Ciclo celular / Checkpoint

Etaracizumab (LM 609) is a humanized monoclonal antibody targeting integrin αvβ3, inhibiting angiogenesis and melanoma growth, used in the study of melanoma.

PT-129 is a RPOTAC degrader that targets the G3BP1/2NTF2 domain (protein-RNA interaction site), facilitating the breakdown of intracellular stress granules. It prevents the formation of stress granules in stressed cells and deconstructs existing ones, thereby disrupting ATF4 transmission and inhibiting cancer cell proliferation. Stress granules (SGs) are membraneless cytoplasmic compartments formed under stress, which aid in the transfer of ATF4 from fibroblasts to tumor cells, promoting fibroblast-related tumor growth. G3BP1/2 serve as central proteins in the SG network, and inhibiting them may reduce the stress resilience of cancer cells within the tumor microenvironment. PT-129 consists of a target protein ligand (red part) G3BP1/2-Targeting ligand-1, an E3 ligase ligand (blue part) Thalidomide 4-fluoride, and a PROTAC linker (black part) Amino-PEG3-C2-acid; the E3 ligase ligand and linker form the complex Thalidomide-NH-PEG3-propionic acid.

Dihydrobaicalein is a natural product from Scutellaria baicalensis, a PLK1 inhibitor (IC50:6.3 μM).Dihydrobaicalein inhibits VRK2 and PLK2.

SNS-314 Mesylate (SNS-314) is an effective and specific Aurora A/B/C inhibitor. SNS-314 is less inhibition of Trk A/B, Fms, Flt4, c-Raf, Axl, and DDR2.

Chiauranib, a potent anticancer agent, inhibits angiogenesis kinases (VEGFR1-3, PDGFRα, c-Kit), Aurora B, and CSF1R with IC50 values of 1-9 nM.

LDC4297 (LDC044297) is a potent and selective CDK7 inhibitor.

N2-Isobutyryl-2-deoxyguanosine(iBu-dG) is a nucleoside analog that can be used to synthesize oligonucleotides.

GS-9191 is a potent inhibitor of DNA polymerase alpha and ß , a prodrug of the novel nucleoside analogue 9-(2-phosphonomethoxyethyl)guanine (PMEG) , which

Aurora kinase inhibitor-2 (IUN-70219) is a cell-permeable anilinoquinazoline that inhibit the activity of Aurora A (IC50 = 0.39 M).

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.

AZ3146 is a selective Mps1 inhibitor with IC50 of ~35 nM.

Palmatine, also known as Burasaine, inhibits dopamine production and may treat flavivirus, jaundice, dysentery, hypertension, and liver issues.

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

OSU-T315 (OSU-T315 (1,5-regioisomer)) (1,5-regioisomer) is a ILK inhibitor.

Cirtuvivint (SM08502) is a potent and orally active CDC-like kinase (CLK) inhibitor that can be used to study arthritis.

Taq DNA polymerase is a thermostable enzyme utilized in polymerase chain reactions (PCR) to amplify DNA sequences [1].

PRT4165 (NSC600157) is a potent PRC1-mediated H2A ubiquitylation inhibitor.

(1E)-CFI-400437 dihydrochloride (CFI-400437 dihydrochloride) is a selective and potent polo-like kinase 4 (PLK4) inhibitor.

AUNP-12 acetate is a polypeptide inhibitor of PD-1 that is equivalent to PD-1 and PD-2 in inhibiting lymphocyte proliferation and effector fuction, in addition

PD-1/PD-L1-IN-53 (compound B3) serves as an inhibitor targeting both the PD-1/PD-L1 and VISTA signaling pathways. It is utilized in cancer research.

Cyclo(-RGDfK) is a selective and potent inhibitor of integrin αvβ3 with an IC50 value of 0.94 nM.Cost-effective and quality-assured.

NKP-1339 (IT-139) induces G2/M cell cycle arrest, blockage of DNA synthesis, and induction of apoptosis via the mitochondrial pathway.

MTH1 ligand 1 functions as a target protein ligand for MTH1, and is utilized in the synthesis of PROTACaTAG 2139.

Rafoxanide as a dual CDK4/6 inhibitor for the treatment of skin cancer.

ddUTP (lithium), at a concentration of 100mM in H20, serves as a nucleotide analog capable of being integrated into DNA, RNA, or other nucleic acids.

CSI86 is a PROTAC degrader targeting MYC, exhibiting antiproliferative activity (IC50: 13-18 μM).

D-F07 is a novel fluorescent IRE-1 RNase inhibitor and a tricyclic chromone with potential anticancer activity.

PF 477736 (PF-736,PF-00477736) is a specifc, effective and ATP-competitive Chk1 inhibitor (Ki: 0.49 nM ) and also inhibits FGFR3, Aurora-A, VEGFR2, Flt3, Fms (

SR31527 chloride: potent KIFC1 inhibitor (IC50 6.6 µM), moderately impairs cell viability & colony growth.

Nolatrexed dihydrochloride (Thymitaq) is a soluble, lipophilic cancer drug that inhibits DNA replication, causing cell cycle arrest and apoptosis.

SP-146 is a selective, potent and non-ATP-competitive Aurora B inhibitor(IC50 : 0.316 nM).

KIRA6 is an effective inhibitor of IRE1α RNase kinase (IC50: 0.6 μM). It can trigger an apoptotic response.

MKLP2-IN-1 (compound 12a) is an inhibitor of MKLP2 that demonstrates excellent oral bioactivity. In vitro, MKLP2-IN-1 inhibits the ATPase activity stimulated by recombinant MKLP2 microtubules and, in a mouse Calu-6 lung cancer model, it effectively suppresses tumor growth.

TAK-901 has been used in trials studying the treatment of Lymphoma, Myelofibrosis, Multiple Myeloma, Myeloid Metaplasia, and Advanced Solid Tumors, among others

BLU-222 is a potent, selective and orally active CDK2 inhibitor. BLU-222 shows robust antitumor activity.

CLK1/2-IN-3 (Cpd-3) is a CLK1 and CLK2 inhibitor with antiproliferative activity that inhibits the activity of CLK and SRPK.

PTC-209 is a potent and selective BMI-1 inhibitor.

MLS000532223 is a selectiveRho family GTPases inhibitor(EC50 : 16 μM to 120 μM).

E7820 (ER68203-00) is an angiogenesis inhibitor by suppressing integrin a2 (a cell adhesion molecule expressed on endothelial cells).

Roniciclib (BAY 1000394) is a potent pan-CDK inhibitor and a novel oral cytotoxic agent. Roniciclib inhibits the activity of cell-cycle CDKs CDK1, CDK2, CDK3, CDK4, and of transcriptional CDKs CDK7 and CDK9 with IC(50) values in the range between 5 and 25 nmol/L.

BMVC-8C3O is a DNA G-quadruplex (G4) ligand.Cost-effective and quality-assured.

WEE1degrader 1 (Compound 10) functions as a Wee1 degrader, exhibiting a DC50 value of 1.5 nM against Wee1. This compound also possesses anticancer properties that inhibit cell proliferation.

RO0270608 is an α4β1/α4β7 integrin antagonist with anti-inflammatory activity for the study of allergic inflammatory responses.

1A-116 is a specific Rac1 inhibitor.

MKC9989 is an inhibitor of Hydroxy aryl aldehydes (HAA). MKC9989 also inhibits IRE1α with an IC50 of 0.23 to 44 μM.

JH-RE-06 disrupts mutagenic translesion synthesis (TLS) by preventing the recruitment of mutagenic POLζ.

CDK9-IN-23 (Example 4) is a potent inhibitor of CDK9, exhibiting an IC50 value of less than 20 nM [1].

LY3177833 is an Cdc7 kinase inhibitor (IC50 : 3.3 nM)

Azenosertib (ZN-c3) is a potent and selective Wee1 inhibitor with balanced potency, ADME, and pharmacokinetic properties. Cost-effective and quality-assured.

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

Dithranol (cignoline) is an anthracene derivative that disrupts MITOCHONDRIA function and structure and is used for the treatment of DERMATOSES, especially

Centrinone (LCR-263) (LCR-263) is a reversible inhibitor of polo-like kinase 4 (PLK4; Ki:0.16 nM).

Zeltociclib is an inhibitor of cyclin-dependent kinases (CDKs) with anti-tumor properties.

CDK8-IN-4 is an inhibitor of CDK8 (IC50: 0.2 nM).

EN4 (EN4 MYC inhibitor) MYC inhibitor is a covalent ligand that targets cysteine 171 (C171) of MYC.

Tosyl-L-Arginine Methyl Ester (TAME (N-4-Tosyl-L-arginine methyl ester)) is an APC inhibitor.

Amenamevir (ASP2151) is a novel helicase-primase inhibitor that is active against varicella-zoster virus and herpes simplex virus types 1 and 2 (EC50: 14 ng/mL

Palmatine chloride an isoquinoline alkaloid, is an important medicinal herbal extract with diverse pharmacological and biological properties.

Indisulam (E 7070) is a dual-action anticancer drug, blocking G1/S cell cycle transition by degrading cyclin E and activating p53/p21.

TR-14035 (MDK-1191) is a dual antagonist of α4β7/α4β1 integrins (IC50s: 7/87nM).

Tegafur (FT 207) is a congener of the antimetabolite fluorouracil with antineoplastic activity.

BWC0977 is an effective topoisomerase inhibitor that disrupts bacterial DNA replication by targeting both DNA gyrase and topoisomerase IV. The minimum inhibitory concentration (MIC90) of BWC0977 against MDR (multi-drug resistant) Gram-negative bacteria ranges from 0.03 to 2 µg/mL.

Mycro 3 is potent and selective for c-Myc in whole cell assays.

TASIN-30 is an inhibitor of EBP, exhibiting a competitive EC50 value of 0.097 μM, and possesses a competitive EC50 value of 50 μM against DHCR7.

ITX3 is a specific, non-toxic, active and selective TrioN RhoGEF inhibitor with IC50 of 76 μM.

GSK_WRN4 is a WRN helicase inhibitor with anti-cancer activity, inhibiting MSI tumor cell growth by inducing DNA double-strand breaks, useful in cancer research

Cyclo(RGDyK) trifluoroacetate is a potent and selective αVβ3 integrin inhibitor with IC50 of 20 nM.

Brr2-IN-2 (Compound 30) is an inhibitor of Brr2, exhibiting an IC50 of 42 nM against Brr2 ATPase.

Eg5-IN-1 is a potent inhibitor of the kinesin family of motor proteins (Eg5) with an IC50 value of 1.97 µM for Eg5.Eg5-IN-1 can be used in cancer research.

ASC-69 (APY69) is a promising potent inhibitor of the PD-1/PD-L1 signaling pathway, classified as a small-molecule compound [1].

T56-LIMKi (T5601640) is a selective inhibitor of LIMK2.

IMT1B (LDC203974) is an oral POLRMT inhibitor that curbs mtDNA expression and has anti-cancer properties.