Ciclo celular/Ponto de verificação

DS18561882: Potent MTHFD2 inhibitor (IC50=0.0063), inhibits MTHFD1 (IC50=0.57), good oral kinetics.

CDK4/6/1 Inhibitor (Crozbaciclib) is a type of CDK4/6 inhibitor (IC50s: 3 and 1 nM).

Ryuvidine is a dual inhibitor of KDM5A and SETD8, an inducer of the DNA damage response, and can be used to study breast cancer and erythroderma.

GS-6620 PM, oral Hep C polymerase inhibitor prodrug, is a potent GS-6620 derivative with limited activity against other viruses.

NSC16168 is a selective ERCC1-XPF inhibitor that inhibits DNA repair and potentiates the antitumor activity of cisplatin.

ProINDY (Pro-indy) is a potent DYRK inhibitor that activates NFAT for the study of Down syndrome.

Anticancer agent 73 inhibits TRBP, disrupting TRBP-Dicer, and hinders HCC growth and spread by altering HCC miRNA and protein expression.

Setrobuvir (ANA-598) is an orally active non-nucleoside HCV NS5B polymerase inhibitor with inhibitory effects on de novo RNA synthesis and primer extension with

Lunresertib (RP-6306) is a potent, selective, and orally active PKMYT1 inhibitor with an IC50 of 14 nM.Cost-effective and quality-assured.

INDY is an ATP-competitive inhibitor of Dyrk1A and Dyrk1B with IC50s of 0.24 μM and 0.23 μM and a Ki of 0.18 μM for Dyrk1A ATP pocket, respectively.

GSK2643943A is a deubiquitylating enzyme (DUB) inhibitor, with an IC 50 of 160 nM for USP20/Ub-Rho. GSK2643943A has anti-tumor efficacy.

Talviraline (Bay 10-8979) is an RNA-induced DNA polymerase inhibitor.Talviraline is a potent inhibitor of HIV-1-induced cell killing and HIV-1 replication in a

PS423 is a substrate-selective protein kinase PDK1 inhibitor that acts by binding to the PIF-pocket allosteric docking site.

USP30 inhibitor 11 (USP30-IN-11) is a USP30 inhibitor that inhibits SVA and can be used in studies of cancer, mitochondrial dysfunction and Parkinson's.

SB 328437 ((S)-methyl 2-(1-naphthamido)-3-(4-nitrophenyl)propanoate) is an effective and selective antagonist of CCR3 (IC50 = 4.5 nM).

CDK-IN-2 (CDK inhibitor II) is a potent and specific CDK9 inhibitor (IC50: <8 nM).

CF-1743 is an anti-varicella zoster virus nucleoside and inhibits VZV replication.

CDK9-IN-9 is a potent and selective CDK9 inhibitor (IC50: 1.8 nM) with anti-cancer activity. It inhibits CDK2 (IC50: 155 nM).

CCT251455, the mitotic kinase monopolar spindle 1 (MPS1/TTK) inhibitor, is a potent (IC50=3 nM) and specific chemical tool.

GSK2163632A is an insulin-like growth factor 1 receptor inhibitor that acts by binding to a novel region of the GRK active site cleft.

5,6,7,8-Tetrahydro-8-deazahomofolic acid is a potential thymidylate synthase (TS) inhibitor and other folate related enzymes inhibitor.

KM05382 inhibits CDK9 and the transcription of GAPDH.

CDK9-IN-19: Potent CDK9 inhibitor, anti-cancer, moderate pharmacokinetics, low hERG impact, effective in AML research.

Methotrexate-gamma-aspartate has growth inhibitory effects. It is used in antibody-targeted liposomes.

Antifolate C1 blocks purine creation, favors uptake via folate receptors/PCFT over RFC.

5,11-methenyltetrahydrohomofolate blocks GAR & AIR transformylase; used as an anti-purine drug.

Diazoketone methotrexate is an analog of methotrexate with potential antitumor activity.

IIIM-290 is an oral CDK inhibitor (IC50s: 90 and 94 nM for CDK2/A and CDK9/T1).

BIO-7662 is an effective and highly selective antagonist of α4β1 integrin.

TAS-114 is a dUTPase and DPD inhibitor that modulates catabolic pathways to improve systemic availability of 5-FU.

FT206 is a carboxamide inhibitor of ubiquitin-specific protease[1].

Spirofylline is an agent of bronchodilator, has the potential for asthma and bronchitis and emphysema treatment.

α2β1 integrin inhibitor

Lamifiban is a nonpeptide glycoprotein IIb/IIIa antagonist. It prevents platelet loss during experimental cardiopulmonary bypass.

Riviciclib, a CDK inhibitor (CDK9/T1, CDK4/D1, CDK1/B), has IC50s: 20, 63, 79 nM respectively, and fights cisplatin-resistant tumors.

8-Azahypoxanthine (NSC-22709) inhibits hypoxanthine-guanine-xanthine phosphoribosyltransferase and has antimalarial properties.

NTRC 0066-0 is a TTK inhibitor that can be used in cancer research.

SC-52012 is a novel and potent fibrinogen receptor antagonist, an RGD mimetic, which inhibits platelet aggregation.

Votoplam functions as a gene splicing modulator, employed in the inhibition of Huntington's disease [1].

UNC-2170 (UNC2170 Maleate) is the methyl-lysine binding protein, 53BP1 ligand.

Fosfluridine tidoxil, a thymidylate synthase inhibitor, is used potentially for the treatment of colorectal cancer, and breast cancer.

BVDU 5′-Triphosphate is an antiviral agent labeled with 5′-Triphosphate that specifically targets viral DNA polymerase.

DCB-3503, a tylophorine analog, may fight cancer and aid immunosuppression by hindering protein synthesis and modulating HSC70 ATPase function.

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

m-Se3 is a potent, selective inhibitor of c-MYC transcription with demonstrated capability to inhibit tumor growth and exhibit anti-cancer activity [1].

Trovafloxacin: broad-spectrum fluoroquinolone, blocks DNA gyrase/topoisomerase IV and PANX1 channel (IC50=4μM).

Litronesib is a selective inhibitor of mitosis-specific kinesin Eg5. It also has antitumor activity.

L 738167 is a potent antagonist of the long-acting fibrinogen receptor.

ICAM-1-IN-1 is a potent and selective E-selectin(IC50 = 7 nM) and ICAM-1(IC50 = 5 nM) inhibitor.

αvβ6 Integrin Inhibitor 2 is a potent inhibitor of αvβ6 integrin, demonstrating an inhibition concentration (IC50) of 96.5 nM.

PVZB1194, a biphenyl-type inhibitor of Kinesin spindle protein Eg5 (KIF11), exhibits anticancer potential by inducing cell cycle arrest and apoptosis through

Tnp 351 is a novel antifolate drug being assessed for chemotherapy of lung cancer.

Phototrexate, a photochromic Methotrexate analog, is a UVA-activated, reversible DHFR inhibitor with antifolate properties (IC50: 6 nM cis vs. 34 μM trans).

Synstatin (92-119) serves as an anti-tumor agent by suppressing angiogenesis and cancer cell invasion, chiefly through the down-regulation of integrin αvβ3 and

WRN Inhibitor 1 (example 7) is an inhibitor of the Werner Syndrome ATP-dependent helicase enzyme (WRN), selectively targeting its helicase domain.

TC-A 2317 HCl inhibits Aurora A kinase (Ki 1.2 nM) over Aurora B (Ki 101 nM), displaying antitumor effects.

COH1 is a ribonucleotide reductase (RR) inhibitor utilized in research pertaining to cancer, mitochondrial diseases, and neurodegenerative disorders [1].

DDD85646 is an inhibitor of T. brucei N-myristoyltransferase with a Ki of 1.44 nM, an IC50 of 2 nM and an EC50 of 2 nM. The IC50 of hNMT is 4 nM.

Sovesudil (PHP-201) is a potent ROCK inhibitor with IC50 of 3.7 nM/2.3 nM for ROCK-I/II; lowers IOP without hyperemia.

T521 is a selective inhibitor of the PBD of Plk1 and shows no inhibitory effect on Plk2 and Plk3.

5'-ODMT cEt N-Bzm5 C Phosphoramidite is a strong modified nucleic acid analog for antisense oligos.

CDK7-IN-25 (CY-16-1) is a potent CDK7 inhibitor with an IC50 value of less than 1nM, utilized in cancer research [1].

ROCK-IN-9 (Compound T345), a ROCK inhibitor, exhibits cytotoxicity in HepG2 cells with an IC50 of 40.8 μM.

ML-099 is a pan Ras-related GTPases activator that activates Rac1, Ras, GTP-binding protein (Rab7), Rab2A and cell division cycle 42.

L-739758 is a glycoprotein IIb/IIIa inhibitor.

GSPT1 degrader-2 is a potent degrader of GSPT1 [1].

pppApG serves as an initial substrate for the synthesis of vRNA (viral RNA) and cRNA (complementary RNA), with applications in influenza virus research [1].

Thymidine-5’-O-(α,β-methylene)diphosphate (TMP-CP), a hydrolytically stable derivative of TDP, functions as an inhibitor of thymidine kinase (Ki = 23 µM).

GGTI 2147 decreased Rac1 activity, down-regulated p65 expression, and ameliorated OGD/R-induced neuronal apoptosis.

Bexotegrast (PLN-74809) inhibits αVβ1/αVβ6 integrins, preventing TGF-β1 activation to treat IPF and PSC.

RIOK2-IN-1 (com 4) is a selective RIOK2 inhibitor with a Kd of 150 nM, though it demonstrates low cellular activity with an IC50 of 14,600 nM.

WRN Inhibitor 4 (Example 107), a cyclic vinyl sulfone-based compound, serves as an inhibitor of the Werner Syndrome ATP-dependent helicase enzyme (WRN).

(±)9(10)-DiHOME, the diol derivative of (±)9(10)-EpOME—a cytochrome P450-derived epoxide of linoleic acid also known as leukotoxin—is formed through the action of soluble epoxide hydrolase (sEH) in neutrophils. It exhibits toxicity towards Sf21 cells expressing sEH as well as tolacZ-expressing control cells, differing from leukotoxin which only harms sEH-containing cells. Furthermore, combined exposure to 9(10)- and 12(13)-DiHOME leads to cell death in rabbit renal proximal tubule cells by disrupting mitochondrial respiration, and causes lung injury, respiratory distress, and mortality in mice, highlighting its role as a toxic lipid mediator. Specifically, 9(10)-DiHOME has been associated with acute respiratory distress syndrome (ARDS), a severe and often deadly complication in patients with major burns. Elevated levels of this compound have been detected in the bronchoalveolar lavage fluid (BALF) of women, but not men, with chronic obstructive pulmonary disease (COPD), and its levels are also increased in patients with allergic asthma, indicating its significance in respiratory conditions.

Abetimus (LJP 394 free base), an immunosuppressant composed of four double-stranded DNA (dsDNA) oligonucleotides, can crosslink anti-dsDNA antibodies on B cell

WRN Inhibitor 3 (example 110), a cyclic vinyl sulfone-based compound, serves as an inhibitor of the Werner Syndrome ATP-dependent helicase enzyme (WRN).

CDK-IN-11, a heterocyclic compound, promotes cardiomyocyte maturation [1].

PD 121373, a Benzothiopyrano-indazole, inhibits nucleic acid synthesis, equally affecting DNA/RNA.

NSC15520 is an RPA inhibitor that inhibits helical destabilization of double-stranded DNA oligonucleotides and can be used to study DNA damage repair.

USP1-IN-3 is a selective inhibitor of USPI that inhibits USPI-UAFI (IC50<30 nM). USP1-IN-3 can be used to study cancer.

KIF18A-IN-7 is an orally active inhibitor targeting KIF18A, demonstrating potent inhibition with an IC50 value of 9.4 nM against the microtubule-dependent

Cytidine 3'-monophosphate, a ribonucleotide, results from the hydrolysis of cytidine 2',3'-cyclic monophosphate via RNase—a process that cytidine 3'-monophosphate itself inhibits. Additionally, it can be dephosphorylated to cytidine by 3'-nucleotidase.