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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
21 Results for "
CHK1 phosphorylation
" in MedChemExpress (MCE) Product Catalog:
Products (21)
21 Results for "CHK1 phosphorylation" in MCE Product Catalog:
6
6 Publications Verification
Synonyms: VX-803; M4344; ATR inhibitor 2
Gartisertib (VX-803) is an ATP-competitive, orally active, and selective ATR inhibitor, with a Ki of <150 pM. Gartisertib potently inhibits ATR-driven phosphorylated checkpoint kinase-1 (Chk1) phosphorylation with an IC50 of 8 nM. Antitumor activity .
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5 Cited Publications
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SB-218078 is a potent, selective, ATP-competitive and cell-permeable checkpoint kinase 1 (Chk1) inhibitor that inhibits Chk1 phosphorylation of cdc25C with an IC50 of 15 nM. SB-218078 is less potently inhibits Cdc2 (IC50 of 250 nM) and PKC (IC50 of 1000 nM). SB-218078 causes apoptosis by DNA damage and cell cycle arrest .
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1 Cited Publications
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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 DNA damage responses including RPA32-phosphorylation and CHK1-phosphorylation in response to UV irradiation .
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1 Cited Publications
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CCB02 is a selective CPAP-tubulin interaction inhibitor, binding to tubulin and competing for the CPAP binding site of β-tubulin, with an IC50 of 689 nM, and shows potent anti-tumor activity. CCB02 shows no inhibition on the cell cycle- and centrosome-related kinases, or the phosphorylation status of Aurora A, Plk1, Plk2, CDK2, and CHK1 .
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1 Cited Publications
Cat. No.: HY-131446
CAS No.: 2120398-39-0
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Chk1-IN-5 is a potent checkpoint kinase 1 (Chk1) inhibitor. Chk1-IN-5 inhibits Chk1 phosphorylation and inhibits tumor growth in colon cancer xenograft model .
Synonyms: ART0380
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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 .
Cat. No.: HY-164734
CAS No.: 2610074-57-0
Synonyms: R-DXd; DS-6000
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Raludotatug Deruxtecan is an antibody-drug conjugate targeting CDH6, with an EC50 of 64.7 ng/mL in humans, 70.4 ng/mL in cynomolgus monkeys, and 228 ng/mL in mice. Raludotatug Deruxtecan specifically binds to CDH6 on the surface of cancer cells, triggers lysosomal internalization, and releases the DXd payload that inhibits TOP1. Raludotatug Deruxtecan induces DNA damage, Chk1 phosphorylation, caspase-3 cleavage, apoptosis, and bystander cell death. Raludotatug Deruxtecan is applicable to research related to serous ovarian cancer and renal cell carcinoma .
Cat. No.: HY-178858
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PROTAC FLT3/CHK1 Degrader-1 is a PROTAC FLT3/CHK1 degrader, with DC50 values of 5.88 nM (FLT3) and 4.17 nM (CHK1), respectively. PROTAC FLT3/CHK1 Degrader-1 can inhibit the phosphorylation of FLT3 downstream signaling effectors STAT5 (Tyr694), AKT (Ser473), and ERK (Tyr204), downregulate the protein level of c-Myc and maintain the expression of p53 protein. PROTAC FLT3/CHK1 Degrader-1 induces Apoptosis in cells. PROTAC FLT3/CHK1 Degrader-1 shows significant anti-tumor efficacy in mice bearing MV-4-11 subcutaneous xenografts. PROTAC FLT3/CHK1 Degrader-1 can be used for the study of acute myeloid leukemia (AML) .
Cat. No.: HY-171785
CAS No.: 2871056-82-3
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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 DNA damage response pathway, inducing tumor cell cycle arrest and apoptosis. CHK1-IN-12 is promising for research of cancers .
Cat. No.: HY-P5961
CAS No.: 289652-77-3
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LSD1/TLK1-IN-1 is an orally active LSD1, TLK1, TLK2, TTK inhibitor with an LSD1 IC50 of 0.247 μM. LSD1/TLK1-IN-1 suppresses phosphorylation of Nek1 at T141 and Rad9 at S328, abrogates the TLK1>Nek1>ATR>Chk1 axis, protects H3K4me1/2 from demethylation, and does not affect LSD2, MAO-A, or MAO-B. LSD1/TLK1-IN-1 induces apoptosis, bypasses cell-cycle arrest, suppresses tumor growth, downregulates PD-L1 expression, enhances T-cell killing response, inhibits gastric cancer cell proliferation. LSD1/TLK1-IN-1 can be used for the research of prostate cancer and gastric cancer .
Cat. No.: HY-119169
CAS No.: 84697-22-3
Synonyms: R 46846
Tubulozole (R 46846) is an orally active inhibitor of tubulin polymerization with an ID50 of 0.34 μM. Tubulozole induces activation of the Chk1 kinase and phosphorylation of ERK1/2, which is required for microtubule formation. Tubulozole arrests Mitosis at the metaphase stage. Tubulozole causes cells to accumulate in the radiosensitive mitotic phase of the cell cycle. Tubulozole exerts anticancer activity against colon cancer. Tubulozole produces a radiosensitizing effect in mouse tumor models and enhances the tumor growth delay effect when combined with γ-ray irradiation. Tubulozole is used in studies related to colon cancer, fascioliasis, MO4 fibrosarcoma, and Lewis lung carcinoma .
Cat. No.: HY-123597
CAS No.: 15427-93-7
Synonyms: DDUG; NCI C04808
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NSC 109555 is an ATP-competitive inhibitor of checkpoint kinase 2 (Chk2; IC50=200 nM in a cell-free kinase assay). It is selective for Chk2 over Chk1 and 16 kinases in a panel but does inhibit Brk, c-Met, IGFR, and LCK with IC50 values of 210, 6,000, 7,400, and 7,100 nM, respectively. NSC 109555 inhibits Chk2 autophosphorylation and phosphorylation of the Chk2 substrate histone H1 in vitro (IC50=240 nM). It inhibits the growth of, and induces autophagy in, L1210 leukemia cells in vitro.2 NSC 109555 (1,250 nM) potentiates gemcitabine-induced cytotoxicity in MIA PaCa-2, CFPAC-1, PANC-1, and BxPC-3 pancreatic cancer cells, as well as reduces gemcitabine-induced increases in Chk2 phosphorylation and enhances gemcitabine-induced production of reactive oxygen species (ROS) in MIA PaCa-2 cells.
Cat. No.: HY-P5961A
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Cat. No.: HY-136270S
CAS No.: 1792214-00-6
Synonyms: VX-803-d8; M4344-d8; ATR inhibitor 2-d8
Cat. No.: HY-189272
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ATR-IN-33 is an ATR kinase inhibitor (IC50 = 9.67 nM). ATR-IN-33 induces apoptosis, exacerbates DNA damage, and causes G1 phase cell cycle arrest by blocking CHK1 phosphorylation and DNA damage response signaling. ATR-IN-33 exhibits selective cytotoxicity against AML cell lines and can be used for research on acute myeloid leukemia .
Cat. No.: HY-10032A
CAS No.: 1247874-19-6
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PF-477736 (hydrochloride) is an ATP-competitive Chk1 inhibitor (Ki 0.49 nM) that also inhibits CK2A1, PKCA, and Akt1, and is a broad-spectrum kinase inhibitor .PF-477736 induces apoptosis via PARP cleavage, caspase-3/7 activation, caspase-independent death, BAX and PUMA upregulation, H2AX phosphorylation, DNA fragmentation, and Chk1 proteasomal degradation, while inhibiting proliferation and preventing mitotic entry .PF-477736 demonstrates selective synthetic lethality in LIMD1-deficient cells, efficacy in subcutaneous xenograft models of LIMD1-deficient tumors, and anti-proliferative activity against leukemia and lymphoma cell lines .PF-477736 induces DNA double-strand breaks and activates the ATM-p53-p21 axis, and sensitizes CHK1i-insensitive neuroblastoma cells to apoptosis with ATM or DNA-PK inhibitors .PF-477736 can be used for the research of non-small cell lung cancer, leukemia, lymphoma, and neuroblastoma .
Cat. No.: HY-106419A
CAS No.: 80427-58-3
Synonyms: Benflurone hydrochloride
Benfluron hydrochloride is an Apoptosis inducer and inhibitor of the HIV-1 Rev-RRE complex, with an IC50 of 5.0 μM against the HIV-1 Rev-RRE complex. Benfluron hydrochloride induces p53 activation, and triggers phosphorylation of Chk1 at serine 345, Chk2 at threonine 68, as well as ERK1/2 at threonine 202 and tyrosine 204. Benfluron hydrochloride activates Caspase 8, Caspase 9 and Caspase 3/7, inhibits HIV-1 viral transcription, and acts as a substrate for 11β-HSD 1 and cytosolic carbonyl reductase. Benfluron hydrochloride can be used in research related to leukemia and HIV-1 infection .
Cat. No.: HY-119169A
CAS No.: 83086-73-1
Synonyms: R 46846 hydrochloride
Tubulozole hydrochloride (R 46846 hydrochloride) is an orally active inhibitor of tubulin polymerization with an ID50 of 0.34 μM. Tubulozole hydrochloride induces activation of the Chk1 kinase and phosphorylation of ERK1/2, which is required for microtubule formation. Tubulozole hydrochloride arrests Mitosis at the metaphase stage. Tubulozole hydrochloride causes cells to accumulate in the radiosensitive mitotic phase of the cell cycle. Tubulozole hydrochloride exerts anticancer activity against colon cancer. Tubulozole hydrochloride produces a radiosensitizing effect in mouse tumor models and enhances the tumor growth delay effect when combined with γ-ray irradiation. Tubulozole hydrochloride is used in studies related to colon cancer, fascioliasis, MO4 fibrosarcoma, and Lewis lung carcinoma .
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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
