Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T3184 |
Kevetrin hydrochloride
Thioureidobutyronitrile HCl,thioureido butyronitrile hydrochloride,4-Isothioureidobutyronitrile hydrochloride |
Mdm2; p53 | Apoptosis |
Kevetrin hydrochloride (4-Isothioureidobutyronitrile hydrochloride) 是一种小分子,是肿瘤抑制蛋白 p53 的激活剂,具有潜在的抗肿瘤活性。 | |||
T31221 |
dBRD9
dBRD-9,dBRD 9 |
PROTACs | PROTAC |
dBRD9是一种 PROTAC。dBRD9是一种双重作用的分子,一部分连接 Bromodomain-containing protein 9 (BRD9)的溴域,另一部分招募小脑 E3泛素连接酶的配体(ligand that recruits the cereblon E3 ubiquitin ligase)。dBRD9对 MOLM-13细胞中 BRD9具有抑制作用,可使其降解,IC50为104 nM。 | |||
T31221L |
dBRD9 HCl
dBRD9 HCl(2170679-45-3 Free base) |
Epigenetic Reader Domain | Chromatin/Epigenetic |
dBRD9 HCl 是一种PROTAC,包含cereblon E3连接酶配体与BRD9抑制剂BI 7273。dBRD9 HCl 是有效和选择性的BRD9降解剂,在MOLM-13细胞中IC50的为56.6nM。dBRD9 HCl 在浓度高达5μM 时不会降解BRD4或BRD7。dBRD9 HCl 在人AML 细胞系中显示出抗增殖作用。 | |||
T81128 |
Sontigidomide
|
||
Sontigidomide(Compound 5)是一种抗肿瘤化合物,能在1 μM浓度下显著抑制MOLM-13细胞增殖,3天内抑制率超过80%。 | |||
T81108 |
SR-1114
|
PROTACs | PROTAC |
SR-1114 是一种创新的PROTACENL降解剂,能够在MV4;11、MOLM-13和OCI/AML-2细胞中迅速降解ENL,其DC50值分别为150 nM 、311 nM 和1.65 μM。 | |||
T79596 |
FLT3-IN-20
|
||
FLT3-IN-20(compound 34f)作为一种高效FLT3抑制剂,对FLT3-D835Y和FLT3-ITD具有强效性,IC50值分别仅为1 nM和4 nM。该化合物在携带FLT3-ITD突变的AML细胞系MV4-11和MOLM-13中展现出显著的抗增殖效果,其中IC50值分别为7 nM和9 nM;对于带有FLT3-ITD-D835Y突变的MOLM-13变体,其IC50值为4 nM。FLT3-IN-20主要用于肿瘤治疗研究领域。 | |||
T73637 | Dot1L-IN-1 TFA | ||
Dot1L-IN-1 TFA 是一种高效选择性Dot1L抑制剂,具有2 pM的Ki值和小于0.1 nM的IC50值。在HeLa细胞中,它能有效抑制H3K79的二甲基化(IC50=3 nM),同时也能在Molm-13细胞中抑制HoxA9启动子的活性(IC50=17 nM)。 | |||
T61768 | FY-56 | ||
FY-56 是一种高效的具有选择性LSD1/KDM1A 抑制剂 (IC50=42 nM),比 MAO-A/B 具有高选择性. FY-56 诱导 MOLM-13 和 MV4-11 细胞分化,具有急性髓系白血病 AML 研究潜力。 | |||
T24045 |
eSM156
eSM 156,eSM-156 |
||
eSM156 is an effective FLT3 inhibitor. It has high antiproliferative activity against acute myeloid leukemia (AML) cells. eSM156 has IC50 (FLT3) = 1.4 nM; EC50 (MV4-11cells) = 150 nM; EC50 (MOLM-13 cells) = 40 nM. | |||
T40168 |
DHODH-IN-16
|
Dehydrogenase | Metabolism |
DHODH-IN-16 是一种有效的二氢乳清酸脱氢酶抑制剂(DHODH,IC50 = 0.396 nM)。 | |||
T37447 |
UZH1
UZH1 |
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UZH1 is a racemate of UZH1a and UZH1b. UZH1a is a potent and selective METTL3 inhibitor, with an IC50 of 280 nM. UZH1b (IC50=28 μM) is essentially inactive. UZH1 can be used for epitranscriptomic modulation of cellular processes. UZH1 has antitumor activity. UZH1 also can be used as a chemical probe for studying METTL3[1]. UZH1a (2.5-160 μM; 72 h) inhibits the growth of MOLM-13, HEK293T, and U2Os cells, with IC50s of 11 μM, 67 μM, and 87 μM, respectively[1].UZH1b (2.5-160 μM; 72 h) inhibits the ... | |||
T81806 |
METTL3-IN-5
|
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METTL3-IN-5(Compound 13)是METTL3抑制剂,对MOLM-13细胞生长的抑制作用显著,其IC50小于2 μM。该化合物对hERG的抑制活性较弱(IC50>30 μM),可应用于AML的研究领域。 | |||
T17878 |
Lenalidomide-C4-NH2 hydrochloride
Cereblon ligand 1 hydrochloride,E3 ligase Ligand-Linker Conjugates 32 hydrochloride |
Others | Others |
Lenalidomide-C4-NH2 hydrochloride is a Cereblon ligand derived from Lenalidomide. It serves as a recruiting agent for the CRBN protein. The compound, known as PROTAC (Compound 24), can be formed by linking Lenalidomide-C4-NH2 hydrochloride to the ligand for the protein. It exhibits inhibitory effects with IC50s of 0.98 nM and 13.7 nM against the growth of RS4;11 and MOLM-13 acute leukemia cell lines, respectively[1]. | |||
T69629 | M‑89 MLL inhibitor | ||
M‑89 is a Highly Potent Inhibitor of the Menin-Mixed Lineage Leukemia (Menin-MLL) Protein−Protein Interaction (Kd = 1.4 nM; IC50 = 25nM). M-89 binds to menin with a Kd value of 1.4 nM and effectively engages cellular menin protein at low nanomolar concentrations. M-89 inhibits cell growth in the MV4;11 and MOLM-13 leukemia cell lines carrying MLL fusion with IC50 values of 25 and 55 nM, respectively, and demonstrates >100-fold selectivity over the HL-60 leukemia cell line lacking MLL fusion. | |||
T61005 | K783-0308 | ||
K783-0308 是有效的、选择性的MNK2和FLT3的双重抑制剂,IC50值分别为 406 和 680nM。 K783-0308 促进急性髓性白血病 (AML)的 细胞凋亡和细胞周期停滞在 G0/G1 期。K783-0308 抑制 MV-4-11 和 MOLM-13 细胞生长,IC50 值分别为 10.4 和 10.5 μM | |||
T62112 |
CDK8-IN-6
|
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CDK8-IN-6 (compound 9) 是一种细胞周期蛋白依赖性激酶8 (CDK8) 的有效抑制剂 (Kd: 13 nM)。CDK8-IN-6 对 MOLM-13、OCI-AML3、MV4-11、NRK 和 H9c2 细胞表现出细胞毒性,他们 IC50s 分别为 11.2、7.5、8.6、20.5、12.5-25 μM。CDK8-IN-6 对 AML 癌症表现出潜在的研究价值。 | |||
T71973 |
Gilteritinib hemifumarate
ASP2215 hemifumarate |
FLT; TAM Receptor | Angiogenesis; Tyrosine Kinase/Adaptors |
Gilteritinib hemifumarate (ASP2215 hemifumarate) 是一种高效的 ATP 竞争性 FLT3(IC50 : 0.29 nM) 和 AXL(IC50: 0.73 nM) 双重抑制剂,可用于治疗复发或难治性 FLT3 突变的 AML。 | |||
T70779 | BPR1J-340 | ||
BPR1J-340 is a potent and selective FLT3 inhibitor with potential anticancer activity. BPR1J-340 was identified as a novel potent FLT3 inhibitor by biochemical kinase activity (IC50 approximately 25 nM) and cellular proliferation (GC50 approximately 5 nM) assays. BPR1J-340 inhibited the phosphorylation of FLT3 and STAT5 and triggered apoptosis in FLT3-ITD(+) AML cells. The pharmacokinetic parameters of BPR1J-340 in rats were determined. BPR1J-340 also demonstrated pronounced tumor growth inhibit... | |||
T2243 |
Serdemetan
JNJ-26854165,N-[2-(1H-吲哚-3-基)乙基]-N'-(4-吡啶基)-1,4-苯二胺 |
Apoptosis; Mdm2; E1/E2/E3 Enzyme; p53 | Apoptosis; Ubiquitination |
Serdemetan (JNJ-26854165) 是一种 HDM2泛素连接酶拮抗剂,能诱导 p53野生型细胞的早期凋亡。 | |||
T10464L |
Atuveciclib Racemate
BAY-1143572 Racemate,阿维西利 |
CDK | Cell Cycle/Checkpoint |
Atuveciclib Racemate (BAY-1143572 Racemate) 是 Atuveciclib 的外消旋混合物。 Atuveciclib 是口服有效的 P-TEFb/CDK9高选择性抑制剂,CDK9/CycT1的 IC50为13 nM。 | |||
T4261 |
BPR1J-097 hydrochloride (1327167-19-0(free base))
|
FLT | Angiogenesis; Tyrosine Kinase/Adaptors |
BPR1J-097 hydrochloride (1327167-19-0(free base)) 是一种新型小分子 FLT-3抑制剂(IC50=11±7 nM),具有很好的体内抗肿瘤活性。 | |||
T62354 |
CDK8-IN-7
|
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CDK8-IN-7 (compound 12) 是一种有效的、选择性的细胞周期蛋白依赖性激酶 8 (CDK8) 抑制剂 (Kd: 3.5 nM)。CDK8-IN-7 对 MOLM-13 细胞 (IC50: 5.9 μM)、OCI-AML3 细胞 (IC50: 4.8 μM)、MV4-11 细胞 (IC50: 5.4 μM)、NRK 细胞 (IC50: 16.2 μM) 和 H9c2 细胞 (IC50: 12.5-25 μM) 具有细胞毒性。CDK8-IN-7 对 AML-癌症表现出研究潜力。 | |||
T61202 |
TDO-IN-1
|
Others | Others |
TDO-IN-1 是一种具有口服活性、有效性和选择性的色氨酸 2,3-双加氧酶 (TDO)抑制剂 ,对吲哚胺-2,3-双加氧酶 具有抑制作用。TDO-IN-1 具有抗肿瘤活性, 能够通过逆转肿瘤组织的局部免疫耐受来发挥作用。 | |||
T39937 |
M-808
|
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M-808 is a potent and efficacious covalent inhibitor, targeting the interaction between Menin and MLL. It demonstrates a high binding affinity with an IC50 value of 2.6 nM. |