Ciclo celular/Ponto de verificação

CDK8-IN-3 is an inhibitor of CDK8.

H3B-968 is a potent inhibitor of Werner syndrome protein (WRN) with an IC50 of approximately 10 nM, effectively targeting its helicase, ATPase, and exonuclease

hDHODH-IN-1 is an inhibitor of human dihydroorotate dehydrogenase (hDHODH) with an anti-inflammatory effect.

BI-1950: potent inhibitor of LFA-1, key in immune function and drug target.

DNA Gyrase-IN-8 is a potent inhibitor of DNA gyrase, demonstrating antimicrobial activity with an IC50 of 8.45 µM [1].

Amotosalen is a Dermatologic Agent.

DMA-IN-1 is a DNA adenine methyltransferase (DAM) inhibitor with an IC50 value of 48 μM.

CDK7-IN-14 (compound 3) is a pyrimidine-derived CDK7 inhibitor applicable for studying cancers associated with transcriptional dysregulation.

GRK2 Inhibitor 2 (Compound 8h), with an IC50 of 19 nM for GRK2 and 137 nM for Aurora-A, enhances β-AR-mediated cAMP accumulation in GRK2-overexpressing HEK293

VER-00158411 is a checkpoint kinase 1 and CHK2 inhibitor (IC50: 4.4 nM and 4.5 nM, respectively).

USP1-IN-5 (compound 10) is a potent inhibitor of both USP1, with an IC50 of less than 50 nM, and MDA-MB-436 cells, where it also exhibits an IC50 of less than

Pelitrexol (AG2037) is a GARFT inhibitor, which can inhibit the activity of mTORC1, block the cell cycle in the s-phase, with antiproliferative activity,NSCLC .

Halofuginone hydrochloride (RU-19110), a derivative of Febrifugine, functions as a competitive inhibitor of prolyl-tRNA synthetase, displaying a Ki value of 18.3 nM. This compound effectively inhibits type-I collagen synthesis, providing therapeutic benefits in osteoarthritis (OA) by impeding TGF-β signaling. Additionally, it serves as a potent pulmonary vasodilator, mainly through the activation of Kv channels and the inhibition of various calcium channels including voltage-gated, receptor-operated, and store-operated ones. Beyond its vascular effects, Halofuginone hydrochloride exhibits a broad spectrum of biological activities, including anti-malarial, anti-inflammatory, anti-cancer, and anti-fibrotic properties, supported by multiple studies.

8-NH2-ATP tetrasodium, an inactive ATP variant, originates from 8-NH2-Ado tetrasodium, which triggers the apoptosis-associated cleavage of poly (ADP-ribose) polymerase [1] [2].

KY386 is a potent and selective DHX33 helicase inhibitor with an IC50 value of 19 nM.

Palmitoyl 3-carbacyclic phosphatidic acid, a palmitoylated Carba-like cyclophosphatidic acid and LPA (lysophosphatidic acid) analog, possesses distinct biological activities compared to LPA, including the inhibition of RhoA activation and melanoma cell migration. This compound has demonstrated efficacy in inhibiting experimental lung metastasis and reducing tumor nodule counts in a B16-F0 xenograft mouse model [1].

CASK-IN-1 is a highly potent and selective CASK inhibitor with a K d value of 0.022 μM.

PLK4-IN-4 (compound 22), a potent inhibitor of PLK4, exhibits an IC50 value of 7.9 nM, suggesting its potential use in cancer research [1].

Wee1 Inhibitor I is an ATP-binding site-targeting Wee1 inhibitor.

CDK9-IN-29 (compound Z11) is a potent inhibitor of CDK9, exhibiting high kinase selectivity and an IC50 value of 3.20 nM.

WRN Inhibitor 5 (Example 157), a cyclic vinyl sulfone-based compound, serves as an inhibitor of Werner Syndrome ATP-dependent helicase enzyme (WRN).

LDC3140 is a potent inhibitor of Cyclin-dependent kinase 7 (CDK7).

GW814408X, a kinase chemical genome group (KCGS) compound, inhibits the AURKC kinase, which is involved in cell cycle progression, checkpoint regulation, and cell division. It exhibits cell line-dependent toxicity, such as cytotoxic effects on HeLa cells, and acts as a protein kinase inhibitor across ATP-dependent and -independent luciferases, potentially impacting Fluc reporter assays [1].

CT1113, a potent inhibitor of both USP28 and USP25, effectively reduces MYC levels in vivo and demonstrates anti-tumor efficacy in a mouse pancreatic cancer CDX

Compound 6k, also known as Anti-hepatic fibrosis agent 2, is an orally active inhibitor of the COL1A1 enzyme and exerts anti-fibrogenic effects by targeting the

Mps1-IN-6 (Compound 9) is a highly effective Mps1 inhibitor with an IC50 value of 6.4 nM and exhibits significant anti-proliferation and anti-tumor effects on

HQ005, a potent CCNK degrader, exhibits an impressive DC50 value of 0.041 µM and functions as a molecular-glue degrader.

TNH, a dimeric compound, possesses the ability to penetrate living cells and facilitate the recruitment of proteins into cellular structures [1].

PD-321852, a Chk1 inhibitor, boosts gemcitabine's effect in pancreatic cancer cells, varying from minimal in Panc1 to >30-fold in MiaPaCa2.

Zaurategrast (CDP323) is an oral α4-integrin antagonist that blocks VCAM-1 interactions and is used to study immune cell trafficking.

BMT-090605: AAK1 inhibitor (IC50=0.6 nM), also affects BIKE (45 nM) and GAK (60 nM), has antinociceptive properties.

CDK9-IN-2, a CDK9 inhibitor from patent WO/2012131594A1, IC50: 5 nM in A2058, 7 nM in H929 at 72hr.

L-Methioninamide hydrochloride is a potent inhibitor of methionyl-tRNA synthetase that reduces the toxicity of CDDP.

Mevociclib (SY-1365) is a highly selective covalent inhibitor of CDK7. SY-1365 possesses therapeutic potential in both hematological and solid tumors.

αvβ1 integrin-IN-2 (compound 32) is a potent inhibitor of ανβ1 and α5β1 integrins, exhibiting IC50 values of 0.9 nM and 33 nM, respectively.

DNA polymerase-IN-3 (Compd 5b), a coumarin derivative, demonstrates inhibitory activity against Taq DNA polymerase and has potential applications in

NVS-SM2 boosts SMN2 splicing, enhances exon 7 inclusion, and raises SMN protein levels orally.

PTC258 is a specific, orally active modulator of the splicing of the Elongator complex protein 1 gene (ELP1), enhancing its expression both in vitro and in vivo

Lerociclib (G1T38) is a CDK4/6 inhibitor with anticancer and antitumor activities, inhibiting CDK4/CyclinD1 and CDK6/CyclinD3.

PLK1/p38γ-IN-1 (compound 14) serves as a dual inhibitor targeting both PLK1 and p38γ kinases, effectively suppressing the proliferation of human hepatocellular

SB-267268: αvβ3 inhibitor (IC50: 0.68 nM human, 0.29 nM mouse), blocks αvβ3/αvβ5 integrins (Ki: 0.9 nM human, 0.5 nM monkey αvβ3, 0.7 nM human αvβ5).

5'-ODMT cEt m5U Phosphoramidite Amidite, a locked nucleic acid (LNA) analog, demonstrates exceptional safety and antisense activity [1] [2].

3-Cyanovinylcarbazole phosphoramidite: an antiviral, hinders viral DNA synthesis, modifies ribonucleotides.

FT671 is a non-covalent, selective USP7 inhibitor, disrupts the stability of USP7 substrates including MDM2, elevates p53, induces p21, inhibits tumor growth.

Pen is an oral cancer drug that blocks DNA synthesis by inhibiting key enzymes and integrating into DNA.

5'-ODMT cEt N-Bz A Phosphoramidite Amidite, a locked nucleic acid (LNA) analogue, exhibits hybridization and mismatch discrimination capabilities similar to LNA, and shows resistance to exonuclease digestion [1].

JNJ-26076713, an oral alpha V integrin blocker, may treat macular edema, AMD, and diabetic retinopathy.

SJ26 is a Wnt1 inhibitor known for its anticancer activity. It inhibits the expression of WNT1 and the downstream signaling pathways mediated by WNT1 in a G-quadruplex structure-dependent manner, thereby suppressing the migratory activity of cancer cells.

DYRKs-IN-2 has antitumor activity. DYRKs-IN-2 is a potent DYRKs inhibitor with IC50s of 30.6 nM and 12.8 nM for DYRK1B and DYRK1A, respectively.

MS-444 (BE-34776) is an MLCK and HuR inhibitor with antitumor activity that can be used to study triple-negative breast cancer and colorectal cancer.

ROCK2-IN-2 is a selective inhibitor of ROCK2 (IC50 of <1 μM).

4′-DTMP (4-Demethyltrimethoprim) is a DHFR inhibitor with antimicrobial activity against Escherichia coli.

AVG-233 is an RNA-dependent RNA polymerase (RdRp) inhibitor with antiviral activity for the study of respiratory syncytial virus infections.

CCT241533 hydrochloride is an effective and selective ATP competitive inhibitor of CHK2 (Ki: 1.16 nM; IC50: 3 nM).

PDD00031705 is a benzimidazolone core cell-inactive Poly (ADP-ribose) glycohydrolase (PARG) inhibitor.

LX7101 is an effective inhibitor of LIMK and ROCK2 (IC50: 24, 1.6, and 10 nM for LIMK1, LIMK2, and ROCK2, respectively). It also inhibits PKA (IC50 <1 nM).

USP7-IN-1 is a selective and reversible ubiquitin-specific protease 7 (USP7) inhibitor (IC50 = 77 μM).

ROCK-IN-8 (Example 4), a ROCK inhibitor, exhibits anti-inflammatory properties and is suitable for respiratory and gastro-intestinal disease research,

Voruciclib hydrochloride is an orally active and selective inhibitor of CDK (Ki: 0.626 nM-9.1 nM).

GSK2850163 is a novel inhibitor of inositol-requiring enzyme-1 alpha (IRE1α) which can inhibit RNase activity and IRE1α kinase activity (IC50s: 200 and 20 nM).

LX7101 is a potent inhibitor of both LIM kinase (LIMK) 1 and 2, and Rho-associated kinase 1 (ROCK1) and ROCK2, with IC50 values of 32, 4.3, 69, and 32 nM, respectively. It is selective, demonstrated by its lack of cross-reactivity in a panel of binding assays involving 78 receptors, transporters, and an additional 430 kinases, at a concentration of 10 μM. The topical administration of LX7101 (3 μl of a 1 mg/ml solution) to the eye has been shown to reduce intraocular pressure in a dexamethasone-induced mouse model of glaucoma.

ROCK2 inhibitor is a chemical compound associated with the therapeutic management of psoriasis.

CCT-251921 is a potent, selective, and orally bioavailable CDK8 inhibitor (IC50: 2.3 nM).

DHODH-IN-14 is an analog of hydroxyfuran pyrimidine A771726.

ROCK-IN-7 (compound 9) serves as a ROCK kinase inhibitor and is utilized in the investigation of ocular conditions, including glaucoma and retinal diseases [1].

DNA polymerase-IN-1 exhibits antiproliferative activity against tumor cells and inhibits Taq DNA polymerase as a DNA polymerase inhibitor.

TAK 029 is a local glycoprotein IIb/IIIa receptor inhibitor.

Chroman 1 is a potent inhibitor of ROCK1 (IC50 = 52 pM) and ROCK2 (IC50 = 1 pM).

AR-13503, a Netarsudil metabolite, is a ROCK inhibitor, potentially treating glaucoma and lowering eye pressure.

Brodimoprim is an inhibitor of dihydrofolate reductase(DHFR).

EHT 5372 inhibits DYRK kinases; IC50: 0.22-221 nM for DYRK1A/B, DYRK2/3, CLK1/2/4, GSK-3α/β.

DHX9-IN-6 is a highly effective ATP-dependent RNA helicase A (DHX9) inhibitor, used in cancer research.

Teclistamab(JNJ-64007957) is a human bispecific monoclonal antibody targeting the CD3 receptor on t-cells and the BCMA for relapsed and refractory multiple myeloma.

ATN-161 is an integrin α5β1 binding peptide and antagonist that inhibits VEGF-induced hCECs migration and angiogenesis.

Senexin C is a CDK8/19 inhibitor with anticancer activity.Senexin C inhibits the growth of MV4-11 leukemia cells.

DHX9-IN-4 is an ATP-dependent RNA helicase DHX9 inhibitor used in cancer research.

AAPK-25, a dual Aurora/PLK inhibitor, disrupts mitosis, induces apoptosis, and has antitumor properties.

Bisindolylmaleimide X hydrochloride (BIM-X hydrochloride) is a potent and selective PKC inhibitor. It is also a potent CDK2 antagonist (IC50: 200 nM).

Netropsin dihydrochloride, a small MGB, blocks topoisomerase I/II, hindering cleavable complex stabilization.

XL413 hydrochloride (BMS-863233 Hydrochloride) is a potent, selective and ATP competitive inhibitor of Cdc7. XL413 hydrochloride also inhibits CK2 and PIM1.

Senexin A hydrochloride functions as a selective inhibitor of CDK8/19, with an IC 50 of 280 nM for CDK8, and specifically inhibits p21-induced transcription without affecting other biological effects of p21. Additionally, it suppresses CMV-GFP induction and the stimulatory activity of the consensus NF-κB-dependent promoters [1] [2].

Mefenidil (McN-2378), a selective cerebral vasodilator, was shown to increase CBF in healthy brains without stimulating O2 uptake in a dog anesthesia model.

NU6300 is a covalent CDK2 inhibitor exhibiting irreversible and ATP-competitive properties and also functions as a GSDMD (Gasdermin D) inhibitor.

CCG-232964 is an orally active Rho/MRTF/SRF inhibitor that suppresses LPA-induced CTGF gene expression [1].

ROCK2-IN-6 hydrochloride (Comp A)为一种选择性ROCK2抑制剂，适用于研究ROCK介导的疾病、自身免疫性病症与炎症。

WRN Inhibitor 2 (example 118), a potent inhibitor of the WRN (Werner Syndrome ATP-dependent helicase enzyme), exhibits a pIC50 value of 7.0 or greater [1].