cdk9-in-7

CDK9-IN-7 is a highly selective and orally active CDK9 cyclin T inhibitor (IC50: 11 nM), which exhibits more potent over other CDKs (CDK4 cyclinD: 148 nM; CDK6 cyclinD: 145 nM).

Acetamide, N-[2-[(5-chloro-2 methoxyphenyl)amino]-4'-methyl[4,5'-bithiazol]-2'-yl]-inhibits pro-matrix metalloproteinase activation and can be used to prevent, treat or ameliorate MMP9 and/or MMP13-mediated syndromes.

Cecropin A (1-7)-Melittin A (2-9) is an antimicrobial peptide with broad-spectrum activity against both Gram-positive and Gram-negative aerobic bacteria, as well as antimalarial properties, without the adverse hemolytic effects commonly associated with bee venom peptides [1].

Nucleoside Derivatives - Xylo-nucleosides; 8-Modified purine nucleosides; Amino nucleosides; N-Methylated alkylated nucleosides

2-Amino -7-propargyl-7,8-dihydro-8-oxo-9-(beta-D-2,3,5-tri-O-actyl-xylofuranosyl)purine is a useful organic compound for research related to life sciences. The catalog number is TNU1331 and the CAS number is 2389988-52-5.

[(2R,3S,4R,5R)-3,4-diacetyloxy-5-[2-amino-7-(cyclopropylmethyl)-8-oxopurin-9-yl]oxolan-2-yl]methyl acetate is a useful organic compound for research related to life sciences and the catalog number is TNU1306.

2-Amino-7-cyclopropylmethyl-7,8-dihydro-8-oxo-9-(beta-D-xylofuranosyl)purine (catalog number TNU0169, CAS number 2389988-30-9) is a valuable organic compound for life sciences research.

(7R,8R,9S,13S,14S,17S)-7-(9-Bromononyl)-13-methyl-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthrene-3,17-diol is a useful organic compound for research related to life sciences. The catalog number is T66315 and the CAS number is 875573-67-4.

2-amino-9-[(2R,3R,4R,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-7-(2,2,2-trifluoroethyl)-6,7,8,9-tetrahydro-1H-purine-6,8-dione is a useful organic compound for research related to life sciences and the catalog number is TNU1307.

7-n-Propyl-7,8-dihydro-8-oxo-9-(beta-D-xylofuranosyl)guanine is a nucleoside derivative (xylo-nucleoside), N-methylated alkylated nucleoside, and an 8-modified purine nucleoside.

2-Amino-7-propargyl-7,8-dihydro-8-oxo-9-(beta-D-3-deoxy-ribofuranosyl)purine is a valuable organic compound for life sciences research (catalog number: TNU1351, CAS number: 2389988-75-2).

Nucleoside Derivatives - 7-Deazapurine nucleosides; Halo-nucleosides; Scaffolds and Templates

CDK-IN-9 (compound 24) is a potent inhibitor of CDK and acts on CDK2 E (IC50: 4 nM). It functions as a molecular gel that induces interaction between CDK12 and DDB1, and can dephosphorylate retinoblastoma protein and RNA polymerase II, thereby inducing apoptosis.

7-Cyclopropylmethyl-7,8-dihydro-8-oxo-9-(b-D-ribofuranosyl)guanine is a useful organic compound for research related to life sciences and the catalog number is TNU0394.

2-Amino-7-propargyl-7,8-dihydro-8-oxo-9-(beta-D-2,5-di-O-acetyl-3-deoxy-3-fluoro-ribofuranosyl)purine is a useful organic compound for research related to life sciences. The catalog number is TNU1353 and the CAS number is 2389986-90-5.

7-Cyclopropyl methyl-7,8-dihydro-8-oxo-9-(β-D-ribofuranosyl)guanine is a purine nucleoside analogue. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis , etc [1] .

7-(Butyn-2-yl)-7,8-dihydro-8-oxo-9-(beta-D-xylofuranosyl)guanine is a nucleoside derivative (xylo-nucleoside), N-methylated alkylated nucleoside, and 8-modified purine nucleoside.

7-Propargyl-7,8-dihydro-8-oxo-9-(beta-D-xylofuranosyl)guanine is a nucleoside derivative categorized as a xylo-nucleoside, N-methylated alkylated nucleoside, and 8-modified purine nucleoside.

7-n-Butyl-7,8-dihydro-8-oxo-9-(beta-D-xylofuranosyl)guanine is a nucleoside derivative (xylo-nucleoside), N-methylated alkylated nucleoside, and 8-modified purine nucleoside.

Nucleoside Derivatives - Xylo-nucleosides; 8-Modified purine nucleosides; N-Methylated alkylated nucleosides

7-Ethyl-7,8-dihydro-8-oxo-9-(beta-D-xylofuranosyl)guanine is a nucleoside derivative (xylo-nucleoside), specifically an N-methylated alkylated nucleoside and an 8-modified purine nucleoside.

(3S,4aS,10aS)-3-(Acetyloxy)-2,3,4,4a,10,10a-hexahydro-6-hydroxy-1,1,4a-trimethyl-7-(1-methylethyl)-9(1H)-phenanthrenone (compound 3), a palmitate derivative extracted from the root of Salvia miltiorrhiza, exhibits anti-cancer properties with DC50s of 25.5 μg mL against HeLa, 37.5 μg mL against HepG2, and 30.2 μg mL against OVCAR-3 human cancer cell lines [1].

(1'R,3a'R,8a'S,9'S,9a'S)-1'-Methyl-3'-oxo-N,N-diphenyl-3',3a',5',7',8',8a',9',9a'-octahydro-1'H-spiro[[1,3]dioxolane-2,6'-naphtho[2,3-c]furan]-9'-carboxamide is a useful organic compound for research related to life sciences. The catalog number is T67324 and the CAS number is 900160-98-7.

Nucleoside Derivatives - Xylo nucleosides, 8-Modified purine nucleosides; N-Methylated alkylated nucleosides

2-Amino-7-propargyl-7,8-dihydro-8-oxo-9-(beta-D-xylofuranosyl)purine is a valuable organic compound for life sciences research [catalog number: TNU1332, CAS number: 2389988-53-6].

3,4,5'-Trimethoxy-3',4'-methylenedioxy-7,9':7',9-diepoxylignan is a natural product for research related to life sciences. The catalog number is TN5420 and the CAS number is 873867-94-8.

CDK9-IN-2 is a specific CDK9 inhibitor with an IC50 of 5 nM in the A2058 skin cell line (72 hours) and 7 nM in the H929 multiple myeloma cell line (72 hours).

CDK9 Antagonist-1 (compounds 11c) is a potent and selective CDK9 degrader based on PROTAC, with an IC50 of 17 μM in MCF-7 cell lines. Natural product Wogonin binds ubiquitin E3 ligase cereblon (CRBN) via a linker to form PROTAC[1]. CDK9|17 μM (IC50, MCF-7 cells) [1]. Bian J , et al. Discovery of Wogonin-based PROTACs against CDK9 and capable of achieving antitumor activity. Bioorg Chem. 2018 Dec;81:373-381.

LL-K9-3, a selective hydrophobic tagging technology (HyT)-based degrader, specifically targets the CDK9-cyclin T1 complex, displaying DC50 values of 589 nM for cyclin T1 and 662 nM for CDK9. This compound consists of the CDK9 inhibitor, SNS 032, linked to a hydrophobic tag via a glycol linker. Notably, LL-K9-3 does not affect the degradation of other CDKs (CDK1, 2, 4, 5, 6, and 7). Tested in 22RV1 cells, it effectively reduces androgen receptor (AR) and cMyc expression by inducing the selective and synchronous degradation of CDK9 and cyclin T1.

CDK7 9-IN-1 is a specific inhibitor of cyclin-dependent kinases 7 9 (CDK7 9), targeting CDK7 with IC50 values of 0.0656 μM without pre-incubation and 0.00574 μM after 3 hours pre-incubation, and displaying inhibitory activity against CDK9 with an IC50 of 2.14 μM after 3 hours pre-incubation, making it valuable for cancer research.

CDK9-IN-27 (Compound 6a), a CDK9 inhibitor with an IC50 of 0.424 μM, induces apoptosis and S-phase cell cycle arrest. It exhibits cytotoxicity against HepG2, HCT-116, and MCF-7 cell lines, with IC50 values ranging from 10.31 to 40.34 μM, rendering it applicable in cancer research [1].

BAY 61-3606 HCl is a cell-permeable, reversible inhibitor of spleen tyrosine kinase. BAY 61-3606 HCl can inhibit degranulation and block cytokine release from mast cells. Oral administration of BAY 61-3606 to rats was shown to suppress antigen-induced passive cutaneous anaphylactic reaction, bronchoconstriction, and bronchial edema. It can also sensitize MCF-7 breast cancer cells to TNF-related apoptosis-inducing ligand (TRAIL)-mediated apoptosis by inhibiting Cdk9. This compound has been used in a pre-clinical model to explore the feasibility of targeting Syk in the treatment of retinoblastoma.

CDK7-IN-20 is a potent, selective, and irreversible inhibitor of Cyclin-Dependent Kinase 7 (CDK7) with an IC50 value of 4 nM, exhibiting over 206-fold selectivity against related kinases [CDK1, CDK2, CDK3, CDK5, CDK6, CDK9, and CDK12]. It holds potential for research into autosomal dominant polycystic kidney disease (ADPKD).

PROTAC CDK9 degrader-2 (compounds 11c) is a potent and selective CDK9 degrader based on PROTAC, with an IC50 of 17 μM in MCF-7 cell lines. Natural product Wogonin binds ubiquitin E3 ligase cereblon (CRBN) via a linker to form PROTAC[1].