor, used as a potential anti-tumor and antiglaucoma drug.

6-Bromovanillin is a biochemical reagent that can be used in the synthesis of caridopa, an aromatic amino acid decarboxylase inhibitor.

(1R,5S,6r)-N-(2-methyl-1-((3-methylpyridin-2-yl)oxy)propan-2-yl)-3-azabicyclo[3.1.0]hexane-6-carboxamide L(+)-Tartaric acid is a potential SSTR4 agonist.

PKG Substrate acetate is a selective substrate for cGMP-dependent protein kinase (PKG).PKG Substrate is a selective substrate for protein kinase G (PKG) with a strong preference for PKG Iα (Km = 59 μM) over PKG II (Km = 305 μM).

(2R)-2,3-Dihydro-5,7-dihydroxy-2-(4-hydroxyphenyl)-6-methoxy-4H-1-benzopyran-4-one is one of the potentially active components in Scutellaria baicalensis.

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.

(S)-6-methoxychroman-3-carboxylic acid is a synthetic compound with a molecular formula of C11H10O5. It is a member of the chroman family of compounds, which are characterized by a seven-membered ring with one oxygen and one carbon atom.

2-(2-fluoro-6-methoxyphenyl)pyrimidine-4-carboxylic acid is commonly used to synthesize compounds with anticancer and antitumor properties.

Arg-Gly-Glu-Ser acetate is a RGD related peptide that is a control for the RGDS activity of fibrinogen binding to activated platelets.

N-[3,5-bis(trifluoroMethyl)phenyl]-N'-[(9R)-6'-Methoxycinchonan-9-yl]- Thiourea is a cinchona alkaloid-derived bifunctional catalyst.

(6Z)-7-Phenyl-7-(3-Pyridinyl)-6-Heptenoic Acid is a derivative of 7-Phenyl-7-(3-Pyridyl) -6-Heptenoic Acid that can be used in biological research.

6'-hydroxydihydrocinchonidine is a metabolite of quinine, with antimicrobial and antitumor activity, and inhibitory effect on Trypanosoma brucei and Streptococcus pneumoniae.

NAcM-OPT HCL is an orally bioavailable cullin neddylation 1 (DCN1) inhibitor that targets N-Acetyl-UBE2M (E2 conjugating enzyme, UBC12) interaction with DCN1 with IC50 of 79 nM.

HC-067047 hydrochloride is a potent and selective TRPV4 antagonist. HC-067047 hydrochloride reversibly inhibited currents through the human, rat, and mouse TRPV4 orthologs with IC50 values of 486 nM, 133nM, and 17 nM, respectively.

Urotensin II, mouse acetate (9047-55-6 free base) is an endogenous ligand for the orphan GPR14 or SENR. It is a potent vasoconstrictor.

6-Methoxynaringenin is an aerial part of Scutellaria barbata D. Don (Lamiaceae) and inhibits NO production efficiently with an IC50 value of 25.8 μM.

6-Hydroxyisatin (ZINC14455608) is a marine derived natural products found in Streptomyces sp.

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

7-Methyl-6-mercaptopurine (7-Methyl-6-thiopurine) is an inhibitor of PRPP aminotransferase, inhibits IMP metabolism and prevents purine, DNA and RNA synthesis.