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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
604 Results for "
SCO2 mutations
" in MedChemExpress (MCE) Product Catalog:
Products (604)
604 Results for "SCO2 mutations" in MCE Product Catalog:
Cat. No.: HY-134813A
MRTX1133 formic is a noncovalent, potent, and selective KRAS G12D inhibitor. MRTX1133 formic optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated KD against KRAS G12D of 0.2 pM. MRTX1133 formic prevents SOS1-catalyzed nucleotide exchange and/or formation of the KRASG12D/GTP/RAF1 complex, thereby inhibiting mutant KRAS-dependent signal transduction. MRTX1133 formic shows efficacy in tumor models harboring KRAS G12D mutations [2].
BAY 2476568 is a potent and mutant-selective inhibitor targeting EGFR exon20 insertion variants. BAY 2476568 potently inhibits the kinase activity of EGFR exon20 insertion mutants (insASV, insSVD, insNPG) with IC50 values of 0.09 nM, 0.21 nM, and 0.11 nM, respectively. BAY 2476568 inhibits EGFR (Y1068) phosphorylation and reduces the phosphorylation of ERK1/2 and Akt (S473) in Ba/F3 cells expressing EGFR exon20 insertion mutants (insASV, insSVD). BAY 2476568 can be used for the study of non-small cell lung cancer (NSCLC) driven by EGFR exon20 insertion mutations [2].
CH7233163 is a noncovalent ATP-competitive inhibitor for EGFR-Del19/T790M/C797S. CH7233163 can overcome Osimertinib (HY-15772)-Resistant EGFR-Del19/T790M/C797S mutation. CH7233163 blocks the EGFR phosphorylation in the Del19/T790M/C797S_NIH3T3 cells. CH7233163 has antitumor activities .
Cat. No.: HY-137433A
CAS No.: 2226167-02-6
Synonyms: D-0316 mesylate
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Befotertinib (D-0316) mesylate is an orally active EGFR inhibitor and ABCB1 inhibitor. Befotertinib mesylate selectively targets EGFR mutations including EGFR T790M, EGFR L858R and delE746-A750, forms covalent bonds with EGFR C797, inhibits oncogenic signaling pathways, and exerts antiproliferative effects. Befotertinib mesylate inhibits ABCB1-mediated drug efflux, activates the ATPase activity of ABCB1, acts as a chemosensitizer and apoptosis enhancer, and restores the sensitivity of multidrug-resistant cancer cells. Befotertinib mesylate can be used in research related to multidrug-resistant cancers and non-small cell lung cancer [2].
Cat. No.: HY-148273R
CAS No.: 2821793-99-9
Synonyms: ASP-3082 (Standard); KRAS G12D inhibitor 17 (Standard)
Setidegrasib (Standard) is the analytical standard of Setidegrasib (HY-148273). This product is intended for research and analytical applications. Setidegrasib (ASP-3082) is a PROTAC KRAS degrader (DC50: 37 nM). Setidegrasib induces the degradation of G12D-mutation KRAS protein. Setidegrasib suppresses p-ERK, p-AKT, p-S6 levels in AsPC-1 cells. Setidegrasib exhibits anti-tumor activity in various cancer xenograft models in mice. Setidegrasib can be used in studies involving KRAS(G12D)-mutated solid tumors, such as non-small cell lung cancer [2] .
Cat. No.: HY-168007
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NSC804515 is an inhibitor of wild-type and R155H mutant p97/VCP ATPase, with an IC50 of about 15 nM for both targets. NSC804515 acts as an antiproliferative agent, disrupts the function of the ubiquitin-proteasome system, induces UbG76V-GFP accumulation, and shows reduced inhibitory potency against p97 variants carrying P510S, K512N, N616F and F618S mutations. NSC804515 can be used in research related to cancer, inclusion body myopathy with early-onset Paget's disease and frontotemporal dementia, as well as familial amyotrophic lateral sclerosis .
Cat. No.: HY-171744
CAS No.: 1333382-32-3
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CX-5279 is an efficient and selective CK2 inhibitor with IC50 values for nCK2 and CK2α of 2.73 and 0.91 nM, respectively. CX-5279 is sensitive to mutations at Val66, Ile174, and V66I174AA, with IC50 values of 13.8, 12.5, and 23.35 nM, respectively. CX-5279's inhibitory activity against PIM1 is very weak, with a IC50 value of 8.52 μM. CX-5279 exhibits anti-proliferative activity in various cancer cell lines. CX-5279 can be used for research on cancers such as pancreatic cancer and leukemia .
Cat. No.: HY-174243
CAS No.: 2933935-13-6
KRASG12D-IN-5 (Compound 241) is an orally active KRAS(G12D) inhibitor with an IC50 of 11 nM. KRASG12D-IN-5 has potent anticancer activity with no significant cytotoxicity against BxPC-3 (WT), KRAS mutation AsPC-1 (G12D) and MIAPaCa-2 cells (G12C) with CC50s of 10.37, 0.76 and 0.3 μM, respectively. KRASG12D-IN-5 can be used for cancer research, such as lung, pancreatic and colorectal cancer .
Cat. No.: HY-175280
CAS No.: 3095033-62-5
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Lck degrader-1 is a molecular glue degrader that recruits cereblon to target LCK and CK1α. Lck degrader-1 promotes the formation of the LCK/CRBN-DDB1 ternary complex with an EC50 of 77.1 nM, and induces the degradation of LCK and CK1α. LCK degradation induced by Lck degrader-1 depends on the G415-containing helical G-loop degron, and maintains LCK-degrading activity in cells with the LCK T316I gatekeeper mutation. Lck degrader-1 can be used for research related to T-cell acute lymphoblastic leukemia (T-ALL) and LCK inhibitor resistance .
Cat. No.: HY-178042
CAS No.: 2756257-56-2
SS-3091 is a pan-KRas inhibitor active across KRas G12D, KRas G12C, KRas G12V, KRas G12S mutants, with minimal effects on non-KRas-driven cancer cells. SS-3091 binds to the KRas·ARaf interaction interface, destabilizes the complex, and attenuates KRas activity. SS-3091 suppresses phosphorylation of S6K, Akt, and ERK. SS-3091 reduces proliferation and decreases colony formation of cancer cells bearing KRas G12 mutations. SS-3091 can be used for the research of KRas-driven cancers .
Cat. No.: HY-178391
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SMU-037 is an orally active and selective ROS1 inhibitor that demonstrates potent activity (IC₅₀ = 6.8 nM) and possesses the ability to penetrate the blood-brain barrier. SMU-037 shows ~25-fold selectivity over ALK, and superior sensitivity against the G2032R mutation. SMU-037 attenuates phosphorylation of ROS1 and downstream MAPK-ERK signaling pathway, leading to cell cycle arrest and apoptosis. SMU-037 effectively suppresses tumor progression in both xenograft and intracranial mouse models. SMU-037 can be used for non-small cell lung cancer (NSCLC) research .
Cat. No.: HY-189204
CAS No.: 3110002-64-4
FGFR2-IN-4 is a selective, orally active FGFR2 inhibitor, with IC50 values of 10.0 nM and 5.8 nM against wild-type FGFR2 and the FGFR2 V565F mutant, respectively. FGFR2-IN-4 induces necroptosis in FGFR2-driven tumor cells. FGFR2-IN-4 induces tumor regression in xenograft models harboring FGFR2 inhibitor-resistant mutations without altering serum phosphate levels. FGFR2-IN-4 is used to investigate FGFR2-driven malignancies, including intrahepatic cholangiocarcinoma and gastric cancer .
Cat. No.: HY-P990256
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Cat. No.: HY-W356181
CAS No.: 95896-78-9
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4,8-DiMeIQx is an orally active mutagen, selective dopaminergic neurotoxicant, and DNA damaging agent. 4,8-DiMeIQx can be isolated from cooked beef, sausage, pork, and chicken. 4,8-DiMeIQx induces reverse mutations in *Salmonella typhimurium* TA98 in the presence or absence of S9 mix, and forms DNA adducts in vivo in rat liver. 4,8-DiMeIQx exhibits selective neurotoxicity toward dopaminergic neurons. 4,8-DiMeIQx shows no activity against non-dopaminergic neurons. 4,8-DiMeIQx can be used in studies related to Parkinson's disease and colorectal cancer [2] .
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Oxiran-2-ylmethanol (Glycidol) is an ester product. Oxiran-2-ylmethanol induces base pair point mutations in bacterial strains and structural chromosome aberrations in cultured cells. Oxiran-2-ylmethanol forms N-(2,3-dihydroxypropyl)valine hemoglobin adducts. Oxiran-2-ylmethanol acts as an animal carcinogen but does not significantly induce micronucleated immature erythrocytes in animal bone marrow. Oxiran-2-ylmethanol enables anionic polymerization to produce linear poly(glycidol). Oxiran-2-ylmethanol can be used for cancer-related research [2] .
Cat. No.: HY-105369
CAS No.: 154015-73-3
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KF-20444 is an orally active ALK inhibitor with blood-brain barrier penetration. KF-20444 exhibits strong inhibitory activity against ALK fusion proteins (EML4-ALK) and ALK resistance mutations (including L1196M, G1202R, and F1174L). KF-20444 effectively suppresses the phosphorylation of ALK in ALK-driven cancer cell lines, thereby inhibiting cancer cell proliferation and inducing apoptosis. KF-20444 demonstrates anti-tumor efficacy in mouse models bearing ALK-positive non-small cell lung cancer (NSCLC) or neuroblastoma. KF-20444 can be used for the study of ALK-driven malignancies .
Cat. No.: HY-112289B
CAS No.: 1429179-08-7
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(1R)-IDH889 is the isomer of IDH889 (HY-112289), and can be used as an experimental control. IDH889 is an orally available, brain penetrant, allosteric and mutant specific inhibitor of isocitrate dehydrogenase 1 (IDH1). IDH889 has potent selectivity for IDH1 R132* mutations, with IC50s of 0.02 μM, 0.072 μM and 1.38 μM for IDH1 R132H, IDH1 R132C and IDH1 wt, respectively. IDH889 shows potent cellular inhibition of R-2-hydroxyglutarate (2-HG) production with an IC50 of 0.014 μM .
Cat. No.: HY-116572
CAS No.: 1678515-13-3
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TASIN-1 hydrochloride is a selective inhibitor of truncated APC TR (adenomatous polyposis coli gene) that exerts cytotoxic effects by inhibiting cholesterol biosynthesis. TASIN-1 hydrochloride specifically targets colorectal cancer (CRC) cells carrying APC truncated mutations, while having no significant toxicity to wild-type APC cells. TASIN-1 hydrochloride exerts cytotoxic effects by targeting Emopamil binding protein (EBP) to inhibit cholesterol biosynthesis, triggering endoplasmic reticulum (ER) stress, reactive oxygen species (ROS) generation, and JNK-mediated apoptosis, and inhibiting Akt survival signaling. TASIN-1 hydrochloride can be used to prevent and intervene in APC mutant colorectal cancer [2] .
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TASIN-1 is a selective inhibitor of truncated APC TR (adenomatous polyposis coli gene) that exerts cytotoxic effects by inhibiting cholesterol biosynthesis. TASIN-1 specifically targets colorectal cancer (CRC) cells carrying APC truncated mutations, while having no significant toxicity to wild-type APC cells. TASIN-1 exerts cytotoxic effects by targeting Emopamil binding protein (EBP) to inhibit cholesterol biosynthesis, triggering endoplasmic reticulum (ER) stress, reactive oxygen species (ROS) generation, and JNK-mediated apoptosis, and inhibiting Akt survival signaling. TASIN-1 can be used to prevent and intervene in APC mutant colorectal cancer [2] .
Cat. No.: HY-15210
CAS No.: 54870-28-9
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Meglitinide is an ATP-sensitive potassium (KATP) channel inhibitor. Meglitinide exhibits IC50 values of 0.26 μM, 0.53 μM and 1.6 μM against KATP channels containing SUR1, SUR2A and SUR2B, respectively, with a Kd value of 7 μM for both SUR1 and SUR2A, and a Kd value of 8 μM for SUR2B. Meglitinide binds to the SUR1, SUR2A and SUR2B subunits with high affinity to close KATP channels, acting on a binding site shared by all SUR subtypes, and its interaction with SUR1 carrying the S1237Y mutation remains unchanged. Meglitinide is applicable to research related to type 2 diabetes .
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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
