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AGI-24512 is a potent methionine adenosyltransferase 2α (MAT2A) inhibitor, with an IC50 of 8 nM. AGI-24512 triggers DNAdamageresponse. AGI-24512 can block proliferation of MTAP-deleted cancer cells in vitro. AGI-24512 can be used for researching anticancer .
FEN1-IN-1 (compound 1) is a small molecule flap endonuclease 1 (FEN1) inhibitor with antitumor activity. FEN1-IN-1 binds to the active site of FEN1 and partly achieves inhibition by the co-ordination of Mg 2+ ions. FEN1-IN-1 initiaties a DNAdamageresponse and activates the ATM checkpoint signalling pathway, the phosphorylation of histone H2AX and the ubiquitination of FANCD2 in mammalian cells. FEN1-IN-1 is promising for research of cancers .
Bendamustine hydrochloride (SDX-105), a purine analogue, is a DNA cross-linking agent. Bendamustine hydrochloride activats DNA-damage stress response and apoptosis. Bendamustine hydrochloride has potent alkylating, anticancer and antimetabolite properties .
Bendamustine (SDX-105 free base), a purine analogue, is a DNA cross-linking agent. Bendamustine activates DNA-damage stress response and apoptosis. Bendamustine has potent alkylating, anticancer and antimetabolite properties .
E235 is an expression regulator of activates transcription factor 4 (ATF4). E235 reduces cell viability by activating integrated stress response (ISR) and DNAdamageresponse signals. E235 has anti-proliferative activity and can be used for tumor research .
Bractoppin is a potent and selective agent-like inhibitor of phosphopeptide recognition by the human BRCA1 tandem(t) BRCT domain (binding IC50: 74 nM). Bractoppin diminishes BRCA1 recruitment to DNA breaks, in turn suppressing damage-induced G2 arrest and assembly of the recombinase, RAD51. Bractoppin preferentially inhibits BRCA1 tBRCT-dependent steps in the DNAdamageresponse .
DDRI-18 is a DNAdamageresponse inhibitor that inhibits the non-homologous end-joining (NHEJ) DNA repair process. DDRI-18 is an effective chemosensitizing agent .
ATR-IN-11 (Compound Hit01) is a potent inhibitor of ataxia telangiectasia and Rad3-related (ATR) kinase. ATR kinase is a key regulating protein within the DNAdamageresponse (DDR), responsible for sensing replication stress (RS). ATR-IN-11 is a promising lead compound for subsequent agent discovery targeting ATR kinase. ATR-IN-11 has the potential for the research of cancer disease .
DNA-PK-IN-9 (compound YK6) is a potent DNA-dependent protein kinase (DNA-PK) inhibitor with an IC50 value of 10.47 nM. DNA-PK-IN-9 can be used for researching anticancer .
Bendamustine-d8 (hydrochloride) is deuterium labeled Bendamustine (hydrochloride). Bendamustine hydrochloride (SDX-105), a purine analogue, is a DNA cross-linking agent. Bendamustine hydrochloride activats DNA-damage stress response and apoptosis. Bendamustine hydrochloride has potent alkylating, anticancer and antimetabolite properties .
NSC15520 is a small molecular inhibitor of Replication Protein A (RPA). NSC15520 specifically recognizes the RPA N-terminal DNA binding domain (DBD), and blocks the interaction of RPA with p53 or RAD9. NSC15520 also inhibtis helix destabilization of a duplex DNA (dsDNA) oligonucleotide, involves in DNA replication, DNA repair, DNA recombination, and DNAdamageresponse signaling .
ML367 is a potent inhibitor of ATPase family AAA domain-containing protein 5 (ATAD5) stabilization, acts as a probe molecule that has low micromolar inhibitory activity. ML367 blocks DNA repair pathways, suppresses general DNAdamageresponses including RPA32-phosphorylation and CHK1-phosphorylation in response to UV irradiation .
Nimustine is an alkylating agent, which induces DNA double-strand breaks (DSBs) and inter-strand crosslinks (ICLs), thereby activating the DNAdamageresponse (DDR) signaling pathway. Nimustine activates p38 MAPK/JNK signaling pathway, and exhibits antitumor activity .
Bendamustine-d8 is the deuterium labeled Bendamustine . Bendamustine (SDX-105 free base), a purine analogue, is a DNA cross-linking agent. Bendamustine activates DNA-damage stress response and apoptosis. Bendamustine has potent alkylating, anticancer and antimetabolite properties .
Bendamustine (hydrochloride) (Standard) is the analytical standard of Bendamustine (hydrochloride). This product is intended for research and analytical applications. Bendamustine hydrochloride (SDX-105), a purine analogue, is a DNA cross-linking agent. Bendamustine hydrochloride activats DNA-damage stress response and apoptosis. Bendamustine hydrochloride has potent alkylating, anticancer and antimetabolite properties .
(R)-(-)-α-Phellandrene ((-)-α-Phellandrene) is an the (R)-(-)-stereoisomer of α-phellandrene. α-phellandrene is an orally active cyclic monoterpene that attenuates inflammatory response, and induces DNAdamage .
Bendamustine (Standard) is the analytical standard of Bendamustine. This product is intended for research and analytical applications. Bendamustine (SDX-105 free base), a purine analogue, is a DNA cross-linking agent. Bendamustine activates DNA-damage stress response and apoptosis. Bendamustine has potent alkylating, anticancer and antimetabolite properties .
JA2131 is a small molecular inhibitor of Poly(ADP-ribose) Glycohydrolase (PARG) (IC50=0.4 μM). JA2131 regulate DNAdamageresponses, causes replication fork stalling and cancer cell death .
Nimustine hydrochloride (ACNU) is the hydrochloride salt form of Nimustine (HY-13703). Nimustine hydrochloride is an alkylating agent, which induces DNA double-strand breaks (DSBs) and inter-strand crosslinks (ICLs), thereby activating the DNAdamageresponse (DDR) signaling pathway. Nimustine hydrochloride activates p38 MAPK/JNK signaling pathway, and exhibits antitumor activity .
Bendamustine-d7 hydrochloride (SDX-105-d7) is the deuterium labeled Bendamustine hydrochloride (HY-B0077). Bendamustine hydrochloride (SDX-105), a purine analogue, is a DNA cross-linking agent. Bendamustine hydrochloride activats DNA-damage stress response and apoptosis. Bendamustine hydrochloride has potent alkylating, anticancer and antimetabolite properties .
p53 Activator 13 (compound 11) is a 6mA methyltransferase CamA inhibitor and a p53 activator. p53 Activator 13 intercalates into CamA-bound DNA via the minor groove, causing a conformational shift that moves the catalytic domain away from the DNA and elicits DNAdamageresponse via p53 activation. p53 Activator 13 can be utilized in cancer research .
Dibenz[a,h]anthracene (DBA) is a polycyclic aromatic hydrocarbon (PAH) of considerable tumorigenicity. Dibenz[a,h]anthracene results in DNA adduct formation leading to the activation of a DNAdamageresponse. Dibenz[a,h]anthracene induces cell cycle arrest and apoptosis via both Tp53-dependent and Tp53-independent mechanisms .
KL-50 is a selective toxin toward tumors that lack the DNA repair protein O 6-methylguanine-DNA-methyltransferase (MGMT), which reverses the formation of O 6-alkylguanine lesions. KL-50 activates DNAdamageresponse pathways and cycle arrest in MGMT-cells, independent of mismatch repair (MMR). KL-50 is promising for research of brain tumors that lack the DNA repair protein MGMT .
Adenosine 5′-diphosphoribose (ADP ribose) is composed of an adenine base attached to a ribose sugar, which is in turn linked to two phosphate groups. Adenosine 5′-diphosphoribose is a key molecule involved in a variety of cellular processes, particularly in the response to DNAdamage and the regulation of gene expression .
BTX161, a thalidomide analog, is an effective CKIα degrader. BTX161 mediates human AML cell CKIα degradation more effectively than lenalidomide and activates the DNAdamageresponse (DDR) and p53, while stabilizing p53 antagonist MDM2.
ATR-IN-12 (Compound 5g) is a potent inhibitor of ataxia telangiectasia and Rad3-related (ATR) kinase with an IC50 value of 0.007 μM. ATR-IN-12 displays good anti-tumor activity and significantly reduces the phosphorylation level of ATR and its downstream signaling protein. ATR-IN-12 is a promising lead compound for subsequent agent discovery targeting ATR kinase .
ATR-IN-23 (Compound 34) is a potent and selective ATR inhibitor with an IC50 of 1.5 nM. ATR-IN-23 has potent antiproliferative effects on LoVo cells and synthetic lethality on HT-29 cells, and can be used in the study of DNAdamageresponse (DDR)-deficient cancers .
Telomeric G4s ligand 1 is a telomeric G-quadruplex ligand that stabilizes telomeric G4 and induces R-loop formation, leading to DNAdamageresponses. Telomeric G4s ligand 1 induces apoptosis and evokes immunogenic cell death (ICD) in tumor cells .
ATM-IN-1 is a potent inhibitor of ATM. ATM is located mainly in the nucleus and microsomes and is involved in cell cycle progression and in the cell cycle checkpoint response to DNAdamage. ATM-IN-1 has the potential for the research of cancer and neurology diseases (extracted from patent WO2021139814A1, compound 3) .
Elimusertib (BAY 1895344) hydrochloride is a potent, orally active and selective ATR inhibitor with an IC50 of 7 nM. Elimusertib hydrochloride has anti-tumor activity . Elimusertib hydrochloride can be used for the research of solid tumors and lymphomas .
Elimusertib (BAY-1895344) is a potent, orally active and selective ATR inhibitor with an IC50 of 7 nM. Elimusertib has anti-tumor activity . Elimusertib can be used for the research of solid tumors and lymphomas .
DNA-PK-IN-8 is a highly potent, selective and orally active DNA-dependent protein kinase (DNA-PK) inhibitor with an IC50 value of 0.8 nM. DNA-PK-IN-8 exhibits synergistic antiproliferative activity against a series of cancer cell lines and significantly suppresses HL-60 tumor growth, when using in combination with Doxorubicin .
HQ461 is a molecular glue that promotes CDK12-DDB1 interaction to trigger cyclin K degradation. HQ461-mediated degradation of cyclin K impairs CDK12 function, resulting in decreased CDK12 substrate phosphorylation, downregulation of DNAdamageresponse genes, and cell death .
Dibenz[a,h]anthracene (Standard) is the analytical standard of Dibenz[a,h]anthracene. This product is intended for research and analytical applications. Dibenz[a,h]anthracene (DBA) is a polycyclic aromatic hydrocarbon (PAH) of considerable tumorigenicity. Dibenz[a,h]anthracene results in DNA adduct formation leading to the activation of a DNAdamageresponse. Dibenz[a,h]anthracene induces cell cycle arrest and apoptosis via both Tp53-dependent and Tp53-independent mechanisms .
APE1-IN-2 (compound AP1) is a Pt(IV) proagent, targeting a critical BER protein, apurinic/apyrimidinic endonuclease 1 (APE1). APE1-IN-2 shows anticancer activity. APE1-IN-2 induces intracellular accumulation of platinum and activates DNAdamageresponse and apoptosis signals .
CDK12/13-IN-3 (Compound 12b) is the orally active inhibitor for CDK that inhibits CDK12 and CDK13 with IC50 of 107.4 nM and 79.4 nM. CDK12/13-IN-3 inhibits the phosphorylation of Ser2 on the CTD of RNA polymerase II, induces DNAdamage, and downregulates the gene expression of DNAdamageresponse (DDR). CDK12/13-IN-3 exhibits antiproliferative activity against multiple cancer cells with IC50 of nanomolar levels. CDK12/13-IN-3 exhibits antitumor effect in mouse models, exhibits good pharmacokinetic properties with an oral bioavailability of 53.6% .
5-Fluoro-2'-deoxycytidine (FdCyd), a fluoropyrimidine nucleoside analogue, is a DNA methyltransferase (DNMT) inhibitor. 5-Fluoro-2'-deoxycytidine is a tumor-selective proagent of thymidylate synthase inhibitor 5-fluoro-2′-dUMP. 5-Fluoro-2'-deoxycytidine can induce cell cycle arrest in tumor cells through the DNAdamageresponse, and it has anti-tumor activity .
ATM Inhibitor-3 (compound 34) is a potent and selective ATM inhibitor, with an IC50 of 0.71 nM. ATM Inhibitor-3 shows inhibition of PI3K kinases family. ATM Inhibitor-3 exhibits favorable metabolic stability .
ATM Inhibitor-4 (compound 39) is a potent and selective ATM inhibitor, with an IC50 of 0.32 nM. ATM Inhibitor-4 shows stronger inhibition of PI3K kinases family. ATM Inhibitor-4 shows a full inhibition of mTOR at 1 μM. ATM Inhibitor-4 exhibits favorable metabolic stability .
NTPO (Nitrilotris methylenephosphonic acid) is a DNA damage inducer, causing genomic DNA damage and fragmentation, activating ATR-mediated cell cycle checkpoints. The DNA damaging effects of NTPO are abrogated by base excision repair (BER) but not nucleotide excision repair (NER) .
MDOLL-0286 is a selective Poly(ADP-ribose) Glycohydrolase (PARG) (ARH3) inhibitor with an IC50 of 2.3μM. MDOLL-0286 can inhibit ARH3’s poly-ADP-ribose hydrolytic activity on cellular substrates. MDOLL-0286 can inhibit DNAdamageresponse. MDOLL-0286 can be used for the research of cancer .
ATR kinase substrate peptide (compound 45) is a potent and selective inhibitor of ATR (Ataxia Telangiectasia and Rad3 related) protein kinase (Ki=6 nM). ATR kinase substrate peptide inhibits ATR activity by competing with ATR kinase ATP-binding sites to block ATR mediated signaling. ATR kinase substrate peptide can be used to study the role of ATR kinase in DNAdamageresponse .
PDIC-NN (PDIC-NS free base) is a STING activator with anticancer activity. PDIC-NN promotes the content and biostability of endogenous cyclic dinucleotides (CDNs). PDIC-NN triggers ROS burst and causes serious damage to mitochondria. PDIC-NN induces cell apoptosis and inhibits DNA replication. PDIC-NN activates cGAS-STING signaling pathway, enhances the immunogenicity of tumor cells and activates a robust innate immune response .
W1131 TFA is a potent STAT3 inhibitor that induces ferroptosis. W1131 inhibits cancer progression in subcutaneous xenograft, organoid, and PDX models of gastric cancer. W1131 effectively alleviates cancer cell chemoresistance to 5-FU (HY-90006). W1131 regulates the cell cycle, DNAdamageresponse, and oxidative phosphorylation, including the IL6-JAK-STAT3 pathway and the ferroptosis pathway .
PDIC-NN dimethanesulfonate (PDIC-NS) is a STING activator with anticancer activity. PDIC-NN dimethanesulfonate promotes the content and biostability of endogenous cyclic dinucleotides (CDNs). PDIC-NN dimethanesulfonate triggers ROS burst and causes serious damage to mitochondria. PDIC-NN dimethanesulfonate induces cell apoptosis and inhibits DNA replication. PDIC-NN dimethanesulfonate activates cGAS-STING signaling pathway, enhances the immunogenicity of tumor cells and activates a robust innate immune response .
7a-Hydroxyfrullanolide has anticancer properties. 7a-Hydroxyfrullanolide reduces polymerization of α-, β-tubulin. 7a-Hydroxyfrullanolide preferrs to bind to β-tubulin over α-tubulin. 7a-Hydroxyfrullanolide also triggers DNAdamageresponse arrests cells in the G2/M-phase. 7a-Hydroxyfrullanolide is an eudesmanolide sesquiterpene lactone (SL) and can be isolated from the flowering plants of the Asteraceae family .
W1131 is a potent STAT3 inhibitor, triggering ferroptosis. W1131 suppresses cancer progression in gastric cancer cell subcutaneous xenograft model, organoids model, and PDX model. W1131 effectively alleviates chemical resistance of cancer cells to 5-FU (HY-90006). W1131 regulates cell cycle, DNAdamageresponse, and oxidative phosphorylation, including IL6-JAK-STAT3 pathway and ferroptosis pathway .
DPQ hydrochloride is a blood-brain barrier permeable and selective PARP-1 inhibitor that blocks PARP-1-mediated DNAdamage repair and NAD +/ATP consumption, thereby inhibiting excessive inflammatory responses. DPQ hydrochloride inhibits NF-κB pathway activation, reduces the expression of pro-inflammatory factors (such as TNF-α, IL-6) and oxidative stress. DPQ hydrochloride can be used in inflammation-related studies of acute lung injury, myocardial infarction, and neurodegenerative diseases .
DPQ is a blood-brain barrier permeable and selective PARP-1 inhibitor that blocks PARP-1-mediated DNAdamage repair and NAD +/ATP consumption, thereby inhibiting excessive inflammatory responses. DPQ inhibits NF-κB pathway activation, reduces the expression of pro-inflammatory factors (such as TNF-α, IL-6) and oxidative stress. DPQ can be used in inflammation-related studies of acute lung injury, myocardial infarction, and neurodegenerative diseases .
CHK1-IN-12 (Compound example 1-5) is an orally active and highly selective checkpoint kinase 1 (CHK1) inhibitor with in vitro enzyme IC50≤10 nM and cellular IC50≤50 nM. CHK1-IN-12 inhibits the phosphorylation activity of CHK1 kinase to block the DNAdamageresponse pathway, inducing tumor cell cycle arrest and apoptosis. CHK1-IN-12 is promising for research of cancers .
5-Fluoro-2'-deoxycytidine (Standard) is the analytical standard of 5-Fluoro-2'-deoxycytidine. This product is intended for research and analytical applications. 5-Fluoro-2'-deoxycytidine (FdCyd), a fluoropyrimidine nucleoside analogue, is a DNA methyltransferase (DNMT) inhibitor. 5-Fluoro-2'-deoxycytidine is a tumor-selective proagent of thymidylate synthase inhibitor 5-fluoro-2′-dUMP. 5-Fluoro-2'-deoxycytidine can induce cell cycle arrest in tumor cells through the DNAdamageresponse, and it has anti-tumor activity .
Antitumor agent-37 possesses potent anti-proliferative and anti-metastasis activities. Antitumor agent-37 induces serious DNAdamage and further leads to high expression of γ-H2AX and p53. Antitumor agent-37 promotes apoptosis of tumor cells through mitochondrial apoptotic pathway Bcl-2/Bax/caspase3. Antitumor agent-37 significantly improves immune response through restraining the expression of PD-L1 to increase CD3+ and CD8+ T infiltrating cells in tumor tissues .
Antitumor agent-36 possesses potent anti-proliferative and anti-metastasis activities. Antitumor agent-36 induces serious DNAdamage and further leads to high expression of γ-H2AX and p53. Antitumor agent-36 promotes apoptosis of tumor cells through mitochondrial apoptotic pathway Bcl-2/Bax/caspase3. Antitumor agent-36 significantly improves immune response through restraining the expression of PD-L1 to increase CD3+ and CD8+ T infiltrating cells in tumor tissues .
NTPO trisodium is a DNA damage inducer, causing genomic DNA damage and fragmentation, activating ATR-mediated cell cycle checkpoints. The DNA damaging effects of NTPO trisodium are abrogated by base excision repair (BER) but not nucleotide excision repair (NER) .
ATR kinase substrate peptide (compound 45) is a potent and selective inhibitor of ATR (Ataxia Telangiectasia and Rad3 related) protein kinase (Ki=6 nM). ATR kinase substrate peptide inhibits ATR activity by competing with ATR kinase ATP-binding sites to block ATR mediated signaling. ATR kinase substrate peptide can be used to study the role of ATR kinase in DNAdamageresponse .
(R)-(-)-α-Phellandrene ((-)-α-Phellandrene) is an the (R)-(-)-stereoisomer of α-phellandrene. α-phellandrene is an orally active cyclic monoterpene that attenuates inflammatory response, and induces DNAdamage .
7a-Hydroxyfrullanolide has anticancer properties. 7a-Hydroxyfrullanolide reduces polymerization of α-, β-tubulin. 7a-Hydroxyfrullanolide preferrs to bind to β-tubulin over α-tubulin. 7a-Hydroxyfrullanolide also triggers DNAdamageresponse arrests cells in the G2/M-phase. 7a-Hydroxyfrullanolide is an eudesmanolide sesquiterpene lactone (SL) and can be isolated from the flowering plants of the Asteraceae family .
rHuGrowth arrest and DNAdamage-inducible protein GADD45 beta/GADD45B, His; Growth Arrest and DNAdamage-Inducible Protein GADD45 Beta; Myeloid Differentiation Primary response Protein MyD118; Negative Growth Regulatory Protein MyD118; GADD45B; MYD118
GADD45B Protein, a pivotal mediator, regulates growth and apoptosis by activating the MTK1/MEKK4 MAPKKK signaling pathway. Interacting with GADD45GIP1, it forms a complex that modulates cellular responses under stress. Its central role in growth and apoptosis underscores its significance in orchestrating cellular processes, positioning GADD45B as a key player in the intricate network of signaling pathways governing cell fate decisions. GADD45B Protein, Human (His) is the recombinant human-derived GADD45B protein, expressed by E. coli , with N-6*His labeled tag.
Bendamustine-d8 (hydrochloride) is deuterium labeled Bendamustine (hydrochloride). Bendamustine hydrochloride (SDX-105), a purine analogue, is a DNA cross-linking agent. Bendamustine hydrochloride activats DNA-damage stress response and apoptosis. Bendamustine hydrochloride has potent alkylating, anticancer and antimetabolite properties .
Bendamustine-d8 is the deuterium labeled Bendamustine . Bendamustine (SDX-105 free base), a purine analogue, is a DNA cross-linking agent. Bendamustine activates DNA-damage stress response and apoptosis. Bendamustine has potent alkylating, anticancer and antimetabolite properties .
Bendamustine-d7 hydrochloride (SDX-105-d7) is the deuterium labeled Bendamustine hydrochloride (HY-B0077). Bendamustine hydrochloride (SDX-105), a purine analogue, is a DNA cross-linking agent. Bendamustine hydrochloride activats DNA-damage stress response and apoptosis. Bendamustine hydrochloride has potent alkylating, anticancer and antimetabolite properties .
Adenosine 5′-diphosphoribose (ADP ribose) is composed of an adenine base attached to a ribose sugar, which is in turn linked to two phosphate groups. Adenosine 5′-diphosphoribose is a key molecule involved in a variety of cellular processes, particularly in the response to DNAdamage and the regulation of gene expression .
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