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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
35 Results for "
myeloma cell lines
" in MedChemExpress (MCE) Product Catalog:
Products (35)
35 Results for "myeloma cell lines" in MCE Product Catalog:
10
10 Publications Verification
Research Areas:
TAS4464 is a long-acting, highly selective covalent inhibitor targeting NEDD8-activating enzyme (NAE) (IC50=0.955 nM), and also inhibits CAII with an IC50 of 0.73 μM, which is less potent than MLN4924 (HY-70062). The IC50 values of TAS4464 against other E1 enzymes UAE and SAE are 449 nM and 1280 nM, respectively. TAS4464 targets NEDD8 in an ATP-dependent manner to inhibit NAE, blocks the neddylation pathway, causes accumulation of CRL ubiquitin ligase substrates (such as CDT1, p27, phosphorylated IκBα), and further induces tumor cell apoptosis. TAS4464 exhibits antiproliferative and cytotoxic effects, and has broad-spectrum antitumor activity against various hematologic and solid tumor cell lines as well as patient-derived tumor cells. TAS4464 has a wide selcetive window, without obvious toxicity. TAS4464 can be used in the research of hematologic malignancies (leukemia, lymphoma, multiple myeloma, etc.) and solid tumors (small cell lung cancer, colorectal cancer, sarcoma, endometrial cancer, ovarian cancer, etc.) .
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10 Publications Verification
Research Areas:
TAS4464 hydrochloride is a long-acting, highly selective covalent inhibitor targeting NEDD8-activating enzyme (NAE) (IC50=0.955 nM), and also inhibits CAII with an IC50 of 0.73 μM, which is less potent than MLN4924 (HY-70062). The IC50 values of TAS4464 hydrochloride against other E1 enzymes UAE and SAE are 449 nM and 1280 nM, respectively. TAS4464 hydrochloride targets NEDD8 in an ATP-dependent manner to inhibit NAE, blocks the neddylation pathway, causes accumulation of CRL ubiquitin ligase substrates (such as CDT1, p27, phosphorylated IκBα), and further induces tumor cell apoptosis. TAS4464 hydrochloride exhibits antiproliferative and cytotoxic effects, and has broad-spectrum antitumor activity against various hematologic and solid tumor cell lines as well as patient-derived tumor cells. TAS4464 hydrochloride has a wide therapeutic window, without obvious toxicity. TAS4464 hydrochloride can be used in the research of hematologic malignancies (leukemia, lymphoma, multiple myeloma, etc.) and solid tumors (small cell lung cancer, colorectal cancer, sarcoma, endometrial cancer, ovarian cancer, etc.) .
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4 Cited Publications
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BI8622 is a specific inhibitor of the ubiquitin ligase HUWE1 with an IC50 of 3.1 μM. BI8622 can decrease the protein expression levels of c-myc and glycolytic markers as well as immune modulatory markers after HUWE1 inhibition in triple-negative breast cancer (TNBC) cell lines. BI8622 significantly protects against cisplatin (HY-17394)-induced acute kidney injury (AKI). BI8622 significantly reduces the growth of multiple myeloma (MM) cell lines and induces cell cycle arrest. BI8622 can prevent HUWE1-dependent TTBK2 ubiquitination. BI8622 can be studied in research for various diseases including medulloblastoma, acute kidney injury, breast cancer and MM .
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INK4C-IN-2 is a p18 INK4C inhibitor. NK4C-IN-2 promotes hematopoietic stem cells (HSCs) division by inhibiting INK4C and activating CDK4/6, with an ED50 of 5.21 nM. INK4C-IN-2 shows no cytotoxic to normal 32D cells, HSCs, leukemia cell lines and myeloma cell lines .
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TCRS-417 (T417) is a small-molecular inhibitor for PBX1. TCRS-417 can directly block PBX1-binding to DNA (IC50 = 6.58 μM), and affects PBX1 transcription. TCRS-417 is able to hammer out the stemness traits of Carboplatin (HY-17393)-resistant (CR) cells to revert to a differentiated status through tacking PBX1 signaling cascade. TCRS-417 significantly suppresses self-renewal and proliferation of cancer cells expressing high levels of PBX1. TCRS-417 can decrease the mRNA levels of FOXM1, NEK2, and E2F2 in cancer cell lines. TCRS-417 is selectively toxic against chr1q-amp myeloma and solid tumor cells .
Cat. No.: HY-P991155
CAS No.: 2988886-91-3
Synonyms: JNJ-79635322; JNJ-5322
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Cat. No.: HY-P99798
CAS No.: 2251756-52-0
Synonyms: AMG 420; BI-836909
Cat. No.: HY-P990980
CAS No.: 2919209-65-5
Synonyms: CND-106; EMB-06
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Cizutamig (CND-106) is a bispecific T-cell engager targeting BCMA and CD3. Cizutamig exhibits immunostimulatory and anti-tumor activities. Cizutamig can be used in research related to relapsed or refractory multiple myeloma and systemic lupus erythematosus .
Synonyms: MK-8998; CX-8998; JZP385
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Suvecaltamide (MK-8998) is a selective T-type calcium channel inhibitor with oral efficacy. Suvecaltamide exhibits no cytotoxicity in myeloma cell lines and does not affect the antitumor efficacy of Bortezomib (BTZ). Suvecaltamide reverses BTZ-induced peripheral neuropathy (CIPN) in mouse and rat models, and helps inhibit myeloma growth .
Synonyms: LCQ-195; AT9311
NVP-LCQ195 (LCQ-195) is an inhibitor of CDK1/2/3/5/9. NVP-LCQ195 induces cell cycle arrest and eventual apoptotic cell death of multiple myeloma (MM) cells. NVP-LCQ195 triggers decreased amplitude of transcriptional signatures related to oncogenesis, drug resistance and stem cell renewal in MM cell lines .
Synonyms: SDS-1-021
CMLD010509 (SDS-1-021) is a highly specific inhibitor of the oncogenic translation program supporting multiple myeloma (MM)-including key oncoproteins such as MYC, MDM2, CCND1, MAF, and MCL-1. CMLD010509 (SDS-1-021) shows an IC50 below 10 nM for most MM cell lines and induces apoptosis. CMLD010509 (SDS-1-021) is a potent and selective translation inhibitor through an eIF4E phosphorylation-independent mechanism .
CST626 is a PROTAC degrader targeting IAP, with DC50 values of 0.7 nM, 2.4 nM and 6.2 nM against XIAP, cIAP1 and cIAP2, respectively. This compound recruits the VHL E3 ubiquitin ligase to form a heterotrimeric complex, thereby inducing ubiquitination and proteasomal degradation of the target proteins. CST626 also exhibits certain degrading activity against VHL30 and VHL19. CST626 inhibits the proliferation and induces apoptosis of various hematologic tumor cell lines, and its anti-tumor effect is further enhanced when used in combination with TNF-α. CST626 can be used in research related to multiple myeloma, acute myeloid leukemia and diffuse large B-cell lymphoma .
Cat. No.: HY-161101
Research Areas:
GSPT1 degrader-19 is a molecular glue degrader targeting GSPT1, IKZF1 and IKZF3, with DC50 values of 0.88 nM, 11.54 nM and 13.84 nM, respectively, in MM.1S multiple myeloma cells. GSPT1 degrader-19 induces cereblon (CRBN)-dependent ubiquitination and proteasomal degradation of IKZF1, IKZF3, GSPT1 and GSPT2, and also reduces ZFP91 protein levels via a CRBN-dependent pathway. GSPT1 degrader-19 exerts antiproliferative effects on cancer cells, induces global proteomic changes including downregulation of novel substrates, and exhibits activity against multiple myeloma and leukemia cell lines. GSPT1 degrader-19 can be used in research related to multiple myeloma and leukemia .
Synonyms: N-(Hydroxymethyl)thalidomide
Research Areas:
CPS-11 (N-(Hydroxymethyl)thalidomide) a Thalidomide (HY-14658) analogue, is a potent anti-cancer agent. CPS-11 inhibits NF-κB, activates NFAT, and repress cytokine expression through elevated ROS. CPS-11 exhibits a wider activity spectrum and higher potency against MM (multiple myeloma) cell lines .
Cat. No.: HY-175164
SVC112 is a translation elongation inhibitor that prevents the cyclic dissociation of EF2 from the ribosome, thereby inhibiting the elongation step of translation. SVC112 shows activity in growth inhibition among cancer cell lines of various origins (acute myeloid leukemia (AML), multiple myeloma (Myeloma), colorectal cancer (CRC), and head and neck squamous cell carcinoma (HNSCC)). SVC112 preferentially impedes ribosomal processing of mRNAs, and decreaseds CSC-related proteins including Myc and Sox2. SVC112 induces apoptosis in hematologic cancer cell lines, while phosphorylation of c-Myc correlates with sensitivity to SVC112 in colorectal cancer cell lines. SVC112 inactivates HNSCC stem cells in vitro and prevents the regrowth of HNSCC tumor xenografts in mice. SVC112 can be used for the study of HNSCC .
Cat. No.: HY-172614
CAS No.: 313527-11-6
Synonyms: RK-552
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RK-0080552 (RK-552) is a NSD2 inhibitor with an IC50 of 0.11 μM, and it exhibits selectivity over histone methyltransferases G9a (IC50: 1.2 μM) and SET7/9 (IC50: >50 μM). RK-0080552 functionally inhibits NSD2 histone methyltransferase activity, reduces the dimethylation level of histone H3 lysine 36, suppresses IRF4 transcription, induces apoptosis and triggers cell death. RK-0080552 inhibits the growth of xenograft tumors and prolongs host survival. RK-0080552 is available for the research of multiple myeloma .
Cat. No.: HY-160843
CAS No.: 20584-81-0
N-ω-chloroacetyl-L-ornithine (NCAO) is a potent reversible competitive ornithine decarboxylase (ODC) inhibitor that exerts cytotoxic and antiproliferative effects on tumor cell lines with EC50 values ranging from 1 to 50.6 µM. NCAO induces tumor cell Apoptosis and inhibits tumor cell migration in vitro. NCAO also exhibits a potent antitumor activity against both solid and ascitic tumors in a mouse model using the myeloma (Ag8) cell line. NCAO is promising for research of antitumor agents .
Cat. No.: HY-174445
CAS No.: 3107801-96-4
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C199 is a PROTAC degrader targeting PRMT4 (DC50 = 106 nM). C199 shows high selectivity for PRMT4 over other protein arginile methyltransferases. C199 exhibits strong cell degradation ability. C199 induces apoptosis in MM cell lines. C199 efficiently clears PRMT4 protein via the VHL-proteasome pathway. C199 has a relatively long half-life and shows strong anti-multiple myeloma (MM) tumor activity .
Cat. No.: HY-13312A
CAS No.: 1008448-19-8
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GTx-134 is a dual insulin-like growth factor 1 receptor/insulin receptor (IGF-1R/IR) inhibitor with an IC50 values for IGF-1R and IR of 97 and 187 nM respectively. GTx-134 inhibits the autophosphorylation of IGF-1R and its downstream signaling pathway (Akt), thereby blocking the proliferation and survival signals of tumor cells. GTx-134 has broad-spectrum inhibitory activity against multiple myeloma cell lines and can induce apoptosis in sensitive cells. GTx-134 significantly inhibits tumor growth in mice with MM1.S cell transplantation. GTx-134 works in synergy with existing therapies (such as protease preparations, immunomodulators). GTx-134 can be used in high-risk myeloma 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
