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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
39 Results for "
ATM kinase
" in MedChemExpress (MCE) Product Catalog:
Products (39)
39 Results for "ATM kinase" in MCE Product Catalog:
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13
Target:
Research Areas:
Elrelesertib (AZD1390) is an orally active, brain-penetrant ATM kinase inhibitor with IC50 values of 0.78 nM. Elrelesertib blocks ATM-dependent DNA damage response, inhibits ATM autophosphorylation and downstream Chk2, Rad50 phosphorylation, and accumulates at DNA breaks. Elrelesertib acts as a radiosensitizer, induces apoptosis, genomic instability, G2-M cell cycle arrest, ROS elevation, and mitochondrial membrane potential alteration. Elrelesertib has low efflux liability against P-gp and BCRP. Elrelesertib can be used for the research of central nervous system malignancies, glioblastoma multiforme, glioma, lung cancer brain metastases, and breast cancer .
11
11 Cited Publications
Cat. No.: HY-19959
CAS No.: 1198097-97-0
Mirin is a potent Mre11-Rad50-Nbs1 (MRN) complex inhibitor. Mirin prevents MRN-dependent activation of ATM (IC50=12 μM) without affecting ATM protein kinase activity, and it inhibits Mre11-associated exonuclease activity. Mirin abolishes the G2/M checkpoint and homology-dependent repair in mammalian cells. Mirin prevents ATM activation in response to DNA double-strand breaks (DSBs) and blocks homology-directed repair (HDR) in mammalian cells .
11
11 Cited Publications
(E/Z)-Mirin is a mixture of (E)-Mirin and Mirin ((Z)-Mirin) (HY-19959) configurations. Among them, Mirin is an inhibitor of MRN (Mre11-Rad50-Nbs1). Mirin prevents MRN-dependent ATM activation without affecting ATM protein kinase activity .
5
5 Cited Publications
CP-466722 is a rapidly reversible inhibitor of ATM, with an IC50 of 0.41 μM, and has no effects on PI3K or closely related PI3K-like protein kinase (PIKK) family members.
4
4 Cited Publications
Synonyms: RP-3500; ATR inhibitor 4
Camonsertib (RP-3500) is an orally active, selective ATR kinase inhibitor (ATRi) with an IC50 of 1.00 nM in biochemical assays. Camonsertib shows 30-fold selectivity for ATR over mTOR (IC50=120 nM) and >2,000-fold selectivity over ATM, DNA-PK, and PI3Kα kinases. Camonsertib has potent antitumor activity .
4
4 Cited Publications
Synonyms: M4076; ATM Inhibitor-5
Target:
Research Areas:
Lartesertib (M4076) is an inhibitor of the serine/threonine protein kinase ATM with high potency. Lartesertib can inhibit the growth of multiple hematopoietic cell lines. Additionally, when combined with the ATR inhibitor Tuvusertib (HY-111451), Lartesertib can promote the death of tumor cells, activate the immune signaling pathway, and exhibit anti-tumor activity .
1
1 Cited Publications
Target:
Research Areas:
GJ071 oxalate induces ATM kinase activity in ataxia telangiectasia (A-T) cells carrying homozygous TGA or TAG stop codons .
Synonyms: ART0380
Research Areas:
ART0380 is a potent, selective and orally active ATR kinase inhibitor. ART0380 potently inhibits human ATR-ATRIP complex with an IC50 of 51.7 nM. ART0380 binds the ATP pocket of the ATR-ATRIP complex, blocks ATR-dependent Chk1 serine 345 phosphorylation, and induces cell cycle disorder and DNA damage. ART0380 demonstrates potent and selective antitumor activity in preclinical models with varying types of ataxia-telangiectasia mutated (ATM) gene aberrancy. ART0380 can be used for the research of cancer, such as colorectal cancer and prostate cancer .
AZ31 is a a potent, highly selective, and orally active ATM inhibitor with an IC50 of <1.2 nM for ATM enzyme, and an IC50 of 46 nM for ATM in cell. AZ31 shows excellent selectivity over ATR (>500-fold) and excellent PIKK-family selectivity and pan-kinase selectivity. AZ31 is a potent radiosensitizer in vitro, it can be used for the research of cancer .
Cat. No.: HY-161615
CAS No.: 3010273-12-5
Research Areas:
PROTAC ATR degrader-2 is a selective ATR PROTAC degrader. PROTAC ATR degrader-2 degrades ATR in acute myeloid leukemia (AML) cells MV-4-11 and MOLM-13, with DC50 values of 22.9 nM and 34.5 nM, respectively. PROTAC ATR degrader-2 has an IC50 of 29.6 nM against ATR, and its IC50 values against ATM and PI3K are both greater than 2000 nM. PROTAC ATR degrader-2 induces apoptosis, DNA damage, and upregulates p53 expression. PROTAC ATR degrader-2 inhibits cancer cell proliferation through the kinase-independent function of ATR protein. PROTAC ATR degrader-2 is applicable to research related to acute myeloid leukemia .
Cat. No.: HY-163944
CAS No.: 3081311-94-3
Research Areas:
LL-K12-18 is a CDK12 kinase inhibitor and a dual-site molecular glue. LL-K12-18 inhibits human CDK12 with an IC50 value of 283.9 nM, and selectively degrades cyclin K via the ubiquitin-proteasome system by stabilizing the CDK12-DDB1 complex. LL-K12-18 downregulates DNA damage response genes, reduces the phosphorylation level of CTD Ser2 in RNA polymerase II, and modulates biomarkers such as ATM, RAD51, γ-H2AX and cleaved PARP, thereby effectively inducing apoptosis and inhibiting proliferation of breast cancer cells. LL-K12-18 exhibits high target selectivity and serves as a research tool for studies on triple-negative breast cancer .
Cat. No.: HY-160096
CAS No.: 1360628-91-6
Research Areas:
M3541 is an orally effective DNA-dependent protein kinase (DNA-PK) inhibitor . M3541 inhibits ionizing radiation-induced ATM autophosphorylation and phosphorylation of downstream substrates (KAP1, CHK2, p53), blocks DSB end resection and homologous recombination repair, and simultaneously induces non-homologous end joining, G2-M phase arrest, polyploidization, and cell death. M3541 can be used for research on solid tumors, acute myeloid leukemia, non-small cell lung cancer, triple-negative breast cancer, etc. .
SKLB-197 showed an IC50 value of 0.013 μM against ATR but very weak or no activity against other 402 protein kinases. It displayed potent antitumor activity against ATM-deficent tumors both in vitro and in vivo.
Cat. No.: HY-174989
ATM-IN-2 is a selective and orally active ATM inhibitor with an IC50 of 4 nM. ATM-IN-2 exhibits excellent kinase selectivity (>700-fold over PIKK family members). ATM-IN-2 exerts its anti-tumor effect by inhibiting ATM phosphorylation and the downstream signaling pathways (p53, H2AX), and promotes cell apoptosis. ATM-IN-2 can be used for the study of chemosensitizer candidate such as colon cancer .
Cat. No.: HY-112477
CAS No.: 724708-21-8
Synonyms: Hymenialdisine analogue-1
Research Areas:
Chk2-IN-1 (compound 1) is a potent and selective inhibitor of checkpoint kinase 2 (Chk2), with IC50s of 13.5 nM and 220.4 nM for Chk2 and Chk1, respectively. Chk2-IN-1 can elicit a strong ataxia telangiectasia mutated (ATM)-dependent Chk2-mediated radioprotection effect .
Cat. No.: HY-150617A
CAS No.: 2020089-41-0
Synonyms: (Rac)-M4076; (Rac)-ATM Inhibitor-5
Target:
Research Areas:
(Rac)-Lartesertib ((Rac)-M4076) is an isoform of Lartesertib (HY-150617). Lartesertib (M4076) is an inhibitor of the serine/threonine protein kinase ATM with high potency. Lartesertib can inhibit the growth of multiple hematopoietic cell lines. Additionally, when combined with the ATR inhibitor Tuvusertib (HY-111451), Lartesertib can promote the death of tumor cells, activate the immune signaling pathway, and exhibit anti-tumor activity .
Cat. No.: HY-155091
CAS No.: 2951007-81-9
ATM Inhibitor-9 (Compd 7a) is a potent ATM inhibitor with IC505 nM for ATM kinase, useful in cancer research .
Cat. No.: HY-153787
CAS No.: 2765544-85-0
ATM inhibitor-6 (A-193) is a selective ATM kinase inhibitor. ATM inhibitor-6 can be used in cancer research .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
